| Description | K-975 is a highly selective, orally active TEAD inhibitor, effectively inhibiting protein-protein interactions between TEAD and YAP1/TAZ. |
| In vitro | K-975可抑制不表达NRF2的恶性胸膜间皮瘤(MPM)细胞系的细胞增殖，抑制NCl-H226细胞中Halo-TAZ与TEAD1/4以及Halo-YAP与内源性TEAD1/4之间的蛋白质-蛋白质相互作用(PPI)，以及在NCl-H661/CTGF-Luc细胞中的报告基因活性，最大抑制率约为70%，在0.1-10000 nM的浓度下，分别在144小时和24小时达到效果[1]。K-975还能降低NCl-H226细胞中IGFBP3、CTGF和NPPB mRNA的表达，并提高FBXO32 mRNA的表达[1]。 |
| In vivo | K-975（10-300 mg/kg；口服，每天两次，持续14天）通过抑制TEAD-YAP1/TAZ信号传导，在MPM异种移植小鼠模型中抑制肿瘤生长[1]。 |
| molecular weight | 287.74 |
| Molecular formula | C16H14ClNO2 |
| CAS | 2563855-03-6 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility | DMSO: 215 mg/mL (747.20 mM), Sonication is recommended. |
| References | 1. Ayumi Kaneda, et al. The novel potent TEAD inhibitor, K-975, inhibits YAP1/TAZ-TEAD protein-protein interactions and exerts an anti-tumor effect on malignant pleural mesothelioma. Am J Cancer Res. 2020 Dec 1;10(12):4399-4415. |