GlpBio

MG-115

目录号: GC10178纯度: >98.00%同义词: MG115,蛋白酶体抑制剂,Carbobenzoxy-L-leucyl-L-leucyl-L-norvalinal, Z-LL-Nva-CHO, Proteasome Inhibitor XII,MG115
MG-115 是一种有效的抑制剂，对 20S 和 26S 蛋白酶体的 Kis 分别为 21 nM 和 35 nM 。
MG-115
Cas No.: 133407-86-0
规格价格库存数量操作
1mg¥350.00现货
1
5mg¥700.00现货
1
10mg¥1,190.00现货
1
25mg¥2,380.00现货
1
50mg¥3,948.00现货
1
10mM (in 1mL DMSO)¥711.00现货
1
电话: 400-920-5774Email: sales@glpbio.cn

文献被引

本产品暂无引用记录;以下为 GlpBio 产品在 Nature / Cell / Science 等顶刊的客户引用样例
  • Nature cover
    Nature
    641, 529–536 (2025)
  • Nature cover
    Nature
    628, 630–638 (2024)
  • Nature cover
    Nature
    632, 686–694 (2024)
  • Nature cover
    Nature
    618, 1017–1023 (2023)
  • Nature cover
    Nature
    610, 366–372 (2022)
  • Cell cover
    Cell
    187(9):2288-2304 (2024)
  • Cell cover
    Cell
    183(7):1867-1883 (2020)
  • Science cover
    Science
    388(6745) (2025)
  • Science cover
    Science
    387(6739) (2025)
  • Science cover
    Science
    387(6734) (2025)
  • Cell Research cover
    Cell Research
    35, 97–116 (2025)
  • Cell Research cover
    Cell Research
    34, 683–706 (2024)
  • Cell Research cover
    Cell Research
    33, 273–287 (2023)
  • Cell Research cover
    Cell Research
    33, 546–561 (2023)
  • Cell Research cover
    Cell Research
    33, 904–922 (2023)
  • Cell Research cover
    Cell Research
    31, 1291–1307 (2021)

产品描述 Description

MG-115 is a potent inhibitor with Kis of 21 nM and 35 nM for 20S and 26S proteasome, respectively [1].

MG-115 (50 μM, 2 h) increased the expression of the insulin receptor and its mature beta subunit by a factor of 3 and 4.2, respectively in Leu1193 and Asp1179 COS-7 mutant cell lines[2].Treated Rat-1 and PC12 cells with MG-115(30 μM, 4 h) can induced apoptosis of both cell types[3]. Iisolated rat islets were cultured and pre-treated with proteasome inhibitors and subsequently exposed for 48 h to 25 U/ml human IL-1beta. Pre-treatment with 10 uM of the proteasome inhibitor MG-115 counteracted the suppressive effects[4]. HCC cells SK-Hep1, HLE and HepG2 were treated with the proteasome inhibitors MG-115. MG-115 induce apoptosis in the three cell types tested in a dose-dependent manner. MG-115 downregulated expression of XIAP in SK-Hep1, and survivin in SK-Hep1 and HepG2[5]. MG-115 decreased within 120 min the aldosterone and corticosterone secretion from freshly dispersed zona glomerulosa and zona fasciculata-reticularis (ZF/R) cells. After a 24-h incubation MG-115 alone lowered corticosterone production and enhanced proliferation rate of cultured ZF/R cells[6]. The proteasome inhibitor MG-115 can inhibit ATF6, which is the direct target of the proteasome-ubiquitin pathway[7]. MG-115 was diminished by adding at a time corresponding to the half time required for germinal vesicle breakdown. Potent inhibition of germinal vesicle breakdown was also observed by microinjection of anti-proteasome-a-subunit antibodies[8]. MG-115 induced a decrease in Bid, Bcl-2, and survivin protein levels, an increase in Bax, loss of the mitochondrial transmembrane potential, cytochrome c release, activation of caspases (-8, -9 and -3), and an increase in the tumor suppressor p53 levels in PC3[9].

