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Stattic Inibitore STAT3

Name: Stattic
Brand: Selleck Chemicals
SKU: S7024
Rating: 5 (279 reviews)

N. Cat.S7024

Stattic, la prima piccola molecola non peptidica, inibisce potentemente l'attivazione di STAT3 e la traslocazione nucleare con una IC50 di 5,1 μM in saggi senza cellule, con alta selettività su STAT1. Stattic induce l'apoptosi.

Stattic STAT inibitore Chemical Structure

Struttura chimica

Peso molecolare: 211.19

Vai a

Controllo Qualità

Lotto: Purezza: 99.88%

99.88

Target correlati	EGFR JAK Pim
Altro STAT Inibitori	Napabucasin (BBI608) NSC 74859 (S3I-201) Cryptotanshinone (Tanshinone C) C188-9 (TTI-101) SH-4-54 BP-1-102 AS1517499 Nifuroxazide HO-3867 Homoharringtonine (HHT)

Coltura cellulare, trattamento e concentrazione di lavoro

Linee cellulari	Tipo di saggio	Concentrazione	Tempo di incubazione	Formulazione	Descrizione dellattività	PMID
H9c2	Function Assay	10 μM	4 h		reverses the effects of IL-27	26339633
NPC	Function Assay	0-7.5 µM			abolishes EMT-like molecular alterations, and cell migration and invasion induced by RKIP knockdown	25915430
HASMC	Function Assay	1.25-5 μM	20 min	DMSO	inhibits p-(Y)-STAT-1,3,5 signals	25849622
H9c2	Function Assay	2/10 μM	2 h	DMSO	abrogates the cytoprotective effects of IL-27 against SH	25820907
A431	Growth Inhibition Assay	2 μM	2 h		blocks EGF-reversed decreases in cell viability	25720435
A431	Growth Inhibition Assay	2 μM	2 h		increases in apoptosis induced by shikonin	25720435
SiHa	Cell Viability Assay	5-75 nM	24 h		shows morphology of a typical apoptotic cell and dose-dependent loss of cell viability	25539644
SiHa	Function Assay	5-75 nM	24 h		reduces the phosphorylation at the tyrosine residue 705	25539644
ECA109	Growth Inhibition Assay	0-20 μM	24 h		IC50=5.50 μM	25492480
TE13	Growth Inhibition Assay	0-20 μM	24 h		IC50=6.15 μM	25492480
KYSE150	Growth Inhibition Assay	0-20 μM	24 h		IC50=12.64 μM	25492480
ECA109	Clonogenic Survival Assay	0.5 μM	24 h		suppresses the clonogenic formation	25492480
TE13	Clonogenic Survival Assay	0.5 μM	24 h		suppresses the clonogenic formation	25492480
KYSE150	Clonogenic Survival Assay	0.5 μM	24 h		suppresses the clonogenic formation	25492480
ECA109	Function Assay	0.5 μM	24 h		enhances IR-induced generation of DSBs	25492480
PC3M-1E8	Function Assay	2.5/5/10 μM	0-4 h		inhibits the STAT3 activation in a dose- and time-dependent manner	25261365
PC3M-1E8	Function Assay	10 μM	24 h		downregulates Bcl-xL, survivin and c-Myc	25261365
PC3M-1E8	Function Assay	10 μM	24 h		inhibits IL-6 induced STAT3 activation and the IL-6-induced STAT3 activation	25261365
PC3M-1E8	Clonogenic Survival Assay	2.5/5/10 μM			inhibits the colony formation significantly	25261365
MDA-MB-231	Function Assay	20 μM	2 h		exhibits Snail and E-cadherin expression	25153349
H9c2	Function Assay	20 µM	30 min	DMSO	abolishes propofol-induced AKT phosphorylation at both ser473 and thr308	25105067
HaCaT	Growth Inhibition Assay	10 µM	20 min	DMSO	enhances sorafenib- and sunitinib-induced growth inhibition	25013907
Caki-1	Growth Inhibition Assay	10 µM	20 min	DMSO	enhances sorafenib- and sunitinib-induced growth inhibition	25013907
HaCaT	Apoptosis Assay	10 µM	20 min	DMSO	increases proportions of apoptotic cells due to treatment with sorafenib or sunitinib	25013907
FHL-primed hNSCs	Cell Viability Assay	0.02-5 μM	72 h		leads to the loss of cell viability at high concentration	24945434
ELL-primed hNSCs	Cell Viability Assay	0.02-5 μM	72 h		leads to the loss of cell viability at high concentration	24945434
