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CAS No. | 2563855-03-6 | Cat. No. | BCP44951 |
Name | K-975 | ||
Synonyms | K975; K 975; | ||
SMILES | CC1=C(C=C(C=C1)NC(=O)C=C)OC2=CC=C(C=C2)Cl | ||
Chemical Name | |||
Formula | C16H14ClNO2 | M. Wt | 287.74 |
Purity | 98% | Storage | Store at 4-8°C |
Description | K-975 is a first-in-class TEAD inhibitor, directly inhibiting YAP/TAZ-TEAD protein-protein interaction and showing a potent anti-tumor effect in malignant pleural mesothelioma. K-975 was covalently bound to an internal cysteine residue located in the palmitate-binding pocket of TEAD. K-975 had a strong inhibitory effect against protein-protein interactions between YAP1/TAZ and TEAD in cell-free and cell-based assays. Furthermore, K-975 potently inhibited the proliferation of NF2-non-expressing MPM cell lines compared with NF2-expressing MPM cell lines. K-975 also suppressed tumor growth and provided significant survival benefit in MPM xenograft models. |
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