| Name | K-975 |
| 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]. |
| 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/Shipping at ambient temperature. |
| Solubility Information | DMSO : 140 mg/mL (486.55 mM), Sonication is recommended.
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| Keywords | Yes-associated protein | YAP1 | YAP | TEAD,YAP1/TAZ | TEAD | TAZ | pleural | mesothelioma | malignant | K-975 | K975 | K 975 | Inhibitor | inhibit | Cys359 | cancer | antitumor |
| Inhibitors Related | AICAR | MY-1076 | YAP-TEAD-IN-3 | Verteporfin | DC-TEADin02 | MSC-4106 | OPN-9652 | VT107 | PY-60 | VT104 | MYF-01-37 | Ki16425 |
| Related Compound Libraries | Highly Selective Inhibitor Library | Cysteine Covalent Library | Bioactive Compound Library | Inhibitor Library | Stem Cell Differentiation Compound Library | Orally Active Compound Library | PPI Inhibitor Library | Bioactive Compounds Library Max | Covalent Inhibitor Library | Wnt/Hedgehog/Notch Compound Library |