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K-975 is a highly selective, orally active TEAD inhibitor, effectively inhibiting protein-protein interactions between TEAD and YAP1/TAZ.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $67 | In Stock | |
5 mg | $163 | In Stock | |
10 mg | $263 | In Stock | |
25 mg | $528 | In Stock | |
50 mg | $747 | In Stock | |
1 mL x 10 mM (in DMSO) | $178 | In Stock |
Description | K-975 is a highly selective, orally active TEAD inhibitor, effectively inhibiting protein-protein interactions between TEAD and YAP1/TAZ. |
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 [1]. K-975 decreases the expression of IGFBP3, CTGF and NPPB mRNAs, and increases the expression of FBXO32 mRNA in NCl-H226 cells [1]. |
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 [1]. |
Molecular Weight | 287.74 |
Formula | C16H14ClNO2 |
Cas No. | 2563855-03-6 |
Smiles | Cc1ccc(NC(=O)C=C)cc1Oc1ccc(Cl)cc1 |
Storage | store at low temperature,keep away from direct sunlight,keep away from moisture | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
Solubility Information | DMSO: 215 mg/mL (747.20 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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