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首页-小分子抑制剂&激动剂-Nuclear Receptor/Transcription Factor-YAP-TEAD-MYF-01-37
MYF-01-37

Chemical Structure : MYF-01-37

CAS No.: 2416417-65-5

MYF-01-37 (MYF-1-37)

货号: PC-73155Not For Human Use, Lab Use Only.

MYF-01-37 (MYF-1-37) is a novel covalent TEAD inhibitor targeting Cys380, binds to palmitoylation pocket in TEAD1, targets YAP dependency upon combined EGFR/MEK inhibition.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

MYF-01-37 (MYF-1-37) is a novel covalent TEAD inhibitor targeting Cys380, binds to palmitoylation pocket in TEAD1, targets YAP dependency upon combined EGFR/MEK inhibition.
MYF-01-37 (MYF-1-37) exhibits inhibition of direct YAP/TEAD interaction in HEK 293T cells and the reduction in canonical YAP target gene CTGF expression in PC-9 cells, this redcution effect 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.
MYF-01-37 (MYF-1-37) combined with OT completely suppressed the increased YAP activity induced by OT treatment in PC-9 YAP reporter cells, led to a robust increase in BMF expression, and to subsequent increase in apoptosis in PC-9 and HCC4006 cells compared to OT alone

物理化学性质&存储条件

分子量 298.309
分子式 C15H17F3N2O
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

1-(3-methyl-3-((3-(trifluoromethyl)phenyl)amino)pyrrolidin-1-yl)prop-2-en-1-one

参考文献

1. Kari J Kurppa, et al. Cancer Cell. 2020 Jan 13;37(1):104-122.e12.

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