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Manumycin A

(Synonyms: 手霉素A) 目录号 : GC10265

A farnesyltransferase inhibitor with antitumor activity

Manumycin A Chemical Structure

Cas No.:52665-74-4

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产品描述

Manumycin A is an antibiotic that act as a potent and selective farnesyltransferase inhibitor [1].

Farnesyltransferase posttranslationally-modifies proteins by adding a farnesyl group to the -SH of the cysteine near the end of target proteins to form a thioether linkage. Farnesylation makes become membrane-associated.

Manumycin A is a potent and selective ras farnesyltransferase inhibitor. In cultured MB cells, Manumycin A (≥10 ?M) blocked p21 ras farnesylation and induced apoptosis [1]. In rat VSMCs, Manumycin A signi?cantly consistently inhibited [3H]-thymidine incorporation in a dose-dependent way and inhibited cell growth. In a trans-well assay, manumycin A (50 ng/ml) inhibited VSMC migration in the presence of 10 ng/ml of PDGF [2].

In myotonic dystrophy type 1 (DM1) mice with 250 CUG repeats, Manumycin A significantly reduced Clcn1 exon 7A inclusion and corrected aberrant splicing of Clcn1 [3].

References:

[1].Wang W, Macaulay RJ.  Apoptosis of medulloblastoma cells in vitro follows inhibition of farnesylation using manumycin A. Int J Cancer. 1999 Jul 30;82(3):430-4.
[2].Kouchi H, Nakamura K, Fushimi K, et al.  Manumycin A, inhibitor of ras farnesyltransferase, inhibits proliferation and migration of rat vascular smooth muscle cells. Biochem Biophys Res Commun. 1999 Nov 2;264(3):915-20.
[3].Oana K, Oma Y, Suo S, et al.  Manumycin A corrects aberrant splicing of Clcn1 in myotonic dystrophy type 1 (DM1) mice. Sci Rep. 2013;3:2142
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Chemical Properties

Cas No. 52665-74-4 SDF
别名 手霉素A
化学名 (R,2Z,4E)-N-((1S,5S,6R)-5-hydroxy-5-((1E,3Z,5Z)-7-((2-hydroxy-5-oxocyclopent-1-en-1-yl)amino)-7-oxohepta-1,3,5-trien-1-yl)-2-oxo-7-oxabicyclo[4.1.0]hept-3-en-3-yl)-2,4,6-trimethyldeca-2,4-dienamide
Canonical SMILES CCCC[C@H](/C=C(/C=C(C(NC1=C[C@@](/C=C/C=C\C=C/C(NC2=C(CCC2=O)O)=O)([C@@H]3O[C@@H]3C1=O)O)=O)/C)C)C
分子式 C31H38N2O7 分子量 550.64
溶解度 DMF: 20 mg/ml,DMF:PBS (pH 7.2) (1:1): 0.5 mg/ml,DMSO: 10 mg/ml,Ethanol: 5 mg/ml 储存条件 Store at -20°C
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1 mM 1.8161 mL 9.0803 mL 18.1607 mL
5 mM 0.3632 mL 1.8161 mL 3.6321 mL
10 mM 0.1816 mL 0.908 mL 1.8161 mL
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