2-Propenamide, N-[3-(4-chlorophenoxy)-4-methylphenyl]-
- Product Name
- 2-Propenamide, N-[3-(4-chlorophenoxy)-4-methylphenyl]-
- CAS No.
- 2563855-03-6
- Chemical Name
- 2-Propenamide, N-[3-(4-chlorophenoxy)-4-methylphenyl]-
- Synonyms
- N-[3-(4-Chlorophenoxy)-4-methylphenyl]acrylamide;2-Propenamide, N-[3-(4-chlorophenoxy)-4-methylphenyl]-;YAP1,Cys359,pleural,TAZ,K 975,inhibit,K-975,Yes-associated protein,YAP,Inhibitor,antitumor,malignant,TEAD,K975,mesothelioma,cancer
- CBNumber
- CB29009022
- Molecular Formula
- C16H14ClNO2
- Formula Weight
- 287.74
- MOL File
- 2563855-03-6.mol
2-Propenamide, N-[3-(4-chlorophenoxy)-4-methylphenyl]- Property
- Boiling point:
- 442.5±45.0 °C(Predicted)
- Density
- 1.235±0.06 g/cm3(Predicted)
- storage temp.
- Store at -20°C, protect from light
- solubility
- DMSO : 220 mg/mL (764.58 mM; Need ultrasonic)
- pka
- 13.09±0.70(Predicted)
N-Bromosuccinimide Price
- Product number
- CS-0158891
- Product name
- K-975
- Packaging
- 5mg
- Price
- $200
- Updated
- 2021/12/16
- Product number
- CS-0158891
- Product name
- K-975
- Packaging
- 10mg
- Price
- $350
- Updated
- 2021/12/16
- Product number
- CS-0158891
- Product name
- K-975
- Packaging
- 25mg
- Price
- $650
- Updated
- 2021/12/16
- Product number
- CS-0158891
- Product name
- K-975
- Packaging
- 50mg
- Price
- $950
- Updated
- 2021/12/16
- Product number
- CS-0158891
- Product name
- K-975
- Packaging
- 100mg
- Price
- $1350
- Updated
- 2021/12/16
2-Propenamide, N-[3-(4-chlorophenoxy)-4-methylphenyl]- Chemical Properties,Usage,Production
Biological Activity
K-975 is a potent, selective and orally active TEAD inhibitor, with a strong inhibitory effect against protein-protein interactions between YAP1/TAZ and TEAD. K-975 covalently binds to Cys359 located in the palmitate-binding pocket of TEAD via an acrylamide structure. K-975 exhibits antitumor activity on malignant pleural mesothelioma[1]. K-975 (0.1-10000 nM; 144 h) inhibits the cell proliferation of NF2-non-expressing malignant pleural mesothelioma (MPM) cell lines[1].K-975 (10-10000 nM; 24 h) inhibits protein-protein interaction (PPI) between Halo-YAP and endogenous TEAD1/4 and Halo-TAZ and TEAD1/4 in NCI-H226 cells[1].K-975 (0.1-10000 nM; 24 h) strongly inhibits the reporter activity in NCI-H661/CTGF-Luc cells, with the maximum inhibition of ~70%, and does not inhibit the reporter activity in NCI-H661/NRF2-Luc cells[1].K-975 (1-10000 nM; 24 h) decreases the expressions of CTGF, IGFBP3, and NPPB mRNAs, and increases the expression of FBXO32 mRNA in NCI-H226 cells[1]. K-975 (10-300 mg/kg; p.o. twice a day for 14 days) inhibits the tumor growth by inhibiting YAP1/TAZ-TEAD signaling in MPM xenograft mouse models[1].
References
[1]. Kaneda A, et, al. The novel potent TEAD inhibitor, K-975, inhibits YAP1/TAZ-TEAD protein-protein interactions and exerts an anti-tumor effect on malignant pleural mesothelioma. Am J Cancer Res. 2020 Dec 1;10(12):4399-4415.
2-Propenamide, N-[3-(4-chlorophenoxy)-4-methylphenyl]- Preparation Products And Raw materials
Raw materials
Preparation Products
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