References:
[1]. Rock KL, Gramm C, 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. doi: 10.1016/s0092-8674(94)90462-6. PMID: 8087844.
[2]. Imamura T, Haruta T, et,al. Involvement of heat shock protein 90 in the degradation of mutant insulin receptors by the proteasome. J Biol Chem. 1998 May 1;273(18):11183-8. doi: 10.1074/jbc.273.18.11183. PMID: 9556607
[3]. Lopes UG, Erhardt P, et,al. p53-dependent induction of apoptosis by proteasome inhibitors. J Biol Chem. 1997 May 16;272(20):12893-6. doi: 10.1074/jbc.272.20.12893. PMID: 9148891.
[4]. Sternesj? J, Karlsen AE, et,al.Involvement of the proteasome in IL-1beta induced suppression of islets of Langerhans in the rat. Ups J Med Sci. 2003;108(1):37-50. doi: 10.3109/2000-1967-122. PMID: 12903836.
[5]. Inoue T, Shiraki K, et,al. Proteasome inhibition sensitizes hepatocellular carcinoma cells to TRAIL by suppressing caspase inhibitors and AKT pathway. Anticancer Drugs. 2006 Mar;17(3):261-8. doi: 10.1097/00001813-200603000-00004. PMID: 16520654.
[6]. Ziolkowska A, Tortorella C, et,al.Accumulation of steroidogenic acute regulatory protein mRNA, and decrease in the secretory and proliferative activity of rat adrenocortical cells in the presence of proteasome inhibitors. Int J Mol Med. 2006 May;17(5):865-8. PMID: 16596272.
[7]. Hong M, Li M, et,al. Endoplasmic reticulum stress triggers an acute proteasome-dependent degradation of ATF6. J Cell Biochem. 2004 Jul 1;92(4):723-32. doi: 10.1002/jcb.20118. PMID: 15211570.
[8].Takagi Sawada M,et,al. The proteasome is an essential mediator of the activation of pre-MPF during starfish oocyte maturation. Biochem Biophys Res Commun. 1997 Jul 9;236(1):40-3. doi: 10.1006/bbrc.1997.6900. PMID: 9223422.
[9].Nam YJ, Lee DH, et,al. 3,4,5-tricaffeoylquinic acid attenuates proteasome inhibition-mediated programmed cell death in differentiated PC12 cells. Neurochem Res. 2014 Aug;39(8):1416-25. doi: 10.1007/s11064-014-1327-x. Epub 2014 May 14. PMID: 24825618.

MG-115 是一种有效的抑制剂，对 20S 和 26S 蛋白酶体的 Kis 分别为 21 nM 和 35 nM [1]。

MG-115（50 μM，2 小时）在 Leu1193 和 Asp1179 COS-7 突变细胞系中分别将胰岛素受体及其成熟 β 亚基的表达提高 3 倍和 4.2 倍[2] .MG-115(30 μM, 4 h)处理Rat-1和PC12细胞可诱导两种细胞的凋亡[3]。培养分离的大鼠胰岛并用蛋白酶体抑制剂预处理，随后暴露 48 小时至 25 U/ml 人 IL-1beta。用 10 uM 蛋白酶体抑制剂 MG-115 进行预处理可抵消抑制作用[4]。用蛋白酶体抑制剂 MG-115 处理 HCC 细胞 SK-Hep1、HLE 和 HepG2。 MG-115 以剂量依赖的方式在三种细胞类型中诱导细胞凋亡。 MG-115 下调 SK-Hep1 中 XIAP 的表达，下调 SK-Hep1 和 HepG2 中 survivin 的表达[5]。 MG-115 在 120 分钟内减少了新鲜分散的球状带和束状带-网状 (ZF/R) 细胞的醛固酮和皮质酮分泌。孵育 24 小时后，单独使用 MG-115 可降低皮质酮的产生并提高培养的 ZF/R 细胞的增殖率[6]。蛋白酶体抑制剂 MG-115 可以抑制 ATF6，ATF6 是蛋白酶体-泛素通路的直接靶点[7]。 MG-115 通过在与生发泡破裂所需的一半时间相对应的时间添加而减少。通过显微注射抗蛋白酶体-a-亚基抗体[8]，也观察到对生发泡破裂的有效抑制。 MG-115 诱导 Bid、Bcl-2 和存活蛋白水平降低，Bax 增加，线粒体跨膜电位丧失，细胞色素 c 释放，半胱天冬酶（-8、-9 和 -3）激活，以及PC3[9] 中肿瘤抑制因子 p53 水平的增加。

