Phomopsin A
(Synonyms: 促微管解聚 A) 目录号 : GC15514
A β-tubulin inhibitor
Cas No.:64925-80-0
Sample solution is provided at 25 µL, 10mM.
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Phomopsin A is a cyclic hexapeptide mycotoxin that inhibits β-tubulin.
Phomopsins are a family of mycotoxins produced by the fungus Phomopsis leptostomiformis grows on lupins, which cause lupinosis, a severe liver disease of grazing animals [1][2].
Microtubules are one of the major components of the cytoskeleton that are essential in several cellular functions such as cell division and morphogenesis. α- and β-tubulins polymerize into microtubules.
Phomopsin A is a cyclic hexapeptide mycotoxin that binds β-tubulin in a vinca domain, partly overlapping with the site targeted by vinblastine and other tubulin inhibitors [2][3]. Phomopsin A noncompetitively inhibited the binding of radiolabeled vinblastine to tubulin with IC50 and Ki values of 0.8 μM and 2.8 μM, respectively. Phomopsin A potently inhibited tubulin-dependent GTP hydrolysis and nucleotide exchange on tubulin [2]. Phomopsin A, a vinca domain antimitotic peptide, also inhibited microtubule assembly [3][4]. Phomopsin A inhibited microtubule growth, modulated the dynamics of microtubules, and induced the self-association of tubulin dimers into single-walled rings and spirals [4].
References:
[1]. Hamel E. Natural products which interact with tubulin in the vinca domain: maytansine, rhizoxin, phomopsin A, dolastatins 10 and 15 and halichondrin B. Pharmacol Ther. 1992;55(1):31-51.
[2]. Cormier A, Marchand M, Ravelli RB, et al. Structural insight into the inhibition of tubulin by vinca domain peptide ligands. EMBO Rep. 2008 Nov;9(11):1101-6.
[3]. Li Y, Kobayashi H, Hashimoto Y, et al. Binding selectivity of rhizoxin, phomopsin A, vinblastine, and ansamitocin P-3 to fungal tubulins: differential interactions of these antimitotic agents with brain and fungal tubulins. Biochem Biophys Res Commun. 1992 Sep 16;187(2):722-9.
[4]. Mitra A, Sept D. Localization of the antimitotic peptide and depsipeptide binding site on beta-tubulin. Biochemistry. 2004 Nov 9;43(44):13955-62.
| Cas No. | 64925-80-0 | SDF | |
| 别名 | 促微管解聚 A | ||
| 化学名 | (2E)-(βS)-3-chloro-β,5-dihydroxy-N-methyl-L-tyrosyl-3,4-didehydro-L-valyl-3-hydroxy-L-isoleucyl-3,4-didehydro-L-prolyl-(2E)-2,3-didehydroisoleucyl-2,3-didehydro-aspartic acid, cyclic (15→3)-ether | ||
| Canonical SMILES | OC(/C(NC(/C(NC([C@H]1N(C([C@@H]2NC([C@H](C(C)=C)NC([C@@H](NC)[C@H](C3=CC(O[C@@]2(CC)C)=C(O)C(Cl)=C3)O)=O)=O)=O)CC=C1)=O)=C(CC)/C)=O)=C\C(O)=O)=O | ||
| 分子式 | C36H45ClN6O12 | 分子量 | 789.2 |
| 溶解度 | DMF: Soluble,DMSO: Soluble,Ethanol: Soluble,Methanol: Soluble | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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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 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.2671 mL | 6.3355 mL | 12.6711 mL |
| 5 mM | 0.2534 mL | 1.2671 mL | 2.5342 mL |
| 10 mM | 0.1267 mL | 0.6336 mL | 1.2671 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 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % 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。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet