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Cathepsin D & E substrate (fluorogenic)

 
BML-P145-0001 1 mg 164.00 USD
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Quenched fluorogenic substrate for cathepsin D (kcat/Km=1.09 x 10 M-1s-1) and cathepsin E (kcat/Km=1.56 x 10 M-1s-1). Mca fluorescence is quenched by the Dnp group until cleavage separates them. Activity of the two enzymes on this substrate can be distinguished by the use of Ascaris pepsin inhibitor, which inhibits cathepsin E, but not cathepsin D. This substrate is also cleaved by MMP-2, MMP-3, MMP-9, but not MMP-1 nor MMP-13. This substrate is useful for inhibitor screening and kinetic analysis. Ex.: 320-340 nm, Em.: 393-420 nm. Mca-Pro-Leu-OH (BML-P127) can be used to calibrate for Mca fluorescence.

Product Specification

Sequence:Mca-Gly-Lys-Pro-Ile-Leu-Phe-Phe-Arg-Leu-Lys(Dnp)-D-Arg-NH2 [Mca= (7-methoxycoumarin-4-yl)acetyl; Dnp=dinitrophenyl]
 
MW:1756.0
 
Source:Synthetic
 
Formulation:Trifluroacetate salt
 
Purity:≥95% (HPLC)
 
Quality Control:Determined by MS.
 
Appearance:Yellow powder
 
Solubility:Soluble in DMSO (1mM) or 50% acetonitrile (10mg/ml).
 
Shipping:Blue Ice Not Frozen
 
Long Term Storage:-20°C
 
Handling:Protect from light. Keep cool and dry.
 

Product Literature References

Cell penetrable, clickable and tagless activity-based probe of human cathepsin L: D. Dana, et al.; Bioorg. Chem. 85, 505 (2019), Application(s): Activity assay, Abstract;
Cathepsin D regulates cathepsin B activation and disease severitypredominantly in inflammatory cells during experimental pancreatitis: A.A. Aghdassi, et al.; J. Biol. Chem. 293, 1018 (2018), Abstract; Full Text
The lysosome system is severely impaired in a cellular model of neurodegeneration induced by HSV-1 and oxidative stress: H. Kristen, et al.; Neurobiol. Aging 68, 5 (2018), Abstract;
Cathepsin D non-proteolytically induces proliferation and migration in human omental microvascular endothelial cells via activation of the ERK1/2 and PI3K/AKT pathways: M.Z.I. Pranjol, et al.; Biochim. Biophys. Acta 1865, 25 (2017), Abstract;
Progranulin-mediated deficiency of cathepsin D results in FTD and NCL-like phenotypes in neurons derived from FTD patients: C. Valdez, et al.; Hum. Mol. Genet. 26, 4861 (2017), Abstract; Full Text
Reduced autophagy leads to an impaired ferritin turnover in senescent fibroblasts: C. Ott, et al.; Free Radic. Biol. Med. 101, 325 (2016), Abstract;
Tasiamide F, a potent inhibitor of cathepsins D and E from a marine cyanobacterium: F.H. Al-Awadhi, et al.; Bioorg. Med. Chem. 24, 3276 (2016), Application(s): In vitro protease inhibition assays, Abstract;
Variable Processing and Cross-presentation of HIV by Dendritic Cells and Macrophages Shapes CTL Immunodominance and Immune Escape: J. Dinter, et al.; PLoS Pathog. 11, e1004725 (2015), Application(s): Cell Culture, Abstract; Full Text
Ascorbic acid modulation of iron homeostasis and lysosomal function in trabecular meshwork cells: P. Xu, et al.; J. Ocul. Pharmacol. Ther. 30, 246 (2014), Abstract; Full Text
Development of a highly potent, selective, and cell-active Inhibitor of cysteine cathepsin L-A hybrid design approach: D. Dana, et al.; Chem. Commun. (Camb.) 50, 10875 (2014), Abstract;
Cathepsin B is up-regulated and mediates extracellular matrix degradation in trabecular meshwork cells following phagocytic challenge: K. Porter, et al.; PLoS One 8, e68668 (2013), Abstract; Full Text
Suppression of lysosome function induces autophagy via a feedback down-regulation of MTOR complex 1 (MTORC1) activity: M. Li, et al.; J. Biol. Chem. 288, 35769 (2013), Abstract; Full Text

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