CA-074 Me

BML-PI126

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Cathepsin inhibitor

Potent and selective irreversible cell permeable cathepsin B inhibitor. Methyl ester (Me) is hydrolyzed by intracellular esterases releasing the active inhibitor. Prevents death of CA1 neurons after ischemia following IV delivery after the ischemic insult. In isolated rat osteoclasts it inhibited bone resorption with a maximal effect at 50 µM. This product is only suitable for in vivo and whole cell experiments. The free acid form must be used for in vitro experiments. Can be used to discriminate between cathepsin B and L/S forms.

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Product Details

Alternative Name	N-(L-3-trans-Propylcarbonyl-oxirane-2-carbonyl)-L-isoleucyl-L-proline methyl ester
Appearance	White solid.
Formula	C₁₉H₃₁N₃O₆
MW	397.5
Purity	≥98% (HPLC)
Sequence	N-(L-3-trans-Propylcarbonyl-oxirane-2-carbonyl)-L-isoleucyl-L-proline methyl ester
Solubility	Soluble in DMSO.

Handling & Storage

Use/Stability	As indicated on product label or CoA when stored as recommended.
Long Term Storage	-20°C
Shipping	Blue Ice

Regulatory Status	RUO – Research Use Only

The interplay between lysosome, protein corona and biological effects of cationic carbon dots: Role of surface charge titratability: Y. Arezki, et al.; Int. J. Pharm. 645, 123388 (2023), Abstract
Lysosomal cathepsins act in concert with Gasdermin-D during NAIP/NLRC4-dependent IL-1β secretion: L. M. Branco, et al.; Cell Death Dis. 13, 1029 (2022), Abstract
Salmonella Flagellin Activates NAIP/NLRC4 and Canonical NLRP3 Inflammasomes in Human Macrophages: Gram, A. M., Wright, J. A., et al.; J. Immunol. 206, 631 (2021), Abstract
Role of Autophagy in Von Willebrand Factor Secretion by Endothelial Cells and in the In Vivo Thrombin-Antithrombin Complex Formation Promoted by the HIV-1 Matrix Protein p17: A. Bugatti, et al.; Int. J. Mol. Sci. 21, 2022 (2020), Abstract — Full Text
Lysosomal dysfunction and autophagy blockade contribute to MDMA-induced neurotoxicity in SH-SY5Y neuroblastoma cells: I.H. Li, et al.; Chem. Res. Toxicol. 33, 903 (2020), Abstract
Cathepsin B Localizes in the Caveolae and Participates in the Proteolytic Cascade in Trabecular Meshwork Cells. Potential New Drug Target for the Treatment of Glaucoma: A. Nettesheim, et al.; J. Clin. Med. 10, 78 (2020), Abstract
Platelet-activating factor (PAF) mediates NLRP3-NEK7 inflammasome induction independently of PAFR: Deng, M., Guo, H., et al.; J. Exp. Med. 216, 2838 (2019), Abstract
The vacuolar-type ATPase inhibitor archazolid increases tumor cell adhesion to endothelial cells by accumulating extracellular collagen: B. Luong, et al.; PLoS One 13, e0203053 (2018), Abstract — Full Text
NLR members NLRC4 and NLRP3 mediate sterile inflammasome activation in microglia and astrocytes: Freeman, L., Guo, H., et al.; J. Exp. Med. 214, 1351 (2017), Abstract
Salinomycin kills cancer stem cells by sequestering iron in lysosomes: Mai, T. T., Hamaï, A., et al.; Nat. Chem. 9, 1025 (2017), Abstract

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CA-074 Me

BML-PI126

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