GSK126 is a potent, highly selective EZH2 methyltransferase inhibitor with IC50 of 9.9 nM, >1000-fold selective for EZH2 over 20 other human methyltransferases.
Reference:
>Nature. 2012 Dec 6;492(7427):108-12. doi: 10.1038/nature11606. Epub 2012 Oct 10.
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Name | GSK126 |
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Iupac Chemical Name | 1-(S)-sec-butyl-N-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-3-methyl-6-(6-(piperazin-1-yl)pyridin-3-yl)-1H-indole-4-carboxamide |
Synonyms | GSK-126;GSK126 |
Molecular Formula | C31H38N6O |
Molecular Weight | 526.67 |
Smile | CC[C@H](C)n1cc(c2c1cc(cc2C(=O)NCc3c(cc([nH]c3=O)C)C)c4ccc(nc4)N5CCNCC5)C |
InChiKey | FKSFKBQGSFSOSM-QFIPXVFZSA-N |
InChi | InChI=1S/C31H38N6O2/c1-6-22(5)37-18-20(3)29-25(30(38)34-17-26-19(2)13-21(4)35-31(26)39)14-24(15-27(29)37)23-7-8-28(33-16-23)36-11-9-32-10-12-36/h7-8,13-16,18,22,32H,6,9-12,17H2,1-5H3,(H,34,38)(H,35,39)/t22-/m0/s1 |
CAS Number | 1346574-57-9 |
MDL | MFCD23381067 |
Related CAS |
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Formulation | Crystalline solid |
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Purity | 98% |
Storage | Store at 0ºCC (short term), -20ºCC (long term), desiccated |
Solubility | Soluble in DMSO |
Handling | |
Shipping Condition | Shipped under ambient temperature |
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