Home Proteases Cysteine Protease inhibitor - Apoptosis related activator Calpeptin For research use only.

Calpeptin

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. Calpeptin attenuates apoptosis and intracellular inflammatory changes in muscle cells.

Calpeptin Chemical Structure

Calpeptin Chemical Structure

CAS No. 117591-20-5

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Calpeptin Related Products

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation 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
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Biological Activity

Description 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. Calpeptin attenuates apoptosis and intracellular inflammatory changes in muscle cells.
Targets
Calpain II (porcine kidney) [1] Calpain I (human platelets) [1] Calpain I (porcine erythrocytes) [1] Papainb [1]
34 nM(ID50) 40 nM(ID50) 52 nM(ID50) 138 nM(ID50)
In vitro
In vitro Calpeptin inhibits 20K phosphorylation in a dose-related manner in platelets stimulated by thrombin, ionomycin or collagen. [1] In differentiating PC12 cells, Calpeptin promotes neurite elongation via inhibition of Calpain activity. [2] In rat retinal ganglion cells, Calpeptin attenuates apoptosis, maintains normal whole-cell membrane potential, and thus provides functional neuroprotection. [3]
Experimental Result Images Methods Biomarkers Images PMID
Immunofluorescence Src / EGFR 29641465
In Vivo
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, Calpeptin reduces the neuronal apoptosis in hippocampal CA1 sector via inhibition of the expression of Caspase-3. [5]
Animal Research Animal Models Feline right ventricular (RV) PO (RVPO) model
Dosages 0.6 mg/kg
Administration i.v.

Chemical Information & Solubility

Molecular Weight 362.46 Formula

C20H30N2O4
CAS No. 117591-20-5 SDF Download Calpeptin SDF
Smiles CCCCC(C=O)NC(=O)C(CC(C)C)NC(=O)OCC1=CC=CC=C1
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 72 mg/mL ( (198.64 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 72 mg/mL

Water : Insoluble


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