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首页-小分子抑制剂&激动剂-Nuclear Receptor/Transcription Factor-YAP-TEAD-K-975
K-975

Chemical Structure : K-975

CAS No.: 2563855-03-6

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K-975 (YAP1-TEAD inhibitor K975)

货号: PC-72171Not For Human Use, Lab Use Only.

K-975 (K975, YAP1-TEAD inhibitor K975) is a potent, specific inhibitor of YAP1/TAZ-TEAD signaling, inhibits YAP1/TAZ-TEAD protein-protein interaction, a pan-TEAD inhibitor binds to Cys359 of TEAD1-YBD.

规格 价格 库存 数量
5 mg ￥1280 In stock
10 mg ￥1980 In stock
25 mg ￥3280 In stock
50 mg ￥5280 In stock
100 mg Get quote
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

K-975 (K975, YAP1-TEAD inhibitor K975) is a potent, specific inhibitor of YAP1/TAZ-TEAD signaling, inhibits YAP1/TAZ-TEAD protein-protein interaction, a pan-TEAD inhibitor binds to Cys359 of TEAD1-YBD.
K-975 showed an inhibitory activity towards TEAD1-YAP1 PPI and TEAD4-YAP1 PPI  in cells using a Halo-tag pull-down assay. Furthermore, K-975 inhibited the palmitoylation of TEAD1-YBD.
K-975 inhibits yes-associated protein 1 (YAP1)-transcriptional enhanced associate domain (TEAD) signaling by the same mechanism as YAP1 siRNA and TEADs siRNA.
K-975 decreased the expressions of CTGF, IGFBP3, and NPPB mRNAs, and increased the expression of FBXO32 mRNA with 24-h treatment in NCI-H226 cells.
K-975 exerts a stronger inhibitory activity towards neurofibromin 2 (NF2)-non-expressing mesothelioma cell lines.
K-975 exerts an anti-tumor effect and significant survival benefit in human mesothelioma xenograft mice.
K-975 exhibits a synergistic effect with a CDK4/6 inhibitor palbociclib in s.c. transplant mouse models of human mesothelioma.

物理化学性质&存储条件

分子量 287.743
分子式 C16H14ClNO2
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

N-(3-(4-chlorophenoxy)-4-methylphenyl)acrylamide

参考文献

1. Kaneda A, et al. Am J Cancer Res. 2020 Dec 1;10(12):4399-4415.

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