Sinefungin (trifluoroacetate salt)
(Synonyms: A 9145,Adenosyl-ornithine,Antibiotic A 9145) 目录号 : GC91760Sinefungin is a purine nucleoside and derivative of S-adenosylhomocysteine that has been found in Streptomyces and has diverse biological activities.
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >95.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Sinefungin is a purine nucleoside and derivative of S-adenosylhomocysteine that has been found in Streptomyces and has diverse biological activities.[1],[2] It inhibits G9a methyltransferase and SET domain-containing protein 7 (SET7) with IC50 values of 10.4 and 2.38 µM, respectively, using histone H3 (1-21) peptide as a substrate and 150 and 9.1 µM, respectively, using full-length histone H3 as a substrate.[3] It also inhibits protein arginine methyltransferase 5 (PRMT5) with IC50 values of 0.31 and 0.69 µM using histone H4 (1-21) peptide and full-length histone H4, respectively, as substrates. Sinefungin (10 mg/kg) reduces renal levels of the mesenchymal marker α-smooth muscle actin (α-SMA), fibrosis markers ferroptosis suppressor protein 1 (Fsp1), collagen 1, collagen 3, and fibronectin, and monomethylation of histone H3 lysine 4 (H3K4me1) in a mouse model of unilateral ureteral obstruction.[4]
References:
[1].Nolan, L.L.Molecular target of the antileishmanial action of sinefunginAntimicrob. Agents Chemother.31(10)1542-1548(1987).
[2].Maguire, M.P., Feldman, P.L., and Rapoport, H.Stereoselective synthesis and absolute stereochemistry of sinefunginJ. Org. Chem.55(3)948-955(1990).
[3].Horiuchi, K.Y., Eason, M.M., Ferry, J.J., et al.Assay development for histone methyltransferasesAssay Drug Dev. Technol.11(4)227-236(2013).
[4].Sasaki, K., Doi, S., Nakashima, A., et al.Inhibition of SET domain-containing lysine methyltransferase 7/9 ameliorates renal fibrosisJ. AM. Soc. Nephrol.27(1)203-215(2016).
| 制备储备液 | |||
 |
1 mg | 5 mg | 10 mg |
| 1 mM | 2.6219 mL | 13.1096 mL | 26.2192 mL |
| 5 mM | 0.5244 mL | 2.6219 mL | 5.2438 mL |
| 10 mM | 0.2622 mL | 1.311 mL | 2.6219 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。