SS	Cell Viability Assay	1-10 μM	72 h	DMSO	causes a dose-dependent inhibition of the viability	24756111
SeAx	Cell Viability Assay	1-10 μM	72 h	DMSO	causes a dose-dependent inhibition of the viability	24756111
HuT-78	Cell Viability Assay	1-10 μM	72 h	DMSO	causes a dose-dependent inhibition of the viability	24756111
CD4+	Apoptosis Assay	10 μm	24 h	DMSO	induces apoptosis strongly	24756111
MCF-7	Growth Inhibition Assay	0.469-3.75 μM	5 d		reduces cell number significantly	24728078
MCF-7/LCC1	Growth Inhibition Assay	0.469-3.75 μM	5 d		reduces cell number significantly	24728078
MCF-7/LCC9	Growth Inhibition Assay	0.469-3.75 μM	5 d		reduces cell number significantly	24728078
HaCaT	Growth Inhibition Assay	10 µM	20 min	DMSO	enhances everolimus-induced cell growth inhibition	24423131
HaCaT	Apoptosis Assay	10 µM	20 min	DMSO	enhances the apoptotic effects of everolimus	24423131
MDA-MB-231	Function Assay	10 µM	24 h	DMSO	reduces P-STAT3 expression	24376586
SUM-159	Function Assay	10 µM	24 h	DMSO	reduces P-STAT3 expression	24376586
SK-BR-3	Function Assay	10 µM	24 h	DMSO	reduces P-STAT3 expression	24376586
MCF7-HER2	Growth Inhibition Assay	0-10 μM	48 h	DMSO	induces cell death dose dependently	24297508
MCF7-HER2	Function Assay	5 μM	24 h	DMSO	diminishes Sox-2, Oct-4, and slug expression	24297508
MCF7-HER2	Function Assay	5 μM	24 h	DMSO	decreases the expression levels of EMT markers, vimentin and slug	24297508
MCF7-HER2	Growth Inhibition Assay	5 μM	24 h	DMSO	enhances cell growth inhibition combined with Herceptin	24297508
HMECs	Function Assay	10 μM	2 h		inhibits IFNα mediated phosphorylation of STAT1, STAT2 and STAT3	24211327
HTR8/SVneo	Function Assay	1 μM	1 h		suppressed OSM-induced STAT3 phosphorylation	24060241
HTR8/SVneo	Function Assay	0.5/1 μM	48 h		restores the expression of E-cadherin suppressed by OSM	24060241
HTR8/SVneo	Function Assay	1 μM	48 h		significantly increases migration by OSM	24060241
C13*	Apoptosis Assay	0-10 μM	24/48 h		induces apoptosis in a dose and time dependent manner	23962558
OV2008	Apoptosis Assay	0-10 μM	24/48 h		induces apoptosis in a dose and time dependent manner	23962558
C13*	Apoptosis Assay		24/48 h		enhances cisplatin-induced apoptosis	23962558
OV2008	Apoptosis Assay		24/48 h		enhances cisplatin-induced apoptosis	23962558
W480	Function Assay	2.5/10 μM	30 min	DMSO	sensitizes cells to chemoradiotherapy in a dose-dependent manner	23934972
SW837	Function Assay	2.5/10 μM	30 min	DMSO	sensitizes cells to chemoradiotherapy in a dose-dependent manner	23934972
T24	Function Assay	2/10/20 μM	24 h		causes dose-dependent inhibition of the CXCL12-induced increase of invading cells	23526079
CNE1	Function Assay	20 µM	48 h		blocks the IL-6 increased phosphorylation of Stat3	23382914
CNE2	Function Assay	20 µM	48 h		blocks the IL-6 increased phosphorylation of Stat3	23382914
HONE1	Function Assay	20 µM	48 h		blocks the IL-6 increased phosphorylation of Stat3	23382914
CNE1	Growth Inhibition Assay	4 μM			significantly reduces cell viability	23382914
CNE1	Function Assay	0-20 μM	0-4 h		inhibits Stat3 activation in a dose- and time-dependent manner	23382914
CNE2	Function Assay	0-20 μM	0-4 h		inhibits Stat3 activation in a dose- and time-dependent manner	23382914
HONE1	Function Assay	0-20 μM	0-4 h		inhibits Stat3 activation in a dose- and time-dependent manner	23382914
CNE1	Cell Viability Assay	0.5-64 μM	48 h		suppresses cell viability in a dose- and time-dependent manner	23382914
CNE2	Cell Viability Assay	0.5-64 μM	48 h		suppresses cell viability in a dose- and time-dependent manner	23382914
HONE1	Cell Viability Assay	0.5-64 μM	48 h		suppresses cell viability in a dose- and time-dependent manner	23382914
