MG-115

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

MG-115 

MG-115 是一种有效和可逆的蛋白酶体抑制剂,对 20S26S 蛋白酶体的 Ki 值分别为 21 nM 和 35 nM。MG-115 特异性抑制蛋白酶体的胰凝乳蛋白酶样活性,诱导 p53 依赖性细胞凋亡。

MG-115

MG-115 Chemical Structure

CAS No. : 133407-86-0

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生物活性

MG-115 is a potent and reversible proteasome inhibitor, with Kis of 21 nM and 35 nM for 20S and 26S proteasome, respectively. MG-115 specifically inhibit the chymotrypsin-like activity of the proteasome, induces p53-dependent apoptosis[1][2][3].

IC50 & Target

Ki: 21 nM (20S proteasome); 35 nM (26 Sproteasome)[1]

体外研究
(In Vitro)

MG-115 (0.1-10 μM; 24 h) dose-dependently decreases the viability of HepG2 cells[3].
MG-115 (0.1-10 μM; 24 h) amplifies the reporter gene expression mediated by CWK18 DNA condensates[3].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[3]

Cell Line: HepG2 cells
Concentration: 0.1, 1, 2, 5, 10 μM
Incubation Time: 24 hours
Result: Dose-dependently decreased cell viability.
Inhibited the proteasomal activity, with an IC50 of 2 μM.

分子量

461.59

Formula

C25H39N3O5

CAS 号

133407-86-0

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

参考文献
  • [1]. Rock KL, et, al. Inhibitors of the proteasome block the degradation of most cell proteins and the generation of peptides presented on MHC class I molecules. Cell. 1994 Sep 9;78(5):761-71.

    [2]. Lopes UG, et, al. p53-dependent induction of apoptosis by proteasome inhibitors. J Biol Chem. 1997 May 16;272(20):12893-6.

    [3]. Kim J, et, al. The proteasome metabolizes peptide-mediated nonviral gene delivery systems. Gene Ther. 2005 Nov;12(21):1581-90.

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