化合物MYF-01-37 T22372

Product Introduction
Bioactivity


英文名: MYF-01-37

描述: MYF-01-37 (1-[3-Methyl-3-[3-(trifluoromethyl)anilino]pyrrolidin-1-yl]prop-2-en-1-one) 是共价TEAD 抑制剂，靶向 Cys380，能够可逆地抑制 YAP/TEAD 相互作用。

体外活性: Pretreating cells with MYF-01–37 led to loss of direct TEAD pull-down by biotin-MYF-01–037 ?from whole-cell lysate, confirming MYF-01–037 binding to TEAD in cells.?This target engagement of TEAD resulted in inhibition of direct YAP/TEAD interaction in HEK 293T cells, and in the reduction in canonical YAP target gene CTGF expression in PC-9 cells.?This reduction was abrogated by the overexpression of TEAD1 C359S mutant that disrupts the covalent binding of the drug to TEAD, but not by overexpression of wild-type TEAD1, demonstrating that the observed inhibition of YAP activity is due to on-target covalent binding of the compound to TEAD.

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 55 mg/ml (184.38 mM)


关键字: Cys380 | MYF 01 37 | MYF-01-37 | inhibit | Inhibitor | MYF0137 | YAP/TEAD | Yes-associated protein | HEK293T | YAP

相关产品: DC-TEADin02 | Verteporfin | YAP-TEAD-IN-2 | VT103 | IK-930 | VT107 | YAP-TEAD-IN-1 acetate | YAP-TEAD-IN-3 | TEAD-IN-6 | Lats-IN-1

相关库: Bioactive Compounds Library Max | Inhibitor Library | PPI Inhibitor Library | Stem Cell Differentiation Compound Library | NO PAINS Compound Library | Bioactive Compound Library

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途