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Pepstatin A HIV Protease inhibitor

Name: Pepstatin A
Brand: Selleck Chemicals
SKU: S7381
Availability: InStock
Rating: 5 (37 reviews)

Cat.No.S7381

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

Chemical Structure

Molecular Weight: 685.89

Jump to Mechanism of Action Cell Culture & Working Concentration Solubility Chemical Information, Storage & Stability Specificity

Quality Control

Batch: Purity: 99.76%

99.76

Related Targets	HDAC Caspase MMP HCV Protease Cysteine Protease DPP Tyrosinase Proteasome Serine Protease Secretase PCSK9 Glutaminase Acyltransferase Thrombin Cathepsin B MALT PAD PREP Neprilysin SGK Aminopeptidase 3C-Like Protease PGDS GOT
Related Products	Limonin Temsavir (BMS-626529) Rosamultin Bevirimat Dextran sulfate sodium (DSS) Mericitabine NBD-556 GS-6207 Azvudine

Cell Culture, Treatment & Working Concentration

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

Chemical Information, Storage & Stability

Molecular Weight	685.89	Formula	C₃₄H₆₃N₅O₉	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	26305-03-3	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	Pepstatin			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

Solubility

In vitro
Batch:

DMSO : 50 mg/mL (72.89 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 3 mg/mL

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Batch:
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.

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.

Mechanism of Action

Targets/IC₅₀/Ki	aspartic protease ^[1] cathepsins D ^[2] cathepsins E ^[2]
In vitro	Pepstatin A shows effective inhibition on aspartic proteinases such as pepsin, cathepsins D and E. In HIV-infected H9 cells, this compound inhibits part of the intracellular processing of the HIV gag protein with no apparent toxicity on HIV-infected cells. ^[1] This chemical laos suppresses the differentiation of osteoclasts by blocking ERK signaling and the inhibition of NFATc1 expression. ^[2]
References	[1] https://pubmed.ncbi.nlm.nih.gov/3045820/ [2] https://pubmed.ncbi.nlm.nih.gov/16567424/ [3] https://pubmed.ncbi.nlm.nih.gov/35974017/ [4] https://pubmed.ncbi.nlm.nih.gov/4912600/

Tech Support

Handling Instructions

Tel: +1-832-582-8158 Ext:3

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Frequently Asked Questions

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

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

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