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2-Propenamide, N-[3-(4-chlorophenoxy)-4-methylphenyl]- manufacturers
- K-975
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- $35.00
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2026-06-02
- CAS:2563855-03-6
- Purity: 99.43%
- Supply Ability: 10g
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| | 2-Propenamide, N-[3-(4-chlorophenoxy)-4-methylphenyl]- Basic information |
| Product Name: | 2-Propenamide, N-[3-(4-chlorophenoxy)-4-methylphenyl]- | | Synonyms: | 2-Propenamide, N-[3-(4-chlorophenoxy)-4-methylphenyl]-;N-[3-(4-Chlorophenoxy)-4-methylphenyl]acrylamide;YAP1,Cys359,pleural,TAZ,K 975,inhibit,K-975,Yes-associated protein,YAP,Inhibitor,antitumor,malignant,TEAD,K975,mesothelioma,cancer;K-975, 10 mM in DMSO | | CAS: | 2563855-03-6 | | MF: | C16H14ClNO2 | | MW: | 287.74 | | EINECS: | | | Product Categories: | | | Mol File: | 2563855-03-6.mol | ![2-Propenamide, N-[3-(4-chlorophenoxy)-4-methylphenyl]- Structure](CAS/20210305/GIF/2563855-03-6.gif) |
| | 2-Propenamide, N-[3-(4-chlorophenoxy)-4-methylphenyl]- Chemical Properties |
| 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) | | form | Solid | | pka | 13.09±0.70(Predicted) | | color | White to off-white | | SMILES | O=C(NC1=CC=C(C)C(OC2=CC=C(C=C2)Cl)=C1)C=C |
| | 2-Propenamide, N-[3-(4-chlorophenoxy)-4-methylphenyl]- Usage And Synthesis |
| Uses | 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]. | | 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]. | | in vivo | 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]. | Animal Model: | Male SCID mice (5 weeks) injected with NCI-H226 or MSTO-211H cells[1] | | Dosage: | 10, 30, 100, 300 mg/kg | | Administration: | P.o. twice a day for 14 days | | Result: | Exhibited strong anti-tumor effect in MPM s.c. xenograft mouse models.
Decreased the expressions of CTGF, IGFBP3, and NPPB, and increased the expression of FBXO32 in the NCI-H226 xenograft model. |
| | 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 |
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