GSK503, EZH2 methyltransferase inhibitor (ab269819)
Key features and details
- Potent and specific EZH2 methyltransferase inhibitor
- CAS Number: 1346572-63-1
Soluble in water to 5 mM, in DMSO to 25 mM and in ethanol to 50 mM
- Form / State: Solid
Overview
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Product name
GSK503, EZH2 methyltransferase inhibitor -
Description
Potent and specific EZH2 methyltransferase inhibitor -
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.
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CAS Number
1346572-63-1 -
Chemical structure
Properties
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Selectivity
Highly selective against a range of human methyltransferases, histone deacetylases, GPCRs, kinases and ion channels.
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Chemical name
N-[(1,2-Dihydro-4,6-dimethyl-2-oxo-3-pyridinyl)methyl]-3-methyl-1-(1- methylethyl)-6-[6-(4-methyl-1-piperazinyl)-3-pyridinyl]-1H-indole-4- carboxamide -
Molecular weight
526.67 -
Molecular formula
C31H38N6O2 -
PubChem identifier
67469117 -
Storage instructions
Shipped at room temperature. Store at -20°C. -
Solubility overview
Soluble in water to 5 mM, in DMSO to 25 mM and in ethanol to 50 mM
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Handling
Refer to SDS for further information.
Need more advice on solubility, usage and handling? Please visit our frequently asked questions (FAQ) page for more details.
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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
Images
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Chemical Structure - GSK503, EZH2 methyltransferase inhibitor (ab269819)
Chemical structure of GSK503, EZH2 methyltransferase inhibitor, 1346572-63-1