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Proteases/Proteasome

Proteasomes are protein complexes inside all eukaryotes and archaea, and in some bacteria. In eukaryotes, proteasomes are located in the nucleus and the cytoplasm. The main function of the proteasome is to degrade unneeded or damaged proteins by proteolysis, a chemical reaction that breaks peptide bonds. Enzymes that help such reactions are called proteases. Proteasomes are part of a major mechanism by which cells regulate the concentration of particular proteins and degrade misfolded proteins. The degradation process yields peptides of about seven to eight amino acids long, which can then be further degraded into shorter amino acid sequences and used in synthesizing new proteins. Proteins are tagged for degradation with a small protein called ubiquitin. The tagging reaction is catalyzed by enzymes called ubiquitin ligases. Once a protein is tagged with a single ubiquitin molecule, this is a signal to other ligases to attach additional ubiquitin molecules. The result is a polyubiquitin chain that is bound by the proteasome, allowing it to degrade the tagged protein. NF-

Products for Proteases/Proteasome

Cat.No. Product Name Information
BCC1991 Tegobuvir Tegobuvir is a specific, covalent inhibitor of the HCV NS5B polymerase.
BCC5547 TZ9 TZ9 is a novel inhibitor of Rad6 ubiquitin conjugating enzyme(E2 enzyme); inhibits MDA-MB-231 cell proliferation with IC50 of ~6 uM.
BCC2366 PK 44 phosphate
BCC2108 VX-222 (VCH-222, Lomibuvir) VX-222 (VCH-222) is a novel, potent and selective inhibitor of HCV polymerase with IC50 of 0.94-1.2 μM, 15.3-fold less effective for mutant M423T, and 108-fold less effective for mutant I482L.
BCC2015 Trelagliptin succinate Trelagliptin succinate (SYR-472 succinate) is a long acting dipeptidyl peptidase-4 (DPP-4) inhibitor that is being developed for the treatment of type 2 diabetes (T2D).
BCC1217 Leupeptin, Microbial Leupeptin hemisulfate is a membrane-permeable thiolprotease inhibitor that inhibits Cathepsin B, Cathepsin H and Cathepsin L, and also impairs amphisome-lysosome fusion. Leupeptin hemisulfate also exhibits anti-inflammatory effect.
BCC3888 GSK744 (S/GSK1265744) Cabotegravir is a potent HIV integrase inhibitor as an oral lead-in tablet and long-acting injectable for the treatment and prevention of HIV infection. Cabotegravir is an inhibitor of OAT1 (IC50 0.81 μM) and OAT3 (IC50 0.41 μM).
BCC2138 S/GSK1349572 Dolutegravir (S/GSK1349572) is a highly potent and orally bioavailable HIV integrase strand transfer inhibitor with an IC50 of 2.7 nM for HIV-1 integrase-catalyzed strand transfer. Dolutegravir (S/GSK1349572) inhibits HIV-1 viral replication with an IC50 of 0.51 nM in peripheral blood mononuclear cells. Dolutegravir retains a high potency against the HIV-1 Y143R, N155H, and G140S/Q148H mutants (EC50=3.6-5.8 nM).
BCC6407 GSK1349572 sodiuM salt Dolutegravir sodium (S/GSK1349572 sodium) is a highly potent and orally bioavailable HIV integrase strand transfer inhibitor with an IC50 of 2.7 nM for HIV-1 integrase-catalyzed strand transfer. Dolutegravir sodium (S/GSK1349572 sodium) inhibits HIV-1 viral replication with an IC50 of 0.51 nM in peripheral blood mononuclear cells. Dolutegravir sodium (S/GSK1349572 sodium) retains a high potency against the HIV-1 Y143R, N155H, and G140S/Q148H mutants (EC50=3.6-5.8 nM).
BCC3772 Doxycycline HCl Doxycycline hydrochloride, an antibiotic, is an orally active and broad-spectrum metalloproteinase (MMP) inhibitor.
BCC1584 gamma-secretase modulator 2 gamma-secretase modulator 2 is a potent and selective γ-secretase modulator for treatment of Alzheimer's disease.
BCC1233 Calpain Inhibitor I, ALLN MG-101 is a potent inhibitor of cysteine proteases which inhibits calpain I, calpain II, cathepsin B and cathepsin L with Kis of 190, 220, 150 and 500 pM, respectively.
BCC2358 Ac-IEPD-AFC Ac-IEPD-AFC (IEPD) is a substrate of Granzyme B.
