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TM2 TEAD抑制剂是一种有效并且可逆的TEA领域转录因子抑制剂(IC50为TEAD4自动棕榈酰化和TEAD2棕榈酰化分别为38 nM和156 nM)。它抑制TEAD-YAP的结合和转录活性。TM2 TEAD抑制剂在YAP依赖型癌症细胞中,无论是单独使用还是与MEK抑制剂联合使用,都显示出强大的抗增殖效果。同时抑制体外YAP依赖的肝脏类器官生长。
TM2 TEAD抑制剂是一种有效并且可逆的TEA领域转录因子抑制剂(IC50为TEAD4自动棕榈酰化和TEAD2棕榈酰化分别为38 nM和156 nM)。它抑制TEAD-YAP的结合和转录活性。TM2 TEAD抑制剂在YAP依赖型癌症细胞中,无论是单独使用还是与MEK抑制剂联合使用,都显示出强大的抗增殖效果。同时抑制体外YAP依赖的肝脏类器官生长。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
10 mg | ¥ 2,360 | 35日内发货 | |
50 mg | ¥ 9,950 | 35日内发货 |
产品描述 | TM2 TEAD inhibitor, a robust and reversible inhibitor of the TEA domain transcription factor, presents dual inhibitory concentrations (IC50) of 38 nM for TEAD4 auto-palmitoylation and 156 nM for TEAD2 palmitoylation. It effectively blocks the TEAD-YAP association and their transcriptional activities, leading to significant antiproliferative effects in YAP-dependent cancer cell lines, both as a standalone agent and in combination with a MEK inhibitor. Additionally, it impedes YAP-dependent liver organoid growth ex vivo. |
分子量 | 435.57 |
分子式 | C26H33N3O3 |
CAS No. | 1008768-41-9 |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
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