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Romidepsin (FK228) HDAC inhibitor

Name: Romidepsin (FK228)
Brand: Selleck Chemicals
SKU: S3020
Rating: 5 (236 reviews)

N. Cat.: S3020

Romidepsin (FK228, Depsipeptide, FR 901228, NSC 630176) is a potent HDAC1 and HDAC2 inhibitor with IC50 of 36 nM and 47 nM in cell-free assays, respectively. This compound controls growth and induces apoptosis in neuroblastoma tumor cells.

Romidepsin (FK228) HDAC inhibitor Chemical Structure

Struttura chimica

Peso molecolare: 540.7

Vai a

Controllo Qualità (Quality Control)

Lotto: Purezza: 99.95%

99.95

Target correlati	Akt Wnt/beta-catenin PKC HSP ROCK Microtubule Associated Integrin Bcr-Abl Actin FAK
Altro HDAC Inibitori	ITF-2357 (Givinostat) Hydrochloride Monohydrate Fimepinostat (CUDC-907) Trichostatin A (TSA) Entinostat (MS-275) RGFP966 Quisinostat (JNJ-26481585) Dihydrochloride Tubastatin A Hydrochloride Tubastatin A Mocetinostat (MGCD0103) Ricolinostat (ACY-1215)

Coltura cellulare, trattamento e concentrazione di lavoro
(Cell Culture, Treatment & Working Concentration)

