2-Propenamide, N-[3-(4-chlorophenoxy)-4-methylphenyl]-
![2-Propenamide, N-[3-(4-chlorophenoxy)-4-methylphenyl]- Structure](CAS/20210305/GIF/2563855-03-6.gif)
- CAS No.
- 2563855-03-6
- Chemical Name:
- 2-Propenamide, N-[3-(4-chlorophenoxy)-4-methylphenyl]-
- Synonyms
- K-975, 10 mM in DMSO;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
- Molecular Weight:
- 287.74
- MDL Number:
- MFCD34179527
- MOL File:
- 2563855-03-6.mol
- MSDS File:
- SDS
- TDS File:
- TDS
| 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 |
| NACRES | NA.28 |
2-Propenamide, N-[3-(4-chlorophenoxy)-4-methylphenyl]- price
| Manufacturer | Product number | Product description | CAS number | Packaging | Price | Updated | Buy |
|---|---|---|---|---|---|---|---|
| Sigma-Aldrich | SML4128 | K-975 ≥95% (HPLC) | 2563855-03-6 | 5 mg | $106 | 2026-04-30 | Buy |
| Sigma-Aldrich | SML4128 | K-975 ≥95% (HPLC) | 2563855-03-6 | 25 mg | $428 | 2026-04-30 | Buy |
| Sigma-Aldrich | SML4128 | K-975 ≥95% (HPLC) | 2563855-03-6 | 1 unit | $399 | 2025-07-31 | Buy |
| ChemScene | CS-0158891 | K-975 99.89% | 2563855-03-6 | 5mg | $107 | 2026-06-04 | Buy |
| ChemScene | CS-0158891 | K-975 99.89% | 2563855-03-6 | 10mg | $182 | 2026-06-04 | Buy |
2-Propenamide, N-[3-(4-chlorophenoxy)-4-methylphenyl]- Chemical Properties, Uses, Production
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
Raw materials
Preparation Products
2-Propenamide, N-[3-(4-chlorophenoxy)-4-methylphenyl]- Suppliers
| Supplier | Tel | Country | ProdList | Advantage | |
|---|---|---|---|---|---|
| Accela ChemBio Co.,Ltd. | 021-50795510 4000665055 | marketing@accelachem.com | China | 10972 | 64 |
| BOC Sciences | 1-631-485-4226; 16314854226 | info@bocsci.com | United States | 9920 | 65 |
| Zhengzhou Alfachem Co., Ltd. | 0371-53765687 18937137882 | 3969243885@qq.com | China | 7734 | 55 |
| Shanghai EFE Biological Technology Co., Ltd. | 021-65675885 18964387627 | info@efebio.com | China | 9799 | 58 |
| Shanghai YuanYe Biotechnology Co., Ltd. | 15026964105 | 2881489226@qq.com | China | 89667 | 60 |
| ShangHai Biochempartner Co.,Ltd | 177-54423994 17754423994 | 2853530910@QQ.com | China | 8000 | 62 |
| SuZhou Medinoah Co.,LTD. | 0512-69561983 13914027025 | zhang_q@medinoah.com | China | 3925 | 58 |
| TargetMol Chemicals Inc. | +1-781-999-5354; +1-00000000000 | marketing@targetmol.com | United States | 32431 | 58 |
| Blocksynth Pharmaceutical Technology Co.,Ltd | 0086-19817745290; 19817745290 | bd@blocksynth.com | China | 5971 | 58 |
| Accela ChemBio Inc. | +1-858-6993322 +86-18019713315 | info@accelachem.com | United States | 21189 | 58 |
