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Calpains

Calpains (calcium-dependent papain-like enzymes) are a family of intracellular enzymes that consist of complex multi-domains and share a calcium-dependent cysteine protease core. With the development of human genome sequencing, a total of fifteen human calpain genes have been identified (CAPN1 to CAPN15). Calpain 1 (μ-calpain) and calpain 2 (m-calpain) are the two most abundant and well studied members of calpain family in mammals, which are heterodimers characterized by consisting of an isoform-specific large subunit (approximately 80 kDa) and a common small subunit (approximately 28 kDa). The large subunit consists of four domains, domain I (function not clear), domain II (cysteine protease domain), domain III (function not clear) and domain IV (Ca2+-binding domain); while the small subunit consists of two domains, domain V (N-terminal glycine-clustering hydrophobic region) and domain VI (C-terminal Ca2+-binding domain).

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  1. Cat.No. Product Name Information
  2. A8170 Z-FA-FMK An inhibitor of cysteine proteases, such as cathepsin B, which do not require a P1 Asp residue.
  3. A2585 MG-132

    MG132 (carbobenzoxy-Leu-Leu-leucinal) as a peptide aldehyde effectively blocks the proteolytic activity of proteasome complex.

  4. C5830 PD 145305
  5. C5347 Calpain Inhibitor XII
  6. A2603 Calpain Inhibitor II, ALLM Calpain inhibitor II (CPI-2) is a cell-permeable inhibitor of calpain I, calpan II, cathepsin L and cathepsin B. 
  7. A2602 Calpain Inhibitor I, ALLN Calpain Inhibitor I is an inhibitor of calpain I, calpain II, cathepsin B and cathepsin L with Ki values of 190 nM, 220 nM, 150 nM and 500 pM, respectively.
  8. A2576 E-64 E-64 is a natural, potent, and irreversible inhibitor of cysteine proteases.Its IC50 values for inhibiting cathepsins K, S, and L, in vitro, are 1.4, 4.1, and 2.5 nM, respectively.
  9. A4410 Acetyl-Calpastatin (184-210) (human) 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.
  10. A4411 Calpeptin Potent, cell-permeable inhibitor of the Ca2+-dependent protease, calpain. Prevents collagen- and thrombin-induced platelet aggregation, probably by blocking calpain induced phospholipase C and thromboxane synthase activation. Potent cathepsin L inhibitor. Recently shown to preferentially inhibit a subset of protein-tyrosine phosphatases.
  11. A4412 MDL 28170 MDL 28170 is a selective inhibitor, which inhibites calpain with Ki values of 10nM and cathepsin B with Ki values of 25 nM while does not inhibit trypsin-like serine proteases.

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