cathepsin-d

Nandrolone phenylpropionate (Nandrolone phenpropionate) is an androgen receptor agonist. It mainly used to treat women with breast cancer and osteoporosis

Mca-GKPILFFRL-Dpa-r-amide, FRET substrate for cathepsin D and E. Also cleaved by napsin A.

Cathepsin D and E FRET Substrate acetate is a fluorogenic substrate for cathepsins D and E but not for B, H, or L. Cathepsin D and E FRET Substrate acetate can be used in mechanistic studies on cathepsins D and E studies.

Cathepsin D and E FRET Substrate acetate is a fluorogenic substrate selectively cleaved by cathepsins D and E at the Phe-Phe amide bond, demonstrating no activity towards cathepsins B, H, or L. This specificity renders it essential for routine assays and mechanistic studies focusing on cathepsins E and D[1].

NB-360 is a potent and brain-penetrable inhibitor of BACE1 and BACE2 with IC50s of 5, 5, and 6 nM for mouse and human BACE1 and BACE2. NB-360 exhibits excellent selectivity over the related aspartyl proteases pepsin, cathepsin E, and cathepsin D.

β-Secretase Inhibitor IV is a potent, cell-active inhibitor of BACE-1, with IC50 values of 15.6 nM and 16.3 nM at BACE-1 concentrations of 2 nM and 100 pM, respectively.

ROC-325 is an effective and orally active inhibitor of autophagy with anticancer activity. ROC-325 induces renal cell carcinoma apoptosis and exhibits favorable selectivity.

TB-11 is an inhibitor of Cathepsin D with IC50 values of 0.126 nM (Cathepsin D), 1.92 nM (Cathepsin E), and 48.8 nM (BACE1). It is primarily utilized in oncological research.

Imarikiren (also known as TAK-272) is a potent, highly selective, orally bioavailable direct renin inhibitor primarily used for treating diabetic nephropathy. In hPRA assays, TAK-272 exhibits strong inhibitory activity against human renin (IC50 = 2.1 nM) and demonstrates excellent selectivity over other aspartic proteases such as pepsin (IC50 > 10 μM) and cathepsin D (IC50 > 10 μM). In rats, TAK-272 shows significantly improved pharmacokinetic properties (F = 25.2%) and, upon oral administration (3 and 10 mg kg), exhibits a dose-dependent, potent, and sustained antihypertensive effect. Currently, TAK-272 HCl is undergoing human clinical trials.

TB-9, a derivative of Tasiamide B, is a potent inhibitor of protease D (cathepsin D), protease E (cathepsin E), and BACE1, with IC50 values of 0.0783 nM, 0.724 nM, and 54.2 nM, respectively.

CatD-IN-1 (Compound 5) is a Cathepsin D inhibitor with an IC50 of 0.44 μM, and it shows potential for research in the field of osteoarthritis.

LY2811376, an orally available non-peptidic β-secretase(BACE1) inhibitor (IC50: 239-249 nM), can decrease Aβ secretion (EC50: 300 nM). It has 10-fold selectivity towards BACE1 over BACE2, and more than 50-fold inhibition over other aspartic proteases including pepsin, cathepsin D, or renin.

Potent and selective β-secretase (BACE) inhibitor (IC50 values are 10.2 and 20.3 nM for human BACE2 and BACE1, respectively). Displays >5,000-fold selectivity for BACE over other proteases including cathepsin D, pepsin and renin. Inhibits Aβ1-40 and Aβ1-42 production in cells expressing mutated APP. Reduces hippocampal and cortical Aβ and sAPPβ levels in an Alzheimer's disease mouse model.

H-Pro-Thr-Glu-Phe-p-nitro-Phe-Arg-Leu-OH is a water-soluble polypeptide that serves as a substrate for the enzymes cathepsin D, pepsin, and pepsinogen, with potential applications in biochemical analysis [1] [2].

Parasin I, a peptide fragment derived from the N-terminal region of histone H2A in catfish (P. asotus), plays a critical role in host defense. This antimicrobial peptide is produced through the action of cathepsin D on histone H2A within the skin mucosa of injured P. asotus. Demonstrating efficacy against a spectrum of Gram-positive and Gram-negative bacteria, as well as fungi, Parasin I exhibits minimum inhibitory concentrations (MICs) of 1-2 µg/ml, 1-4 µg/ml, and 1-2 µg/ml, respectively.

Tasiamide B is a linear peptide and Cathepsin D inhibitor discovered in the marine cyanobacterium Symploca sp. This compound serves as an excellent template for the development of aspartic protease inhibitors. Tasiamide B effectively targets skin cancer through its strong interaction with the protein HSP90.