K-975

SKU: orb1297777

Description

K-975 is a potent and selective oral TEAD inhibitor that disrupts the TEAD-YAP1/TAZ protein-protein interaction. It is used in cancer research, particularly for mesothelioma and other malignancies driven by Hippo pathway dysregulation, and has demonstrated efficacy in both cellular assays and in vivo models.

Research Area

Stem Cell & Developmental Biology

Key Properties

• CAS Number: 2563855-03-6
• MW: 287.74
• Purity: 99.91% (May vary between batches)
• Formula: C₁₆H₁₄ClNO₂
• SMILES: Cc1ccc(NC(=O)C=C)cc1Oc1ccc(Cl)cc1
• Target: Others,YAP
• Solubility: DMSO:140 mg/mL (486.55 mM)

Bioactivity

• In Vivo:
  K-975 (10-300 mg/kg; p.o. twice daily for 14 days) suppresses tumor growth by inhibiting TEAD-YAP1/TAZ signaling in MPM xenograft mouse models .
• In Vitro:
  K-975 inhibits the cell proliferation of NRF2-non-expressing malignant pleural mesothelioma (MPM) cell lines, protein-protein interaction (PPI) between Halo-TAZ and TEAD1/4 and Halo-YAP and endogenous TEAD1/4 in NCl-H226 cells and the reporter activity in NCl-H661/CTGF-Luc cells with the maximum of ~70%, at concentration of 0.1-10000 nM at 144 h and 24 h, respectively . K-975 decreases the expression of IGFBP3, CTGF and NPPB mRNAs, and increases the expression of FBXO32 mRNA in NCl-H226 cells .
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Storage & Handling

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

Alternative Names

YAP, TAZ, TEAD,YAP1/TAZ, TEAD, Yes-associated protein, YAP1, pleural, mesothelioma, K975, K-975, K 975, inhibit, malignant, Inhibitor, Cys359, cancer, antitumor

Compound Identifiers

PubChem CID

155353714