Home Proteases HIV Protease inhibitor - Cysteine Protease inhibitor - Autophagy inhibitor Pepstatin A For research use only.

Pepstatin A

Synonyms: Pepstatin

Pepstatin A (Pepstatin) is a potent aspartic protease inhibitor, and also inhibits HIV replication. Pepstatin A is also an inhibitor of cathepsins D and cathepsins E. Pepstatin A inhibits autophagy by suppressing lysosomal proteases.

Pepstatin A Chemical Structure

Pepstatin A Chemical Structure

CAS No. 26305-03-3

Purity & Quality Control

Pepstatin A Related Products

Signaling Pathway

HIV Protease Signaling Pathways

HIV Protease Signaling Pathway

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
MDA-MB-231 Function assay 3 days Inhibition of secreted cathepsin D in human MDA-MB-231 cells using Mca-Gly-Lys-Pro-Ile-Leu-PhePhe-Arg-Leu-Lys-(Dnp)-D-Arg-NH2 as substrate pretreated for 3 days under pH 6.6 conditioned media followed by substrate addition measured at 5 mins interval for , IC50=0.0001μM. 29087712
MDA-MB-231 Function assay 3 days Inhibition of secreted cathepsin E in human MDA-MB-231 cells using Mca-Gly-Lys-Pro-Ile-Leu-PhePhe-Arg-Leu-Lys-(Dnp)-D-Arg-NH2 as substrate pretreated for 3 days under pH 6.6 conditioned media followed by substrate addition measured at 5 mins interval for , IC50=0.0001μM. 29087712
MCF7 Function assay Inhibition of cathepsin D in human MCF7 cells by fluorescence assay, IC50=0.005μM. 19715320
MCF7 Function assay Inhibition of cathepsin E in human MCF7 cells by fluorescence assay, IC50=0.005μM. 19715320
MDA-MB-231 Function assay 4 hrs Inhibition of cathepsin D in human MDA-MB-231 cells using Mca-Gly-Lys-Pro-Ile-Leu-PhePhe-Arg-Leu-Lys-(Dnp)-D-Arg-NH2 as substrate pretreated for 4 hrs followed by compound washout and subsequent substrate addition measured at 30 secs interval for 30 mins , IC50=0.1μM. 29087712
MDA-MB-231 Function assay 4 hrs Inhibition of cathepsin E in human MDA-MB-231 cells using Mca-Gly-Lys-Pro-Ile-Leu-PhePhe-Arg-Leu-Lys-(Dnp)-D-Arg-NH2 as substrate pretreated for 4 hrs followed by compound washout and subsequent substrate addition measured at 30 secs interval for 30 mins , IC50=0.1μM. 29087712
MDA-MB-231 Function assay 4 hrs Inhibition of cathepsin D in human MDA-MB-231 cells using Mca-Gly-Lys-Pro-Ile-Leu-PhePhe-Arg-Leu-Lys-(Dnp)-D-Arg-NH2 as substrate pretreated for 4 hrs followed by compound washout and subsequent 10 mins trypsinization prior to substrate addition measured , IC50=1μM. 29087712
MDA-MB-231 Function assay 4 hrs Inhibition of cathepsin E in human MDA-MB-231 cells using Mca-Gly-Lys-Pro-Ile-Leu-PhePhe-Arg-Leu-Lys-(Dnp)-D-Arg-NH2 as substrate pretreated for 4 hrs followed by compound washout and subsequent 10 mins trypsinization prior to substrate addition measured , IC50=1μM. 29087712
MCF7 Function assay 1 hr Inhibition of cathepsin D in human MCF7 cells treated for 1 hr measured after washout and trypsin treatment by fluorescence assay, IC50=5μM. 19715320
MCF7 Function assay 1 hr Inhibition of cathepsin E in human MCF7 cells treated for 1 hr measured after washout and trypsin treatment by fluorescence assay, IC50=5μM. 19715320
NB1643 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for NB1643 cells 29435139
A673 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for A673 cells) 29435139
SK-N-MC qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-MC cells 29435139
TC32 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for TC32 cells 29435139
Click to View More Cell Line Experimental Data

Biological Activity

Description Pepstatin A (Pepstatin) is a potent aspartic protease inhibitor, and also inhibits HIV replication. Pepstatin A is also an inhibitor of cathepsins D and cathepsins E. Pepstatin A inhibits autophagy by suppressing lysosomal proteases.
Targets
aspartic protease [1] cathepsins D [2] cathepsins E [2]
In vitro
In vitro

Pepstatin A shows effective inhibition on aspartic proteinases such as pepsin, cathepsins D and E. In HIV-infected H9 cells, pepstatin A inhibits part of the intracellular processing of the HIV gag protein with no apparent toxicity on HIV-infected cells. [1]

Pepstatin A laos suppresses the differentiation of osteoclasts by blocking ERK signaling and the inhibition of NFATc1 expression. [2]
Cell Research Cell lines NCM460 cells
Concentrations 10 μM
Incubation Time 24 h
Method

Cells were treated with indicated concentrations of drug.

Chemical Information & Solubility

Molecular Weight 685.89 Formula

C34H63N5O9
CAS No. 26305-03-3 SDF Download Pepstatin A SDF
Smiles CC(C)CC(C(CC(=O)O)O)NC(=O)C(C)NC(=O)CC(C(CC(C)C)NC(=O)C(C(C)C)NC(=O)C(C(C)C)NC(=O)CC(C)C)O
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 50 mg/mL ( (72.89 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 3 mg/mL

Water : Insoluble


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In vivo
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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Frequently Asked Questions

Question 1:
Do you have recommended in-vivo solvent for S7381 please?

Answer:
S7381 could be dissolved in 5%DMSO+40%PEG300+5%tween-80+ddH2O up to 2mg/ml.

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