Search Result
Results for "
Protease Inhibitors
" in MedChemExpress (MCE) Product Catalog:
4
Biochemical Assay Reagents
27
Isotope-Labeled Compounds
Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
-
- HY-155691
-
|
HIV Protease
|
Infection
|
HIV-1 protease-IN-12 (compound 35b) is a HIV-1 protease inhibitor with an IC50 of 0.51 nM. HIV-1 protease-IN-12 also inhibits drug-resistant variant .
|
-
-
- HY-125148
-
|
HIV Protease
|
Infection
|
AQ148 is a HIV-1 protease inhibitor (Ki=137 nM). The IC50 values ??of AQ148 for the inhibition of HIV-1, HIV-2 and SIV aspartic proteases are 1.5 μM, 3.4 μM and 5 μM, respectively .
|
-
-
- HY-146804
-
|
HIV
HIV Protease
|
Infection
|
HIV-1 protease-IN-3 (compound 14) is a potent inhibitor of HIV-1 protease (IC50=71 nM; EC50=0.86 μM) .
|
-
-
- HY-155690
-
|
HIV Protease
|
Infection
|
HIV-1 protease-IN-11 (compound 34a) is a HIV-1 protease inhibitor with an IC50 of 0.41 nM. HIV-1 protease-IN-11 also exhibits significant activity against drug-resistant variant .
|
-
-
- HY-123608
-
|
HIV Protease
|
Infection
|
JE-2178 is an orally available HIV-1 protease inhibitor with IC50 and Ki values are 15 and 0.318 nM respectively. JE-2178 has antiviral activity .
|
-
-
- HY-122453
-
|
HIV Protease
|
Infection
|
Palinavir is a potent human immunodeficiency virus type 1 (HIV-1) and type 2 (HIV-2) protease inhibitor with an IC50 of 0.5-30 nM . Palinavir has antiviral activity .
|
-
-
- HY-150691
-
|
SARS-CoV
|
Cancer
|
SARS 3CLpro-IN-1 (Compound 3b) is a SARS 3CL protease inhibitor with an IC50 value of 95 μM, as a specific stereo isomer
of the octahydroisochromene scaffold, directs the P1 site imidazole .
|
-
-
- HY-161270
-
|
HIV Protease
|
Infection
|
HIV-1 protease-IN-13 (compound 18d) is a potent HIV-1 protease inhibitor with an IC50 value of 0.54 nM. HIV-1 protease-IN-13 also shows potent activity against HIV-1DRVRS (DRV-resistant mutation) and HIV-1NL4_3 variant (wild type) .
|
-
-
- HY-149639
-
|
Virus Protease
|
Infection
|
NS2B-NS3pro-IN-1 is a potent inhibitor of Zika Virus NS2B-NS3 protease, with EC50 of 50 μM, that plays an important role in Zika virus (ZIKV) cycle .
|
-
-
- HY-157778
-
|
SARS-CoV
|
Infection
|
MK-7845 is a reversible covalent SARS-CoV-2 3CL protease inhibitor with an IC50 of 8.7 nM .
|
-
-
- HY-145435
-
|
SARS-CoV
|
Infection
|
SARS-CoV-2-IN-12 (Compound 27) is a potent SARS-CoV-2-related 3C-like protease inhibitor (Ki=32.1 pM) for preventing SARS-CoV-2 viral replication and that could be useful in the research of COVID-19 .
|
-
-
- HY-149640
-
-
-
- HY-158763
-
TG0205221
|
SARS-CoV
Cathepsin
Virus Protease
|
Infection
|
MPI8 (TG0205221) is an inhibitor of the major protease of SARS-CoV-2 (MPro) with high antiviral activity. MPI8 exerts its antiviral effect by dual and selective inhibition of SARS-CoV-2 MPro and host cell cysteine protease L (cathepsin L). This dual inhibition enhanced the overall antiviral potency and effect of MPI8. MPI8 can be used in clinical studies of COVID-19 .
|
-
-
- HY-W790014
-
|
Cathepsin
|
Infection
|
Z-FG-NHO-BzOME is a cysteine protease inhibitor that selectively inhibits cathepsin B, cathepsin L, cathepsin S, and papain .