Linee cellulari	Tipo di saggio	Concentrazione	Tempo di incubazione	Formulazione	Descrizione dell'attività	PMID
SU-DHL4	Cell Viability Assay	2.5-15 nM	72 h		induces cytotoxicity in a concentration-dependent manner	25790907
U2932	Cell Viability Assay	2.5-15 nM	72 h		induces cytotoxicity in a concentration-dependent manner	25790907
OCI-LY7	Cell Viability Assay	2.5-15 nM	72 h		induces cytotoxicity in a concentration-dependent manner	25790907
Farage	Cell Viability Assay	2.5-15 nM	72 h		induces cytotoxicity in a concentration-dependent manner	25790907
LY7/EBV	Cell Viability Assay	2.5-15 nM	72 h		induces cytotoxicity in a concentration-dependent manner	25790907
U2932/EBV	Cell Viability Assay	2.5-15 nM	72 h		induces cytotoxicity in a concentration-dependent manner	25790907
HCT116	Growth Inhibition Assay	5-5000 nM	24 h	DMSO	induces cell death in a concentration-dependent manner	25492515
ACH-2	Function Assay	1-9 nM	24 h		induces HIV-1 Env expression	25149467
MCF-10A	Growth Inhibition Assay				IC50=0.17±0.01 nM	24954856
MCF-7	Growth Inhibition Assay				IC50=1.10±0.20 nM	24954856
SK-BR-3	Growth Inhibition Assay				IC50=1.00±0.35 nM	24954856
MDA-MB-231	Growth Inhibition Assay				IC50=0.68±0.14 nM	24954856
PC3	Growth Inhibition Assay				IC50=1.65±0.35 nM	24954856
HCT116	Growth Inhibition Assay				IC50=1.00±0.00 nM	24954856
HCT116-p21-/-	Growth Inhibition Assay				IC50=1.26±0.37 nM	24954856
S1	Growth Inhibition Assay				IC50=7.67±0.29 nM	24954856
SW620	Growth Inhibition Assay				IC50=0.93±0.29 nM	24954856
LOX-IMVI	Growth Inhibition Assay				IC50=0.87±0.03 nM	24954856
UACC-62	Growth Inhibition Assay				IC50=0.56±0.16 nM	24954856
MDA-MB-435	Growth Inhibition Assay				IC50=0.90±0.06 nM	24954856
SF-295	Growth Inhibition Assay				IC50=0.88±0.15 nM	24954856
A549	Growth Inhibition Assay				IC50=1.26±0.24 nM	24954856
H460	Growth Inhibition Assay				IC50=2.58±0.80 nM	24954856
EKVX	Growth Inhibition Assay				IC50=1.33±0.34 nM	24954856
H146	Growth Inhibition Assay				IC50=0.22±0.07 nM	24954856
H526	Growth Inhibition Assay				IC50=0.15±0.03 nM	24954856
HuT-78	Growth Inhibition Assay				IC50=1.73±0.44 nM	24954856
HA	Growth Inhibition Assay	0.625-10nM	48 h		induces a significantly stronger inhibition of cell proliferation co-treated with bortezomib	24771510
MS-275	Growth Inhibition Assay	0.625-10nM	48 h		induces a significantly stronger inhibition of cell proliferation co-treated with bortezomib	24771510
CD4 T	Growth Inhibition Assay		48 h		EC50=4.5±1.0 nM	24722454
CD4 T	Growth Inhibition Assay		48 h		CC50=107±126 nM	24722454
CD4+ T	Growth Inhibition Assay				EC50=3 nM	24495105
A549	Growth Inhibition Assay	10–100 nM	24/36/48 h		inhibits cell growth in both concentration- and time-dependent manner	24485799
JJN3	Growth Inhibition Assay		24/48 h		EC50<1 nM; 48 h	24030150
OPM-2	Growth Inhibition Assay		24/48 h		EC50s=1 nM; 48 h	24030150
RPMI-8226	Growth Inhibition Assay		24/48 h		EC50s=1.8 nM; 48 h	24030150
U266	Growth Inhibition Assay		24/48 h		EC50s=10 nM; 48 h	24030150
CA46	Apoptosis Assay		6 h		induces blunt apoptosis	23966164
DG75	Apoptosis Assay		6 h		induces no apoptosis	23966164
Ramos	Apoptosis Assay		6 h		induces extensive apoptosis	23966164
ST486	Apoptosis Assay		6 h		induces extensive apoptosis	23966164
HuT78	Apoptosis Assay	1/10/100 nM	48 h		induces apoptosis at 1 nM	23532732
DpVp35	Apoptosis Assay	1/10/100 nM	48 h		induces blunt apoptosis	23532732
DpVp50	Apoptosis Assay	1/10/100 nM	48 h		induces blunt apoptosis	23532732
DpP75	Apoptosis Assay	1/10/100 nM	48 h		induces blunt apoptosis	23532732
SKOV-3	Growth Inhibition Assay	1–20nM	72 h	DMSO	reduces cell viability alone and combined with cisplatin	23010348
Brca1 WT	Growth Inhibition Assay	1–20nM	72 h	DMSO	reduces cell viability alone and combined with cisplatin	23010348
Brca1 Null	Growth Inhibition Assay	1–20nM	72 h	DMSO	reduces cell viability alone and combined with cisplatin	23010348
OVCAR-8	Growth Inhibition Assay	1–20nM	72 h	DMSO	reduces cell viability alone and combined with cisplatin	23010348
NCI/ADR-RES	Growth Inhibition Assay	1–20nM	72 h	DMSO	reduces cell viability alone and combined with cisplatin	23010348
HCT116	Growth Inhibition Assay	5 nM-50 μM	24 h	DMSO	inhibits cell growth in a concentration-dependent manner	22924958
RKO	Growth Inhibition Assay	5 nM-50 μM	24 h	DMSO	inhibits cell growth in a concentration-dependent manner	22924958
CO115	Growth Inhibition Assay	5 nM-50 μM	24 h	DMSO	inhibits cell growth in a concentration-dependent manner	22924958
HFS	Growth Inhibition Assay	5 nM	24/48/72 h		inhibits cell growth time-dependently	22106282
LNCaP	Growth Inhibition Assay	5 nM	24/48/72 h		inhibits cell growth time-dependently	22106282
A549	Growth Inhibition Assay	5 nM	24/48/72 h		inhibits cell growth time-dependently	22106282
697	Growth Inhibition Assay				IC50 = 2.5 nM	21538216
697-R	Growth Inhibition Assay				IC50 = 8.6 nM	21538216
HUT78	Growth Inhibition Assay				IC50=1 nM	21198545
THJ-16T	Growth Inhibition Assay	1 nM	24 h		inhibits cell growth	20810568
HCT116	Function Assay	20 nM	8 h		modulates transcript levels for hundreds of genes in either direction	20739454
B104	Function Assay	2 nM	24/48/72 h		increases the surface expression of CD20	20686505
HL-60	Cytotoxicity Assay	1-500 nM	24 h		induces cytotoxicity in a concentration-dependent manner	20624163
HP100	Cytotoxicity Assay	1-500 nM	24 h		induces cytotoxicity in a concentration-dependent manner	20624163
HL-60	Function Assay	10 nM	4/6/16 h		induces the generation of hydrogen peroxide from 4h	20624163
HP100	Function Assay	10 nM	4/6/16 h		induces the generation of hydrogen peroxide from 4h	20624163