实验参考方法 Experimental Reference Method

Kinase experiment [1]:

Preparation Method

Proteasome fractions were prepared from rabbit psoas muscle homogenates by differential centrifugation and were resolved into 26S and 20S particles by precipitation with ammonium sulfate (0%-38% and 40%-80%, respectively) followed by chromatography sequentially on a Mono Q and a Superose 6 column. Peptide-AMC substrates and inhibitor(including MG-115) (1-10 μl) in DMSO were added to 2 ml of assay buffer that for the 20S proteasome contained 20 mM Tris-HCI, 0.5 mM EDTA, and 0.035% SDS (pH 8.0); for the 26S proteasome, contained 20 mM Tris-HCI, 1 mM ATP, and 2 mM MgCls (pH 8.0); for cathepsin B, contained 100 mM NaOAc, 5 mM EDTA, and 2 mM DTT; and for calpain, contained 20 mM Tris-HCI, 1 mM CaCl2, and 2 mM DTT (pH 8.0). After equilibration at 37℃ (proteasomes and cathepsin B) or 20℃ (calpain), enzyme (1-5 μl) was added, and reaction progress was monitored by the increase in fluorescence emission at 440 nm (lar, 380 nm).

Applications

MG-115 is a more potent inhibitor with Kis of 21 nM and 35 nM for 20S and 26S proteasome, respectively.
Cell experiment [2]:

Cell lines

Rat-1 and PC12 cells

Preparation Method

Actively proliferating Rat-1 fibroblasts and PC12 pheochromocytoma cells were treated with PSI and MG-115. After 4 h of treatment, apoptosis was assayed by DNA fragmentation.

Reaction Conditions

30 μM MG-115 for 4 h

Applications

Both Rat-1 and PC12 cells underwent apoptosis following treatment with MG-115.

References:

[1]. Rock KL, Gramm C, 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. doi: 10.1016/s0092-8674(94)90462-6. PMID: 8087844.

[2]. Lopes UG, Erhardt P, et,al. p53-dependent induction of apoptosis by proteasome inhibitors. J Biol Chem. 1997 May 16;272(20):12893-6. doi: 10.1074/jbc.272.20.12893. PMID: 9148891.

产品文档 Product Documents

Purity:>98.00%Appearance:A solid

化学性质Chemical Properties

CAS 号
133407-86-0
同义词
MG115,蛋白酶体抑制剂,Carbobenzoxy-L-leucyl-L-leucyl-L-norvalinal, Z-LL-Nva-CHO, Proteasome Inhibitor XII,MG115
化学名
benzyl N-[(2S)-4-methyl-1-[[(2S)-4-methyl-1-oxo-1-[[(2S)-1-oxopentan-2-yl]amino]pentan-2-yl]amino]-1-oxopentan-2-yl]carbamate
SMILES
CCCC(C=O)NC(=O)C(CC(C)C)NC(=O)C(CC(C)C)NC(=O)OCC1=CC=CC=C1
分子式
C25H39N3O5
分子量
461.59 g/mol
溶解性
25mg/mL in DMSO, 25mg/mL in DMF, 30mg/mL in Ethanol
保存条件
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°C，然后在超声波浴中震荡一段时间。
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。

计算工具摩尔浓度 / 稀释 / 分子量 / 单位换算 / 体内配方 / 溶解度

g/mol