|
-
-
- HY-144820
-
|
Ser/Thr Protease
|
Infection
|
JO146 is a Chlamydia trachomatis high temperature requirement A (CtHtrA) protease inhibitor with IC50s of 21.86 and 1.15 μM for CtHtrA and human neutrophil elastase (HNE), respectively. JO146 can be used to inhibits bacterial infections .
|
-
-
- HY-161762
-
|
Virus Protease
|
Infection
|
RA-0002034 is a Chikungunya virus (CHIKV) nsP2 protease inhibitor with an IC50 of 58 nM. RA-0002034 covalently modifies the catalytic cysteine in a site-specific manner .
|
-
-
- HY-15899
-
|
HIV Protease
HIV
Drug Metabolite
|
Infection
|
Des(benzylpyridyl) Atazanavir (compound M1) is a N-dealkylation product of Atazanavir (HY-17367) metabolite. Atazanavir is a highly selective HIV-1 protease inhibitor. Des(benzylpyridyl) Atazanavir may contribute to the effectiveness Atazanavir but also to the toxicity and interactions. Des(benzylpyridyl) Atazanavir can be used for further research of Atazanavir effects .
|
-
-
- HY-17541
-
|
Cathepsin
|
Others
|
Cysteine Protease inhibitor is an inhibitor of cysteine protease.
|
-
-
- HY-17541A
-
|
Cathepsin
|
Others
|
Cysteine Protease inhibitor hydrochloride is an inhibitor of cysteine protease.
|
-
-
- HY-124379
-
TPCK
1 Publications Verification
L-1-Tosylamido-2-phenylethyl chloromethyl ketone; L-TPCK
|
Ser/Thr Protease
HPV
Apoptosis
PDK-1
|
Infection
Neurological Disease
Inflammation/Immunology
Cancer
|
TPCK (L-1-Tosylamido-2-phenylethyl chloromethyl ketone; L-TPCK) is an effective serine protease inhibitor and also a blocker of the PDK1/Akt pathway. TPCK can modify the E7 protein in actively keratinocyte cells. TPCK can induce cellular apoptosis, suppress tumor growth, reduce hypoxic-ischemic brain injury in rat pups, and affect vascular permeability in inflamed rats .
|
-
-
- HY-125712
-
|
HIV
HIV Protease
|
Infection
|
CGP 53820 is an inhibitor for HIV protease, inhibits the complex of HIV-1 and HIV-2 protease with Ki of 9 and 53 nM for HIV-1 protease and HIV-2 protease. CGP 53820 can be used in AIDS research .
|
-
-
- HY-18234
-
-
-
- HY-P0018
-
Pepstatin A
|
HIV Protease
Autophagy
|
Infection
Inflammation/Immunology
|
Pepstatin (Pepstatin A) is a specific, orally active aspartic protease inhibitor produced by actinomycetes, with IC50s of 4.5 nM, 6.2 nM, 150 nM, 290 nM, 520 nM and 260 nM for hemoglobin-pepsin, hemoglobin-proctase, casein-pepsin, casein-proctase, casein-acid protease and hemoglobin-acid protease, respectively. Pepstatin also inhibits HIV protease .
|
-
-
- HY-P0018A
-
Pepstatin A Trifluoroacetate
|
HIV Protease
Autophagy
|
Infection
Inflammation/Immunology
|
Pepstatin (Pepstatin A) Trifluoroacetate is a specific, orally active aspartic protease inhibitor produced by actinomycetes, with IC50s of 4.5 nM, 6.2 nM, 150 nM, 290 nM, 520 nM and 260 nM for hemoglobin-pepsin, hemoglobin-proctase, casein-pepsin, casein-proctase, casein-acid protease and hemoglobin-acid protease, respectively. Pepstatin Trifluoroacetate also inhibits HIV protease .
