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Hypothemycin

(Synonyms: 寄端霉素) 目录号 : GC43885

A resorcylic acid lactone polyketide with diverse biological activities

Hypothemycin Chemical Structure

Cas No.:76958-67-3

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Description

Hypothemycin is a resorcylic acid lactone polyketide originally isolated from H. tricothecoides that has diverse biological activities, including fungicidal, kinase inhibitory, and anticancer properties.[1],[2],[3],[4,][5],[6] It is active against the pathogenic fungi P. litchii, completely inhibiting spore germination when used at a concentration of 0.78 µg/ml.[2] Hypothemycin inhibits MEK (IC50 = 15 nM) and other protein kinases containing a conserved cysteine residue in the ATP-binding domain, including ERK, PDGFR, VEGFR, PKD1, and MAPKAP5/MK5.[3],[4] It also inhibits transforming growth factor β-activated kinase 1 (TAK1) in vitro (IC50 = 33 nM).[5] Hypothemycin inhibits proliferation of cancer cell lines dependent on activating mutations, including A549, MV-4-11, and EOL1 cells (IC50s = 6, 0.006, and 0.0004 µM, respectively) and reduces tumor growth in Ma44 and HCT116 mouse xenograft models when administered at a dose of 25 mg/kg per day.[4],[6]

Reference:
1. Agatsuma, T., Takahashi, A., Kabuto, C., et al. Revised structure and stereochemistry of hypothemycin. Chem. Pharm. Bull. 41(2), 373-375 (1993).
2. Xu, L., Xue, J., Wu, P., et al. Antifungal activity of hypothemycin against Peronophythora litchii in vitro and in vivo. J. Agric. Food Chem. 61(42), 10091-10095 (2013).
3. Zhao, A., Lee, S.H., Mojena, M., et al. Resorcylic acid lactones: Naturally occurring potent and selective inhibitors of MEK. J. Antibiot. (Tokyo) 52(12), 1086-1094 (1999).
4. Schirmer, A., Kennedy, J., Murli, S., et al. Targeted covalent inactivation of protein kinases by resorcylic acid lactone polyketides. Proc. Nat. Acad. Sci. USA 103(11), 4234-4239 (2006).
5. 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 analogues. Bioorg. Med. Chem. 23(21), 6993-6999 (2015).
6. Tanaka, H., Nishida, K., Sugita, K., et al. Antitumor efficacy of hypothemycin, a new Ras-signaling inhibitor. Jpn. J. Cancer Res. 90(10), 1139-1145 (1999).

化学性质

Cas No. 76958-67-3 SDF
别名 寄端霉素
化学名 (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
Canonical SMILES COC1=CC(O)=C(C(O[C@@H](C)C/C=C\C2=O)=O)C([C@@H]3[C@](O3)([H])C[C@H](O)[C@@H]2O)=C1
分子式 C19H22O8 分子量 378.4
溶解度 DMSO: 10 mg/ml 储存条件 Store at -20°C
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1 mM 2.6427 mL 13.2135 mL 26.4271 mL
5 mM 0.5285 mL 2.6427 mL 5.2854 mL
10 mM 0.2643 mL 1.3214 mL 2.6427 mL
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