calpain

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].

MDL-28170 (Calpain Inhibitor III) is a cysteine protease.

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].

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.

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.

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

Calpain Inhibitor-2 is a lipophilic calpain inhibitor, and they showed moderate to good anti-proliferative effects in vitro compared to melanoma cell lines (A-375 and B-16F1) and PC-3 prostate cancer cells. was able to inhibit the invasion of 80% of DU-145 cells.

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

Calpain-1, Human Erythrocyte, is an intracellular cysteine protease regulated by Ca2+ [Ca(2+)]. This compound also possesses neuroprotective properties.

Calpain-2-IN-1 is a selective calpain-2 inhibitor that prolongs ERK activation and thus enhances learning and memory.

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

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

MG-132 (Z-Leu-Leu-Leu-al) is a 26S proteasome inhibitor (IC50=100 nM) that is cell-permeable and reversible. MG-132 acts as an autophagy activator and also induces apoptosis.

Acetyl-Calpastatin (184-210)(human) acetate is a potent, selective and reversible calpain inhibitor with Ki values of 0.2 nM and 6 μM for µ-calpain and cathepsin L, respectively.

Aloxistatin (E64d) is an inhibitor of cysteine protease with blood platelet aggregation inhibiting activity. Aloxistatin is an irreversible, membrane-permeable inhibitor of lysosomal and cytosolic cysteine proteases with the ability to inhibit calpain activity in intact platelets.

Calpeptin is a potent, cell-permeable calpain inhibitor.

(1S,2R)-Alicapistat ((1S,2R)-ABT-957) is a highly efficient, orally active compound that selectively inhibits human calpains 1 and 2, showing promise for Alzheimer's disease (AD) therapy [1]. It effectively addresses the metabolic liability associated with carbonyl reduction and demonstrates potent inhibition of calpain 1 with an IC50 value of 395 nM [2].

Aureusimine B, also known as phevalin, is a natural pyrazinone produced by certain fungi and by Staphylococcus spp., including S. aureus. Its synthesis appears to be initiated by a conserved nonribosomal peptide synthetase that creates a dipeptide (phenylalanine-valine) aldehyde, which then undergoes cyclization and oxidation. Aureusimine B inhibits calpain in a casein hydrolysis assay (IC50 = 1.3 μM), contributes to S. aureus infection in mice, and alters human keratinocyte gene expression.

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

Pheleuin is a pyrazinone derivative synthesized from a dipeptide aldehyde. Although the biological activity of this compound has not been reported, similar diketopiperazines are known to inhibit calpain and/or regulate S. aureus virulence factor expression.

Selective calpain inhibitor. Strongly inhibits calpain I (Ki = 0.2 nM) and II but does not inhibit papain, trypsin and cathepsin L (Ki = 6 μM). Increases secretion of amyoid β-protein (Aβ) 42, Aβ40 and Aβ42 ratio.

Isovalerylcarnitine (3-methylbutyrylcarnitine) is a small molecule compound produced by the catabolism of L-leucine and the accumulation of isovaleric acid. Isovalerylcarnitine is also a selective and effective calpain activator that can promote cell apoptosis. Isovalerylcarnitine is related to isovaleric acidemia and can be used as a marker of isovaleric acidemia.

Dehydrotrametenolic acid (Dehydroeburicoic acid) induces necrotic cell death that involves Ca(2+) overload, mitochondrial dysfunction, and calpain activation in human glioblastomas.

A-933548 is a potent Calpain inhibitor. A-933548 features enhanced selectivity versus related cysteine protease cathepsins, favorable microsomal stability, and efficacy in cellular assays.

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

AK 275 is a calpain inhibitor that prevents degradation of cytoskeletal and myelin proteins in spinal cord in vitro.

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].

Calpastatin subdomain B is a bioactive peptide that inhibits calpain activity.

AK 295, also known as CX 295, is a dipeptide inhibitor of alpha-ketoamide calpain.

PD150606 is a selective nonpeptide calpain inhibitor with neuroprotective activity that inhibits μ-calpains and m-calpains. Inhibits erythrocyanine-induced Ca2+ efflux and interferes with excitotoxicity-dependent motor neuron death.

SNJ-1945 is a calpain inhibitor with more favorable retinal penetration, high oral bioavailability, and long half-life. SNJ1945 rescued defective function in lissencephaly. SNJ-1945 protects SH-SY5Y cells against MPP(+) and rotenone. SNJ-1945 reduces murine retinal cell death in vitro and in vivo. SNJ-1945 has good aqueous solubility, can prevents the heart from KCl arrest-reperfusion injury associated with the impairment of total Ca(2+) handling by inhibiting the proteolysis of alpha-fodrin as a cardioplegia.

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

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

Calpastatin (184-210), an acetylated synthetic peptide derived from human calpastatin, effectively inhibits the calcium-dependent cysteine proteases, calpain I (µ-calpain) and calpain II (m-calpain), which require micromolar and millimolar calcium concentrations, respectively. Unlike its action on calpains, this 27 amino acid peptide does not inhibit papain (a cysteine protease) or trypsin (a serine protease). Encoded by exon 1B of Ac-calpastatin (184-210), it aligns with a section of inhibitory domain 1, showcasing its specificity and inhibitory function towards calpain enzymes.

A-953227 is a highly effective and selective inhibitor of calpain. A-953227 features enhanced selectivity versus related cysteine protease cathepsins, favorable microsomal stability, and efficacy in cellular assays.

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].

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].

EP 459 is a thiol and calpain protease inhibitor.

2,3-Diphospho-D-glyceric acid pentasodium salt is a highly anionic polyphosphorus compound located within the concave center of red blood cells, where it decreases oxygen affinity by binding to hemoglobin. This endogenous compound selectively inhibits vascular calcification (VC) and effectively postpones the formation of crystalline calpain particles (CPP). Additionally, it inhibits calcification in the mouse vascular smooth muscle cell line (MOVAS) without eliciting cytotoxic effects [1].

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

Penicillide is a fungal metabolite originally isolated from Penicillium that has diverse biological activities. It is an inhibitor of calpain 2/m-calpain (IC50 = 7.1 μM) and acyl-coenzyme A:cholesterol acyltransferase (ACAT; IC50 = 22.9 μM). It is also an antagonist of oxytocin receptors (IC50 = 67 μM). Penicillide inhibits RNA synthesis in P388 murine leukemia cells.