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Cycloheximide Eiwitsyntheseremmer

Name: Cycloheximide
Brand: Selleck Chemicals
SKU: S7418
Rating: 5 (515 reviews)

Cat.Nr.S7418

Cycloheximide, een antifungale antibioticum, is een eukaryote eiwitsyntheseremmer met een IC50 van respectievelijk 532,5 nM en 2880 nM voor eiwitsynthese en RNA synthesis in vivo. Cycloheximide onderdrukt ferroptose en remt autofagie.Cycloheximide (NSC-185) kan worden gebruikt om diermodellen van Dysmnesia te induceren.Oplossingen zijn onstabiel en moeten vers worden bereid.Dit product is een gevaarlijke chemische stof (acute toxiciteit/ontvlambaar/huidcorrosief). Gebruik het met een beschermend gezichtsmasker, handschoenen en kleding.

Cycloheximide Fungal remmer Chemical Structure

Chemische structuur

Moleculair gewicht: 281.35

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Kwaliteitscontrole

Batch: Zuiverheid: 99.96%

99.96

Gerelateerde doelwitten	PD-1/PD-L1 CXCR STING AhR Immunology & Inflammation related CD markers Interleukins Anti-infection Antioxidant COX
Overige Fungal Inhibitoren	Tolnaftate Manogepix (E1210) Amorolfine HCl Isavuconazole Thimerosal Allicin Neticonazole Hydrochloride Juglone Pseudolaric Acid B Neticonazole