HL-60	Function Assay	10-500 nM	4 h		decreases the histone deacetylase (HDAC) activity	20624163
HP100	Function Assay	10-500 nM	4 h		decreases the histone deacetylase (HDAC) activity	20624163
11z	Kinase Assay	3-100 nM			reduces HDAC enzymatic activity (IC50 = 6.5 ± 0.6 nmol/L)	20605144
SKOV-3	Growth Inhibition Assay	4/8/16 nM	48 h		inhibits cell growth in a concentration-dependent manner	20404564
OVCAR-3	Growth Inhibition Assay	4/8/16 nM	48 h		inhibits cell growth in a concentration-dependent manner	20404564
HBL-2	Growth Inhibition Assay	2-10 nM	24 h		IC50=4.3 nM	20068080
Jeko-1	Growth Inhibition Assay	2-50 nM	24 h		IC50=11 nM	20068080
Granta-519	Growth Inhibition Assay	5-40 nM	24 h		IC50=58.5 nM	20068080
L1236	Cytotoxicity Assay	1 nM-100 μM	48 h		EC50=0.07 μM	19233470
L428	Cytotoxicity Assay	1 nM-100 μM	48 h		EC50=0.43 μM	19233470
KM-H2	Cytotoxicity Assay	1 nM-100 μM	48 h		EC50=0.58 μM	19233470
L540Cy	Cytotoxicity Assay	1 nM-100 μM	48 h		EC50=0.16 μM	19233470
G401	Function Assay	10 nM	24/48/72 h	DMSO	increases CDKN1C expression	19221586
STM91-01	Function Assay	10 nM	24/48/72 h	DMSO	increases CDKN1C expression	19221586
SJSC	Function Assay	10 nM	24/48/72 h	DMSO	increases CDKN1C expression	19221586
BT16	Function Assay	10 nM	24/48/72 h	DMSO	increases CDKN1C expression	19221586
NCI-H1299	Growth Inhibition Assay				IC50=4.6±0.2 ng/ml	19179890
NCI-2882	Growth Inhibition Assay				IC50=1.6±0.04 ng/ml	19179890
HCC95	Growth Inhibition Assay				IC50=2.5±0.05 ng/ml	19179890
NCI-H23	Growth Inhibition Assay				IC50=2.9±0.2 ng/ml	19179890
NCI-H157	Growth Inhibition Assay				IC50=1.6±0.02 ng/ml	19179890
NCI-H460	Growth Inhibition Assay				IC50=2.1±0.07 ng/ml	19179890
NCI-H1975	Growth Inhibition Assay				IC50=1.3±0.04 ng/ml	19179890
NCI-H820	Growth Inhibition Assay				IC50=2.4±0.1 ng/ml	19179890
NCI-H1650	Growth Inhibition Assay				IC50=4.9±0.3 ng/ml	19179890
DTC1	Growth Inhibition Assay				IC50=0.51 nM	18566246
KAO	Growth Inhibition Assay				IC50=0.91 nM	18566246
SU-CCS-1	Growth Inhibition Assay				IC50=0.89 nM	18566246
SYO-1	Growth Inhibition Assay				IC50=0.67 nM	18566246
FUJI	Growth Inhibition Assay				IC50=1.31 nM	18566246
SKNMC	Growth Inhibition Assay				IC50=1.17 nM	18566246
402-91	Growth Inhibition Assay				IC50=1.26 nM	18566246
1765-92	Growth Inhibition Assay				IC50=1.77 nM	18566246
JN-DSRCT-1	Growth Inhibition Assay				IC50=1.25 nM	18566246
NMS-2PC	Growth Inhibition Assay				IC50=0.81 nM	18566246
HL60	Growth Inhibition Assay				IC50=1.86 nM	18566246
A549	Growth Inhibition Assay				IC50=3.24 nM	18566246
SW480	Growth Inhibition Assay				IC50=2.69 nM	18566246
MCF7	Growth Inhibition Assay				IC50=3.55 nM	18566246
PC-3	Growth Inhibition Assay				IC50=2.51 nM	18566246
MMRU	Growth Inhibition Assay				IC50=2.57 nM	18566246
Hs68	Growth Inhibition Assay				IC50=>10 nM	18566246
hMSC-001F	Growth Inhibition Assay				IC50=>10 nM	18566246
mammalian cells	Function assay				Inhibition of Histone deacetylase 4 in mammalian cells, IC50 = 0.51 μM.	14584932
mammalian cells	Function assay				Inhibition of Histone deacetylase 1 induced acetylated histone in mammalian cells., EC50 = 36 μM.	14584932
MCF7	Growth inhibition assay				Growth inhibition of MCF7 cells, IC50 = 0.00075 μM.	17958342
A498	Cytotoxicity assay		6 days		Cytotoxicity against human A498 cells after 6 days by MTT assay, TGI = 0.028 μM.	21967146
COLO205	Cytotoxicity assay		6 days		Cytotoxicity against human COLO205 cells after 6 days by MTT assay, TGI = 0.031 μM.	21967146
U251	Cytotoxicity assay		6 days		Cytotoxicity against human U251 cells after 6 days by MTT assay, TGI = 0.031 μM.	21967146
RXF393	Cytotoxicity assay		6 days		Cytotoxicity against human RXF393 cells after 6 days by MTT assay, TGI = 0.062 μM.	21967146
MDA-MB-468	Cytotoxicity assay		6 days		Cytotoxicity against human MDA-MB-468 cells after 6 days by MTT assay, TGI = 0.09 μM.	21967146
COLO205	Cytotoxicity assay		6 days		Cytotoxicity against human COLO205 cells after 6 days by MTT assay, LC50 = 0.092 μM.	21967146
UACC257	Cytotoxicity assay		6 days		Cytotoxicity against human UACC257 cells after 6 days by MTT assay, TGI = 0.095 μM.	21967146
U251	Cytotoxicity assay		6 days		Cytotoxicity against human U251 cells after 6 days by MTT assay, LC50 = 0.13 μM.	21967146
A498	Cytotoxicity assay		6 days		Cytotoxicity against human A498 cells after 6 days by MTT assay, LC50 = 0.2 μM.	21967146
NCI-H322M	Cytotoxicity assay		6 days		Cytotoxicity against human NCI-H322M cells after 6 days by MTT assay, TGI = 0.23 μM.	21967146
SF295	Cytotoxicity assay		6 days		Cytotoxicity against human SF295 cells after 6 days by MTT assay, TGI = 0.25 μM.	21967146
RXF393	Cytotoxicity assay		6 days		Cytotoxicity against human RXF393 cells after 6 days by MTT assay, LC50 = 0.3 μM.	21967146
NCI60	Cytotoxicity assay		6 days		Cytotoxicity against human NCI60 cells after 6 days by MTT assay, TGI = 0.33 μM.	21967146
SN12C	Cytotoxicity assay		6 days		Cytotoxicity against human SN12C cells after 6 days by MTT assay, TGI = 0.34 μM.	21967146
MDA-MB-231	Cytotoxicity assay		6 days		Cytotoxicity against human MDA-MB-231 cells after 6 days by MTT assay, TGI = 0.35 μM.	21967146
ACHN	Cytotoxicity assay		6 days		Cytotoxicity against human ACHN cells after 6 days by MTT assay, TGI = 0.73 μM.	21967146
SN12C	Cytotoxicity assay		6 days		Cytotoxicity against human SN12C cells after 6 days by MTT assay, LC50 = 1.5 μM.	21967146
UO31	Cytotoxicity assay		6 days		Cytotoxicity against human UO31 cells after 6 days by MTT assay, TGI = 1.55 μM.	21967146
Caki1	Cytotoxicity assay		6 days		Cytotoxicity against human Caki1 cells after 6 days by MTT assay, TGI = 1.89 μM.	21967146
