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HMB-Val-Ser-Leu-VE
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
HMB-Val-Ser-Leu-VE图片
CAS NO:862891-04-1
包装与价格:
包装价格(元)
1mg电议
5mg电议
10mg电议
25mg电议

产品介绍
Cas No.862891-04-1
化学名N-(3-hydroxy-2-methylbenzoyl)-L-valyl-N-[(1S,2E)-4-ethoxy-1-(2-methylpropyl)-4-oxo-2-butenyl]-L-serinamide
Canonical SMILESOC1=CC=CC(C(N[C@@H](C(C)C)C(N[C@@H](CO)C(N[C@@H](CC(C)C)/C=C/C(OCC)=O)=O)=O)=O)=C1C
分子式C26H39N3O7
分子量505.6
溶解度≤20mg/ml in ethanol;20mg/ml in DMSO;20mg/ml in dimethyl formamide
储存条件Store at -20℃
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

HMB-Val-Ser-Leu-VE is an irreversible, cell-permeable, potent and specific inhibitor of the trypsin-like activity of the 20S proteasome with IC50 value of 33 nM [1].

The 20S proteasome is a 700 kDa, cylinder-shaped protease with multiple catalytic centers within the ubiquitin-proteasome pathway and plays an important role in the selective degradation of intracellular proteins. Proteasomes remove abnormal proteins and play an important role in cell-cycle progression and apoptosis [1][2].

HMB-Val-Ser-Leu-VE is a tripeptide-based compound bearing a C-terminal vinyl ester that acts as a potent and selective inhibitor of the trypsin-like activity of the 20S proteasome with IC50 value of 33 nM [1]. In two colon-carcinoma cell lines (COO115, HCT116), HMB-Val-Ser-Leu-VE was nontoxic and did not affect cell proliferation. In HLA-A2 positive lymphoblastoid cells, HMB-Val-Ser-Leu-VE caused a dose-dependent increase of CLG-specific killing, suggesting that HMB-Val-Ser-Leu-VE favored the generation and presentation of immunogenic peptides presented by MHC class I molecules [1].

References:
[1].  Marastoni M, Baldisserotto A, Cellini S, et al. Peptidyl vinyl ester derivatives: new class of selective inhibitors of proteasome trypsin-like activity. J Med Chem. 2005 Jul 28;48(15):5038-42.
[2].  DeMartino GN, Slaughter CA. The proteasome, a novel protease regulated by multiple mechanisms.