Celkweek, behandeling & werkconcentratie

Cellijnen	Assaytype	Concentratie	Incubatietijd	Activiteitsbeschrijving	PMID
CEM	Anticancer assay			Tested in vitro for anticancer activity against CEM cells, IC50 = 0.12 μM.	10072683
9L	Anticancer assay			Tested in vitro for anticancer activity against 9L cells, IC50 = 0.2 μM.	10072683
SK-MEL-28	Anticancer assay			Tested in vitro for anticancer activity against SK-MEL-28 cells, IC50 = 1 μM.	10072683
Vero	Cytotoxicity assay			Tested in vitro for cytotoxicity against Vero cells, IC50 = 1.2 μM.	10072683
LNCaP	Anticancer assay			Tested in vitro for anticancer activity against LNCaP cells, IC50 = 1.2 μM.	10072683
MCF-7	Anticancer assay			Tested in vitro for anticancer activity against MCF-7 cells, IC50 = 1.5 μM.	10072683
PBM	Cytotoxicity assay			Tested in vitro for cytotoxicity against PBM cells, IC50 = 2.1 μM.	10072683
HepG2	Anticancer assay			Tested in vitro for anticancer activity against HepG2 cells, IC50 = 2.5 μM.	10072683
SK-MES-1	Anticancer assay			Tested in vitro for anticancer activity against SK-MES-1 cells, IC50 = 2.7 μM.	10072683
PC-3	Anticancer assay			Tested in vitro for anticancer activity against PC-3 cells, IC50 = 3.5 μM.	10072683
Jurkat T-cells	Function assay			Inhibitory concentration against Human Jurkat T cells, IC50 = 0.93 μM.	10212121
Jurkat T-cells	Function assay			Inhibitory concentration against Human Jurkat T cells, IC80 = 1.54 μM.	10212121
Jurkat T-cells	Function assay		48 hours	Inhibitory concentration was evaluated on human Jurkat T-cells after their exposure for 48 hours, IC50 = 0.93 μM.	11052798
Jurkat T-cells	Function assay		48 hours	Inhibitory concentration was evaluated on human Jurkat T-cells after their exposure for 48 hours, IC80 = 1.54 μM.	11052798
CEM	Cytotoxicity assay			Cytotoxicity was determined in CEM cells, relative to RVT, IC50 = 0.08 μM.	15081000
PBM	Cytotoxicity assay			Cytotoxicity was determined in PBM cells, relative to RVT, IC50 = 0.46 μM.	15081000
Vero	Cytotoxicity assay			Cytotoxicity was determined in Vero cells, relative to RVT, IC50 = 0.53 μM.	15081000
HeLa	Function assay			Inhibition of hypoxia-induced HIF1 activation in human HeLa cells by luciferase reporter gene assay, IC50 = 0.036 μM.	15974627
medulloblastoma cells	Antiproliferative assay			Antiproliferative activity against mouse medulloblastoma cells harboring heterozygous ptch1 gene by MTT assay, EC50 = 0.042 μM.	17417631
neural precursor cells	Antiproliferative assay			Antiproliferative activity against mouse neural precursor cells by colony formation assay, EC50 = 0.054 μM.	17417631
astrocyte cells	Antiproliferative assay			Antiproliferative activity against mouse astrocyte cells by MTT assay, EC50 = 0.071 μM.	17417631
neural precursor cells	Antiproliferative assay			Antiproliferative activity against mouse neural precursor cells by MTT assay, EC50 = 0.142 μM.	17417631
HeLa	Cytotoxicity assay		24 hrs	Cytotoxicity against human HeLa cells after 24 hrs, CD50 = 0.1 μM.	18394884
3T3	Cytotoxicity assay		72 hrs	Cytotoxicity against mouse 3T3 cells after 72 hrs by MTT assay, IC50 = 0.912 μM.	18771242
HeLa	Function assay		2 hrs	Inhibition of protein synthesis in human HeLa cells assessed as [35S]cysteine/methionine utilization after 2 hrs by scintillation spectroscopy, IC50 = 0.5325 μM.	20118940
HeLa	Function assay		2 hrs	Inhibition of transcriptional activity in human HeLa cells assessed as [3H]uridine utilization after 2 hrs by scintillation counting, IC50 = 2.8801 μM.	20118940
3T3	Cytotoxicity assay		72 hrs	Cytotoxicity against mouse 3T3 cells after 72 hrs by MTT assay, IC50 = 0.26 μM.	20356064
BESM	Function assay		88 hrs	Antitrypanosomal activity against Trypanosoma cruzi amastigotes infected in BESM cells measured after 88 hrs postinfection by HTS assay, EC50 = 0.4 μM.	20547819
NIH/3T3	Cytotoxicity assay		48 hrs	Cytotoxicity against mouse NIH/3T3 cells after 48 hrs by MTT assay, IC50 = 1.1 μM.	21899268
MDA-MB-231	Cytotoxicity assay		48 hrs	Cytotoxicity against human MDA-MB-231 cells after 48 hrs by MTT assay, IC50 = 1.2 μM.	21899268
AGS	Cytotoxicity assay		48 hrs	Cytotoxicity against human AGS cells after 48 hrs by MTT assay, IC50 = 3.6 μM.	21899268
HT-29	Cytotoxicity assay		48 hrs	Cytotoxicity against human HT-29 cells after 48 hrs by MTT assay, IC50 = 12.8 μM.	21899268
HepG2-A16-CD81	Function assay	10 uM		NOVARTIS: Antimalarial liver stage activity measured as reduction in Plasmodium yoelii schizont area in HepG2-A16-CD81 cells by immuno-fluorescence, and median schizont size at 10uM compound concentration, IC50 = 0.0781 μM.	22096101
3T3	Cytotoxicity assay		72 hrs	Cytotoxicity against mouse 3T3 cells after 72 hrs by MTT assay, IC50 = 0.26 μM.	22437110
HepG2	Function assay			HARVARD: Inhibition of liver stage Plasmodium berghei infection in HepG2 cells, IC50 = 0.047 μM.	22586124
PA1	Cytotoxicity assay		24 hrs	Cytotoxicity against human PA1 cells after 24 hrs by MTT assay, IC50 = 40.6 μM.	23202484
PA1	Growth inhibition assay		24 hrs	Growth inhibition of human PA1 cells after 24 hrs by MTT assay, IC50 = 40.6 μM.	28011220
3T3	Cytotoxicity assay			Cytotoxicity against mouse 3T3 cells by SRB assay, IC50 = 0.3 μM.	29247859
CEM	Cytotoxicity assay		5 days	Cytotoxicity against human CEM cells assessed as decrease in cell viability after 5 days by MTT assay, IC50 = 0.2 μM.	29778528
