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UMI-77
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。
UMI-77图片
CAS NO:518303-20-3
规格:98%
分子量:468.34
包装与价格:
包装价格(元)
5mg电议
25mg电议

产品介绍
Mcl-1 inhibitor, novel
CAS:518303-20-3
分子式:C18H14BrNO5S2
分子量:468.34
纯度:98%
存储:Store at -20°C

Background:

UMI-77 is a novel small-molecule inhibitor of Mcl-1 with Ki and IC50 values of 0.49 μM and 0.31 μM [1].


Myeloid cell leukemia-1 (Mcl-1) is a member of the prosurvival Bcl-2 family and is a potent anti-apoptotic protein. Mcl-1 acts as an important survival factor in a broad range of human cancers [1].


UMI-77 is a novel small-molecule Mcl-1 inhibitor. In FP-based binding assays, UMI-77 potently and selectively displaced fluorescent labeled BID-BH3 peptide from Mcl-1 protein with Ki value of 0.49μM and bound to the BH3 binding pocket of Mcl-1 protein. UMI-77 bound to A1/Bfl-1, Bcl-w, Bcl-2 and Bcl-xL with Ki values of 5.33, 8.19, 23.83 and 32.99μM. In a pull-down assay, UMI-77 at 10 μM effectively and dose-dependently inhibited the interactions between BL-Noxa and cellular Mcl-1. It was reported that Mcl-1 regulates pro-apoptotic Bax and Bak proteins and preventing their pro-apoptotic activity. UMI-77 dose-dependently inhibited the binding of Mcl-1 to Bax with IC50 value of 1.43μM. In PC cells, UMI-77 inhibited cell growth and induced apoptosis in a time and dose-dependent way [1].


In BxPC-3 xenografted SCID mice model, UMI-77 exhibited robust anti-tumor efficacy with no toxicity. Also, UMI-77 decreased the anti-apoptotic protein survivin, which potently inhibited apoptosis by antagonizing caspase activity [1].


Reference:
[1].  Abulwerdi F, Liao C, Liu M, Azmi AS, et al. A novel small-molecule inhibitor of mcl-1 blocks pancreatic cancer growth in vitro and in vivo. Mol Cancer Ther, 2014, 13(3): 565-575.