GSK343

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EZH2 inhibitor

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Catalog No. A13114

Availability:Stock in USAIn stock

Product Name Catalog No. Price Qty
GSK343 5mg A13114-5

Regular Price: $50.00

Special Price: $40.00

GSK343 10mg A13114-10

Regular Price: $80.00

Special Price: $64.00

GSK343 25mg A13114-25

Regular Price: $150.00

Special Price: $120.00

GSK343 50mg A13114-50

Regular Price: $250.00

Special Price: $200.00

Products are for laboratory research use only. Not for human use. We do not sell to patients.

Quick Overview

GSK343 is a potent histone H3-lysine 27 (H3K27) methyltransferase EZH2 inhibitor (IC= 4 nM). Diplays 1000-fold selectivity for other HMTs except EZH1 (60-fold selectivity). GSK343 inhibits H3K27 methylation in HCC1806 cells with an IC of <200nM (measured by immunofluorescence).

GSK343

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Chemical Information

Catalog Num A13114
Actions Inhibitor
M. Wt 541.69
Formula C31H39N7O2
Solubility DMSO
Purity >98%
Storage at -20°C 3 years Powder
CAS No. 1346704-33-3
Synonyms GSK-343, GSK 343
SMILES code CCCC1=C(C(=O)NC(=C1)C)CNC(=O)C2=C3C=NN(C3=CC(=C2)C4=CC(=NC=C4)N5CCN(CC5)C)C(C)C
Chemical Name 1-isopropyl-N-((6-methyl-2-oxo-4-propyl-1,2-dihydropyridin-3-yl)methyl)-6-(2-(4-methylpiperazin-1-yl)pyridin-4-yl)-1H-indazole-4-carboxamide.

Biological Activity

Description
GSK343 is a potent histone H3-lysine 27 (H3K27) methyltransferase EZH2 inhibitor (IC= 4 nM). Diplays 1000-fold selectivity for other HMTs except EZH1 (60-fold selectivity). GSK343 inhibits H3K27 methylation in HCC1806 cells with an IC of <200nM (measured by immunofluorescence).
Targets
EZH2 (Cell-free assay) EZH1 (Cell-free assay)
4 nM240 nM

Solubility

Solubility (25°C)* In vitro DMSO 1 mg/mL heating (1.84 mM)
Water <1 mg/mL (<1 mM)
Ethanol 4 mg/mL (7.38 mM)
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Adooq tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

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