|
-
-
- HY-P0018C
-
Pepstatin A acetate
|
HIV Protease
Autophagy
|
Infection
Inflammation/Immunology
|
Pepstatin (Pepstatin A) acetate is a specific, orally active aspartic protease inhibitor produced by actinomycetes, with IC50s of 4.5 nM, 6.2 nM, 150 nM, 290 nM, 520 nM and 260 nM for hemoglobin-pepsin, hemoglobin-proctase, casein-pepsin, casein-proctase, casein-acid protease and hemoglobin-acid protease, respectively. Pepstatin acetate also inhibits HIV protease .
|
-
-
- HY-155054
-
|
Parasite
|
Infection
|
Cysteine protease inhibitor-3 (Compound 15) is a Cysteine protease inhibitor. Cysteine protease inhibitor-3 inhibits Pf3D7, PfW2, PfFP2 and PfFP3 with IC50s of 0.74 μM, 1.05 μM, 3.5 μM, and 4.9 μM, respectively. Cysteine protease inhibitor-3 has anti-plasmodial efficacy against both drug-sensitive and drug-resistant parasites .
|
-
-
- HY-101877
-
(3S,4S)-Statine; (S,S)-Statine
|
Others
|
Endocrinology
|
Statine is an unusual amino acid that occurs twice in the sequence of pepstatin, a protease inhibitor that is active against pepsin and other acid proteases.
|
-
-
- HY-P0018B
-
Pepstatin A Ammonium
|
HIV Protease
Autophagy
|
Infection
Inflammation/Immunology
|
Pepstatin (Pepstatin A) Ammonium is a specific, orally active aspartic protease inhibitor produced by actinomycetes, with IC50s of 4.5 nM, 6.2 nM, 150 nM, 290 nM, 520 nM and 260 nM for hemoglobin-pepsin, hemoglobin-proctase, casein-pepsin, casein-proctase, casein-acid protease and hemoglobin-acid protease, respectively. Pepstatin Ammonium also inhibits HIV protease .
|
-
-
- HY-169012
-
-
-
- HY-18234A
-
-
-
- HY-130366
-
|
Others
|
Others
|
JG-365 is an HIV-1 protease inhibitor that binds to the active site of HIV-1 protease.
|
-
-
- HY-P4243
-
|
Ser/Thr Protease
|
Others
|
Dansyl-Glu-Gly-Arg-Chloromethylketone is a protease inhibitor, and inhibits serine/threonine proteases. Dansyl-Glu-Gly-Arg-Chloromethylketone inhibits activated porcine factor IX .
|
-
-
- HY-153921
-
|
Dengue virus
|
Infection
|
DEPN-8 is a WNV protease substrate. DEPN-8 is used for dengue virus protease inhibitor development .
|
-
-
- HY-P2502
-
|
HCV Protease
HCV
|
Infection
|
Hepatitis Virus C NS3 Protease Inhibitor 2 is a product-based peptide inhibitor of hepatitis C virus (HCV) NS3 protease, with a Ki of 41 nM .
|
-
-
- HY-P4243A
-
|
Ser/Thr Protease
|
Others
|
Dansyl-Glu-Gly-Arg-Chloromethylketone TFA is a protease inhibitor, and inhibits serine/threonine proteases. Dansyl-Glu-Gly-Arg-Chloromethylketone TFA inhibits activated porcine factor IX .
|
-
-
- HY-123415
-
|
HIV Protease
Renin
|
Infection
|
PD 134922 is a potent renin and HIV-1 protease inhibitor with an IC50 of 15 nM against HIV-1 protease .
|
-
-
- HY-W129596
-
|
Virus Protease
|
Infection
|
Policresulen is a potent inhibitor of DENV2 NS2B/NS3 protease (IC50 of 0.48 μg/mL). Policresulen inhibits DENV2 replication in BHK-21 cells with IC50 of 4.99 μg/mL. Policresulen acts as a competitive inhibitor of the protease, and slightly affects the protease stability .
|
-
-
- HY-155076
-
|
HIV Protease
|
Infection
|
HIV-1 protease-IN-9 (compound 5b) is a HIV-1 protease inhibitor, with a Ki of 0.028 nM. HIV-1 protease-IN-9 shows potent antiviral activity, with an IC50 of 66.8 nM .
