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Cathepsin D & E substrate (fluorogenic)

Synthetic substrate useful for inhibitor screening and kinetic analysis
BML-P145-0001 1 mg 206.00 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 Details

Sequence:Mca-Gly-Lys-Pro-Ile-Leu-Phe-Phe-Arg-Leu-Lys(Dnp)-D-Arg-NH2 [Mca= (7-methoxycoumarin-4-yl)acetyl; Dnp=dinitrophenyl]
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
Long Term Storage:-20°C
Handling:Protect from light. Keep cool and dry.
Regulatory Status:RUO - Research Use Only

Product Literature References

Cathepsin D: Analysis of its potential role as an amyloid beta degrading protease: L. Gallwitz, et al.; Neurobiol. Dis. 175, 105919 (2022), Abstract;
The molecular network of the proteasome machinery inhibition response is orchestrated by HSP70, revealing vulnerabilities in cancer cells: M. Oroń, et al.; Cell Rep. 40, 111428 (2022), Abstract;
USP17 is required for peripheral trafficking of lysosomes: J. Lin, et al.; EMBO Rep. 23, e51932 (2022), Abstract;
Trehalose Reduces the Secreted Beta-Amyloid Levels in Primary Neurons Independently of Autophagy Induction: I. Benito-Cuesta, et al.; Metabolites 11, 421 (2021), Abstract;
Analysis of cathepsin B and cathepsin L treatment to clear toxic lysosomal protein aggregates in neuronal ceroid lipofuscinosis: A. Di Spiezio, et al.; Biochim. Biophys. Acta Mol. Basis Dis. 1867, 166205 (2021), Abstract;
Post-Golgi carriers, not lysosomes, confer lysosomal properties to pre-degradative organelles in normal and dystrophic axons: P.P.Y. Lie, et al.; Cell Rep. Med. 35, 109034 (2021), Abstract;
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;
Discovery of a small molecule targeting autophagy via ATG4B inhibition and cell death of colorectal cancer cells in vitro and in vivo: Y. Fu, et al.; Autophagy 15, 295 (2019), Abstract; Full Text
Regulation of Autophagic Flux by the 20S Proteasome: E. Njomen, et al.; Cell Chem. Biol. 26, 1283 (2019), 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
Dynamic MTORC1-TFEB feedback signaling regulates hepatic autophagy, steatosis and liver injury in long-term nutrient oversupply: H. Zhang, et al.; Autophagy 14, 1779 (2018), Abstract;
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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