Vero	Cytotoxicity assay		3 days	Cytotoxicity against African green monkey Vero cells assessed as decrease in cell viability after 3 days by MTT assay, IC50 = 0.2 μM.	29778528
3T3	Cytotoxicity assay		48 hrs	Cytotoxicity against rat 3T3 cells after 48 hrs by MTT assay, IC50 = 0.61 μM.	30146096
MCF7	Function assay	10 ug/mL	1 hr	Inhibition of HIF1alpha RNA translation in human MCF7 cells at 10 ug/mL pretreated for 1 hr prior to metabolic labeling by SDS-PAGE analysis	22607231
AGS	Apoptosis assay	150 ug/mL	48 hrs	Induction of apoptosis in human AGS cells assessed as early apoptosis level at 150 ug/mL after 48 hrs by Annexin V-FITC apoptosis assay	21899268
TC32	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells	29435139
A673	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells	29435139
DAOY	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells	29435139
Saos-2	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells	29435139
BT-37	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells	29435139
RD	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells	29435139
SK-N-SH	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells	29435139
BT-12	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells	29435139
NB1643	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells	29435139
OHS-50	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells	29435139
BT-12	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for BT-12 cells	29435139
LAN-5	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for LAN-5 cells	29435139
Rh41	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells	29435139
SK-N-SH	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-SH cells	29435139
A673	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for A673 cells)	29435139
BT-37	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for BT-37 cells	29435139
Rh30	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh30 cells	29435139
U-2 OS	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for U-2 OS cells	29435139
OHS-50	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for OHS-50 cells	29435139
RD	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for RD cells	29435139
SJ-GBM2	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells	29435139
SK-N-MC	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells	29435139
NB-EBc1	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells	29435139
SK-N-MC	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-MC cells	29435139
SJ-GBM2	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SJ-GBM2 cells	29435139
TC32	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for TC32 cells	29435139
SJ-GBM2	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Orthogonal 3D viability screen for SJ-GBM2 cells	29435139
T47D	Function assay	10 uM	4 hrs	Inhibition of 1,10-phenanthroline-induced HIF1alpha activation in human T47D cells at 10 uM after 4 hrs by Western blotting	15974627
T47D	Function assay	0.3 uM	4 hrs	Inhibition of 1,10-phenanthroline-induced HIF1alpha activation in human T47D cells at 0.3 uM after 4 hrs by Western blotting	15974627
T47D	Function assay	3 uM	16 hrs	Inhibition of hypoxia-induced HIF1 activation in human T47D cells at 3 uM after 16 hrs by luciferase reporter gene assay	15974627
T47D	Function assay	0.7 uM	16 hrs	Inhibition of 1,10-phenanthroline-induced HIF1 activation in human T47D cells at 0.7 uM after 16 hrs by luciferase reporter gene assay	15974627
T47D	Function assay	10 uM	16 hrs	Inhibition of hypoxia-induced VEGF expression in human T47D cells at 10 uM after 16 hrs by ELISA	15974627
T47D	Function assay	0.3 uM	4 hrs	Inhibition of hypoxia-induced HIF1alpha activation in human T47D cells at 0.3 uM after 4 hrs by Western blotting	15974627
T47D	Function assay	10 uM	4 hrs	Inhibition of hypoxia-induced HIF1alpha activation in human T47D cells at 10 uM after 4 hrs by Western blotting	15974627
neural precursor cells	Function assay	3 uM		Induction of neurosphere phenotype changes in mouse neural precursor cells at 3 uM	17417631
HeLa	Cytotoxicity assay			Cytotoxicity against human HeLa cells assessed as inhibition of DNA replication by imaging analysis	18066055
HeLa	Function assay			Inhibition of mitosis in human HeLa cells by imaging analysis	18066055
HEK293T	Function assay	50 uM	30 mins	Effect on polyribosome profiling in human HEK293T cells assessed as depletion of polysomes at 50 uM after 30 mins by spectrophotometry	20118940
T47D	Antiproliferative assay	10 uM	48 hrs	Antiproliferative activity against human T47D cells at 10 uM after 48 hrs by SRB assay	23434131
MDA-MB-231	Antiproliferative assay	10 uM	48 hrs	Antiproliferative activity against human MDA-MB-231 cells at 10 uM after 48 hrs by SRB assay	23434131
NCI-H460	Function assay	10 ug/mL	up to 9 hrs	Reduction of HSP1 stability in human NCI-H460 cells assessed as protein degradation at 10 ug/mL up to 9 hrs by Western blot analysis	24746225
HeLa	Cytotoxicity assay	25 uM	18 hrs	Cytotoxicity against human HeLa cells assessed as reduction in cell viability at 25 uM after 18 hrs by inverse MTT assay	25028062
RAW264.7	Function assay	70 uM	6 hrs	Inhibition of luminescence emission in mouse RAW264.7 cells transfected with luciferase plasmid containing universal promoter PKG at 70 uM after 6 hrs by luciferase reporter gene assay	25667960
Klik om meer experimentele gegevens over de cellijn te bekijken