C666-1	Cell Viability Assay	0.5-64 μM	48 h		suppresses cell viability in a dose- and time-dependent manner	23382914
CNE1	Apoptosis Assay	10 µM	48 h		induces apoptosis	23382914
CNE2	Apoptosis Assay	10 µM	48 h		induces apoptosis	23382914
HONE1	Apoptosis Assay	10 µM	48 h		induces apoptosis	23382914
CNE2	Cell Viability Assay	1/2 μM	48 h		sensitize cells to radiotherapy	23382914
HONE1	Cell Viability Assay	1/2 μM	48 h		sensitize cells to radiotherapy	23382914
C666-1	Cell Viability Assay	1/2 μM	48 h		sensitize cells to radiotherapy	23382914
HEC-1A	Function Assay	1 μM	24 h	DMSO	blocks the MUC20-enhanced invasion triggered by 10% FBS	23262208
RL95-2	Function Assay	1 μM	24 h	DMSO	blocks the MUC20-enhanced invasion triggered by 10% FBS	23262208
HEC-1A	Function Assay	1 μM	24 h	DMSO	blocks the MUC20-enhanced invasion triggered by EGF	23262208
RL95-2	Function Assay	1 μM	24 h	DMSO	blocks the MUC20-enhanced invasion triggered by EGF	23262208
CT26	Function Assay	20 mM	1 h		suppresses HGF-induced VEGF expression	23233163
UM-SCC-17B	Growth Inhibition Assay				IC50=2.562 ± 0.409 μM, GI50=1.279 ± 0.194 μM	22770899
OSC-19	Growth Inhibition Assay				IC50=3.481 ± 0.953 μM, GI50=1.366 ± 0.770 μM	22770899
Cal33	Growth Inhibition Assay				IC50=2.282 ± 0.423 μM, GI50=1.349 ± 0.363 μM	22770899
UM-SCC-22B	Growth Inhibition Assay				IC50=2.648 ± 0.542 μM, GI50=1.320 ± 0.204 μM	22770899
UM-SCC-17B	Function Assay	0-30 μM	0-24 h		inhibits STAT3 activation dose and time dependently	22770899
OSC-19	Function Assay	0-30 μM	0-24 h		inhibits STAT3 activation dose and time dependently	22770899
Cal33	Function Assay	0-30 μM	0-24 h		inhibits STAT3 activation dose and time dependently	22770899
UM-SCC-22B	Function Assay	0-30 μM	0-24 h		inhibits STAT3 activation dose and time dependently	22770899
U-87MG	Cell Viability Assay	0-10 μM	72 h	DMSO	inhibits cell viability dose dependently	25436682
U-373MG	Cell Viability Assay	0-10 μM	72 h	DMSO	inhibits cell viability dose dependently	25436682
SH-SY5Y	Cell Viability Assay	0-10 μM	72 h	DMSO	inhibits cell viability dose dependently	25436682
Tu-9648	Cell Viability Assay	0-10 μM	72 h	DMSO	inhibits cell viability dose dependently	25436682
Neuro-2a	Cell Viability Assay	0-10 μM	72 h	DMSO	inhibits cell viability dose dependently	25436682
PCNs	Cell Viability Assay	0-10 μM	72 h	DMSO	inhibits cell viability dose dependently	25436682
PGCs	Cell Viability Assay	0-10 μM	72 h	DMSO	inhibits cell viability dose dependently	25436682
RAW264.7	Function Assay	10 μM	12 h		abrogates the mRNA expressions of JAK2, STAT1, STAT2, and STAT3 induced by DON and T-2 toxin	22454431
RAW264.7	Apoptosis Assay	5/10 μM	45 min		enhances toxins induced apoptosis and MMP loss	22454431
SW480	Cell Viability Assay	5/10/20 μM	72 h		inhibits cell viability of the ALDH+/CD133+ cells	21900397
HCT116	Cell Viability Assay	5/10/20 μM	72 h		inhibits cell viability of the ALDH+/CD133+ cells	21900397
DLD-1	Cell Viability Assay	5/10/20 μM	72 h		inhibits cell viability of the ALDH+/CD133+ cells	21900397
SNU387	Cell Viability Assay	20 μM	24 h		reduces cell viability	21311975
SNU398	Cell Viability Assay	20 μM	24 h		reduces cell viability	21311975
HepG2	Cell Viability Assay	20 μM	24 h		reduces cell viability	21311975
Huh-7	Cell Viability Assay	20 μM	24 h		reduces cell viability	21311975
VSMC	Growth Inhibition Assay	3/5/10 μM	30 min	DMSO	prevents PDGF- and thrombin-mediated VSMC proliferation in a dose-dependent manner	20847306
MDA-MB-231	Apoptosis Assay	10 μM	24 h	DMSO	induces apoptosis	17114005
MDA-MB-435S	Apoptosis Assay	10 μM	24 h	DMSO	induces apoptosis	17114005
