Cathepsin
Cathepsins are protease enzymes, categorized into multiple families. They can be serine protease, cysteine protease, or aspartyl protease. There were about 15 classes of cathepsins in humans. Cathepsin E is expressed on a broad range of immune cells, cathepsin K on skin fibroblasts, and cathepsin L only in the placenta. Cathepsin A causes the inactivation of bioactive peptides such as bradykinin, substance P, oxytocin, angiotensin I and endothelin-I. Cathepsin A can inhibit autophagy. Cathepsin B promotes amyloid plaque, and various carcinomas. This enzyme is instrumental in both basal and EGF (epidermal growth factor)-stimulated lung cancer cell migration. Prorenin, the precursor of kidney-secreted hormone renin, can be activated by cathepsin B.
Cathepsin B from amoeba can cleave several human proteins including immunoglobulins (IgA, IgG, IgM), hemoglobin, collagen, fibronectin, and albumin. Cathepsin D cleaves fibronectin and laminin. Cathepsin D can express on desmosomes, the intercellular junctions, causing desquamation. Cathepsin E is frequently implicated in antigen processing via the MHC class II pathway. Cathepsin K is highly effective in degrading collagens. Cathepsin K also degrades gelatin, the latter being a hydrolysis product of collagen. Cathepsin L degrades fibronectin, insulin receptor, and insulin-like growth factor 1 receptor (IGF-1R). Cathepsin V (or L2), an elastase, is involved in cancer invasion and metastasis. Cathepsins degrade lowdensity lipoprotein (LDL-P) and attenuate cholesterol efflux from macrophages, leading to foam cell formation. The foam cells are responsible for atherosclerosis and coronary artery disease. Fibrosis and cancer, among other inflammatory diseases, are the resultant of perturbed ECM.
References
1.Patel S,et al. Biomed Pharmacother. 2018 Sep;105:526-532.
Cathepsin B from amoeba can cleave several human proteins including immunoglobulins (IgA, IgG, IgM), hemoglobin, collagen, fibronectin, and albumin. Cathepsin D cleaves fibronectin and laminin. Cathepsin D can express on desmosomes, the intercellular junctions, causing desquamation. Cathepsin E is frequently implicated in antigen processing via the MHC class II pathway. Cathepsin K is highly effective in degrading collagens. Cathepsin K also degrades gelatin, the latter being a hydrolysis product of collagen. Cathepsin L degrades fibronectin, insulin receptor, and insulin-like growth factor 1 receptor (IGF-1R). Cathepsin V (or L2), an elastase, is involved in cancer invasion and metastasis. Cathepsins degrade lowdensity lipoprotein (LDL-P) and attenuate cholesterol efflux from macrophages, leading to foam cell formation. The foam cells are responsible for atherosclerosis and coronary artery disease. Fibrosis and cancer, among other inflammatory diseases, are the resultant of perturbed ECM.
References
1.Patel S,et al. Biomed Pharmacother. 2018 Sep;105:526-532.
Metabolic Enzyme/Protease
11β-HSD(15)
15-PGDH(1)
ACC(10)
ACE(15)
AChE(47)
Adenylate Cyclase(12)
ALDH(14)
Aldose Reductase(5)
Aminopeptidase(19)
BACE(19)
Casein Kinase(51)
CAT(5)
Cathepsin(9)
CETP(13)
COMT(2)
CPG2(1)
CYPs(6)
Decarboxylase(3)
Dehydrogenase(131)
DGAT(4)
Dopamine beta-hydroxylase(2)
DPP(32)
Elastase(6)
FAAH(28)
Factor Xa(31)
Fatty Acid Synthase(17)
Ftase(2)
FXR(26)
Glucokinase(1)
GSNOR(2)
Guanylate Cyclase(13)
HMGCR(17)
IDH(7)
IDO(20)
IMPDH(2)
LDH(2)
LDL(8)
Lipase(17)
Lipid(12)
MAGL(6)
MAO(72)
MMP(78)
NAMPT(12)
Neprilysin(7)
Other Targets(10)
P450(112)
PAI-1(9)
Phosphatase(95)
Phospholipase(65)
PPAR(115)
Protein Phosphatase/PTP(6)
Renin(8)
Retinoid Receptor(37)
SCD(6)
Steroid Sulfatase (STS)(2)
Thioredoxin(1)
TPH(5)
Transferase(37)
Vitamin(44)
Xanthine Oxidase (XAO)(11)
Cathepsin
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N-CBZ-Phe-Arg-AMC
产品货号 : M29712
cas no: 65147-22-0
N-CBZ-Phe-Arg-AMC (Z-FR-AMC) is a substrate for serine proteases, including cathepsins, kallikrein and plasmin.Absorption/emission of substrate = 330/390 nm (weak fluorescence); absorption/emission of end product (AMC) = 342/441 nm (strong fluorescence). -
Aloxistatin
产品货号 : M16402
cas no: 88321-09-9
一种不可逆的膜渗透性溶酶体和胞质半胱氨酸蛋白酶抑制剂,能够抑制完整血小板中的钙蛋白酶活性。 -
ONO-5334
产品货号 : M16307
cas no: 868273-90-9
一种有效、选择性、口服活性的组织蛋白酶 K 抑制剂,对人、兔和大鼠组织蛋白酶 K 的 Ki 值分别为 0.1 nM、0.049 nM 和 0.85 nM。 -
Odanacatib
产品货号 : M15252
cas no: 603139-19-1
一种有效、选择性、可逆且具有口服活性的组织蛋白酶 K 抑制剂,IC50 为 0.2 nM。 -
L 873724
产品货号 : M15251
cas no: 603139-12-4
L 873724 是一种有效的选择性非碱性组织蛋白酶 K 抑制剂,IC50 为 0.2 nM。