GSK126, EZH2 methyltransferase inhibitor (ab269816)
Key features and details
- Potent and selective EZH2 methyltransferase inhibitor
- CAS Number: 1346574-57-9
- Soluble in DMSO to 5 mM
- Form / State: Solid
- Source: Synthetic
Overview
-
Product name
GSK126, EZH2 methyltransferase inhibitor -
Description
Potent and selective EZH2 methyltransferase inhibitor -
Biological description
Potent inhibitor EZH2 methyltransferase inhibitor (Ki = 93 pM). Selective (>150-fold) versus EZH1. Greater than 1000-fold selective against a panel of 20 other human methyltransferases including both SET-domain-containing and non-SET-domain-containing methyltransferases. Decreases global H3K27me3 levels. Inhibits B-cell lymphoma cell proliferation in vitro. Inhibits EZH2 mutant tumor growth in xenograft models. Reactivates silenced PRC2 target genes and inhibits the proliferation of EZH2 mutant DLBCL cell lines and corresponding xenografts mice. Literature suggests that GSK126 is a potential treatment for EZH2 mutant lymphoma (McCabe et al)
-
CAS Number
1346574-57-9 -
Chemical structure
Properties
-
Chemical name
N-[(1,2-Dihydro-4,6-dimethyl-2-oxo-3- pyridinyl)methyl]-3-methyl-1-[(1S)-1-methylpropyl]-6-[6-(1-piperazinyl)-3- pyridinyl]-1H-indole-4-carboxamide -
Molecular weight
526.67 -
Molecular formula
C31H38N6O2 -
PubChem identifier
68210102 -
Storage instructions
Shipped at room temperature. Store at -20°C. -
Solubility overview
Soluble in DMSO to 5 mM -
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.
-
SMILES
CC[C@H](C)N1C=C(C2=C(C=C(C=C21)C3=CN=C(C=C3)N4CCNCC4)C(=O)NCC5=C(C=C(NC5=O)C)C)C -
Source
Synthetic
-
Research areas
Images
-
Chemical Structure - GSK126, EZH2 methyltransferase inhibitor (ab269816)
Chemical structure of GSK126, EZH2 methyltransferase inhibitor, 1346574-57-9