BCC2104 BMS-708163 (Avagacestat) Avagacestat (BMS-708163) is a potent inhibitor of γ-secretase, with IC50s of 0.27 nM and 0.30 nM for Aβ42 and Aβ40 inhibition; Avagacestat (BMS-708163) also inhibits NICD (Notch IntraCellular Domain) with IC50 of 0.84 nM and shows weak inhibition of CYP2C19, with IC50 of 20 μM.
BCC5531 BI 224436 BI 224436 is a novel HIV-1 noncatalytic site integrase inhibitor with EC50 values of less than 15 nM against different HIV-1 laboratory strains.
BCC6073 RETF-4NA
BCC1583 gamma-secretase modulator 1 γ-secretase inhibitior-1 is a gamma-secretase modulator, γ-secretase inhibitior-1 is useful for Alzheimer's disease.
BCC2351 Calpeptin Calpeptin is a potent, cell penetrating calpain inhibitor, with an ID50 of 40 nM for Calpain I in human platelets. Calpeptin is also an inhibitor of cathepsin K.
BCC2102 LY2811376 LY2811376 is the first orally available non-peptidic β-secretase (BACE1) inhibitor with IC50 of 239 nM-249 nM, that acts to decrease Aβ secretion with EC50 of 300 nM, and demonstrates to have 10-fold selectivity towards BACE1 over BACE2, and more than 50-fold inhibition over other aspartic proteases including cathepsin D, pepsin, or renin.
BCC1764 MK-5172 potassium salt Grazoprevir potassium salt (MK-5172 potassium salt) is a selective inhibitor of Hepatitis C virus NS3/4a protease with broad activity across genotypes and resistant variants, with Kis of 0.01 nM (gt1b), 0.01 nM (gt1a), 0.08 nM (gt2a), 0.15 nM (gt2b), 0.90 nM (gt3a), respectively.
BCC2533 Daclatasvir (BMS-790052)
BCC6417 MK3102 Omarigliptin(MK-3102) is a potent, selective and long-acting DPP-4 inhibitor with IC50 of 1.6 nM; highly selective over all proteases tested (IC50 > 67 μM).
BCC1545 Edoxaban tosylate monohydrate Edoxaban tosylate monohydrate (DU-176b monohydrate) is a selective, potent and orally active factor Xa (FXa) inhibitor with Kis of 0.561 nM and 2.98 nM for free FXa and prothrombinase, respectively. Edoxaban tosylate monohydrate is an anticoagulant agent and can be used for stroke prevention. Edoxaban tosylate monohydrate is a also weak inhibitor of thrombin and factor IXaβ (FIXa), with Kis of 6.00 μM and 41.7 μM, respectively, exhibits >10 000-fold selectivity for FXa. Edoxaban tosylate monohydrate has antithrombotic properties and has potential for thromboembolic diseases treatment.
BCC2350 Acetyl-Calpastatin (184-210) (human) Selective calpain inhibitor
BCC3616 P 22077 P 22077 is a cell-permeable ubiquitin-specific protease 7 (USP7) inhibitor with an EC50 of 8.01 μM. It also inhibits USP47 with an EC50 of 8.74 μM.
BCC4113 USP7-USP47 inhibitor USP7/USP47 inhibitor is a selective ubiquitin-specific protease 7/47 (USP7/USP47) inhibitor, with EC50s of 0.42 μM and 1.0 μM, respectively.
BCC7981 TC-E 5006
BCC1921 Saquinavir Saquinavir(Ro 31-8959) is an HIV Protease inhibitor used in antiretroviral therapy.
BCC1421 Bivalirudin Trifluoroacetate Bivalirudin, a peptide anticoagulant, is a direct thrombin inhibitor for anticoagulation in the setting of invasive cardiology, particularly percutaneous coronary intervention.
BCC1223 Batimastat (BB-94) Batimastat is a potent broad spectrum MMP inhibitor with IC50 of 3, 4, 4, 6, and 20 nM for MMP-1, MMP-2, MMP-9, MMP-7 and MMP-3, respectively.
BCC2075 Batimastat sodium salt Batimastat sodium salt is a potent broad spectrum MMP inhibitor with IC50 of 3, 4, 4, 6, and 20 nM for MMP-1, MMP-2, MMP-9, MMP-7 and MMP-3, respectively.
BCC1141 CA 074 CA-074 is a potent inhibitor of cathepsin B with a Ki of 2 to 5 nM.
BCC1763 MK-5172 hydrate Grazoprevir hydrate (MK-5172 hydrate) is a selective inhibitor of Hepatitis C virus NS3/4a protease with broad activity across genotypes and resistant variants, with Kis of 0.01 nM (gt1b), 0.01 nM (gt1a), 0.08 nM (gt2a), 0.15 nM (gt2b), 0.90 nM (gt3a), respectively.