NCI60	Cytotoxicity assay		6 days		Cytotoxicity against human NCI60 cells after 6 days by MTT assay, LC50 = 3.5 μM.	21967146
MDA-MB-231	Cytotoxicity assay		6 days		Cytotoxicity against human MDA-MB-231 cells after 6 days by MTT assay, LC50 = 4.08 μM.	21967146
MDA-MB-468	Cytotoxicity assay		6 days		Cytotoxicity against human MDA-MB-468 cells after 6 days by MTT assay, LC50 = 4.14 μM.	21967146
ACHN	Cytotoxicity assay		6 days		Cytotoxicity against human ACHN cells after 6 days by MTT assay, LC50 = 5.37 μM.	21967146
UACC257	Cytotoxicity assay		6 days		Cytotoxicity against human UACC257 cells after 6 days by MTT assay, LC50 = 5.46 μM.	21967146
NCI-H322M	Cytotoxicity assay		6 days		Cytotoxicity against human NCI-H322M cells after 6 days by MTT assay, LC50 = 9.02 μM.	21967146
SF295	Cytotoxicity assay		6 days		Cytotoxicity against human SF295 cells after 6 days by MTT assay, LC50 = 10.2 μM.	21967146
Caki1	Cytotoxicity assay		6 days		Cytotoxicity against human Caki1 cells after 6 days by MTT assay, LC50 = 20.9 μM.	21967146
NCI-H23	Antitumor assay	1.6 to 2.4 mg/kg	up to 5 days		Antitumor activity against human NCI-H23 cells implanted intraperitoneally in mouse assessed as inhibition of tumor cell growth at 1.6 to 2.4 mg/kg, ip administered on day 1 to 4 measured on day 5 by hollow fiber assay	21967146
NCI-H522	Antitumor assay	1.6 to 2.4 mg/kg	up to 5 days		Antitumor activity against human NCI-H522 cells implanted intraperitoneally in mouse assessed as inhibition of tumor cell growth at 1.6 to 2.4 mg/kg, ip administered on day 1 to 4 measured on day 5 by hollow fiber assay	21967146
OVCAR5	Antitumor assay	1.6 to 2.4 mg/kg	up to 5 days		Antitumor activity against human OVCAR5 cells implanted intraperitoneally in mouse assessed as inhibition of tumor cell growth at 1.6 to 2.4 mg/kg, ip administered on day 1 to 4 measured on day 5 by hollow fiber assay	21967146
SW620	Antitumor assay	1.6 to 2.4 mg/kg	up to 5 days		Antitumor activity against human SW620 cells implanted intraperitoneally in mouse assessed as inhibition of tumor cell growth at 1.6 to 2.4 mg/kg, ip administered on day 1 to 4 measured on day 5 by hollow fiber assay	21967146
MDA-MB-435	Antitumor assay	1.6 to 2.4 mg/kg	up to 5 days		Antitumor activity against human MDA-MB-435 cells implanted intraperitoneally in mouse assessed as inhibition of tumor cell growth at 1.6 to 2.4 mg/kg, ip administered on day 1 to 4 measured on day 5 by hollow fiber assay	21967146
COLO205	Antitumor assay	1.6 to 2.4 mg/kg	up to 5 days		Antitumor activity against human COLO205 cells implanted intraperitoneally in mouse assessed as inhibition of tumor cell growth at 1.6 to 2.4 mg/kg, ip administered on day 1 to 4 measured on day 5 by hollow fiber assay	21967146
LOXIMVI	Antitumor assay	1.6 to 2.4 mg/kg	up to 5 days		Antitumor activity against human LOXIMVI cells implanted intraperitoneally in mouse assessed as inhibition of tumor cell growth at 1.6 to 2.4 mg/kg, ip administered on day 1 to 4 measured on day 5 by hollow fiber assay	21967146
UACC62	Antitumor assay	1.6 to 2.4 mg/kg	up to 5 days		Antitumor activity against human UACC62 cells implanted intraperitoneally in mouse assessed as inhibition of tumor cell growth at 1.6 to 2.4 mg/kg, ip administered on day 1 to 4 measured on day 5 by hollow fiber assay	21967146
MDA-MB-231	Antitumor assay	1.6 to 2.4 mg/kg	up to 5 days		Antitumor activity against human MDA-MB-231 cells implanted intraperitoneally in mouse assessed as inhibition of tumor cell growth at 1.6 to 2.4 mg/kg, ip administered on day 1 to 4 measured on day 5 by hollow fiber assay	21967146
SF295	Antitumor assay	1.6 to 2.4 mg/kg	up to 5 days		Antitumor activity against human SF295 cells implanted intraperitoneally in mouse assessed as inhibition of tumor cell growth at 1.6 to 2.4 mg/kg, ip administered on day 1 to 4 measured on day 5 by hollow fiber assay	21967146
U251	Antitumor assay	1.6 to 2.4 mg/kg	up to 5 days		Antitumor activity against human U251 cells implanted intraperitoneally in mouse assessed as inhibition of tumor cell growth at 1.6 to 2.4 mg/kg, ip administered on day 1 to 4 measured on day 5 by hollow fiber assay	21967146
OVRAC3	Antitumor assay	1.6 to 2.4 mg/kg	up to 5 days		Antitumor activity against human OVRAC3 cells implanted intraperitoneally in mouse assessed as inhibition of tumor cell growth at 1.6 to 2.4 mg/kg, ip administered on day 1 to 4 measured on day 5 by hollow fiber assay	21967146
LLC	Function assay				Inhibition of HDAC-mediated HIF-1alpha activity in mouse LLC cells, IC50 = 2 μM.	22305612
NCI-H522	Growth inhibition assay				Growth inhibition of human NCI-H522 cells by sulforhodamine B colorimetric method, GI50 = 0.0018 μM.	23313638
LOXIMVI	Growth inhibition assay				Growth inhibition of human LOXIMVI cells by sulforhodamine B colorimetric method, GI50 = 0.0025 μM.	23313638
A549	Growth inhibition assay				Growth inhibition of human A549 cells by sulforhodamine B colorimetric method, GI50 = 0.0026 μM.	23313638
OVCAR5	Growth inhibition assay				Growth inhibition of human OVCAR5 cells by sulforhodamine B colorimetric method, GI50 = 0.0028 μM.	23313638
MKN74	Growth inhibition assay				Growth inhibition of human MKN74 cells by sulforhodamine B colorimetric method, GI50 = 0.003 μM.	23313638
NCI-H460	Growth inhibition assay				Growth inhibition of human NCI-H460 cells by sulforhodamine B colorimetric method, GI50 = 0.003 μM.	23313638
HCT116	Growth inhibition assay				Growth inhibition of human HCT116 cells by sulforhodamine B colorimetric method, GI50 = 0.0031 μM.	23313638
HCC2998	Growth inhibition assay				Growth inhibition of human HCC2998 cells by sulforhodamine B colorimetric method, GI50 = 0.0031 μM.	23313638