AsPC1	Antiproliferative assay		72 hrs		Antiproliferative activity against human AsPC1 cells assessed as inhibition of cell proliferation after 72 hrs by MTS assay, IC50 = 1.32 μM.	24904966
MDA-MB-231	Antiproliferative assay		72 hrs		Antiproliferative activity against ER-negative and triple-negative human MDA-MB-231 cells assessed as inhibition of cell proliferation after 72 hrs by MTS assay, IC50 = 2.89 μM.	24904966
MCF7	Antiproliferative assay		72 hrs		Antiproliferative activity against ER-positive human MCF7 cells assessed as inhibition of cell proliferation after 72 hrs by MTS assay, IC50 = 3.6 μM.	24904966
PANC1	Antiproliferative assay		72 hrs		Antiproliferative activity against human PANC1 cells assessed as inhibition of cell proliferation after 72 hrs by MTS assay, IC50 = 3.77 μM.	24904966
MDA-MB-231	Cytotoxicity assay		48 hrs		Cytotoxicity against human MDA-MB-231 cells assessed as growth inhibition after 48 hrs by MTT assay, IC50 = 1.56 μM.	26396689
MDA-MB-435S	Cytotoxicity assay		48 hrs		Cytotoxicity against human MDA-MB-435S cells assessed as growth inhibition after 48 hrs by MTT assay, IC50 = 1.87 μM.	26396689
MCF7	Cytotoxicity assay		48 hrs		Cytotoxicity against human MCF7 cells assessed as growth inhibition after 48 hrs by MTT assay, IC50 = 2.16 μM.	26396689
A549	Cytotoxicity assay		48 hrs		Cytotoxicity against human A549 cells assessed as growth inhibition after 48 hrs by MTT assay, IC50 = 2.5 μM.	26396689
DU145	Cytotoxicity assay		48 hrs		Cytotoxicity against human DU145 cells assessed as growth inhibition after 48 hrs by MTT assay, IC50 = 2.5 μM.	26396689
PANC1	Cytotoxicity assay		48 hrs		Cytotoxicity against human PANC1 cells assessed as growth inhibition after 48 hrs by MTT assay, IC50 = 2.9 μM.	26396689
HCT116	Antiproliferative assay		72 hrs		Antiproliferative activity against human HCT116 cells after 72 hrs by MTT assay, IC50 = 1.08 μM.	27718470
MDA-MB-231	Antiproliferative assay		72 hrs		Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by MTT assay, IC50 = 1.68 μM.	27718470
MCF7	Antiproliferative assay		72 hrs		Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay, IC50 = 2.36 μM.	27718470
A549	Antiproliferative assay		72 hrs		Antiproliferative activity against human A549 cells after 72 hrs by MTT assay, IC50 = 4.4 μM.	27718470
AD293	Function assay		6 hrs		Inhibition of IFNgamma-stimulated GFP/FLAG-tagged STAT3 dimerization in human AD293 cells incubated for 6 hrs by Western blot analysis, IC50 = 5.1 μM.	30228000
MDA-MB-231	Function assay	1 to 10 uM	12 hrs		Inhibition of STAT3 phosphorylation at Tyr705 in human MDA-MB-231 cells at 1 to 10 uM after 12 hrs by western blot analysis	24904966
MDA-MB-231	Anticancer assay	1 to 10 uM	48 hrs		Anticancer activity against human MDA-MB-231 cells assessed as cell growth inhibition, apoptosis and cellular morphological changes at 1 to 10 uM after 48 hrs by light microscopy	24904966
MDA-MB-231	Function assay	1 to 10 uM	12 hrs		Decrease in STAT3 protein expression in human MDA-MB-231 cells at 1 to 10 uM after 12 hrs by western blot analysis	24904966
MCF7	Function assay		12 hrs		Inhibition of STAT3 phosphorylation at Y705 in human MCF7 cells after 12 hrs by Western blot analysis	26396689
MDA-MB-435S	Function assay		12 hrs		Inhibition of STAT3 phosphorylation at Y705 in human MDA-MB-435S cells after 12 hrs by Western blot analysis	26396689
MDA-MB-231	Function assay		12 hrs		Inhibition of STAT3 phosphorylation at Y705 in human MDA-MB-231 cells after 12 hrs by Western blot analysis	26396689
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Informazioni chimiche, conservazione e stabilità

