calpain

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.

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

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

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

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.

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].

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.

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.

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.

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

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.

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].

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

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

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

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