- Inhibitory Selectivity
|Catalog No.||Product Name||Solubility(25°C)|
|S1115||Odanacatib (MK-0822)||<1 mg/mL||100 mg/mL||<1 mg/mL|
|S7379||E-64||11 mg/mL||71 mg/mL||<1 mg/mL|
|S3025||PMSF||<1 mg/mL||35 mg/mL||15 mg/mL|
|S7393||Aloxistatin||<1 mg/mL||68 mg/mL||68 mg/mL|
|S7420||CA-074 methyl ester (CA-074 Me)||79 mg/mL||79 mg/mL||79 mg/mL|
|S3692||N-Ethylmaleimide (NEM)||25 mg/mL||25 mg/mL||25 mg/mL|
|S2847||Cathepsin Inhibitor 1||<1 mg/mL||80 mg/mL||50 mg/mL|
|S7396||Calpeptin||<1 mg/mL||72 mg/mL||72 mg/mL|
|S7386||MG-101 (ALLN)||<1 mg/mL||76 mg/mL||76 mg/mL|
|S7391||Z-FA-FMK||<1 mg/mL||77 mg/mL||34 mg/mL|
|S7380||Leupeptin Hemisulfate||95 mg/mL||95 mg/mL||95 mg/mL|
|S7392||Loxistatin Acid (E-64C)||2 mg/mL||62 mg/mL||62 mg/mL|
|S7424||PD 151746||<1 mg/mL||47 mg/mL||47 mg/mL|
- Cysteine Protease Inhibitors (13)
- New Cysteine Protease Products
|Catalog No.||Information||Product Use Citations||Product Validations|
Odanacatib (MK 0822) is a potent, selective, and neutral inhibitor of cathepsin K (human/rabbit) with IC50 of 0.2 nM/1 nM, and demonstrated high selectivity versus off-target cathepsin B, L, S. Phase 3.
E-64 is an irreversible and selective cysteine protease inhibitor, and also inhibits papain, calpain, and cathepsins B and H, but not serine proteases or aspartic proteases. The IC50 for papain is 9 nM.
PMSF is an irreversible serine/cysteine protease inhibitor.
Aloxistatin is an irreversible and membrane-permeable cysteine protease inhibitor with blood platelet aggregation inhibiting activity.
CA-074 Me is a membrane-permeable derivative of CA-074 and acts as an irreversible cathepsin B inhibitor.
N-Ethylmaleimide (NEM) is an organic compound that is derived from maleic acid. It is an irreversible inhibitor of all cysteine peptidases, with alkylation occurring at the active site thiol group.
Cathepsin Inhibitor 1 is an inhibitor of Cathepsin (L, L2, S, K, B) with pIC50 of 7.9, 6.7, 6.0, 5.5 and 5.2, respectively.
Calpeptin is a potent, cell-permeable calpain inhibitor with ID50 of 52 nM, 34 nM, 138 nM, and 40 nM for Calpain I (porcine erythrocytes), Calpain II (porcine kidney), Papainb, and Calpain I (human platelets), respectively.
Western blotting detection of focal adhesion kinase (FAK) expression and its cleaved fragments with different treatments. DTX represents docetaxel, CPP represents calpeptin (a calpain inhibitor). The experiments were carried out 3 times, obtaining essentially similar results.
MG-101 (ALLN) is a cell-permeable and potent inhibitor of cysteine proteases including calpains and lysosomal cathepsins.
Z-FA-FMK is an irreversible cysteine protease inhibitor, and also inhibits effector caspases.
Leupeptin Hemisulfate is a reversible inhibitor of serine and cysteine proteases. It inhibits cathepsin B (Ki = 6 nM), calpain (Ki = 10 nM), trypsin (Ki = 35 nM), plasmin (Ki = 3.4 μM), and kallikrein (Ki = 19 μM), and has no effect against chymotrypsin, elastase, renin, or pepsin.
Loxistatin Acid (E-64C), a derivative of E-64, is an irreversible and membrane-permeant cysteine protease inhibitor.
PD 151746 is a selective, cell-permeable calpain inhibitor with Ki of 0.26 μM for μ-Calpain, about 20-fold selectivity over m-calpain.
(A) Quantification of mS100a7a15 mRNA expression of skin from normal and imiquimod-induced psoriatic mouse backs at 5 days. (B) Immunoblot of mS100a7a15, IL-1α and calpain-1 in skin extracts from normal and imiquimod-induced psoriatic mouse backs. (C) HE staining and immunohistochemical analysis of mS100a7a15, calpain-1 in skin tissues as described in fig 4A. The scale bars represent 100 μm. All data are representative of three independent experiments with n = 6 and are means ± SEM. P values were determined by two-tailed t test. *** P<0.001.