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MYF-01-37
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
MYF-01-37图片
CAS NO:2416417-65-5
包装与价格:
包装价格(元)
2 mg电议
5 mg电议
10 mg电议
25 mg电议
50 mg电议
100 mg电议
200 mg电议

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

产品描述

MYF-01-37 is a novel covalent TEAD inhibitor.

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.

Cas No.

2416417-65-5

分子式

C15H17F3N2O

分子量

298.309

别名

1-[3-Methyl-3-[3-(trifluoromethyl)anilino]pyrrolidin-1-yl]prop-2-en-1-one

储存和溶解度

DMSO:55 mg/ml (184.38 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years