516483

Pepstatin A, Penetratin

A Pepstatin A that is ~75% less potent against Cathespins D/E than PepA in cell-free assays.

• Synonym(s): Pepstatin A, Penetratin, PepA-RQIKIWFQNRRMKWKK-OH, PepA-Antp₄₃₋₅₈
• Empirical Formula (Hill Notation): C₁₃₈H₂₂₉N₃₉O₂₈S
• Molecular Weight: 2914.60
• UNSPSC Code: 12352202
• NACRES: NA.77

Properties

• Quality Level: 100
• Assay: ≥97% (HPLC)
• form: lyophilized solid
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze; desiccated (hygroscopic); protect from light
• color: white
• solubility: water: 1 mg/mL
• shipped in: wet ice
• storage temp.: −20°C

Description

General description

A Pepstatin A (PepA; Cat. No. 516481) penetratin (pAntp_43-58) conjugate (PepA-P) that is ~75% less potent against Cathespins D/E (IC₅₀ = 920 nM) than PepA in cell-free assays, presumably due to its decreased solubility. However, with its enhanced permeability, PepA-P is much more active than PepA in inhibiting cellular aspartic protease activity in MCF7 (94.1% vs. 54.6% inhibition wtih 10 µM respective compound), Boleths, and Dendritic cultures. PepA-P, but not PepA, effectively interferes with antigen processing by primary APCs and the subsequent activation of antigen-specific memory T cells.

Packaging

Packaged under inert gas

Warning

Toxicity: Standard Handling (A)

Sequence

PepA-Arg-Gln-Ile-Lys-Ile-Trp-Phe-Gln-Asn-Arg-Arg-Met-Lys-Trp-Lys-Lys-CO₂H

Physical form

Supplied as a trifluoroacetate salt.

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Other Notes

Zaidi, N., et al. 2007. Biochem. Biophys. Res. Commun.364, 243.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Safety Information

• Storage Class Code: 11 - Combustible Solids
• WGK: WGK 1
• Flash Point(F): Not applicable
• Flash Point(C): Not applicable