K-975

K-975

K647962-5mg

5mg

≥98%

-20°C储存

超低温冰袋运输

K-975 is a potent, selective and orally active TEAD inhibitor, with a strong inhibitory effect against protein-protein interactions between YAP1/TAZ and TEAD. K-975 covalently binds to Cys359 located in the palmitate-binding pocket of TEAD via an acrylamide structure. K-975 exhibits antitumor activity on malignant pleural mesothelioma In Vitro K-975 (0.1-10000 nM; 144 h) inhibits the cell proliferation of NF2-non-expressing malignant pleural mesothelioma (MPM) cell lines. K-975 (10-10000 nM; 24 h) inhibits protein-protein interaction (PPI) between Halo-YAP and endogenous TEAD1/4 and Halo-TAZ and TEAD1/4 in NCI-H226 cells. K-975 (0.1-10000 nM; 24 h) strongly inhibits the reporter activity in NCI-H661/CTGF-Luc cells, with the maximum inhibition of ~70%, and does not inhibit the reporter activity in NCI-H661/NRF2-Luc cells. K-975 (1-10000 nM; 24 h) decreases the expressions of CTGF , IGFBP3 , and NPPB mRNAs, and increases the expression of FBXO32 mRNA in NCI-H226 cells. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Proliferation AssayCell Line: NF2-non-expressing MPM and NF2-expressing malignant MPM cells Concentration: 0.1, 1, 10, 100, 1000, 10000 nM Incubation Time: 144 hours Result: Had a stronger inhibitory effect against NF2-non-expressing cell lines than NF2-expressing cell lines. Inhibited the proliferation of MSTO-211H cells, an NF2-expressing cell line. Western Blot AnalysisCell Line: NCI-H226 cells Concentration: 10, 100, 1000, 10000 nM Incubation Time: 24 hours Result: Inhibited TEAD1-YAP1 PPI and TEAD4-YAP1 PPI. Inhibited TEAD1-TAZ PPI and TEAD4-TAZ PPI. In Vivo K-975 (10-300 mg/kg; p.o. twice a day for 14 days) inhibits the tumor growth by inhibiting YAP1/TAZ-TEAD signaling in MPM xenograft mouse models . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Male SCID mice (5 weeks) injected with NCI-H226 or MSTO-211H cells Dosage: 10, 30, 100, 300 mg/kg Administration: P.o. twice a day for 14 days Result: Exhibited strong anti-tumor effect in MPM s.c. xenograft mouse models.\nDecreased the expressions of CTGF , IGFBP3 , and NPPB , and increased the expression of FBXO32 in the NCI-H226 xenograft model. Form:Solid IC50& Target:TEAD

K-975 是一种强效、选择性和口服活性 TEAD 抑制剂，对 YAP1/TAZ 和 TEAD 之间的蛋白-蛋白相互作用有很强的抑制作用。K-975 通过丙烯酰胺与位于 TEAD 棕榈酸酯结合袋中的 Cys359 共价结合，从而抑制 TEAD 与 YAP1/TAZ 之间的蛋白质相互作用。

2563855-03-6

C16H14ClNO2

287.74 g/mol

155353714

N-[3-(4-chlorophenoxy)-4-methylphenyl]prop-2-enamide

1S/C16H14ClNO2/c1-3-16(19)18-13-7-4-11(2)15(10-13)20-14-8-5-12(17)6-9-14/h3-10H,1H2,2H3,(H,18,19)

KPXAHQSIROUBPH-UHFFFAOYSA-N

CC1=C(C=C(C=C1)NC(=O)C=C)OC2=CC=C(C=C2)Cl

155353714

DMSO : 220 mg/mL (764.58 mM; Need ultrasonic)