|2-((4-(4-溴苯基磺酰氨基)-1-羟基萘-2-基)硫代)乙酸|CsnPharm

CAS No.: 518303-20-3

UMI-77 Catalog No. CSN18313

Synonyms: UMI-77

UMI-77 is a selective Mcl-1 SMI inhibitor, binding to the BH3 binding groove of Mcl-1 with Ki of 490 nM.

规格	价格	促销价格	库存	数量

400-920-2911

sales@csnpharm.cn

tech@csnpharm.cn

加入购物车大规格询价

加入收藏

产品咨询

400-920-2911

sales@csnpharm.cn

tech@csnpharm.cn

纯度 & 质量文件批次:

靶点选择性

生物活性

实验方案

技术信息

生物活性

靶点 Mcl-1

Ki:490nM
描述Mcl-1 (Myeloid cell leukemia-1) is an anti-apoptotic protein, which is a member of the Bcl-2 family. Mcl-1 is involved in the regulation of apoptosis versus cell survival, and in the maintenance of cell viability but not of proliferation. Mcl-1 mediates its effects by interactions with a number of other regulators of apoptosis^[3]. UMI-77 is a Mcl-1 inhibitor. In FP-based binding assays, UMI-77 potently and selectively displaced fluorescent labeled BID-BH3 peptide from Mcl-1 protein. UMI-77 bound to the BH3 binding pocket of Mcl-1 and the Ki value was 0.49 μM^[4]. In a pull-down assay, starting from the concentration of 10 μM , UMI-77 dose-dependently inhibited the interactions between BL-Noxa and cellular Mcl-1 in 2LMP cell lysates. In a SPR-based binding assay, it was reported that UMI-77 dose-dependently inhibited the binding of Mcl-1 to Bax with IC50 value of 1.43 μM. UMI-77 inhibited the growth of BxPC-2 and Panc-1 cells with IC50 values of 3.4 μM and 4.4 μM, respectively^[4]. UMI-77 incubated at the concentrations of 3 μM or 10 μM for 48h induced apoptosis in esophageal squamous cell carcinoma KYSE150 and KYSE510 cells, as evidenced by cleavage of caspase-3 and PARP^[5]. In BxPC-3 xenograft model established in SCID mice, UMI-77 administrated i.v. at the dose of 60 mg/kg for a total of 10 doses significantly inhibited tumor growth^[4].
作用机制UMI-77 is a Mcl-1 inhibitor. Docking and spectroscopy studies revealed that UMI-77 bound to the BH3 binding pocket of Mcl-1^[4].
动物研究
剂量
Mice: 60 mg/kg^[2] (i.v.)

给药途径
i.v.
参考文献

动物研究
剂量	Mice: 60 mg/kg^[2] (i.v.)
给药途径	i.v.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.1352 mL
- 10.6760 mL
- 21.3519 mL
- 5 mM
- 0.4270 mL
- 2.1352 mL
- 4.2704 mL
- 10 mM
- 0.2135 mL
- 1.0676 mL
- 2.1352 mL

技术信息

CAS号

518303-20-3

储存条件

粉末: Keep in dark place,Inert atmosphere,Room temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C18H14BrNO5S2

运输

蓝冰

分子量

468.34

别名

UMI-77

溶解度

DMSO	93.0 mg/mL (198.6 mM)
Water	Insoluble
Ethanol	90.0 mg/mL (192.2 mM) warming

动物实验配方

5% DMSO+30% PEG 300+dd water

6 mg/mL

大规格询价

号为必填项

姓名: 邮箱: 手机号:

留言:

提交

UMI-77 Catalog No. CSN18313

靶点选择性

请登录您的专属账户

确认信息