BCC1762 MK-5172 Grazoprevir (MK-5172) is a selective inhibitor of Hepatitis C virus NS3/4a protease with broad activity across genotypes and resistant variants, with Kis of 0.01 nM (gt1b), 0.01 nM (gt1a), 0.08 nM (gt2a), 0.15 nM (gt2b), 0.90 nM (gt3a), respectively.
BCC1234 Calpain Inhibitor II, ALLM Cathepsin inhibitor,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.
BCC2349 Spinorphin Enkephalin-degrading and ACE inhibitor
BCC1455 Cathepsin S inhibitor LY 3000328 is a potent and selective Cathepsin S (Cat S) inhibitor with IC50s of 7.7 and 1.67 nM for hCat S and mCat S, respectively.
BCC5453 PI-1840 PI-1840 is a potent and selective inhibitor for chymotrypsin-like (CT-L) (IC50 value = 27 ± 0.14 nM) over trypsin-like and peptidylglutamyl peptide hydrolyzing (IC50 values >100 μM) activities of the proteasome.
BCC5537 (±)-BI-D (±)-BI-D is a potent ALLINI(An allosteric IN inhibitor) that binds integrase at the LEDGF/p75 binding site.
BCC2105 LY3039478 Crenigacestat is an orally active Notch and γ-secretase inhibitor, with an IC50 of ∼1nM in most of the tumor cell lines tested.
BCC1765 MK-5172 sodium salt Grazoprevir sodium salt (MK-5172 sodium salt) is a selective inhibitor of Hepatitis C virus NS3/4a protease with broad activity across genotypes and resistant variants, with Kis of 0.01 nM (gt1b), 0.01 nM (gt1a), 0.08 nM (gt2a), 0.15 nM (gt2b), 0.90 nM (gt3a), respectively.
BCC2382 4-Chlorophenylguanidine hydrochloride Urokinase inhibitor
BCC2119 GM 6001 Ilomastat (GM6001) is a potent and broad spectrum matrix metalloprotease (MMP) inhibitor, inhibits MMPs (IC50s, 1.5 nM for MMP-1; 1.1 nM for MMP-2; 1.9 nM for MMP-3; 0.5 nM for MMP-9), with a Ki of 0.4 nM for human skin fibroblast collagenase (MMP-1).
BCC1585 gamma-secretase modulator 3 gamma-secretase modulator 3 is a gamma-secretase modulator.
BCC2143 Olmesartan medoxomil Olmesartan medoxomil is a potent and selective angiotensin AT1 receptor inhibitor with IC50 of 66.2 μM.
BCC5795 Y-29794 oxalate
BCC6241 MKT 077 MKT-077 is a rhodacyanine dye and also a heat shock protein 70 (Hsp70) inhibitor which exhibits significant antitumor activity.
BCC3649 CA-074 Me CA-074 methyl ester is a specific inhibitor of Cathepsin B, which has potent bioactivities such as neuroprotective, anti-cancer, and anti-inflamatory effects.
BCC5922 JMV 390-1
BCC1922 Saquinavir mesylate Saquinavir mesylate is an HIV Protease Inhibitor used in antiretroviral therapy.
BCC5357 Talabostat mesylate Talabostat mesylate (Val-boroPro mesylate; PT100 mesylate) is an orally active and nonselective dipeptidyl peptidase IV (DPP-IV) inhibitor (IC50 < 4 nM; Ki = 0.18 nM) and the first clinical inhibitor of fibroblast activation protein (FAP) (IC50 = 560 nM), inhibits DPP8/9 (IC50 = 4/11 nM; Ki = 1.5/0.76 nM), quiescent cell proline dipeptidase (QPP) (IC50 = 310 nM), DPP2, and some other DASH family enzymes. Antineoplastic and hematopoiesis- stimulating activities.
BCC6030 Decanoyl-RVKR-CMK
BCC2368 Sivelestat sodium salt Sivelestat sodium(ONO5046; LY544349; EI546) is a competitive inhibitor of human neutrophil elastase(IC50 = 44 nM; Ki=200 nM); also inhibited leukocyte elastase obtained from rabbit, rat, hamster and mouse.
BCC2118 Marimastat Marimastat (BB2516) is a broad spectrum and orally bioavailable inhibitor of MMPs, with potent activity against MMP-9 (IC50=3 nM), MMP-1 (IC50=5 nM), MMP-2 (IC50=6 nM), MMP-14 (IC50=9 nM) and MMP-7 (IC50=13 nM), used in the treatment of cancer. Marimastat (BB2516) is an angiogenesis and metastasis inhibitor, which limits the growth and production of blood vessels. As an antimetatstatic agent it prevents malignant cells from breaching the basement membranes.
