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SKLB-03176

CAT: 0013-GTR19231918Size: 5 mgDry Ice: NoHazardous: No
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CAT#:0013-GTR19231918Size:5 mg
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24/48H Stock Items & 2 to 6 Weeks non Stock Items.
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Description
SKLB-03176 (SKLB03176) is a potent, selective, covalent EZH2 inhibitor with IC50 of 47 nM, covalently binds to the SAM pocket of EZH2.SKLB-03176 showed good inhibitory activity against mutations EZH2 Y641F, EZH2 Y641N, and EZH2A677G at 200 nM concentration.SKLB-03176 exhibited weak activity against other targets, such as 5 histone methyltransferases and more than 30 kinases, >50-fold selective for EZH2 over the highly homologous H3K27 methyltransferase EZH1 (IC50=2.45 uM) .SKLB-03176 inhibited the activity of a variety of EZH2 mutants and significantly inhibited the expression of H3K27Me3 in cells.SKLB-03176 showed no cytotoxicity to normal cells.
CAS Number
2609675-22-9
Purity
>98%
Smiles
C (C1=C (C (NC (=O) C=C) =CC (C2=CN=C (N3CCNCC3) C=C2) =C1) C) (=O) NCC1C (NC (C) =CC=1CC) =O
Molecular Formula
C29H34N6O3
Molecular Weight
514.618666172028
Notes
For research use only.

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