Chemische informatie, Opslag en Stabiliteit

Moleculair gewicht	281.35	Formule	C₁₅H₂₃NO₄	Opslag (Vanaf de ontvangstdatum)	3 years-20°C powder
CAS-nr.	66-81-9	--		Opslag van stamoplossingen	1 jaar-80°Cin oplosmiddel 1 maand-20°Cin oplosmiddel
Synoniemen	NSC-185, Actidione, Naramycin A, CHX, FT 3422-2, NM-MCD 80			Smiles	CC1CC(C(=O)C(C1)C(CC2CC(=O)NC(=O)C2)O)C

Oplosbaarheid

In vitro
Batch:

DMSO : 56 mg/mL (199.04 mM)
(Met vocht verontreinigde DMSO kan de oplosbaarheid verminderen. Gebruik verse, watervrije DMSO.)

Ethanol : 56 mg/mL

Water : 15 mg/mL

Molariteitscalculator

Massa	Concentratie	Volume	Moleculair gewicht
=	×	×

Verdunningscalculator Moleculair gewicht calculator

In vivo Batch:
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.
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.
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.

In vivo Formuleringscalculator (Heldere oplossing)

Stap 1: Voer de onderstaande informatie in (Aanbevolen: Een extra dier voor het geval van verlies tijdens het experiment)

Dosering: mg/kg Gemiddeld gewicht van dieren: g Doseervolume per dier:μL Aantal dieren:

Stap 2: Voer de in vivo formulering in (Dit is alleen de calculator, geen formulering. Neem eerst contact met ons op als er geen in vivo formulering is in het gedeelte Oplosbaarheid.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Berekeningsresultaten:

Werkconcentratie: mg/ml;

Methode voor het bereiden van DMSO-mastervloeistof: mg geneesmiddel vooraf opgelost in μL DMSO ( Concentratie mastervloeistof mg/mL, Neem eerst contact met ons op als de concentratie de DMSO-oplosbaarheid van de partij geneesmiddel overschrijdt. )

Methode voor het bereiden van in vivo formulering: Neem μL DMSO mastervloeistof, voeg vervolgens toeμL PEG300, mengen en helder maken, voeg vervolgens toeμL Tween 80, mengen en helder maken, voeg vervolgens toe μL ddH₂O, mengen en helder maken.

Methode voor het bereiden van in vivo formulering: Neem μL DMSO mastervloeistof, voeg vervolgens toe μL Maïsolie, mengen en helder maken.

Opmerking: 1. Zorg ervoor dat de vloeistof helder is voordat u het volgende oplosmiddel toevoegt.
2. Zorg ervoor dat u het/de oplosmiddel(en) in de juiste volgorde toevoegt. U moet ervoor zorgen dat de verkregen oplossing, bij de vorige toevoeging, een heldere oplossing is voordat u verdergaat met het toevoegen van het volgende oplosmiddel. Fysische methoden zoals vortexen, echografie of een warmwaterbad kunnen worden gebruikt om het oplossen te bevorderen.

Werkingsmechanisme

In vitro	Cycloheximide, een eiwitsyntheseremmer, vermindert GSIV-geïnduceerde gastheerceldood door de blootstelling aan fosfatidylserine en het verlies van ΔΨm door apoptose/necrose te verminderen.
In vivo	Deze verbinding, een eiwitsyntheseremmer, beïnvloedt het geheugen door modulatoren van geheugenvorming te veranderen als een secundair gevolg van de remming van eiwitsynthese.
Referenties	[1] https://pubmed.ncbi.nlm.nih.gov/26548846/ [2] https://pubmed.ncbi.nlm.nih.gov/22610049/ [3] https://pubmed.ncbi.nlm.nih.gov/5541758/ [4] https://pubmed.ncbi.nlm.nih.gov/30916348/

Toepassingen

Methoden	Biomarkers	PMID
Western blot	β-catenin / MSX2 LIFR / gp130 / TfR BIP / P-P70S6K / P62 / ATF4 / Actin / LC3-I / LC3-II CYP87A3 ERK3 / IRP2	12095419
RNA blot	PDI-2 / tubulin / rRNA LEF1 / Cyc-D1 / IGF-1 / HGF / VEGF / KGF / GAPDH	18713834
Immunofluorescence	SCD6 / DHH1 / XRNA α-eIF3 / α-Dcp1 TUNEL Rpl25 / Nhp6 β-Catenin	18713834

Informatie klinische proef

(gegevens van https://clinicaltrials.gov, bijgewerkt op 2024-05-22)

NCT-nummer	Rekrutering	Aandoeningen	Sponsor/Medewerkers	Startdatum	Fasen
NCT03700788	Not yet recruiting	Apical Periodontitis	University of Southern California	May 30 2023	Phase 3
NCT05506566	Recruiting	Tumor\|Positron-Emission Tomography	First Affiliated Hospital of Fujian Medical University	May 1 2022	Phase 1\|Phase 2
NCT02202304	Withdrawn	Periodontal Disease\|Caries	Rosa Moreno Lopez\|Ivoclar Vivadent AG\|University of Aberdeen	September 10 2017	Phase 4
NCT01521325	Completed	Mesothelioma\|Pancreatic Cancer\|Ovarian Cancer\|Non-small Cell Lung Cancer	Morphotek	September 2011	Phase 1
NCT02168374	Completed	Dental Caries	Aline R F de Castilho\|Fundação de Amparo à Pesquisa do Estado de São Paulo\|University of Campinas Brazil	March 2008	Phase 2

Technische ondersteuning

Gebruiksaanwijzing

Tel: +1-832-582-8158 Ext:3

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