MKN1	Growth inhibition assay				Growth inhibition of human MKN1 cells by sulforhodamine B colorimetric method, GI50 = 0.0032 μM.	23313638
SKOV3	Growth inhibition assay				Growth inhibition of human SKOV3 cells by sulforhodamine B colorimetric method, GI50 = 0.0033 μM.	23313638
HT-29	Growth inhibition assay				Growth inhibition of human HT-29 cells by sulforhodamine B colorimetric method, GI50 = 0.0033 μM.	23313638
KM12	Growth inhibition assay				Growth inhibition of human KM12 cells by sulforhodamine B colorimetric method, GI50 = 0.0034 μM.	23313638
DMS114	Growth inhibition assay				Growth inhibition of human DMS114 cells by sulforhodamine B colorimetric method, GI50 = 0.0036 μM.	23313638
SF539	Growth inhibition assay				Growth inhibition of human SF539 cells by sulforhodamine B colorimetric method, GI50 = 0.0036 μM.	23313638
U251	Growth inhibition assay				Growth inhibition of human U251 cells by sulforhodamine B colorimetric method, GI50 = 0.0039 μM.	23313638
SF295	Growth inhibition assay				Growth inhibition of human SF295 cells by sulforhodamine B colorimetric method, GI50 = 0.004 μM.	23313638
MCF7	Growth inhibition assay				Growth inhibition of human MCF7 cells by sulforhodamine B colorimetric method, GI50 = 0.0042 μM.	23313638
NCI-H23	Growth inhibition assay				Growth inhibition of human NCI-H23 cells by sulforhodamine B colorimetric method, GI50 = 0.0046 μM.	23313638
OVCAR3	Growth inhibition assay				Growth inhibition of human OVCAR3 cells by sulforhodamine B colorimetric method, GI50 = 0.0046 μM.	23313638
MKN7	Growth inhibition assay				Growth inhibition of human MKN7 cells by sulforhodamine B colorimetric method, GI50 = 0.0049 μM.	23313638
SF268	Growth inhibition assay				Growth inhibition of human SF268 cells by sulforhodamine B colorimetric method, GI50 = 0.0049 μM.	23313638
MDA-MB-231	Growth inhibition assay				Growth inhibition of human MDA-MB-231 cells by sulforhodamine B colorimetric method, GI50 = 0.0055 μM.	23313638
OVCAR8	Growth inhibition assay				Growth inhibition of human OVCAR8 cells by sulforhodamine B colorimetric method, GI50 = 0.0055 μM.	23313638
DMS273	Growth inhibition assay				Growth inhibition of human DMS273 cells by sulforhodamine B colorimetric method, GI50 = 0.0058 μM.	23313638
DU145	Growth inhibition assay				Growth inhibition of human DU145 cells by sulforhodamine B colorimetric method, GI50 = 0.006 μM.	23313638
RXF631L	Growth inhibition assay				Growth inhibition of human RXF631L cells by sulforhodamine B colorimetric method, GI50 = 0.0066 μM.	23313638
HBC4	Growth inhibition assay				Growth inhibition of human HBC4 cells by sulforhodamine B colorimetric method, GI50 = 0.0069 μM.	23313638
SNB75	Growth inhibition assay				Growth inhibition of human SNB75 cells by sulforhodamine B colorimetric method, GI50 = 0.0072 μM.	23313638
BSY1	Growth inhibition assay				Growth inhibition of human BSY1 cells by sulforhodamine B colorimetric method, GI50 = 0.0085 μM.	23313638
NCI-H226	Growth inhibition assay				Growth inhibition of human NCI-H226 cells by sulforhodamine B colorimetric method, GI50 = 0.0089 μM.	23313638
SNB78	Growth inhibition assay				Growth inhibition of human SNB78 cells by sulforhodamine B colorimetric method, GI50 = 0.0096 μM.	23313638
HBC5	Growth inhibition assay				Growth inhibition of human HBC5 cells by sulforhodamine B colorimetric method, GI50 = 0.013 μM.	23313638
MKN45	Growth inhibition assay				Growth inhibition of human MKN45 cells by sulforhodamine B colorimetric method, GI50 = 0.014 μM.	23313638
MKN28	Growth inhibition assay				Growth inhibition of human MKN28 cells by sulforhodamine B colorimetric method, GI50 = 0.017 μM.	23313638
PC3	Growth inhibition assay				Growth inhibition of human PC3 cells by sulforhodamine B colorimetric method, GI50 = 0.018 μM.	23313638
ACHN	Growth inhibition assay				Growth inhibition of human ACHN cells by sulforhodamine B colorimetric method, GI50 = 0.02 μM.	23313638
OVCAR4	Growth inhibition assay				Growth inhibition of human OVCAR4 cells by sulforhodamine B colorimetric method, GI50 = 0.02 μM.	23313638
St-4	Growth inhibition assay				Growth inhibition of human St-4 cells by sulforhodamine B colorimetric method, GI50 = 0.022 μM.	23313638
HCT15	Growth inhibition assay				Growth inhibition of human HCT15 cells by sulforhodamine B colorimetric method, GI50 = 0.45 μM.	23313638
CD4+ T	Function assay		7 days		Reactivation of latent HIV1 NL4-3-Luc expression in human naive CD4+ T cells treated 7 days post-infection measured after 48 hrs by luminescence plate reader analysis, EC50 = 0.003 μM.	24495105
NCI-H522	Cytotoxicity assay				Cytotoxicity against human NCI-H522 cells by SRB assay, GI50 = 0.0018 μM.	24589486
LOXIMVI	Cytotoxicity assay				Cytotoxicity against human LOXIMVI cells by SRB assay, GI50 = 0.0025 μM.	24589486
A549	Cytotoxicity assay				Cytotoxicity against human A549 cells by SRB assay, GI50 = 0.0026 μM.	24589486
OVCAR5	Cytotoxicity assay				Cytotoxicity against human OVCAR5 cells by SRB assay, GI50 = 0.0028 μM.	24589486
NCI-H460	Cytotoxicity assay				Cytotoxicity against human NCI-H460 cells by SRB assay, GI50 = 0.003 μM.	24589486
MKN74	Cytotoxicity assay				Cytotoxicity against human MKN74 cells by SRB assay, GI50 = 0.003 μM.	24589486
HCC2998	Cytotoxicity assay				Cytotoxicity against human HCC2998 cells by SRB assay, GI50 = 0.0031 μM.	24589486
HCT116	Cytotoxicity assay				Cytotoxicity against human HCT116 cells by SRB assay, GI50 = 0.0031 μM.	24589486
MKN1	Cytotoxicity assay				Cytotoxicity against human MKN1 cells by SRB assay, GI50 = 0.0032 μM.	24589486
