Hypothemycin
Cat. No.：YN350048
| 产品名称: | Hypothemycin |
| CAS No.: | 76958-67-3 |
| Chemical Name: | (1aR,3S,4S,6Z,9S,15bR)-1a,8,9,15b-tetrahydro-3,4,12-trihydroxy-14-methoxy-9-methyl-3H-oxireno[k][2]benzoxacyclotetradecin-5,11(2H,4H)-dione |
| Synonyms: | 寄端霉素 |
| 分子量: | 378.37 |
| 分子式: | C₁₉H₂₂O₈ |
| SMILES: | COC1=CC(O)=C(C(O[C@@H](C)C/C=C\C2=O)=O)C([C@@H](O3)[C@@]3([H])C[C@H](O)[C@@H]2O)=C1 |
| 存储: | Please store the product under the recommended conditions in theCertificate of Analysis. |
| 运输: | Room temperature in continental US; may vary elsewhere. |
| 产品描述: | Hypothemycin 是由真菌产生的聚酮化合物，是一种多激酶抑制剂，对VEGFR2/VEGFR1，MEK1/MEK2，FLT-3，PDGFRβ/PDGFRα和ERK1/ERK2的Ki值分别为 10/70 nM，17/38 nM, 90 nM，900 nM/1.5 μM 和 8.4/2.4 μM。 |
| IC50和靶点: | [{name:"VEGFR2:10 nM (Ki)"},{name: "VEGFR1:70 nM (Ki)"},{name: "MEK1:17 nM (Ki)"},{name: "MEK2:38 nM (Ki)"},{name: "FLT-3:90 nM (Ki)"},{name: "PDGFRα:1.5 μM (Ki)"},{name: "PDGFRβ:900 nM (Ki)"},{name: "ERK1:8.4 μM (Ki)"},{name: "ERK2:2.4 μM (Ki)"}] |
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Agatsuma, T., Takahashi, A., Kabuto, C., et al.Revised structure and stereochemistry of hypothemycinChem. Pharm. Bull.41(2),373-375(1993)
Xu, L., Xue, J., Wu, P., et al.Antifungal activity of hypothemycin against Peronophythora litchii in vitro and in vivoJ. Agric. Food Chem.61(42),10091-10095(2013)
Zhao, A., Lee, S.H., Mojena, M., et al.Resorcylic acid lactones: Naturally occurring potent and selective inhibitors of MEKJ. Antibiot. (Tokyo)52(12),1086-1094(1999)
Schirmer, A., Kennedy, J., Murli, S., et al.Targeted covalent inactivation of protein kinases by resorcylic acid lactone polyketidesProc. Natl. Acad. Sci. USA103(11),4234-4239(2006)
Fakhouri, L., El-Elimat, T., Hurst, D.P., et al.Isolation, semisynthesis, covalent docking and transforming growth factor beta-activated kinase 1 (TAK1)-inhibitory activities of (5Z)-7-oxozeaenol analoguesBioorg. Med. Chem.23(21),6993-6999(2015)
Tanaka, H., Nishida, K., Sugita, K., et al.Antitumor efficacy of hypothemycin, a new Ras-signaling inhibitorJpn. J. Cancer Res.90(10),1139-1145(1999)
