Calpain is a Ca2+-mediated cytosolic cyctein protease existed in various cells. Calpeptin is a potent calpain inhibitor with ID50 values of 52 nM, 34 nM, 138 nM, and 40 nM for Calpain I (porcine erythrocytes), Calpain II (porcine kidney), Papain, and Calpain I (human platelets), respectively. In platelets stimulated by A23187, 66% of ABP and 69% of P235 remained undegraded in the presence of 10μg/mL calpeptin, in comparison to 26% of ABP and 40% of P235 remained without calpeptin. The activity of intrinsic calpain in platelets was completely abolished by the treatment of 100μg/mL calpeptin[4]. Calpeptin at the concentration of 34nM reduced calpain activity by 44% in the homogenate of proliferating PC12 cells. When PCI2 cells were incubated with NGF and 36μM calpeptin for 17h, the probabilities for a PCI2 cell to extend a given maximal neurite length were increased as compared to non-calpeptin-treated cells[5]. In a murine model of middle cerebral artery occlusion, the intra-cerebroventricle injection of calpeptin (50μg dissolved in 5μL DMSO) before the occlusion resulted in a significant reduction of neuronal apoptosis in hippocampal CA1 sector, as compared to DMSO-treated animals, via the inhibition of caspase-3 expression[6].
Calpeptin/钙肽素 细胞实验
Cell Line
Concentration
Treated Time
Description
References
Vero E6 cells
50 µM
12 hours to 24 hours
To study the effect of Calpeptin on the cleavage of SARS-CoV-2 viral proteins, it was found that Calpeptin treatment significantly reduced the cleavage products at N19, S260, and S637 sites.
Nat Commun. 2021 Sep 21;12(1):5553.
N2a cells
40 µM
24 hours
To test the effect of Calpeptin on NF protein degradation in N2a cells, results showed that Calpeptin significantly increased the levels of all three NF proteins.
Autophagy. 2023 Apr;19(4):1277-1292.
Rat primary cortical neurons
50 µM
24 hours
To investigate the effect of Calpeptin on okadaic acid-induced cleavage of DLP1 and spectrin. Results showed that Calpeptin completely inhibited the okadaic acid-induced cleavage of DLP1 and spectrin.
Aging Cell. 2019 Jun;18(3):e12912.
HEK293 cells
30 µg/ml
3 hours
To study the effect of Calpeptin on ABCA1 protein levels, results showed that Calpeptin treatment significantly increased ABCA1 protein levels.
J Clin Invest. 2003 Jan;111(1):99-107.
Mouse peritoneal macrophages
20 µg/ml
3 hours
To study the effect of Calpeptin on ABCA1 protein levels in mouse peritoneal macrophages, results showed that Calpeptin treatment significantly increased ABCA1 protein levels.
J Clin Invest. 2003 Jan;111(1):99-107.
Mouse primary hepatocytes
15 µg/ml
3 hours
To study the effect of Calpeptin on ABCA1 protein levels in mouse primary hepatocytes, results showed that Calpeptin treatment significantly increased ABCA1 protein levels.
J Clin Invest. 2003 Jan;111(1):99-107.
Bovine aortic endothelial cells
10 µM
30 minutes
To investigate the effect of Calpeptin on VEGF-induced NO• production in endothelial cells, results showed that Calpeptin significantly inhibited VEGF-induced NO• production.
Circ Res. 2009 Jan 2;104(1):50-9.
Intestinal epithelial cells (IECs)
1 μg/ml
4 hours
To study the effect of Calpeptin on caspase 3 activation in MDP-stimulated IECs, results showed that Calpeptin treatment prevented caspase 3 activation.
J Clin Invest. 2015 Mar 2;125(3):1098-110.
Rat hippocampal neurons
50 µM
4 hours
To investigate the effect of Calpeptin on AMPA-induced down-regulation of TARPγ8 and GluA1 protein levels, results showed that Calpeptin significantly blocked the AMPA-induced down-regulation of TARPγ8 and GluA1.
Acta Pharmacol Sin. 2016 Mar;37(3):303-11.
Rat primary cortical neurons
50 µM
4 hours
To investigate the effect of Calpeptin on glutamate-induced cleavage of DLP1 and spectrin. Results showed that Calpeptin significantly inhibited the glutamate-induced cleavage of DLP1 and spectrin.
Aging Cell. 2019 Jun;18(3):e12912.
Primary cortical neurons from CRND8 APP transgenic mice
50 µM
4 hours
To investigate the effect of Calpeptin on DLP1 and spectrin cleavage in primary cortical neurons from CRND8 APP transgenic mice. Results showed that Calpeptin inhibited the cleavage of DLP1 and spectrin in CRND8 mouse neurons.
Aging Cell. 2019 Jun;18(3):e12912.
Calpeptin/钙肽素 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
Mice
C57BL/6J mice
FemOral vein injection
20 mg/kg
Single injection, analyzed after 4 hours
To study the effect of ApoA-I injection on ABCA1 protein levels in mouse liver and peritoneal macrophages, results showed that ApoA-I injection significantly increased ABCA1 protein levels.
J Clin Invest. 2003 Jan;111(1):99-107.
Mice
DSS-induced colitis model
Intraperitoneal injection
5 mg/kg
Daily for 5 days
To study the effect of Calpeptin on DSS-induced colitis in mice, results showed that Calpeptin treatment reduced weight loss and improved architectural distortion and epithelial cell death.
J Clin Invest. 2015 Mar 2;125(3):1098-110.
Zebrafish
Transgenic GFP-Lc3 zebrafish embryos
Embryo water
50 μM
24 hours
Calpeptin significantly induced the formation of Lc3-positive puncta and colocalization with autolysosomes, and upregulated the conversion of endogenous Lc3.
Autophagy. 2009 May;5(4):520-6
Mice
SMA mouse models
Subcutaneous injection
6 μg/g
Once daily until postnatal day 8
To study the effect of Calpeptin on survival and motor function in SMA mice, results showed that Calpeptin treatment increased SMN protein levels and improved motor function
Calpain I (porcine erythrocytes), ID50:52 nM
Calpain II (porcine kidney), ID50:40 nM
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细胞研究
细胞系
浓度
检测类型
检测时间
活性说明
数据源
COS7 cells
50 μM
Function assay
24 h
Induction of autophagy in african green monkey COS7 cells assessed as increase in autophagosome at 50 uM after 24 hrs by electron microscopy
18391949
HeLa cells
50 μM
Function assay
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
PC12 cells
10 μM
Function assay
96 h
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
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