EZH2 inhibitor C36

Chemical Structure : EZH2 inhibitor C36

加入收藏

货号: PC-27108Not For Human Use, Lab Use Only.

EZH2 inhibitor C36 is a potent, selective and allosteric EZH2-PRC2 inhibitor with IC50 of 2.27 nM in AlphaLisa assays, inhibits both the basal and activated forms of the PRC2 complex containing EZH2, but not EZH1, in a SAM-noncompetitive manner.

规格	价格	库存	数量
25 mg		Get quote
50 mg		Get quote
100 mg		Get quote

获取报价单

* 请选择数量再加入购物车

or Bulk Inquiry

大包装，大折扣！

E-mail: sales@probechem.com

Tech Support: tech@probechem.com

生物&药学活性

EZH2 inhibitor C36 is a potent, selective and allosteric EZH2-PRC2 inhibitor with IC50 of 2.27 nM in AlphaLisa assays, inhibits both the basal and activated forms of the PRC2 complex containing EZH2, but not EZH1, in a SAM-noncompetitive manner.
C36 inhibits the methyltransferase activity of PRC2 and PRC2-JARID2 with IC50 values of 121 and 66 nM, respectively.
C36 binds to a pocket at the interface of SET-Activation-Loop (SAL), stimulation-responsive motif (SRM), and I-SET domain of EZH2, and WD40 domain of EED.
C36 binding induces conformational changes and disrupts allosteric communication between EZH2 and ligand-bound EED.
EZH2 inhibitor C36 greatly reduced H3K27me3 in DLBCL cell lines harboring EZH2 wild-type (Toledo, OCI-ly19, SU-DHL-1) or GOF mutants (WSU-DLCL2, SU-DHL-4, Karpas422 Pfeiffer).
C36 efficiently inhibits H3K27 trimethylation and PRC2 target gene expression in tumor cells and xenograft tumors with low hematotoxicity.

物理化学性质&存储条件

分子量	481.99
分子式	C24H28ClN7O2
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	2-(2-((((1,4-trans)-4-((8-chloro-1,7-naphthyridin-2-yl)amino)cyclohexyl)methyl)amino) pyrimidin-5-yl)-N-(oxetan-3-yl)acetamide

参考文献

1. Cao T, et al. Adv Sci (Weinh). 2026 Jun 18:e76025.