产品名称

英文名称：EI1

同义词

1418308-27-6、EI1、KB-145943、6-cyano-N-[(4,6-dimethyl-2-oxo-1H-pyridin-3-yl)methyl]-1-pentan-3-ylindole-4-carboxamide、6-Cyano-N-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-1-(pentan-3-yl)-1H-indole-4-carboxamide、6-Cyano-N-[(1,2-dihydro-4,6-dimethyl

产品性质

CAS编号：1418308-27-6

分子式：C23H26N4O2

分子量：390.48

PubChem编号：72199293

英文别名：1418308-27-6|EI1|KB-145943|6-cyano-N-[(4,6-dimethyl-2-oxo-1H-pyridin-3-yl)methyl]-1-pentan-3-ylindole-4-carboxamide|6-Cyano-N-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-1-(pentan-3-yl)-1H-indole-4-carboxamide|6-Cyano-N-[(1,2-dihydro-4,6-dimethyl

规格或纯度：96%

英文名称：EI1

生化机理：EI1 demonstrated potent, concentration-dependent inhibition of the enzymatic activity against both Ezh2 wild-type and Y641F mutant enzymes with IC50 of 15 ± 2 nM and 13 ± 3 nM, respectively. Althoμgh SAM is the common cofactor for all HMTs, EI1 showed remarkable selectivity against Ezh2 over other HMTs. EI1 dramatically inhibited the H3K27me3 and H3K27me2 levels in these cells in a dose-dependent manner, but H3K27me1 was largely unchanged. The effect was similar in these cell lines, althoμgh they have different basal H3K27me3 and H3K27me2 levels. For example, in WSU-DLCL2, SU-DHL6, and Karpas422 with Ezh2 mutations, the H3K27me3 level was much higher than that in DLBCL cells with wild-type Ezh2.Potent (IC 50 = 15 nM for wild-type enzyme; 13 nM for Y641F mutant enzyme) EZH2 inhibitor. Selective versus EZH1 (142-fold). Highly selective (>10,000-fold) against\xa0 a panel of 10 other human methyltransferases.

储存温度：避光,-20°C储存

运输条件：超低温冰袋运输

备注：有毒，请参阅SDS以获取更多信息。需要更多关于溶解度，用法和处理的建议吗？请访问我们的常见问题（FAQ）页面以获取更多详细信息。

产品介绍：EI1是EZH2选择性抑制剂，对野生型EZH2和EZH2 Y641F突变型的IC50分别为15 nM和13 nM。EI1 is a potent and selective EZH2 inhibitor with IC50 of 15 nM and 13 nM for EZH2 (WT) and EZH2 (Y641F), respectively.

IUPAC Name：6-cyano-N-[(4,6-dimethyl-2-oxo-1H-pyridin-3-yl)methyl]-1-pentan-3-ylindole-4-carboxamide

INCHI：InChI=1S/C23H26N4O2/c1-5-17(6-2)27-8-7-18-19(10-16(12-24)11-21(18)27)22(28)25-13-20-14(3)9-15(4)26-23(20)29/h7-11,17H,5-6,13H2,1-4H3,(H,25,28)(H,26,29)

InChi Key：PFHDWRIVDDIFRP-UHFFFAOYSA-N

Canonical SMILES：CCC(CC)N1C=CC2=C(C=C(C=C21)C#N)C(=O)NCC3=C(C=C(NC3=O)C)C

Isomeric SMILES：CCC(CC)N1C=CC2=C(C=C(C=C21)C#N)C(=O)NCC3=C(C=C(NC3=O)C)C

PubChem CID：72199293

CAS Registry No.：1418308-27-6

溶解性：insoluble in H2O; insoluble in EtOH; ≥19.5 mg/mL in DMSO

敏感性：对光线敏感

产品包装