HT-29	Cytotoxicity assay				Cytotoxicity against human HT-29 cells by SRB assay, GI50 = 0.0033 μM.	24589486
SKOV3	Cytotoxicity assay				Cytotoxicity against human SKOV3 cells by SRB assay, GI50 = 0.0033 μM.	24589486
KM12	Cytotoxicity assay				Cytotoxicity against human KM12 cells by SRB assay, GI50 = 0.0034 μM.	24589486
SF539	Cytotoxicity assay				Cytotoxicity against human SF539 cells by SRB assay, GI50 = 0.0036 μM.	24589486
293T	Function assay		30 mins		Inhibition of human HDAC1 expressed in human 293T cells using Ac-KGLGK(Ac)-MCA as substrate after 30 mins by fluorescence assay, IC50 = 0.0036 μM.	24589486
DMS114	Cytotoxicity assay				Cytotoxicity against human DMS114 cells by SRB assay, GI50 = 0.0036 μM.	24589486
U251	Cytotoxicity assay				Cytotoxicity against human U251 cells by SRB assay, GI50 = 0.0039 μM.	24589486
SF295	Cytotoxicity assay				Cytotoxicity against human SF295 cells by SRB assay, GI50 = 0.004 μM.	24589486
MCF7	Cytotoxicity assay				Cytotoxicity against human MCF7 cells by SRB assay, GI50 = 0.0042 μM.	24589486
OVCAR3	Cytotoxicity assay				Cytotoxicity against human OVCAR3 cells by SRB assay, GI50 = 0.0046 μM.	24589486
NCI-H23	Cytotoxicity assay				Cytotoxicity against human NCI-H23 cells by SRB assay, GI50 = 0.0046 μM.	24589486
SF268	Cytotoxicity assay				Cytotoxicity against human SF268 cells by SRB assay, GI50 = 0.0049 μM.	24589486
MKN7	Cytotoxicity assay				Cytotoxicity against human MKN7 cells by SRB assay, GI50 = 0.0049 μM.	24589486
OVCAR8	Cytotoxicity assay				Cytotoxicity against human OVCAR8 cells by SRB assay, GI50 = 0.0055 μM.	24589486
MDA-MB-231	Cytotoxicity assay				Cytotoxicity against human MDA-MB-231 cells by SRB assay, GI50 = 0.0055 μM.	24589486
DMS273	Cytotoxicity assay				Cytotoxicity against human DMS273 cells by SRB assay, GI50 = 0.0058 μM.	24589486
DU145	Cytotoxicity assay				Cytotoxicity against human DU145 cells by SRB assay, GI50 = 0.006 μM.	24589486
RXF631L	Cytotoxicity assay				Cytotoxicity against human RXF631L cells by SRB assay, GI50 = 0.0066 μM.	24589486
HBC4	Cytotoxicity assay				Cytotoxicity against human HBC4 cells by SRB assay, GI50 = 0.0069 μM.	24589486
SNB75	Cytotoxicity assay				Cytotoxicity against human SNB75 cells by SRB assay, GI50 = 0.0072 μM.	24589486
BSY1	Cytotoxicity assay				Cytotoxicity against human BSY1 cells by SRB assay, GI50 = 0.0085 μM.	24589486
NCI-H226	Cytotoxicity assay				Cytotoxicity against human NCI-H226 cells by SRB assay, GI50 = 0.0089 μM.	24589486
SNB78	Cytotoxicity assay				Cytotoxicity against human SNB78 cells by SRB assay, GI50 = 0.0096 μM.	24589486
HBC5	Cytotoxicity assay				Cytotoxicity against human HBC5 cells by SRB assay, GI50 = 0.013 μM.	24589486
MKN45	Cytotoxicity assay				Cytotoxicity against human MKN45 cells by SRB assay, GI50 = 0.014 μM.	24589486
MKN28	Cytotoxicity assay				Cytotoxicity against human MKN28 cells by SRB assay, GI50 = 0.017 μM.	24589486
PC3	Cytotoxicity assay				Cytotoxicity against human PC3 cells by SRB assay, GI50 = 0.018 μM.	24589486
ACHN	Cytotoxicity assay				Cytotoxicity against human ACHN cells by SRB assay, GI50 = 0.02 μM.	24589486
OVCAR4	Cytotoxicity assay				Cytotoxicity against human OVCAR4 cells by SRB assay, GI50 = 0.02 μM.	24589486
St-4	Cytotoxicity assay				Cytotoxicity against human St-4 cells by SRB assay, GI50 = 0.022 μM.	24589486
293T	Function assay		30 mins		Inhibition of mouse HDAC6 expressed in human 293T cells using Ac-KGLGK(Ac)-MCA as substrate after 30 mins by fluorescence assay, IC50 = 0.39 μM.	24589486
HCT15	Cytotoxicity assay				Cytotoxicity against human HCT15 cells by SRB assay, GI50 = 0.45 μM.	24589486
mink Mv1Lu	Function assay		24 hrs		Increase in human wild type p21 protein expression in mink Mv1Lu cells after 24 hrs by p21 promoter assay in presence of 0.1 mM dithiothreitol, EC1000 = 0.0157 μM.	24997578
HCT116	Antiproliferative assay		48 hrs		Antiproliferative activity against human HCT116 cells after 48 hrs in presence of DTT by MTT assay, IC50 = 0.003 μM.	25147612
MOLT4	Antiproliferative assay		72 hrs		Antiproliferative activity against human MOLT4 cells after 72 hrs by CCK8 assay, GI50 = 0.00206 μM.	26331334
DU145	Antiproliferative assay		72 hrs		Antiproliferative activity against human DU145 cells after 72 hrs by CCK8 assay, GI50 = 0.00255 μM.	26331334
U937	Antiproliferative assay		72 hrs		Antiproliferative activity against human U937 cells after 72 hrs by CCK8 assay, GI50 = 0.00341 μM.	26331334
HLF	Antiproliferative assay		72 hrs		Antiproliferative activity against human HLF cells after 72 hrs by CCK8 assay, GI50 = 0.00489 μM.	26331334
WI38	Antiproliferative assay		72 hrs		Antiproliferative activity against human WI38 cells after 72 hrs by CCK8 assay, GI50 = 0.00539 μM.	26331334
U937	Function assay		24 hrs		Inhibition of HDAC6 in human U937 cells assessed as reduction of alpha-tubilin acetylation at 5 nM to 5 uM after 24 hrs by Western blot analysis	26331334
HCT116	Antiproliferative assay		72 hrs		Antiproliferative activity against human HCT116 cells assessed as cell viability incubated for 72 hrs by coulter counter method, IC50 = 0.028 μM.	26481659
IGROV1/Pt1	Antiproliferative assay		72 hrs		Antiproliferative activity against human IGROV1/Pt1 cells assessed as cell viability incubated for 72 hrs by coulter counter method, IC50 = 0.08 μM.	26481659
IGROV1	Antiproliferative assay		72 hrs		Antiproliferative activity against human IGROV1 cells assessed as cell viability incubated for 72 hrs by coulter counter method, IC50 = 0.22 μM.	26481659
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Informazioni chimiche, conservazione e stabilità (Chemical Information, Storage & Stability)

