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YH239-EE
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
YH239-EE图片
CAS NO:1364488-67-4
规格:98%
分子量:504.41
包装与价格:
包装价格(元)
10mg电议
50mg电议

产品介绍
p53-MDM2 antagonist, potent
CAS:1364488-67-4
分子式:C25H27Cl2N3O4
分子量:504.41
纯度:98%
存储:Store at -20°C

Background:

YH239-EE is a potent antagonist of p53-MDM2 [1].


p53 is a transcription factor and functions as a tumor suppressor. MDM2 is a negative regulator of p53. The interaction of p53 and MDM2 has emerged as a novel target for anticancer drugs [1].


YH239-EE is a potent p53-MDM2 antagonist. In OCI-AML-3 cells, YH239-EE potently inhibited cell proliferation. In AML cell lines, YH239-EE induced a cell cycle arrest and cell accumulation in the sub-G1 phase. YH239-EE induced apoptosis by 11.8-fold, 5.6-fold and 13.1-fold in OCI-AML-3, MOLM-13 and NB4 AML cell lines, respectively. In MOLM-13 cells, YH239 exhibited almost no apoptotic effect. However, YH239-EE significantly induced apoptosis. In MOLM-13 cells, (+)-YH239-EE and (?)-YH239-EE inhibited metabolic activity with EC50 values of 7.5 μM and 25.2 μM and induced apoptosis with 13.7% and 51.5% viable cells, respectively. (+)-YH239-EE (20 μM) induced p53 and significantly activated caspase 3 and 7 [1].


Reference:
[1].  Huang Y, Wolf S, Beck B, et al. Discovery of highly potent p53-MDM2 antagonists and structural basis for anti-acute myeloid leukemia activities. ACS Chem Biol, 2014, 9(3): 802-811.