Art. -Nr.: HY-100223

Calpeptin

28 Cited Publications

Kundenbewertung

Based on 28 publication(s) in Google Scholar

Calpeptin is a potent, cell penetrating calpain inhibitor, with an ID₅₀ of 40 nM for Calpain I in human platelets. Calpeptin is also an inhibitor of cathepsin K.

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Reinheit: 99.17%
CAS. Nr.: 117591-20-5
Formel: C₂₀H₃₀N₂O₄
Molecular Weight:362.46

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

Calpeptin Chemical Structure

CAS. Nr.: 117591-20-5

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (28)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

Calpeptin is a potent, cell penetrating calpain inhibitor, with an ID₅₀ of 40 nM for Calpain I in human platelets^[1]. Calpeptin is also an inhibitor of cathepsin K^[2].

IC₅₀ & Target

cathepsin K

Alle Cathepsin Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
HeLa	IC₅₀	17.7 μM Compound: 4	Antiviral activity against human rhinovirus-14 in HeLa cells Antiviral activity against human rhinovirus-14 in HeLa cells	10.1016/S0960-894X(96)00537-9

In Vitro

Calpeptin (0-100 nM, 24 hours) treatment suppresses the proliferation of both WI38 VA13 and IMR90 cells in a dose-dependent manner. Calpeptin (1000 pg/ml, 24 hours) inhibits IL-6-induced cell proliferation of lung fibroblasts^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay^[3]

Cell Line:

WI38 VA13 and IMR90 cells
Concentration:

0-100 nM
Incubation Time:

24 hours
Result:

Suppressed the proliferation in a dose-dependent manner.

In Vivo

Calpeptin with Bleo (0.04 mg/mouse, i.p., 3 times weekly, 28 days) administration significantly inhibits the collagen deposition and increases of calpain activity in the NSC-125066 treated mouse lung tissues^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

C57BL/6 female mice (Eight-week-old)^[3].
Dosage:

0.04 mg/mouse.
Administration:

Intraperitoneally three times weekly for 28 days (together with Bleo).
Result:

Inhibited the collagen deposition and increase of calpain activity in the NSC-125066 treated mouse lung tissues.

Chemical Information

CAS. Nr. 117591-20-5
Appearance Solid
Molecular Weight 362.46
Formel C₂₀H₃₀N₂O₄
Color White to off-white
SMILES

O=C(OCC1=CC=CC=C1)N[C@H](C(N[C@H](C=O)CCCC)=O)CC(C)C
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Publications (28)

All Histological Imaging/StainingIFWBIn Vivo Efficacy Study

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Journal Impact Factor

J Nanobiotechnology

Nucleophosmin3 carried by small extracellular vesicles contribute to white adipose tissue browning. [Abstract]

2022 Mar 28;20(1):165. PMID: 35346213

Calpeptin purchased from MedChemExpress. Usage Cited in: J Nanobiotechnology. 2022 Mar 28;20(1):165. [Abstract]

Cell immunofluorescence assay confirming the presence of NPM3-EGFP in recipient cells via the transwell assay, GW4869 or Calpeptin (50 nM, 48 h) was used to block sEVs release, scale bar=50 μm.
Adv Sci (Weinh)

Calpain-2-Mediated Endothelial Focal Adhesion Disruption in Thoracic Aortic Dissection. [Abstract]

2025 Apr 2:e2501112. PMID: 40171827

Calpeptin purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2025 Apr 2:e2501112. [Abstract]

Calpeptin (0.01 mg/mL/g via intraperitoneal injection, administered three times per week, starting 3 days prior to BAPN treatment. Representative microscopic images of aorta sections stained with H&E and EVG (scale bar: 100 μm).

Calpeptin purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2025 Apr 2:e2501112. [Abstract]

HAECs were treated with 1 μmol Angiotensin II (AngII) for 24 hours. The calpain inhibitor Calpeptin was administered at a concentration of 10 μmol for 1 hour prior to the Ang II treatment. Representative Western blot images for Calpain-2, Itgav, Itgb3, Talin1, Vinculin, and VE-cadherin are shown, withGAPDH serving as the loading control.