Peso molecolare	211.19	Formula	C₈H₅NO₄S	Conservazione (Dalla data di ricezione)	3 anni-20°Cpolvere
N. CAS	19983-44-9	Scarica SDF		Conservazione delle soluzioni stock	1 anno-80°Cin solvente 1 mese-20°Cin solvente
Sinonimi	N/A			Smiles	C1=CC(=CC2=C1C=CS2(=O)=O)[N+](=O)[O-]

Solubilità

In vitro
Lotto:

DMSO : 42 mg/mL (198.87 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 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.	2.100mg/ml (9.94mM)	Taking the 1 mL working solution as an example, add 50 μL of 42 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.
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.	1.000mg/ml (4.74mM)	Taking the 1 mL working solution as an example, add 50 μL of 10.9 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 make it clear. Volume up to 1 mL. The mixed solution should be used immediately for optimal results.
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.	0.800mg/ml (3.79mM)	Taking the 1 mL working solution as an example, add 50 μL of 16 mg/ml clear 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.
Clear solution	10%DMSO 1 40%PEG300 2 5%Tween80 3 45%ddH2O Validato dai laboratori Selleck. Se necessiti di modifiche a questa formulazione, contatta il nostro team di vendita per test personalizzati.	4.800mg/ml (22.73mM)	Taking the 1 mL working solution as an example, add 100 μL of 48 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 make it clear; then continue to add 450 μL of 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 lesperimento)

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 cè 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, nellaggiunta precedente, sia una soluzione limpida prima di procedere allaggiunta del solvente successivo. Metodi fisici come il vortex, gli ultrasuoni o il bagno dacqua calda possono essere utilizzati per facilitare la dissoluzione.

