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K-975
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。
K-975图片
CAS NO:2563855-03-6
包装与价格:
包装价格(元)
1 mg电议
5 mg电议
10 mg电议
25 mg电议
50 mg电议
100 mg电议
1 mL*10 mM(in DMSO)电议

产品介绍
K-975是一种高选择性的具有口服活性的TEAD抑制剂,可有效抑制TEAD和YAP1/TAZ之间的蛋白质-蛋白质相互作用。

产品描述

K-975 is a highly selective, orally active TEAD inhibitor, effectively inhibiting protein-protein interactions between TEAD and YAP1/TAZ.

体外活性

K-975 inhibits the cell proliferation of NRF2-non-expressing malignant pleural mesothelioma (MPM) cell lines, protein-protein interaction (PPI) between Halo-TAZ and TEAD1/4 and Halo-YAP and endogenous TEAD1/4 in NCl-H226 cells and the reporter activity in NCl-H661/CTGF-Luc cells with the maximum of ~70%, at concentration of 0.1-10000 nM at 144 h and 24 h, respectively [1]. K-975 decreases the expression of IGFBP3, CTGF and NPPB mRNAs, and increases the expression of FBXO32 mRNA in NCl-H226 cells [1].

体内活性

K-975 (10-300 mg/kg; p.o. twice a day for 14 days) suppresses the growth of tumors via inhibiting TEAD-YAP1/TAZ signaling in MPM xenograft mouse models [1].

Cas No.

2563855-03-6

分子式

C16H14ClNO2

分子量

287.74

别名

K-975

储存和溶解度

DMSO:215 mg/mL (747.20 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years