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Hypothemycin
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
Hypothemycin图片
CAS NO:76958-67-3
包装:1mg
市场价:3009元

产品介绍
Hypothemycin 是一种真菌聚酮化合物，是一种多激酶抑制剂，对 VEGFR2/VEGFR1、MEK1/MEK2、FLT-3、 PDGFRβ/PDGFRα，和 ERK1/ERK2，分别。
Cas No.76958-67-3
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 SMILESCOC1=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
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

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).