A dual EZH1 and EZH2 inhibitor; inhibits PRC2 containing EZH1 or EZH2 as the catalytic subunit in cell-free assays (IC50s = 8.4 and 2.5 nM

Valemetostat – 10 mg

Brand:
Cayman
CAS:
1809336-39-7
Storage:
-20
UN-No:
Non-Hazardous - /

Valemetostat is a dual inhibitor of enhancer of zeste homolog 1 (EZH1) and EZH2.{58162} It inhibits polycomb repressive complex 2 (PRC2) containing EZH1 or EZH2 as the catalytic subunit in cell-free assays (IC50s = 8.4 and 2.5 nM, respectively). Valemetostat inhibits trimethylation of histone H3 lysine 27 in HCT116 cells (IC50 = 0.44 nM). It inhibits the growth of Karpas-422 diffuse large B cell lymphoma (DLBCL) cells (GI50 = 4.8 nM).  

 

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SKU: 31674 - 10 mg Category:

Description

A dual EZH1 and EZH2 inhibitor; inhibits PRC2 containing EZH1 or EZH2 as the catalytic subunit in cell-free assays (IC50s = 8.4 and 2.5 nM, respectively); inhibits trimethylation of histone H3 lysine 27 in HCT116 cells (IC50 = 0.44 nM); inhibits the growth of Karpas-422 DLBCL cells (GI50 = 4.8 nM)

Formal name: (2R)-7-chloro-N-[(1,2-dihydro-4,6-dimethyl-2-oxo-3-pyridinyl)methyl]-2-[trans-4-(dimethylamino)cyclohexyl]-2,4-dimethyl-1,3-benzodioxole-5-carboxamide

Synonyms:  (R)-OR-S2|DS-3201b

Molecular weight: 488

CAS: 1809336-39-7

Purity: ≥98%

Formulation: A crystalline solid

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