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Pepstatin A

Name: Pepstatin A
Brand: Selleck Chemicals
SKU: S7381
Rating: 5 (35 reviews)

Synonyms: Pepstatin

Catalog No.S7381 Purity:99.76%

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

CAS No. 26305-03-3

Purity & Quality Control

Batch: Purity: 99.76%

99.76

Pepstatin A Related Products

Related Targets	HIV-1 capsid HIV-1 caspid	Click to Expand
Related Products	Limonin Temsavir (BMS-626529)	Click to Expand
Related Compound Libraries	FDA-approved Drug Library Natural Product Library Bioactive Compound Library-I Protease Inhibitor Library Ubiquitination Compound Library	Click to Expand

Signaling Pathway

HIV Protease Signaling Pathway

Cell Data

Cell Lines	Assay Type	Incubation Time	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

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.

References

[4] Umezawa H, et al. J Antibiot (Tokyo). 1970 May;23(5):259-62.

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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)	3 years-20°Cpowder	Storage of Stock Solutions Aliquot the stock solutions to avoid repeated freeze-thaw cycles	1 year-80°Cin solvent
Storage (From the date of receipt)	3 years-20°Cpowder		1 month-20°Cin solvent

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

Molecular Weight Calculator

In vivo Batch: Add solvents to the product individually and in order.				In vivo Formulation Calculator
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

Preparing Stock Solutions

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

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

Tel: +1-832-582-8158 Ext:3
If you have any other enquiries, please leave a message.

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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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