calpain

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.

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

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.

Tacalcitol monohydrate(Curatoderm monohydrate), a vitamin D3 analog that promotes bone development by regulating calcium ions, can be used to study psoriasis.

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.

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.

(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].

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

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].

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].

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

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-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-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.

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

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

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.

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

Alicapistat (ABT-957) is a human calpains 1 and 2 inhibitor. It can potentially be used to treat Alzheimer's disease (AD).

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

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.