Meccanismo dazione

Caratteristiche	Stattic is the first non-peptide small molecule with inhibitory activity against STAT3 SH2 domain regardless of the STAT3 phosphorylation state in vitro.
Targets/IC₅₀/Ki	STAT3 (Cell-free assay) 5.1 μM
In vitro	Stattic inibisce il legame di un peptide contenente fosfotirosina derivato dal recettore gp130 al dominio SH2 di STAT3 in modo fortemente dipendente dalla temperatura. Questo composto ha solo un effetto molto debole sul legame di un peptide tirosina-fosforilato al dominio SH2 della tirosina chinasi Lck. E non inibisce la dimerizzazione di altri due fattori di trascrizione dimerici (c-Myc/Max e Jun/Jun). Inibisce anche i fosfopeptidi marcati con fluoresceina ai domini SH2 di STAT1 e STAT5b. Questa sostanza chimica inibisce selettivamente il legame del DNA degli omodimeri STAT3 a una concentrazione di 10 μM. È stato dimostrato che inibisce la fosforilazione cellulare di STAT3 a Tyr705 con scarso effetto sulla fosforilazione di STAT1 a Tyr701 (nelle cellule HepG2) o sulla fosforilazione di JAK1, JAK2 e c-Src (nelle cellule MDA-MB-231 e MDA-MB-235S). Questo composto aumenta il tasso apoptotico delle linee cellulari di cancro al seno dipendenti da STAT3.
Saggio chinasico	Screening ad alto rendimento e saggi di polarizzazione della fluorescenza
Saggio chinasico	Lo screening viene eseguito a circa 30 °C. La specificità dei risultati dello screening viene convalidata in saggi analoghi per il legame dei composti di prova ai domini SH2 di STAT1, STAT5 e Lck. La concentrazione finale dei componenti del tampone utilizzati per tutti i saggi FP è 10 mM HEPES (pH 7,5), 1 mM EDTA, 0,1% Nonidet P-40, 50 mM NaCl e 10% DMSO. L'assenza di ditiotreitolo è essenziale per l'attività inibitoria. Le sequenze dei peptidi sono: STAT3, 5-carbossifluoresceina-GY(PO₃H₂)LPQTV-NH₂; STAT1, 5-carbossifluoresceina-GY(PO₃H₂)DKPHVL; STAT5, 5-carbossifluoresceina-GY(PO₃H₂)LVLDKW; e Lck, 5-carbossifluoresceina-GY(PO₃H₂)EEIP. Per l'analisi di specificità a 30 °C, le proteine vengono utilizzate a 150 nM (STAT1, STAT3 e STAT5). Per l'analisi di specificità a 37 °C, le proteine vengono utilizzate a 370 nM (STAT3) o 100 nM (Lck). Le proteine vengono incubate con i composti di prova in provette Eppendorf alle temperature indicate per 60 minuti prima dell'aggiunta dei rispettivi peptidi marcati con 5-carbossifluoresceina (concentrazione finale: 10 nM). Prima della misurazione a temperatura ambiente, le miscele vengono lasciate equilibrare per almeno 30 minuti. I composti di prova vengono utilizzati alle concentrazioni indicate diluite da una soluzione madre 20× in DMSO. Le curve di legame e le curve di inibizione vengono adattate con SigmaPlot. Tutte le curve di competizione vengono ripetute tre volte in esperimenti indipendenti.
Riferimenti	[1] https://pubmed.ncbi.nlm.nih.gov/17114005/ [2] https://pubmed.ncbi.nlm.nih.gov/21521803/

Applicazioni

Metodi	Biomarcatori	PMID
Western blot	p-STAT3 / STAT3 Survivin / c-Myc / Bcl-xl PARP / C-PARP / Caspase-3 / C-Caspse-3	25261365
Immunofluorescence	p-STAT3 / STAT3 / Survivin	25261365
Growth inhibition assay	Cell viability	23382914
ELISA	BDNF	27456333

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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):