Calpeptin purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2025 Apr 2:e2501112. [Abstract]

Pharmacological inhibition of calpain using Calpeptin (0.01 mg/mL/g via intraperitoneal injection, administered three times per week, starting 3 days prior to BAPN treatment.
ACS Cent Sci

Evaluation of SARS-CoV-2 Main Protease Inhibitors Using a Novel Cell-Based Assay. [Abstract]

2022 Feb 23;8(2):192-204. PMID: 35229034

Calpeptin purchased from MedChemExpress. Usage Cited in: ACS Cent Sci. 2022 Feb 23;8(2):192-204. [Abstract]

CAPNS1 degradation was mediated by calpain activity. HEK293T cells transfected with HA or HA-CRBN for 36 hours were subsequently treated with dimethyl sulfoxide (DMSO), Calpeptin (10 μM), or MG-132 (10 μM) for an additional 12 hours, after which western blotting was performed.
ACS Sens

A Sensitive Green-Red FRET Sensor for Calpain-1 Utilizing Heterodimeric Fluorescent Proteins from Distinct Evolutionary Origins. [Abstract]

2026 Mar 27;11(3):1891-1907. PMID: 41837894
Cell Death Discov

Protein expression of nucleolar protein 12 in the retina and its implication in protection of retina from UV irradiation damage. [Abstract]

2024 Mar 11;10(1):130. PMID: 38467618
Cell Rep

SERPINB3-MYC axis induces the basal-like/squamous subtype and enhances disease progression in pancreatic cancer. [Abstract]

2023 Nov 18;42(12):113434. PMID: 37980563
J Med Chem

Probing Ligand Binding Sites on Large Proteins by Nuclear Magnetic Resonance Spectroscopy of Genetically Encoded Non-Canonical Amino Acids. [Abstract]

2023 Apr 13;66(7):5289-5304. PMID: 36920850
Antioxid Redox Signal

c-Jun-N terminal kinase mediated degradation of γ-glutamylcysteine ligase catalytic subunit inhibits GSH recovery after acetaminophen treatment: role in sustaining JNK activation and liver injury. [Abstract]

2023 Jun;38(16-18):1071-1081. PMID: 36333933
RSC Adv

Ginsenoside Rk1 inhibits cell proliferation and promotes apoptosis in lung squamous cell carcinoma by calcium signaling pathway. [Abstract]

2019 Aug 13;9(43):25107-25118. PMID: 35528653
Cells

Detection of Calpain-Mediated Beclin-1 Cleavage for Drug Discovery in Inflammatory Bowel Diseases. [Abstract]

2026 May 18;15(10):917. PMID: 42193926
Int Dent J

Calpain-1 Potentiates Periodontal Regeneration via PHLPP1-ERK-Driven Osteogenesis in Periodontal Ligament Stem Cells. [Abstract]

2025 Dec 6;76(1):109309. PMID: 41353895
Toxicology

Effects of CdTe quantum dot exposure on the calcium signaling pathway in rat dorsal root ganglion cells ND7/23. [Abstract]

2025 Jun 4:154212. PMID: 40480474
Chem Biol Interact

Interfering TRIB3 protects the blood brain barrier through PI3K/Akt pathway to alleviate cerebral ischemia-reperfusion injury in diabetes mellitus mice. [Abstract]

2024 Jan 5:387:110807. PMID: 37980971
Chem Biol Interact

Cisplatin-induced pyroptosis is mediated via the CAPN1/CAPN2-BAK/BAX-caspase-9-caspase-3-GSDME axis in esophageal cancer. [Abstract]

2022 Jul 1;361:109967. PMID: 35525317
PLoS Pathog

Influenza A virus inhibits TET2 expression by endoribonuclease PA-X to attenuate type I interferon signaling and promote viral replication. [Abstract]

2023 Jul 27;19(7):e1011550. PMID: 37498975
Sci Rep

Hepatitis C virus NS3/4A inhibitors and other drug-like compounds as covalent binders of SARS-CoV-2 main protease. [Abstract]

2022 Jul 16;12(1):12197. PMID: 35842458
Cell Signal

Targeting Filamin A alleviates ovariectomy-induced bone loss in mice via the WNT/β-catenin signaling pathway. [Abstract]

2022 Feb:90:110191. PMID: 34774991
J Cell Mol Med

Calpain-2 plays a pivotal role in the inhibitory effects of propofol against TNF-α-induced autophagy in mouse hippocampal neurons. [Abstract]

2020 Aug;24(16):9287-9299. PMID: 32627970
Mol Hum Reprod

Semaphorin 4C regulates ovarian steroidogenesis through RHOA/ROCK1-mediated actin cytoskeleton rearrangement. [Abstract]

2023 Apr 29;29(5):gaad010. PMID: 36892447
Neurotox Res

Calpain Inhibitor Calpeptin Improves Alzheimer's Disease-Like Cognitive Impairments and Pathologies in a Diabetes Mellitus Rat Model. [Abstract]

2022 Oct;40(5):1248-1260. PMID: 36018506
Biochim Biophys Acta Mol Cell Biol Lipids

Melatonin ameliorates ox-LDL-induced lipid accumulation and enhances ABCA1 expression in VSMCs via inhibition of the TRPV1-Ca2+-calpain signaling pathway. [Abstract]

2026 Jan;1871(1):159704. PMID: 41213324
Int J Med Sci

Acid-electrolyzed functional water-induces Interleukin-1α release from Intracellular Storage Sites in Oral Squamous Cell Carcinoma. [Abstract]

