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MW 526.7 Da. Potent (IC50 = nM; Ki = 3 nM) and specific EZH2 methyltransferase inhibitor. Selective against EZH1 (IC50 = 633 nM). At least 4000-fold selective over a panel of 20 other human methyltransferases. Highly selective against a range of human histone deacetylases, GPCRs, kinases and ion channels. Reduces cellular H3K27me3 levels. Inhibits growth of diffuse large B-cell lymphoma cells. Inhinits melanoma growth and metastasis in mouse models.

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Images

Chemical Structure - GSK503, EZH2 methyltransferase inhibitor (AB269819), expandable thumbnail

Key facts

Form
Solid
Molecular weight
526.7 Da
Molecular formula
C31H38N6O2
PubChem identifier
67469117
Nature
Synthetic

Target data

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MW 526.7 Da. Potent (IC50 = nM; Ki = 3 nM) and specific EZH2 methyltransferase inhibitor. Selective against EZH1 (IC50 = 633 nM). At least 4000-fold selective over a panel of 20 other human methyltransferases. Highly selective against a range of human histone deacetylases, GPCRs, kinases and ion channels. Reduces cellular H3K27me3 levels. Inhibits growth of diffuse large B-cell lymphoma cells. Inhinits melanoma growth and metastasis in mouse models.

Key facts

PubChem identifier
67469117
Solubility

Soluble in water to 5 mM.

Soluble in DMSO to 25 mM.

Soluble in ethanol to 50 mM.

Biochemical name
N-((4,6-Dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-1-isopropyl-3-methyl-6-(6-(4-methylpiperazin-1-yl)pyridin-3-yl)-1H-indole-4-carboxamide
Biological description

Potent (IC50 = nM; Ki = 3 nM) and specific EZH2 methyltransferase inhibitor. Selective against EZH1 (IC50 = 633 nM). At least 4000-fold selective over a panel of 20 other human methyltransferases. Highly selective against a range of human histone deacetylases, GPCRs, kinases and ion channels. Reduces cellular H3K27me3 levels. Inhibits growth of diffuse large B-cell lymphoma cells. Inhinits melanoma growth and metastasis in mouse models.

Canonical SMILES
CC1=CC(=C(C(=O)N1)CNC(=O)C2=C3C(=CN(C3=CC(=C2)C4=CN=C(C=C4)N5CCN(CC5)C)C(C)C)C)C
InChI
InChI=1S/C31H38N6O2/c1-19(2)37-18-21(4)29-25(30(38)33-17-26-20(3)13-22(5)34-31(26)39)14-24(15-27(29)37)23-7-8-28(32-16-23)36-11-9-35(6)10-12-36/h7-8,13-16,18-19H,9-12,17H2,1-6H3,(H,33,38)(H,34,39)
InChIKey
HRDQQHUKUIKFHT-UHFFFAOYSA-N
IUPAC name
N-[(4,6-dimethyl-2-oxo-1H-pyridin-3-yl)methyl]-3-methyl-6-[6-(4-methylpiperazin-1-yl)pyridin-3-yl]-1-propan-2-ylindole-4-carboxamide

Storage

Shipped at conditions
Ambient - Can Ship with Ice
Appropriate short-term storage conditions
-20°C
Appropriate long-term storage conditions
-20°C

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1 product image

  • Chemical Structure - GSK503, EZH2 methyltransferase inhibitor (ab269819), expandable thumbnail

    Chemical Structure - GSK503, EZH2 methyltransferase inhibitor (ab269819)

    Chemical structure of GSK503, EZH2 methyltransferase inhibitor, 1346572-63-1

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Product protocols

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