Cysteine Protease Inhibitors
| Cat.No. | Product Name | Information | Product Use Citations | Product Validations |
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| S7424 | PD 151746 | 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. |
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| S7392 | Loxistatin Acid (E-64C) | Loxistatin Acid (E-64C, NSC 694279, EP 475), a derivative of E-64, is an irreversible and membrane-permeant cysteine protease inhibitor. This compound inhibits cathepsin L, a cysteine protease required for SARS-CoV-2 viral entry. |
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| E2886 | LY3000328 | LY 3000328 (Z-FL-COCHO, Compound 5) is a potent and selective Cathepsin S (Cat S) inhibitor with IC50s of 7.7 and 1.67 nM for human Cat S and mouse Cat S, respectively. |
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| S7395New | PD 150606 | PD 150606 is a potent and selective inhibitor of calpainwith Ki values of 0.21 µM for µ-calpain and 0.37 µM for m-calpain. It exhibits neuroprotective effects by reducing hypoxic/hypoglycemic injury in cerebrocortical neurons and excitotoxic damage in cerebellar Purkinje cells. |
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| S0722 | Cruzain-IN-1 | Cruzain-IN-1 is a selective inhibitor of trypanosomal cysteine proteases and a covalent and reversible Cruzain inhibitor with an IC50 of 10 nM. | ||
| P1157 | Z-FY-CHO | Z-FY-CHO (Z-Phe-Tyr-CHO) is a potent and specific inhibitor of Cathepsin L (CTSL) that ameliorates cell apoptosis and preserves effective autophagic degradation. | ||
| S0194 | Balicatib | Balicatib (AAE-581) is a potent and selective inhibitor of the osteoclastic enzyme cathepsin K. | ||
| S5611 | 2-cyano-Pyrimidine | 2-cyano-Pyrimidine is a cathepsin K inhibitor with an IC50 of 170 nM. | ||
| E4453 | Cathepsin G Inhibitor I | Cathepsin G Inhibitor I exhibits reversible, competitive cathepsin G inhibition with IC50 and Ki values of 53 nM and 63 nM respectively. It can be used in antigen-processing studies and for modulation of T cell response in situ and in vivo. | ||
| S3012 | Pazopanib | Pazopanib (GW786034) is a novel multi-target inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFR, FGFR, c-Kit and c-Fms/CSF1R with IC50 of 10 nM, 30 nM, 47 nM, 84 nM, 74 nM, 140 nM and 146 nM in cell-free assays, respectively. This compound induces cathepsin B activation and autophagy. |
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| S7420 | CA-074 methyl ester (CA-074 Me) | CA-074 methyl ester (CA-074 Me, Cathepsin B Inhibitor IV) is a membrane-permeable derivative of CA-074 and acts as an irreversible cathepsin B inhibitor. |
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| S7381 | Pepstatin A | Pepstatin A (Pepstatin) is a potent aspartic protease inhibitor, and also inhibits HIV replication. Pepstatin A is also an inhibitor of cathepsins D and cathepsins E. Pepstatin A inhibits Autophagy by suppressing lysosomal proteases. |
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| S7380 | Leupeptin Hemisulfate | 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. |
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| S3025 | PMSF | PMSF (Phenylmethylsulfonyl Fluoride, Benzylsulfonyl fluoride) is an irreversible serine/cysteine protease inhibitor. |
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| S7394 | MDL-28170 | MDL-28170 (Calpain Inhibitor III) is a potent and selective calpain inhibitor of calpain that penetrates the blood-brain barrier and inhibits brain cysteine Protease activity after systemic administration. This compound is also an inhibitor of γ-secretase. |
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| S4591 | Nitroxoline | Nitroxoline (8-Hydroxy-5-nitroquinoline, 5-nitroquinolin-8-ol, 5-Nitro-8-quinolinol, 5-Nitro-8-hydroxyquinoline) is a urinary antibacterial agent active against susceptible gram-positive and gram-negative organisms commonly found in urinary tract infections. This compound impairs tumour progression in vitro and in vivo by inhibiting cathepsin B activity. |
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