Peso molecolare	540.7	Formula	C₂₄H₃₆N₄O₆S₂	Conservazione (Dalla data di ricezione)	3 anni-20°Cpolvere
N. CAS	128517-07-7	--		Conservazione delle soluzioni stock	1 anno-80°Cin solvente 1 mese-20°Cin solvente
Sinonimi	FK228, Depsipeptide, FR 901228, NSC 630176,			Smiles	CC=C1C(=O)NC(C(=O)OC2CC(=O)NC(C(=O)NC(CSSCCC=C2)C(=O)N1)C(C)C)C(C)C

Solubilità (Solubility)

In vitro
Lotto:

DMSO : 10 mg/mL (18.49 mM)
(Il DMSO contaminato da umidità può ridurre la solubilità. Utilizzare DMSO fresco e anidro.)

Water : Insoluble

Ethanol : Insoluble

Calcolatore di Molarità

Massa	Concentrazione	Volume	Peso molecolare
=	×	×

Calcolatore di Diluizione Calcolatore del Peso Molecolare

In vivo Lotto:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 95% Corn oil Validato dai laboratori Selleck. Se necessiti di modifiche a questa formulazione, contatta il nostro team di vendita per test personalizzati.	0.750mg/ml (1.39mM)	Taking the 1 mL working solution as an example, add 50 μL of 15 mg/mL clarified DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validato dai laboratori Selleck. Se necessiti di modifiche a questa formulazione, contatta il nostro team di vendita per test personalizzati.	0.150mg/ml (0.28mM)	Taking the 1 mL working solution as an example, add 50 μL of 3 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	2% DMSO 1 30% PEG 300 2 5%Tween 80 3 ddH2O Validato dai laboratori Selleck. Se necessiti di modifiche a questa formulazione, contatta il nostro team di vendita per test personalizzati.	5.000mg/ml (9.25mM)	Taking the 1 mL working solution as an example, add 20 μL of 100 mg/ml clear DMSO stock solution to 300 μL of PEG300, mix evenly to clarify it; add 50 μL Tween-80 to the above system, mix evenly to clarify it; Then continue to add 630 μL ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.

Calcolatore di formulazione in vivo (Soluzione chiara)

Passo 1: Inserire le informazioni di seguito (Consigliato: Un animale aggiuntivo per tenere conto della perdita durante l'esperimento)

Dosaggio: mg/kg Peso medio degli animali: g Volume di dosaggio per animale:μL Numero di animali:

Passo 2: Inserire la formulazione in vivo (Questo è solo il calcolatore, non la formulazione. Contattateci prima se non c'è una formulazione in vivo nella sezione Solubilità.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Risultati del calcolo:

Concentrazione di lavoro: mg/ml;

Metodo per preparare il liquido master di DMSO: mg farmaco predissolto in μL DMSO ( Concentrazione del liquido master mg/mL, Vi preghiamo di contattarci prima se la concentrazione supera la solubilità del DMSO del lotto del farmaco. )

Metodo per preparare la formulazione in vivo: Prendere μL DMSO liquido master, quindi aggiungereμL PEG300, mescolare e chiarire, quindi aggiungereμL Tween 80, mescolare e chiarire, quindi aggiungere μL ddH₂O, mescolare e chiarire.

Metodo per preparare la formulazione in vivo: Prendere μL DMSO liquido master, quindi aggiungere μL Olio di mais, mescolare e chiarire.

Nota: 1. Si prega di assicurarsi che il liquido sia limpido prima di aggiungere il solvente successivo.
2. Assicurarsi di aggiungere il/i solvente/i in ordine. È necessario assicurarsi che la soluzione ottenuta, nell'aggiunta precedente, sia una soluzione limpida prima di procedere all'aggiunta del solvente successivo. Metodi fisici come il vortex, gli ultrasuoni o il bagno d'acqua calda possono essere utilizzati per facilitare la dissoluzione.

