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Calpain and cathepsin inhibitor
BML-PI101-0010 10 mg 154.00 USD
BML-PI101-0050 50 mg 626.00 USD
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Replaces Prod. #: ALX-260-014

Membrane permeable inhibitor of calpain I and II, cathepsin L and cathepsin K (IC50=0.11 nM). Promotes neurite elongation in differentiating PC12 cells. Prevents Ca2+-ionophore induced degradation of actin binding protein and P235 in platelets. Inhibits myosin light chain phosphorylation in platelets stimulated by collagen, ionomycin (Prod. No. ALX-450-006) or thrombin. Inhibits LPS induced iNOS transcription and NF-κB activation, possibly via proteasome inhibition.

Product Details

Alternative Name:Z-Leu-norleucinal, N-Benzyloxycarbonyl-L-leucyl-norleucinal
Purity:≥98% (HPLC)
Appearance:White to off-white powder.
Solubility:Soluble in DMSO (25mg/ml), 100% ethanol (25mg/ml or dimethyl formamide (5mg/ml).
Shipping:Blue Ice
Long Term Storage:-20°C
Use/Stability:Stable for up to 1 year when stored at -20°C. Stock solutions are stable for up to 3 months at -20°C.
Handling:Protect from light and moisture. Packaged under inert gas. After reconstitution, prepare aliquots and store at -20°C.
Technical Info/Product Notes:Concentrations for intact cells: 30µM (platelets), 10µM (myoblast cells)

Note: Product is not sterile.
Regulatory Status:RUO - Research Use Only
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Product Literature References

Simvastatin reduces the carcinogenic effect of 3-methylcholanthrene in renal epithelial cells through histone deacetylase 1 inhibition and RhoA reactivation: C.C. Chang, et al.; Sci. Rep. 9, 4606 (2019), Abstract; Full Text
The Coagulation and Immune Systems Are Directly Linked through the Activation of Interleukin-1α by Thrombin: L.C. Burzynski, et al.; Immunity 50, 1033 (2019), Abstract;
Effect of SI-591, a new class of cathepsin K inhibitor with peptidomimetic structure, on bone metabolism in vitro and in vivo: T. Fujii, et al.; Bone 81, 427 (2015), Application(s): Human and Rat Cathepsin K assays, Abstract;
Human normal bronchial epithelial cells: a novel in vitro cell model for toxicity evaluati: W. Feng, et al.; PLoS One 10, e0123520 (2015), Application(s): Cell Culture, Abstract; Full Text
Membrane-Permeable Calpain Inhibitors Promote Rat Oral Mucosal Epithelial Cell Proliferation by Inhibiting IL-1α Signaling: M. Kondo, et al. ; PLoS One 10, e0134240 (2015), Application(s): Cell culture, Abstract; Full Text
Exploration of the P1 SAR of aldehyde cathepsin K inhibitors: J.G. Catalano, et al.; Bioorg. Med. Chem. Lett. 14, 275 (2004), Abstract;
Inhibitors of the proteasome pathway interfere with induction of nitric oxide synthase in macrophages by blocking activation of transcription factor NF-kappa B: J.M. Griscavage, et al.; PNAS 93, 3308 (1996), Abstract; Full Text
Endogenous cleavage of phospholipase C-beta 3 by agonist-induced activation of calpain in human platelets: Y. Banno, et al.; J. Biol. Chem. 270, 4318 (1995), Abstract;
Calpeptin, a calpain inhibitor, promotes neurite elongation in differentiating PC12 cells: M. Pinter, et al.; Neurosci. Lett. 170, 91 (1994), Abstract;
Comparison of the effect of calpain inhibitors on two extralysosomal proteinases: the multicatalytic proteinase complex and m-calpain: M.E. Figueiredo-Pereira, et al.; J. Neurochem. 62, 1989 (1994), Abstract;
Role of intracellular proteases in differentiation of L6 myoblast cells: C. Ebisui, et al.; Biochem. Mol. Biol. Int. 32, 515 (1994), Abstract;
Specificity of calcium-activated neutral proteinase (CANP) inhibitors for human mu CANP and mCANP: K. Saito and R.A. Nixon; Neurochem. Res. 18, 231 (1993), Abstract;
Cell-penetrating inhibitors of calpain: S. Mehdi; TIBS 16, 150 (1991), Abstract;
Inhibitory effect of di- and tripeptidyl aldehydes on calpains and cathepsins: T. Sasaki, et al.; J. Enz. Inhib. 3, 195 (1990), Abstract;

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