GSK343, histone H3-lysine 27 (H3K27) methyltransferase EZH2 inhibitor (ab218610)
Key features and details
- Potent, selective, cell-permeable histone H3-lysine 27 (H3K27) methyltransferase EZH2 inhibitor
- CAS Number: 1346704-33-3
- Purity: > 99%
- Soluble in DMSO to 25 mM
- Form / State: Solid
- Source: Synthetic
Overview
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Product name
GSK343, histone H3-lysine 27 (H3K27) methyltransferase EZH2 inhibitor -
Description
Potent, selective, cell-permeable histone H3-lysine 27 (H3K27) methyltransferase EZH2 inhibitor -
Alternative names
- GSK 343
- N-[(1,2-Dihydro-6-methyl-2-oxo-4-propyl-3-pyridinyl)methyl]-1-(1-methylethyl)-6-[2-(4-methyl-1-piperazinyl)-4-pyridinyl]-1H-indazole-4-carboxamide
- N-[(6-Methyl-2-oxo-4-propyl-1,2-dihydropyridin-3-yl)methyl]-6-[2-(4-methylpiperazin-1-yl)pyridin-4-yl]-1-(propan-2-yl)-1H-indazole-4-carboxamide
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Biological description
Potent, selective, cell-permeable histone H3-lysine 27 (H3K27) methyltransferase EZH2 inhibitor. Inhibits EZH2 enzymatic activity (IC50 = 4 nM). Displays 60 fold selectivity for EZH2 over EZH1, and 1000 fold or greater selectivity against other histone methyltransferases. Inhibits H3K27 methylation in HCC1806 cells (IC50
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Purity
> 99% -
CAS Number
1346704-33-3 -
Chemical structure
Properties
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Chemical name
1-Isopropyl-N-((6-methyl-2-oxo-4-propyl-1,2-dihydropyridin-3-yl)methyl)-6-(2-(4-methylpiperazin-1-yl)pyridine-4-yl)-1H-indazole-4-carboxamide -
Molecular weight
541.69 -
Molecular formula
C31H39N7O2 -
PubChem identifier
71268957 -
Storage instructions
Shipped at 4°C. Store at -20°C. Store under desiccating conditions. -
Solubility overview
Soluble in DMSO to 25 mM -
Handling
Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20°C. Generally, these will be useable for up to one month. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour.
Need more advice on solubility, usage and handling? Please visit our frequently asked questions (FAQ) page for more details.
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SMILES
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 -
Source
Synthetic
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Research areas
