Calpeptin
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.
For research use only. We do not sell to patients.
- Purity: 99.17%
- CAS No.: 117591-20-5
- Formula: C20H30N2O4
- Molecular Weight:362.46
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) Calpeptin
More- J Nanobiotechnology. 2022 Mar 28;20(1):165. [Abstract]
- Adv Sci (Weinh). 2025 Apr 2:e2501112. [Abstract]
- ACS Cent Sci. 2022 Feb 23;8(2):192-204. [Abstract]
- ACS Sens. 2026 Mar 27;11(3):1891-1907. [Abstract]
- Cell Death Discov. 2024 Mar 11;10(1):130. [Abstract]
- Cell Rep. 2023 Nov 18;42(12):113434. [Abstract]
- J Med Chem. 2023 Apr 13;66(7):5289-5304. [Abstract]
- Antioxid Redox Signal. 2023 Jun;38(16-18):1071-1081. [Abstract]
- RSC Adv. 2019 Aug 13;9(43):25107-25118. [Abstract]
- Cells. 2026 May 18;15(10):917. [Abstract]
- Int Dent J. 2025 Dec 6;76(1):109309. [Abstract]
- Toxicology. 2025 Jun 4:154212. [Abstract]
- Chem Biol Interact. 2024 Jan 5:387:110807. [Abstract]
- Chem Biol Interact. 2022 Jul 1;361:109967. [Abstract]
- PLoS Pathog. 2023 Jul 27;19(7):e1011550. [Abstract]
- Sci Rep. 2022 Jul 16;12(1):12197. [Abstract]
- Cell Signal. 2022 Feb:90:110191. [Abstract]
- J Cell Mol Med. 2020 Aug;24(16):9287-9299. [Abstract]
- Mol Hum Reprod. 2023 Apr 29;29(5):gaad010. [Abstract]
- Neurotox Res. 2022 Oct;40(5):1248-1260. [Abstract]
- Biochim Biophys Acta Mol Cell Biol Lipids. 2026 Jan;1871(1):159704. [Abstract]
- Int J Med Sci. 2021 Feb 18;18(8):1746-1752. [Abstract]
- J Diabetes Investig. 2024 Oct;15(10):1365-1376. [Abstract]
- Hum Exp Toxicol. 2022 Jan-Dec:41:9603271221108321. [Abstract]
- Biomed Pharmacother. 2024 Nov:180:117606. [Abstract]
- bioRxiv. 2024 Feb 5.
- Heliyon. 2023 Jun 16;9(7):e17316. [Abstract]
- Research Square Preprint. 2022 Feb.
Customer Validation & Images
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Histological Imaging/Staining
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WB
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In Vivo Efficacy Study
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IF
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WB
All Cathepsin Isoforms
More
Biological Activity
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cathepsin K |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HeLa | IC50 |
17.7 μM
Compound: 4
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Antiviral activity against human rhinovirus-14 in HeLa cells
Antiviral activity against human rhinovirus-14 in HeLa cells
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10.1016/S0960-894X(96)00537-9 |
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.
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Cell Line:WI38 VA13 and IMR90 cells
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Concentration:0-100 nM
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Incubation Time:24 hours
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Result:Suppressed the proliferation in a dose-dependent manner.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6 female mice (Eight-week-old)[3].
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Dosage:0.04 mg/mouse.
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Administration:Intraperitoneally three times weekly for 28 days (together with Bleo).
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Result:Inhibited the collagen deposition and increase of calpain activity in the NSC-125066 treated mouse lung tissues.
Chemical Information
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CAS No. 117591-20-5
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Appearance Solid
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Molecular Weight 362.46
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Formula C20H30N2O4
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Color White to off-white
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SMILES
O=C(OCC1=CC=CC=C1)N[C@H](C(N[C@H](C=O)CCCC)=O)CC(C)C
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (28)
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Journal Impact Factor
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Most Recent
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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.
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Adv Sci (Weinh)
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.
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ACS Cent Sci
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.
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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 -
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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 -
Solvent & Solubility
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- 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.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
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Data Sheet (273 KB)
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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)
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Handling Instructions (2659 KB)
References
[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]
Complete Stock Solution Preparation Table
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.
| 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 |
Calpeptin Related Classifications
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