K-975

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

K-975 是一种高选择性、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.(In Vitro):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 . K-975 decreases the expression of IGFBP3, CTGF and NPPB mRNAs, and increases the expression of FBXO32 mRNA in NCl-H226 cells .(In Vivo):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 .

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. Cell Proliferation Assay Cell 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 Analysis Cell Line:NCI-H226 cells Concentration:10, 100, 1000, 10000 nMIncubation Time:24 hoursResult:Inhibited TEAD1-YAP1 PPI and TEAD4-YAP1 PPI.Inhibited TEAD1-TAZ PPI and TEAD4-TAZ PPI.

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. 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.Decreased the expressions of CTGF, IGFBP3, and NPPB, and increased the expression of FBXO32 in the NCI-H226 xenograft model.

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Others

Other Targets

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2563855-03-6

287.74

C16H14ClNO2

>98% (HPLC)

In Vitro:?DMSO : 220 mg/mL (764.58 mM)

CC1=CC=C(NC(=O)C=C)C=C1OC1=CC=C(Cl)C=C1

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(-20℃)

With Ice Pack

≥ 2 years