Meccanismo d'azione (Mechanism of Action)

Caratteristiche	More effective than other classical HDAC inhibitors such as TSA, TPX, and butyrate.
Targets/IC₅₀/Ki	HDAC1 (Cell-free assay) 36 nM HDAC2 (Cell-free assay) 47 nM
In vitro	A differenza del TSA, la forma attiva redFK di Romidepsin inibisce fortemente HDAC1 e HDAC2 con IC50 di 1,6 nM e 3,9 nM, rispettivamente, ma è relativamente debole nell'inibire HDAC4 e HDAC6 con IC50 25 nM e 790 nM, rispettivamente. Questo composto è 17-23 volte più debole di redFK nell'inibire questi HDAC con IC50 di 36 nM, 47 nM, 510 nM e 14 μM, rispettivamente. Il trattamento con questa sostanza chimica nelle cellule HeLa induce l'acetilazione degli istoni e l'espressione di p21 con EC50 di 3,0 nM, più fortemente di redFK con EC50 di 11 nM a causa dell'instabilità di redFK. Oltre all'arresto in G2/M, questo composto provoca la down-regulation della ciclina D1 e un'induzione di p21 indipendente da p53, portando all'inibizione di CDK e alla defosforilazione di Rb con conseguente arresto della crescita nella fase G1 precoce. È 100 volte più potente del TSA e 1.000.000 di volte più potente del butirrato nell'inibire la proliferazione delle cellule A549. Questo agente inibisce la crescita delle cellule U-937, K562 e CCRF-CEM con IC50 di 5,92 nM, 8,36 nM e 6,95 nM, rispettivamente. Promuove l'apoptosi nelle cellule di leucemia linfatica cronica (LLC) a una concentrazione corrispondente a quella in cui si verifica l'acetilazione di H3 e H4 e l'inibizione di HDAC, coinvolgendo selettivamente l'attivazione della caspasi 8 e della caspasi effettrice 3, nonché la down-regulation della proteina c-FLIP. In 11 delle 13 (85%) linee cellulari di carcinoma a cellule renali e in 16 delle 37 (43%) altre linee cellulari tumorali, questo composto up-regola i recettori di morte tumorale e potenzia l'uccisione tumorale mediata dalle cellule natural killer (NK). Esibisce citotossicità dipendente dalla concentrazione contro un pannello di linee cellulari di linfoma a cellule del mantello (MCL).
Saggio chinasico	Attività inibitoria di HDAC
Saggio chinasico	Per il saggio enzimatico, 10 μL di istoni marcati con [³H]acetile (25.000 cpm/10 μg) vengono aggiunti a 90 μL della frazione enzimatica HDAC estratta da cellule 293T che sovraesprimono HDAC1 o HDAC2 in presenza di concentrazioni crescenti di Romidepsin, e la miscela viene incubata a 37 °C per 15 minuti. La reazione enzimatica è lineare per almeno 1 ora. La reazione viene interrotta con l'aggiunta di 10 μL di HCl concentrato. L'acido [³H]acetico rilasciato viene estratto con 1 mL di etilacetato, e 0,9 mL dello strato solvente vengono prelevati in 5 mL di soluzione acquosa di scintillante II per la determinazione della radioattività. I valori di IC50 vengono determinati da almeno tre curve dose-risposta indipendenti.
In vivo	Il trattamento con Romidepsin inibisce potentemente la neovascolarizzazione dell'embrione di pollo e quella di topi adulti nel saggio del plug di Matrigel. La somministrazione di questo composto a 0,1-1 mg/kg due volte a settimana prolunga significativamente la sopravvivenza di topi portatori di linfoma U-937, con tempi di sopravvivenza mediani di 30,5 (0,56 mg/kg) e 33 giorni (0,32 mg/kg), rispettivamente (vs. 20 giorni nei topi di controllo).
Riferimenti	[1] https://pubmed.ncbi.nlm.nih.gov/12208741/ [2] https://pubmed.ncbi.nlm.nih.gov/10952788/ [3] https://pubmed.ncbi.nlm.nih.gov/12481415/ [4] https://pubmed.ncbi.nlm.nih.gov/11774279/ [5] https://pubmed.ncbi.nlm.nih.gov/12234611/ [6] https://pubmed.ncbi.nlm.nih.gov/12649137/ [7] https://pubmed.ncbi.nlm.nih.gov/16849582/ [8] https://pubmed.ncbi.nlm.nih.gov/18223231/ [9] https://pubmed.ncbi.nlm.nih.gov/20068080/

Applicazioni (Applications)

Metodi	Biomarcatori	PMID
Western blot	p21 / Cyclin D1 AcH3(K9) / Ac-α-Tubulin(K40) / Ac-NFκB2(K310) p65 / 3MeH3(K27) HDAC3 / HDAC4 / HDAC6 / HDAC2 γH2AX / PARP1 / Cleaved caspase3 / BAK / p21(waf1/cip1) / XIAP Cyclin E1 / BRCA1 / E2F1 / Cleaved PARP / H3Ac pAKT(S473) / pAKT(T308) / AKT	19682393
Growth inhibition assay	Cell viability	27444036
Immunofluorescence	SS18/TLE1 Cleaved caspase-3	27120803

Informazioni sullo studio clinico (Clinical Trial Information)

(dati da https://clinicaltrials.gov, aggiornato il 2024-05-22)

Numero NCT	Reclutamento	Condizioni	Sponsor/Collaboratori	Data di inizio	Fasi
NCT03770000	Completed	T Cell Lymphoma	Rhizen Pharmaceuticals SA	March 12 2019	Phase 1\|Phase 2
NCT02616965	Active not recruiting	Cutaneous T-cell Lymphoma (CTCL)	Fox Chase Cancer Center\|Seagen Inc.\|Celgene Corporation	February 22 2017	Phase 1
NCT02616874	Completed	HIV	IrsiCaixa\|Germans Trias i Pujol Hospital\|Fundación FLS de Lucha Contra el Sida las Enfermedades Infecciosas y la Promoción de la Salud y la Ciencia\|Hospital Clinic of Barcelona\|Hospital de Sant Pau\|HIVACAT\|University of Oxford\|BCN Checkpoint	February 2016	Phase 1

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):