A cell permeable, selective calpain inhibitor
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Calpain Inhibitor III

Item No. 14283

Technical Information
Formal Name
N-[(1S)-1-[[(1-formyl-2-phenylethyl)amino]carbonyl]-2-methylpropyl]-carbamic acid, phenylmethyl ester
CAS Number
88191-84-8
Synonyms
  • MDL 28170
Molecular Formula
C22H26N2O4
Formula Weight
Purity
≥95%
Formulation
A crystalline solid
DMF: 14 mg/mlDMF:PBS (pH 7) (1:10): 0.09 mg/mlDMSO: 12.5 mg/mlEthanol: 3.3 mg/ml
SMILES
O=C(N[C@@H](C(C)C)C(NC(CC1=CC=CC=C1)C([H])=O)=O)OCC2=CC=CC=C2
InChi Code
InChI=1S/C22H26N2O4/c1-16(2)20(24-22(27)28-15-18-11-7-4-8-12-18)21(26)23-19(14-25)13-17-9-5-3-6-10-17/h3-12,14,16,19-20H,13,15H2,1-2H3,(H,23,26)(H,24,27)/t19?,20-/m0/s1
InChi Key
NGBKFLTYGSREKK-ANYOKISRSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    The calpains are a family of calcium-dependent cysteine proteases that catalyze limited proteolysis of substrates.1 Calpain Inhibitor III is a cell permeable, selective inhibitor of μ-calpain (calpain-1) and m-calpain (calpain-2).2 Calpain Inhibitor III crosses the blood-brain barrier to inhibit brain cysteine protease activity and has been reported to have neuroprotective effects in numerous rodent neurotrauma models, including spinal cord injury, cortical impact trauma, neonatal hypoxia-ischemia, and focal cerebral ischemia.3 Additionally, Calpain Inhibitor III has been shown to attenuate depression in myocardial contractile performance that occurs during reperfusion following cardiac ischemia.4

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Mellgren, R.L. Specificities of cell permeant peptidyl inhibitors for the proteinase activities of μ-calpain and the 20 S proteasome. The Journal of Biological Chemisty 272(47), 29899-29903 (1997).

    2. Mehdi, S. Cell-penetrating inhibitors of calpain. Trends Biochem. Sci. 16(4), 150-153 (1991).

    3. Thompson, S.N., Carrico, K.M., Mustafa, A.G., et alA pharmacological analysis of the neuroprotective efficacy of the brain- and cell-permeable calpain inhibitor MDL-28170 in the mouse controlled cortical impact traumatic brain injury model. J. Neurotrauma 27(12), 2233-2243 (2010).

    4. Urthaler, F., Wolkowicz, P.E., Digerness, S.B., et alMDL-28170, a membrane-permeant calpain inhibitor, attenuates stunning and PKC proteolysis in reperfused ferret hearts. Cardiovasc. Res. 35(1), 60-67 (1997).