YH239-EE;1H-Indole-2-carboxylic acid, 6-chloro-3-[1-[[(4-chlorophenyl)methyl]formylamino]-2-[(1,1-dimethylethyl)amino]-2-oxoethyl]-, ethyl ester;YH239-?EE;YH 239 EE
Cas No.
1364488-67-4
分子式
C25H27Cl2N3O4
分子量
504.41
包装储存
Powder -20°C 3 years;4°C 2 years
产品详情
YH239-EE是YH239的乙酯形式,是p53-MDM2的拮抗剂、凋亡诱导剂。
生物活性
YH239-EE, ethyl ester of the free carboxylic acid compound YH239, is a potent p53-MDM2 antagonizing and apoptosis-inducing agent.
IC50 value:
Target: MDM2/p53
YH239-EE inhibits the growth of OCI-AML-3 cells with wild type p53 by inhibiting the p53-MDM2 interaction. YH239-EE induces cell cycle arrest and causes potent cell apoptosis via activation of p53 and downstream targets in four AML cells (OCI-AML-3 and MOLM-13 with wt p53, NB4 with p53 mutation, and HL60 with p53 deletion).
性状
Solid
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
参考文献
[1]. Huang Y, et al. Discovery of highly potent p53-MDM2 antagonists and structural basis for anti-acute myeloid leukemia activities. ACS Chem Biol. 2014 Mar 21;9(3):802-11.