BCC3620 Ritonavir Ritonavir (ABT 538) is an inhibitor of HIV protease used to treat HIV infection and AIDS.
BCC4313 ML-323 ML-323 is a reversible, potent USP1-UAF1 inhibitor with IC50 of 76 nM in a Ub-Rho assay. The measured inhibition constants of ML-323 for the free enzyme (Ki) is 68 nM.
BCC2088 NSC 632839 hydrochloride NSC632839 is a nonselective isopeptidase inhibitor, which inhibits USP2, USP7, and SENP2 with EC50s of 45±4 μM, 37±1 μM, and 9.8±1.8 μM, respectively.
BCC4138 Nelfinavir Nelfinavir (AG-1341) is a potent and orally bioavailable HIV-1 protease inhibitor (Ki=2 nM) and antiviral agent for the treatment of HIV infection. Nelfinavir is a broad-spectrum, anticancer agent.
BCC1794 Nelfinavir Mesylate Nelfinavir Mesylate (AG 1343 Mesylate) is a potent and orally bioavailable HIV-1 protease inhibitor (Ki=2 nM) and antiviral agent for the treatment of HIV infection. Nelfinavir Mesylate (AG 1343 Mesylate) is a broad-spectrum, anticancer agent.
BCC3619 Amprenavir (agenerase) Amprenavir (VX-478) is a HIV protease inhibitor(Ki=0.6 nM) used to treat HIV infection.
BCC6523 VR23 VR23 is a small molecule that potently inhibits the activities of trypsin-like proteasomes (IC50=1 nM), chymotrypsin-like proteasomes (IC50=50-100 nM), and caspase-like proteasomes (IC50=3 μM).
BCC2354 PMPA (NAALADase inhibitor) 2-PMPA is a potent and selective inhibitor of glutamate carboxypeptidase II (GCPII) with an IC50 of 300 pM.
BCC2341 Compound W
BCC2002 Tipranavir Tipranavir (PNU-140690) inhibits the enzymatic activity and dimerization of HIV-1 protease, exerts potent activity against multi-protease inhibitor (PI)-resistant HIV-1 isolates with IC50s of 66-410 nM.
BCC2353 PD 150606 PD 150606 is a selective, cell-permeable non-peptide calpain inhibitor with Ki values of 0.21 μM and 0.37 μM for μ- and m-calpains respectively, which is neuroprotective.
BCC7020 Butabindide oxalate
BCC2377 Ro 32-3555 Cipemastat is a potent, competitive inhibitor of human collagenases 1, 2 and 3 with Kis of 3.0, 4.4 and 3.4 nM, respectively.
BCC3972 C527 C527 is a is a pan DUB enzyme inhibitor, with a high potency for the USP1/UAF1 complex (IC50=0.88 μM).
BCC3621 Lopinavir Lopinavir is a potent HIV protease inhibitor with Ki of 1.3 pM.
BCC6382 Ximelagatran Ximelagatran (H 376/95) is an orally active thrombin inhibitor that selectively and competitively inhibits both free and clot-bound thrombin. Ximelagatran is an anticoagulant agent with a rapid onset of anticoagulant effect, predictable, dose-dependent pharmcokinetics and pharmacodynamics.
BCC1502 CTS-1027 CTS-1027 is a potent small molecule inhibitor of MMPs, with IC50s of 0.3 nM, 0.5 nM for MMP2, MMP13, respectively, and has > 1,000 fold selectivity over MMP1.
BCC1827 Otamixaban Otamixaban(FXV673) is a potent (Ki = 0.5 nM), selective, rapid acting, competitive and reversible fXa inhibitor that effectively inhibits both free and prothrombinase-bound fXa.
BCC5394 GW311616 hydrochloride GW-311616 is a potent, orally bioavailable, long duration and selective human neutrophil elastase (HNE) inhibitor with IC50 value of 22 nM and Ki value of 0.31 nM.
BCC5393 GW311616 GW-311616 is a potent, orally bioavailable, long duration and selective human neutrophil elastase (HNE) inhibitor with IC50 value of 22 nM and Ki value of 0.31 nM.
BCC3622 Atazanavir Atazanavir (BMS-232632) is a highly selective HIV-1 protease inhibitor for the treatment of HIV infection, and is the first protease inhibitor approved for once-daily administration. Atazanavir (BMS-232632) is a substrate and inhibitor of CYP3A4, and an inhibitor and inducer of P-glycoprotein (P-gp).
