HMB-Val-Ser-Leu-VE

HMB-Val-Ser-Leu-VE

Catalog Number:
L002372941APE
Mfr. No.:
APE-C4090
Price:
$226
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      • Overview
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          Background

          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].

          [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.

      • Properties
        • Alternative Name
          N-(3-hydroxy-2-methylbenzoyl)-L-valyl-N-[(1S,2E)-4-ethoxy-1-(2-methylpropyl)-4-oxo-2-butenyl]-L-serinamide
          CAS Number
          862891-04-1
          Molecular Formula
          C26H39N3O7
          Molecular Weight
          505.6
          Appearance
          A crystalline solid
          Purity
          98.00%
          Solubility
          ≤20mg/ml in ethanol;20mg/ml in DMSO;20mg/ml in dimethyl formamide
          Storage
          Store at -20°C

          * For Research Use Only

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