MYF-01-37

SKU: orb1305966

Description

MYF-01-37 is a novel, covalent small-molecule inhibitor targeting the TEAD transcription factors. It is a valuable research tool for investigating the Hippo signaling pathway in cancer biology, with utility in both in vitro and in vivo experimental models.

Research Area

Stem Cell & Developmental Biology

Key Properties

• CAS Number: 2416417-65-5
• MW: 298.3
• Purity: 99.50% (May vary between batches)
• Formula: C₁₅H₁₇F₃N₂O
• SMILES: CC1(CCN(C1)C(=O)C=C)Nc1cccc(c1)C(F)(F)F
• Target: YAP
• Solubility: DMSO:55 mg/mL (184.38 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (6.7 mM)

Bioactivity

• In Vitro:
  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.
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

HEK293T, Inhibitor, inhibit, MYF 01 37, MYF0137, MYF-01-37, Cys380, 1-[3-Methyl-3-[3-(trifluoromethyl)anilino]pyrrolidin-1-yl]prop-2-en-1-one, TEAD, Yes-associated protein, YAP/TEAD, YAP

Compound Identifiers

PubChem CID

146567795