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。

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

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].

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].

2563855-03-6

C16H14ClNO2

287.74

K-975

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