K-975

K-975CAS号: 2563855-03-6分子式: C16H14ClNO2分子量: 287.74描述储存/保存方法可溶性/溶解性In vitro(体外研究)In vivo(体内研究)

产品描述
描述
K-975 is a highly selective, orally active TEAD inhibitor, effectively inhibiting protein-protein interactions between TEAD and YAP1/TAZ.
储存/保存方法
Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.
基本信息
可溶性/溶解性
DMSO:215 mg/mL (747.20 mM)
生物活性
In vitro(体外研究)
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].
In vivo(体内研究)
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].