Manumycin A
(Synonyms: 手霉素A) 目录号 : GC10265A farnesyltransferase inhibitor with antitumor activity
Cas No.:52665-74-4
Sample solution is provided at 25 µL, 10mM.
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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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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Shipping Condition | 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。 |
制备储备液 | |||
1 mg | 5 mg | 10 mg | |
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 |
第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量) | ||||||||||
给药剂量 | mg/kg | 动物平均体重 | g | 每只动物给药体积 | ul | 动物数量 | 只 | |||
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% DMSO % % Tween 80 % saline | ||||||||||
计算重置 |
计算结果:
工作液浓度: mg/ml;
DMSO母液配制方法: mg 药物溶于 μL DMSO溶液(母液浓度 mg/mL,
体内配方配制方法:取 μL DMSO母液,加入 μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入 μL saline,混匀澄清。
1. 首先保证母液是澄清的;
2.
一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。
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