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Join us! · InformexUSA 2012 · New Orleans, Louisiana · February 14-17, 2012 · Booth 2514

HMB-Val-Ser-Leu-VE

Cayman Chemical Item Number 10007713

(CAS 862891-04-1)

HMB-Val-Ser-Leu-VE (CAS 862891-04-1)

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Description

The 20S proteasome is a 700 kDa, multi-subunit cylinder-shaped protein that functions as the central protease within the ubiquitin-proteasome pathway utilized by cells for the regulated degradation of proteins.1,2 HMB-val-ser-leu-VE is a tripeptide bearing a C-terminal vinyl ester which acts as a potent, selective inhibitor of the trypsin-like activity of the 20S proteasome. It inhibits the tryptic-like, chymotryptic-like, and post acidic activities of the purified 20S proteasome with IC50 values of 0.33 µM, >10 µM, and >10 µM, respectively.3 HMB-val-ser-leu-VE is cell permeable and stable (t1/2 ~6 hours) in in vitro assays.

1 DeMartino, G.N., and Slaughter, C.A. The proteasome, a novel protease regulated by multiple mechanisms. J Biol Chem 274(32) 22123-22126 (1999).

2 Ciechanover, A. The ubiquitin-proteasome proteolytic pathway. Cell 79 13-21 (1994).

3 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 48 5038-5042 (2005).

Formal 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
Formula Weight 505.6
Formulation A crystalline solid
Purity ≥98%
λmax 210 nm
Stability 2 years
Storage -20°C
Shipping Room temperature in continental US; may vary elsewhere
SMILES
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OC1=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

Background Reading

Ciechanover, A. The ubiquitin-proteasome proteolytic pathway. Cell 79 13-21 (1994).

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 48 5038-5042 (2005).

DeMartino, G.N., and Slaughter, C.A. The proteasome, a novel protease regulated by multiple mechanisms. J Biol Chem 274(32) 22123-22126 (1999).

HMB-Val-Ser-Leu-VE is available in the following screening library:

Size Price Quantity Subtotal
1 mg $57.00 $0.00
5 mg $257.00 $0.00
10 mg $456.00 $0.00
25 mg $998.00 $0.00
Bulk Contact
Cart Total $0.00

This product is available in custom sizes and/or larger quantities.

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Pricing updated 2012-02-12. Prices are subject to change without notice.

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Warning This product is not for human or veterinary use.

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