BCC2376 PD 166793 Broad spectrum MMP inhibitor
BCC3623 Darunavir Darunavir(TMC114) is an HIV protease inhibitor.
BCC2100 YO-01027 (Dibenzazepine, DBZ) YO-01027 (Dibenzazepine;DBZ) is a potent γ-secretase inhibitor with IC50 values of 2.92 and 2.64 nM for Notch and APPL cleavage, respectively.
BCC2101 LY-411575 LY-411575 is a potent γ-secretase inhibitor with IC50 of 0.078 nM/0.082 nM (membrane/cell-based), and also inhibits Notch S3 cleavage with IC50 of 0.39 nM.
BCC5443 LY-411575 isomer 1 LY-411575 isomer 1 is an isomer of LY411575, which is a potent γ-secretase inhibitor.
BCC2103 LY-900009
BCC2373 CP 471474
BCC2139 BIBR 953 (Dabigatran, Pradaxa) Dabigatran (BIBR 953), an oral anticoagulant, is a reversible, potent, competitive direct thrombin inhibitor (Ki=4.5 nM). Dabigatran (BIBR 953) also inhibits thrombin-induced platelet aggregation (IC50=10 nM).
BCC3738 BIBR-1048 Dabigatran etexilate (BIBR 1048) is an orally active prodrug of Dabigatran. Dabigatran etexilate has anticoagulant effects and is used for the prophylaxis of venousthromboembolism and stroke due to atrial fibrillation.
BCC1413 BCX 1470 BCX 1470 inhibits the esterolytic activity of factor D (IC50=96 nM) and C1s (IC50=1.6 nM), 3.4- and 200-fold better, respectively, than that of trypsin.
BCC1414 BCX 1470 methanesulfonate BCX 1470 methanesulfonate inhibits the esterolytic activity of factor D (IC50=96 nM) and C1s (IC50=1.6 nM), 3.4- and 200-fold better, respectively, than that of trypsin.
BCC6399 KNK437 KNK437 is a HSP inhibitor, and inhibits the induction of HSP105, HSP70, and HSP40.
BCC2375 ONO 4817 Broad spectrum MMP inhibitor
BCC3909 Bestatin trifluoroacetate Bestatin trifluoroacetate is an inhibitor of CD13 (Aminopeptidase N)/APN and leukotriene A4 hydrolase, used for cancer treatment.
BCC4896 Cathepsin Inhibitor 1 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.
BCC1581 Fosamprenavir Calcium Salt Fosamprenavir Calcium Salt (GW433908G) is a phosphate ester prodrug of the antiretroviral protease inhibitor Amprenavir, with improved solubility. Anti-HIV infection.
BCC2114 Atazanavir sulfate (BMS-232632-05) Atazanavir sulfate (BMS-232632 sulfate) is a highly selective HIV-1 protease inhibitor for the treatment of HIV infection, and is the first protease inhibitor approved for once-daily administration. Atazanavir sulfate (BMS-232632 sulfate) is a substrate and inhibitor of CYP3A4, and an inhibitor and inducer of P-glycoprotein (P-gp).
BCC2378 UK 356618 UK 356618 (Compound 4j) is a potent and selective inhibitor of matrix metalloprotease-3 (MMP-3) with an IC50 of 5.9 nM. UK 356618 is less potent against MMP-1, MMP-2, MMP-9, MMP-13 and MMP-14 compared with MMP-3.
BCC2379 UK 370106 UK-370106 is a potent and highly selective MMP-3 (IC50 of 23 nM) and MMP-12 (IC50 of 42 nM) inhibitor with >1200-fold higher potency than MMP-1, MMP-2, MMP-9, and MMP-14, and about 100-fold than MMP-13 and MMP-8. UK-370106 potently inhibits cleavage of [3H]-fibronectin by MMP-3 (IC50 of 320 nM) and has little effect on keratinocyte migration in vitro.
BCC2347 Fumagillin Fumagillin(NSC9168) is a complex biomolecule and used as an antimicrobial agent. Fumagillin can inhibits HIV‐1 infection through the inhibition of HIV-1 viral protein R (Vpr) activity.
BCC2309 Tosedostat (CHR2797) Tosedostat is an aminopeptidase inhibitor.
BCC2365 NVP DPP 728 dihydrochloride
BCC7995 2-MPPA
BCC2374 GI 254023X GI254023X is a potent MMP9 and ADAM10 inhibitor with IC50s of 2.5 and 5.3 nM, respectively.
BCC5916 CGS 35066