|
-
-
- HY-151197
-
|
HIV Protease
|
Infection
|
HIV protease-IN-1 (compound 1·succinate) is a potent HIV protease non-peptidic inhibitor, can be used to research AIDS .
|
-
-
- HY-144646
-
-
-
- HY-106920
-
KNI 272; Kynostatin; NSC 651714
|
HIV Protease
|
Infection
|
Kynostatin 272 (KNI 272) is a potent HIV protease inhibitor. Kynostatin 272 inhibits the activity of the HIV protease by simulating the substrate transition state of the HIV protease, thus preventing a key step in the replication of the HIV virus. Kynostatin 272 provides an important research foundation for the development of drugs for HIV and AIDS .
|
-
-
- HY-168050
-
|
Virus Protease
|
Infection
|
nsP2 Protease-IN-1 is a potent irreversible covalent inhibitor of Chikungunya (CHIKV) nsP2 cysteine protease with an IC50 value of 60 nM. nsP2 Protease-IN-1 demonstrates potent antialphavirus activity, inhibiting CHIKV and VEEV replication with EC50 = 0.01 and 0.3 µM, respectively .
|
-
-
- HY-19236
-
-
-
- HY-159847
-
-
-
- HY-P2054
-
|
HIV Protease
|
Infection
|
Mvt-101 is a hexapeptide-based inhibitor of HIV-1 protease. Mvt-101 is also reduced-peptide-bond inhibitor. Mvt-101 inhibits reproduction of the HIV virus by blocking protease action .
|
-
-
- HY-19101
-
|
Kallikrein
|
Cardiovascular Disease
|
ONO-3307 is a protease inhibitor that competitively inhibits a variety of proteases including trypsin, thrombin, plasma kallikrein, plasmin, pancreatic kallikrein, and chymotrypsin. ONO-3307 alleviates endotoxin-induced experimental disseminated intravascular coagulation (DIC) in rats. ONO-3307 can be used in the study of thrombosis and protease-mediated diseases .
|
-
-
- HY-146888
-
|
HIV Protease
|
Infection
|
HIV-1 protease-IN-2 is a potent HIV-1 protease inhibitor with an IC50 of 2.53 nM. HIV-1 protease-IN-2 shows antiviral activity against DRV (Darunavir)-sensitive or DRV-resistant HIV-1 variants .
|
-
-
- HY-116537
-
-
-
- HY-147650
-
|
HIV Protease
|
Infection
|
HIV-1 protease-IN-5 (Compound 13c) is a HIV-1 protease inhibitor with an IC50 of 1.64 nM. HIV-1 protease-IN-5 shows remarkable activity against wild-type and DRV-resistant HIV-1 variants .
|
-
-
- HY-100227
-
E 64c
2 Publications Verification
|
Cathepsin
SARS-CoV
|
Metabolic Disease
|
E 64c is a derivative of naturally occurring epoxide inhibitor of cysteine proteases, a Calcium-activated neutral protease (CANP) inhibitor and a very weak irreversible cathepsin C inhibitor. E 64c exhibits entry-blocking effect for MERS-CoV.
|
-
- HY-160036
-
|
PCSK9
|
Metabolic Disease
|
PCSK9-IN-22 (compound 29) is an orally active inhibitor of PCSK9. PCSK9-IN-22 inhibits the interaction of the protein with LDLR in vivo .
|
-
- HY-162229
-
|
SARS-CoV
|
Infection
|
GRL-190-21 (compound 5e) is an inhibitor for SARS-Cov-2-Mpro with a Ki of 0.04 nM and exhibits antiviral activity in VeroE6 cells with EC50 of 0.26 μM. GRL-190-21 reduces the infectivity, replication, and cytopathic effect of SARS-CoV-2 without significant toxicity .
|
-
- HY-17041
-
TMC114 Ethanolate
|
HIV
HIV Protease
|
Infection
|
Darunavir ethanolate (TMC114 Ethanolate) is a potent HIV protease inhibitor used to treat and prevent HIV/AIDS. Darunavir has a Ki of 1 nM for wild type HIV-1 protease.
