research use only

Calpeptin Cysteine Protease inhibitor

Name: Calpeptin
Brand: Selleck Chemicals
SKU: S7396
Availability: InStock
Rating: 5 (28 reviews)

Cat.No.S7396

Calpeptin is a potent, cell-permeable calpain inhibitor with ID50 of 52 nM, 34 nM, 138 nM, and 40 nM for Calpain I (porcine erythrocytes), Calpain II (porcine kidney), Papainb, and Calpain I (human platelets), respectively. This compound attenuates apoptosis and intracellular inflammatory changes in muscle cells.

Chemical Structure

Molecular Weight: 362.46

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

Quality Control

Batch: Purity: >97%

Related Targets	HDAC Caspase MMP HCV Protease DPP Tyrosinase HIV Protease Proteasome Serine Protease Secretase PCSK9 Glutaminase Acyltransferase Thrombin Cathepsin B MALT PAD PREP Neprilysin Carboxypeptidase SGK Aminopeptidase 3C-Like Protease PSMA PGDS GOT
Related Products	Aloxistatin (E64d) Odanacatib MG-101 (ALLN) E-64 Z-FA-FMK N-Ethylmaleimide (NEM) Cathepsin Inhibitor 1 PD 151746 Loxistatin Acid (E-64C) Cruzain-IN-1 Z-FY-CHO Anti-CTSS / Cathepsin S (Fsn0503h) PD 150606 Cathepsin S Antibody [D17A22] LY3000328 MG132 SSS Calpain 1 Antibody [A6K6] Balicatib Calpain 2 Large Subunit (M-type) Antibody [K24F11] 2-cyano-Pyrimidine Cathepsin G Inhibitor I

Cell Culture, Treatment & Working Concentration

Cell Lines	Assay Type	Concentration	Incubation Time	Activity Description	PMID
PC12	Autophagy assay	10 uM	96 hrs	Induction of autophagy in undifferentiated rat stable inducible PC12 cells expressing EGFP-HDQ74 assessed as EGFP-HDQ74 clearance at 10 uM after 96 hrs by calpain activation assay	18391949
PC12	Autophagy assay	10 uM	96 hrs	Induction of autophagy in differentiated rat stable inducible PC12 cells expressing A53T alpha-synuclein assessed as A53T alpha-synuclein clearance at 10 uM after 96 hrs by calpain activation assay	18391949
COS7	Autophagy assay	50 uM	48 hrs	Induction of autophagy in african green monkey COS7 cells expressing EGFP-HDQ74 assessed as inhibition of PLC-epsilon overexpression-induced EGFP-HDQ74 aggregation at 50 uM after 48 hrs	18391949
PC12	Autophagy assay	10 uM	96 hrs	Induction of autophagy in undifferentiated rat stable inducible PC12 cells expressing A53T alpha-synuclein assessed as A53T alpha-synuclein clearance at 10 uM after 96 hrs by calpain activation assay	18391949
PC12	Autophagy assay	10 uM	96 hrs	Induction of autophagy in differentiated rat stable inducible PC12 cells expressing EGFP-HDQ74 assessed as EGFP-HDQ74 clearance at 10 uM after 96 hrs by calpain activation assay	18391949
HeLa	Autophagy assay	50 uM		Induction of autophagy in human HeLa cells expressing EGFP-LC3 assessed as increase in LC3-2 level at 50 uM in presence of 400 nM bafilomycin A1	18391949
COS7	Autophagy assay	50 uM	24 hrs	Induction of autophagy in african green monkey COS7 cells assessed as increase in autophagosome at 50 uM after 24 hrs by electron microscopy	18391949
COS7	Autophagy assay	50 uM	48 hrs	Induction of autophagy in african green monkey COS7 cells expressing EGFP-HDQ74/rheb assessed as reduction in EGFP-HDQ74 aggregation at 50 uM after 48 hrs	18391949
COS7	Autophagy assay	50 uM	24 hrs	Induction of autophagy in african green monkey COS7 cells expressing EGFP-LC3 assessed as increase in EGFP-LC3 vesicle at 50 uM after 24 hrs	18391949
HeLa	Antiviral assay			Antiviral activity against human rhinovirus-14 in HeLa cells, IC50=17.7μM.	ChEMBL
HeLa	Cytotoxic assay			Cytotoxic activity against HeLa cells using XTT assay, TC50=22.1μM.	ChEMBL
NMuMG	Function assay	25 to 50 uM	24 to 72 hrs	Inhibition of calpain in mouse NMuMG cells assessed as suppression of TGFbeta1-induced calpain activity by measuring Filamin-A levels at 25 to 50 uM incubated for 24 to 72 hrs by Western blot analysis	ChEMBL
NMuMG	Function assay	25 to 50 uM	24 to 72 hrs	Inhibition of calpain in mouse NMuMG cells assessed as suppression of TGFbeta1-induced EMT by measuring alpha-SMA expression at 25 to 50 uM incubated for 24 to 72 hrs by Western blot analysis	ChEMBL
Click to View More Cell Line Experimental Data

Chemical Information, Storage & Stability

Molecular Weight	362.46	Formula	C₂₀H₃₀N₂O₄	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	117591-20-5	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			Smiles	CCCCC(C=O)NC(=O)C(CC(C)C)NC(=O)OCC1=CC=CC=C1

Solubility

In vitro
Batch:

DMSO : 72 mg/mL (198.64 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 72 mg/mL

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection 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.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	3.600mg/ml (9.93mM)	Taking the 1 mL working solution as an example, add 50 μL of 72 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.600mg/ml (1.66mM)	Taking the 1 mL working solution as an example, add 50 μL of 12 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
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	Calpain II (porcine kidney) ^[1] 34 nM(ID50) Calpain I (human platelets) ^[1] 40 nM(ID50) Calpain I (porcine erythrocytes) ^[1] 52 nM(ID50) Papainb ^[1] 138 nM(ID50)
In vitro	Calpeptin inhibits 20K phosphorylation in a dose-related manner in platelets stimulated by thrombin, ionomycin or collagen. ^[1] In differentiating PC12 cells, this compound promotes neurite elongation via inhibition of Calpain activity. ^[2] In rat retinal ganglion cells, it attenuates apoptosis, maintains normal whole-cell membrane potential, and thus provides functional neuroprotection. ^[3]
In vivo	In a feline right ventricular (RV) PO (RVPO) model, calpeptin (0.6 mg/kg, i.v.) blocks the activation of calpain and caspase-3, cleavage of their substrates, and cardiomyocyte programmed cell death. ^[4] In a rat focal cerebral ischemia–reperfusion injury model, this compound reduces the neuronal apoptosis in hippocampal CA1 sector via inhibition of the expression of Caspase-3. ^[5]
References	[1] https://pubmed.ncbi.nlm.nih.gov/2839170/ [2] https://pubmed.ncbi.nlm.nih.gov/8041520/ [3] https://pubmed.ncbi.nlm.nih.gov/16600192/ [4] https://pubmed.ncbi.nlm.nih.gov/18487434/ [5] https://pubmed.ncbi.nlm.nih.gov/20473717/

Applications

Methods	Biomarkers	Images	PMID
Immunofluorescence	Src / EGFR		29641465

Tech Support

Handling Instructions

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

If you have any other enquiries, please leave a message.

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):