calpain 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.

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

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

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.

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.

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].

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

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].

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].

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

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].

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].

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

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.

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.