|
-
- HY-136575
-
|
Virus Protease
|
Infection
|
4-Hydroxy-2-methylbenzenesulfonic acid ammonium is an impurity of Policresulen. Policresulen is a potent NS2B/NS3 protease inhibitor with an IC50 of 0.48 μg/mL. Policresulen effectively inhibits the replication of DENV2 virus in BHK-21 cells with an IC50 of 4.99 μg/mL. Policresulen acted as a competitive inhibitor of the protease, and slightly affected the protease stability .
|
-
- HY-136574
-
|
Virus Protease
|
Infection
|
2-Hydroxy-4-methylbenzenesulphonic acid ammonium is an impurity of Policresulen. Policresulen is a potent NS2B/NS3 protease inhibitor with an IC50 of 0.48 μg/mL. Policresulen effectively inhibits the replication of DENV2 virus in BHK-21 cells with an IC50 of 4.99 μg/mL. Policresulen acted as a competitive inhibitor of the protease, and slightly affected the protease stability .
|
-
- HY-134616
-
Uristatin
|
Ser/Thr Protease
Apoptosis
|
Neurological Disease
Inflammation/Immunology
|
Ulinastatin (Uristatin) is a trypsin and serine protease inhibitor. Ulinastatin is the main protein binding inhibitor of various trypsin, chymotrypsin, and various pancreatic proteases. Ulinastatin shows neuroprotective, anti-inflammatory, anti-apoptotic, anti-oxidant effects .
|
-
- HY-G0009
-
Desthiazolylmethyloxycarbonyl Ritonavir
|
Drug Metabolite
|
Infection
|
Ritonavir metabolite is a metabolite of Ritonavir, which is a HIV protease inhibitor.
|
-
- HY-121240
-
-
- HY-169102
-
|
Virus Protease
|
Infection
|
CHIKV nsP2 protease-IN-1(compound J13) is an oral active non-structural protein 2 protease inhibitor with the EC50 of 0.39 μM aganist of CHIKV S27. CHIKV nsP2 protease-IN-1 can be used for study of Chikungunya virus .
|
-
- HY-136573
-
|
Virus Protease
|
Infection
|
5-Hydroxytoluene-2,4-disulphonic acid diammonium is an impurity of Policresulen. Policresulen is a potent NS2B/NS3 protease inhibitor with an IC50 of 0.48 μg/mL. Policresulen effectively inhibits the replication of DENV2 virus in BHK-21 cells with an IC50 of 4.99 μg/mL. Policresulen acted as a competitive inhibitor of the protease, and slightly affected the protease stability .
|
-
- HY-151250
-
|
HIV Protease
|
Infection
|
HIV-1 protease-IN-7 (compound 16) is an orally active HIV-1 protease inhibitor (IC50=3.52 nM, EC50=37 nM) .
|
-
- HY-U00261
-
-
- HY-117747
-
JCR 424; XM 323
|
HIV Protease
|
Infection
|
DMP 323 is a potent, nonpeptide cyclic urea inhibitor of HIV protease, effective against both HIV type 1 and type 2. Designed using structural information and database searching, it competitively inhibits the cleavage of both peptide and HIV-1 gag polyprotein substrates. DMP 323 shows comparable potency to other highly effective HIV protease inhibitors like A-80987 and Ro-31-8959. Importantly, its efficacy against HIV protease remains unaffected by human plasma or serum, suggesting low affinity for plasma proteins. Furthermore, DMP 323 demonstrates minimal inhibition of various mammalian proteases at concentrations much higher than those needed for HIV protease inhibition, highlighting its specificity for viral targets .
|
-
- HY-146012
-
|
HIV
|
Infection
|
HIV-1 protease-IN-4 (Compound II-22) is a potent HIV-1 protease inhibitor. HIV-1 protease-IN-4 is a proagent of atazanavir. HIV-1 protease-IN-4 as a proagent that delivers the parent 1 to rat plasma with a 5-fold higher AUC and 67-fold higher C24 when compared to oral administration of the parent agent .
