calpain inhibitor-1

Calpain Inhibitor-1 (compound 36) is a highly potent and selective inhibitor of Calpain 1 (Cal1), a cysteine protease, with an IC50 value of 100 nM and a Ki value of 2.89 μM.

MG-101 (Calpain inhibitor I) is a cell-permeable and potent inhibitor of cysteine proteases including calpains and lysosomal cathepsins.

Calpain Inhibitor XII (Z-L-Nva-CONH-CH2-2-Py) is a selective and potent inhibitor of calpain I, inhibits calpain II and cathepsin B. Calpain Inhibitor XII shows antiviral activity against coronavirus in cell culture.

PD151746 is a calpain inhibitor with a 20-fold selectivity for u-calpain (Ki = 0.26 ± 0.03 μM) over m-calpain (Ki = 5.33 ± 0.77 μM). Its IC50 values are 0.26 ± 0.03 μM (Ki for μ-calpain) and 5.33 ± 0.77 μM (Ki for m-calpain) [1]. In vitro, PD151746 targets calpain and reduces oxLDL-induced cytotoxicity [2].

Neurodegenerative Disorder-Targeting Compound 1 is a calpain inhibitor [1].

Alicapistat (ABT-957) is an inhibitor of human calpain 1 and calpain 2. Alicapistat (ABT-957) has been investigated in the context of Alzheimer's disease research. The selective inhibition of calpain proteases by Alicapistat (ABT-957) supports its application in studies of neurodegeneration, proteolytic signaling pathways, neuronal injury mechanisms, and calpain-associated cellular processes.

ALLM (Calpain inhibitor II), a potent calpain and cathepsin protease inhibitor, not only prevents neuronal cell death but also enhances chronic neurological function following spinal cord injury (SCI)[1][2].

SARS-CoV-2 3CLpro-IN-34 (Compound 55) is a highly effective non-covalent inhibitor of the SARS-CoV-2 3CLpro protease, with an IC50 of 1.9 μM. It also inhibits the SARS-CoV-1 3CL protease, displaying an IC50 of 3.2 μM, and shows strong selectivity for host cysteine proteases such as cathepsins L/K and calpain. Furthermore, SARS-CoV-2 3CLpro-IN-34 exhibits antiviral activity in SARS-CoV-2 infected cells, with an EC50 of 25 μM, is unaffected by P-gp inhibitors, and does not cause significant cytotoxicity. This compound can be utilized in the study of SARS-CoV-2 infections.

SJA6017 is a inhibitor of calpain-1 (IC50 = 7.5 nM) and calpain-2 ( IC50 = 78 nM). SJA6017 also inhibits cathepsins B (IC50s = 15 nM) and cathepsins L (IC50s = 1.6 nM). SJA6017 reduces apoptotic cell death, preserves spinal cord tissue and improves functi

Calpain-2-IN-1 (Formula 1A) is a selective calpain-2 inhibitor with Ki values of 181 nM for calpain-1 and 7.8 nM for calpain-2, applicable for neurodegenerative diseases and other synaptic dysfunction disorders.

Calpeptin is a cell-permeable Calpain inhibitor (IC50 = 5 nM), and its ID50 value for human platelet Calpain I is 40 nM. Calpeptin is also an effective inhibitor of Cathepsin K (IC50 = 0.11 nM).

Calpain Inhibitor XI, a reversible covalent inhibitor of calpain-1, is utilized in the research of neurodegenerative disorders.

Acetyl-Calpastatin(184-210)(human) TFA, a potent, selective, and reversible calpain inhibitor, has Ki values of 0.2 nM for µ-calpain and 6 μM for cathepsin L, indicating high specificity and efficacy in enzyme inhibition [1] [2].

Ac-Leu-Leu-Norleucinol (ALLN), a calpain inhibitor, is employed in the research of Acetaminophen-induced acute liver damage. It effectively reduces levels of glutamic-oxalacetic transaminase (ALT) and glutamic-pyruvic transaminase (AST) [1].

Z-LLY-FMK (Calpain Inhibitor IV) inhibits calpain, a family of proteases involved in the apoptosis of various cell systems, and specifically suppresses intestinal cell apoptosis following common bile duct ligation [1].

Z-Leu-Tyr-Chloromethylketone is a calpain inhibitor [1].

Calpain Inhibitor V (Mu-Val-HPh-FMK) is a cell-permeable, irreversible calpain inhibitor with demonstrated anti-chlamydial activity [1].

(Rac)-Neurodegenerative Disorder-Targeting Compound 1 is a calpain inhibitor.

NA-184, a selective calpain-2 inhibitor, prevents TBI-induced cell death with an EC50 of 0.13 mg/kg [1].

Dazcapistat is a potent calpain inhibitor with IC50s of <3 μM for calpain 1, calpain 2, and calpain 9, respectively.