The product is acknowledged to be less potent against Cathespins D/E than PepA in cell-free assays. For intact cells, the following publication may be of interest for result comparison: "Biochem Biophys Res Commun. 2007 Dec 14;364(2):243-9. doi: 10.1016/j.bbrc.2007.09.114. Epub 2007 Oct 4.
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
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All Photos(2)
About This Item
Empirical Formula (Hill Notation):
C138H229N39O28S
Molecular Weight:
2914.60
UNSPSC Code:
12352202
NACRES:
NA.77
Pricing and availability is not currently available.
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Quality Level
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
General description
A Pepstatin A (PepA; Cat. No. 516481) penetratin (pAntp43-58) 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
Storage Class Code
11 - Combustible Solids
WGK
WGK 1
Flash Point(F)
Not applicable
Flash Point(C)
Not applicable
Certificates of Analysis (COA)
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Adrienn Skopál et al.
The Journal of biological chemistry, 298(5), 101888-101888 (2022-04-04)
Adenosine A2A receptor (A2AR)-dependent signaling in macrophages plays a key role in the regulation of inflammation. However, the processes regulating A2AR targeting to the cell surface and degradation in macrophages are incompletely understood. For example, the C-terminal domain of the
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What is the comparative performance of the inhibitor selection for use with intact cells, given that the product description indicates it is approximately 75% less potent against Cathespins D/E than PepA?
1 answer-
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