2021 Feb 18;18(8):1746-1752. PMID: 33746591
J Diabetes Investig

Calpeptin improves the cognitive function in Alzheimer's disease-like complications of diabetes mellitus rats by regulating TXNIP/NLRP3 inflammasome. [Abstract]

2024 Oct;15(10):1365-1376. PMID: 39171660
Hum Exp Toxicol

Calpain-mediated cleavage of mitochondrial fusion/fission proteins in acetaminophen-induced mice liver injury. [Abstract]

2022 Jan-Dec:41:9603271221108321. PMID: 35713544
Biomed Pharmacother

Cereblon mediates macrophage differentiation and microglial phagocytosis by regulating calpain protease activity. [Abstract]

2024 Nov:180:117606. PMID: 39454366
bioRxiv

2024 Feb 5.
Heliyon

Calpeptin may reverse glucocorticoid-resistance of allergic rhinitis associated with cigarette smoke exposure by down-regulating interferon regulatory factor 1. [Abstract]

2023 Jun 16;9(7):e17316. PMID: 37449098
Research Square Preprint

2022 Feb.

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 100 mg/mL (275.89 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.7589 mL

13.7946 mL

27.5893 mL

5 mM

0.5518 mL

2.7589 mL

5.5179 mL

10 mM

0.2759 mL

1.3795 mL

2.7589 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 5 mg/mL (13.79 mM); Clear solution

This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (273 KB)
SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Tsujinaka T, et al. Synthesis of a new cell penetrating calpain inhibitor (calpeptin). Biochem Biophys Res Commun. 1988 Jun 30;153(3):1201-8. [Content Brief]

[2]. Catalano JG, et al. Design of small molecule ketoamide-based inhibitors of cathepsin K. Bioorg Med Chem Lett. 2004 Feb 9;14(3):719-22. [Content Brief]

[3]. Tabata C, et al. The calpain inhibitor calpeptin prevents pulmonary fibrosis in mice. Clin Exp Immunol. 2010 Dec;162(3):560-7. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.7589 mL	13.7946 mL	27.5893 mL	68.9731 mL
	5 mM	0.5518 mL	2.7589 mL	5.5179 mL	13.7946 mL
	10 mM	0.2759 mL	1.3795 mL	2.7589 mL	6.8973 mL
	15 mM	0.1839 mL	0.9196 mL	1.8393 mL	4.5982 mL
	20 mM	0.1379 mL	0.6897 mL	1.3795 mL	3.4487 mL
	25 mM	0.1104 mL	0.5518 mL	1.1036 mL	2.7589 mL
	30 mM	0.0920 mL	0.4598 mL	0.9196 mL	2.2991 mL
	40 mM	0.0690 mL	0.3449 mL	0.6897 mL	1.7243 mL
	50 mM	0.0552 mL	0.2759 mL	0.5518 mL	1.3795 mL
	60 mM	0.0460 mL	0.2299 mL	0.4598 mL	1.1496 mL
	80 mM	0.0345 mL	0.1724 mL	0.3449 mL	0.8622 mL
	100 mM	0.0276 mL	0.1379 mL	0.2759 mL	0.6897 mL

Keywords

Calpeptin

28 Cited Publications

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Calpeptin

Apoptosis Compound Library

Immunology/Inflammation Compound Library

Metabolism/Protease Compound Library

Anti-Cancer Compound Library

Covalent Screening Library

Ubiquitination Compound Library

Anti-Blood Cancer Compound Library

Angiogenesis-Related Compound Library

Human Metabolite Library

Coagulation and Anti-coagulation Compound Library

Protease Inhibitor Library

Cell Death Library

Anti-Hematopathy Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Covalent Screening Library Plus

Bioactive Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

High-Throughput Bioactive Compound Library

Mass Spectrometry Human Metabolite Library

Posttranslational Modification Library

Publications Citing Use of MedChemExpress (MCE) Calpeptin

Alle Cathepsin Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (28)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Calpeptin

Apoptosis Compound Library

Immunology/Inflammation Compound Library

Metabolism/Protease Compound Library

Anti-Cancer Compound Library

Covalent Screening Library

Ubiquitination Compound Library

Anti-Blood Cancer Compound Library

Angiogenesis-Related Compound Library

Human Metabolite Library

Coagulation and Anti-coagulation Compound Library

Protease Inhibitor Library

Cell Death Library

Anti-Hematopathy Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Covalent Screening Library Plus

Bioactive Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

High-Throughput Bioactive Compound Library

Mass Spectrometry Human Metabolite Library

Posttranslational Modification Library

Publications Citing Use of MedChemExpress (MCE) Calpeptin

Alle Cathepsin Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (28)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Calpeptin Related Classifications

HY-100223 Related Classifications