|
-
- HY-120673
-
-
- HY-144688
-
|
HIV
|
Infection
|
HIV-1 protease-IN-1 (Compound 1e) is a potent inhibitor of HIV-1 protease with an IC50 of 90 pM. HIV-1 protease-IN-1 demonstrates antiviral activity with EC50 value of 89 nM against B-HIV. HIV-1 protease-IN-1 exhibits activity with EC50 value of 13.59 nM against C-HIV strain ZM246. HIV-1 protease-IN-1 shows remarkable activity with EC50 value of 8.23 nM against C-HIV strain Indie [1].
|
-
- HY-150549
-
|
HIV Protease
HIV
|
Infection
Inflammation/Immunology
|
HIV-1 protease-IN-6 (compound 17d) is a potent HIV-1 protease inhibitor, with an IC50 of 21 pM and a Ki of 4.7 pM, respectively. HIV-1 protease-IN-6 exhibits potent antiviral activity to DRV (darunavir)-resistant variant, even more than wild type virus .
|
-
- HY-169166
-
|
HIV Protease
|
Infection
|
HIV-1 protease-IN-14 (compound 5ae) is a potent HIV-1 protease inhibitor with Ki values of 0.28, 56.9 nM for WT HIV-1 PR, R41T HIV-1 PR, respectively. HIV-1 protease-IN-14 shows low cytotoxicity .
|
-
- HY-153045
-
|
Deubiquitinase
|
Cancer
|
BAY-805 is a selective inhibitor of ubiquitin-specific protease USP21. BAY-805 has high selectivity for deubiquitinating enzyme (DUB) targets, kinases, proteases and other common target enzymes .
|
-
- HY-12821
-
-
- HY-126034
-
-
- HY-120812
-
|
HIV Protease
|
Infection
|
HIV-IN-11 is part of the hydroxylaminoglutaramide (HAPA) transition state isomeric series of HIV protease inhibitors and is a potent and selective inhibitor of HIV-1 protease. HIV-IN-11 competitively inhibits HIV-1 PR (Ki: 0.049 nM) and potently inhibits replication of HIV(IIIb)-infected MT4 lymphocytes at concentrations of 25.0-50.0 nM. HIV-IN-11 displays a longer half-life than indinavir sulfate in animal models and serves as a promising second-generation HIV protease inhibitor .
|
-
- HY-120331
-
|
HIV
HIV Protease
|
Infection
|
U-89360E is an inhibitor for HIV-1 protease. U-89360E inhibits the protease of HIV-1 wildtype, V82D mutant and V82N mutant with Ki of 20 nM, 560 nM and 2100 nM, respectively .
|
-
- HY-120757
-
|
Others
|
Others
|
LP-130 is a statin-based inhibitor that is a universal inhibitor with nanomolar inhibitory activity against all tested retroviral proteases. Crystal structure studies of its binding to different retroviral proteases have shown that it can adapt to different active site regions to achieve inhibition.
|
-
- HY-B0689C
-
(threo)-MK-639; (threo)-L735524
|
Others
|
Infection
|
(Threo)-Indinavir is a protease inhibitor that plays an important role in HIV/AIDS suppression. (Threo)-Indinavir is used as a component of highly active antiretroviral suppression. By inhibiting the viral protease, (threo)-Indinavir ((threo)-MK-639) is able to effectively block the replication of the HIV virus .
|
-
- HY-155379
-
|
Virus Protease
|
Infection
|
β-Herpesvirus protease-IN-1 (compound 19) is a β-herpesvirus protease inhibitor with IC50s of 2.5 μM and 0.33 μM for HCMVPro and HHV6Pro, respectively .
|
-
- HY-17003
-
-
- HY-B0496
-
Phenylmethylsulfonyl fluoride; Benzylsulfonyl fluoride
|
Cathepsin
|
Others
|
PMSF is an irreversible serine/cysteine protease inhibitor commonly used in the preparation of cell lysates.
|
-
- HY-N12716
-
-
- HY-121514
-
|
Others
|
Others
|
Talopeptin is a metal protease inhibitor that can be produced by the streptomyces MK-23 .
|
-
- HY-125494
-
SC-55389A
|
HIV
|
Infection
|
Droxinavir (SC-55389A) hydrochloride is an antiviral compound that functions as an HIV protease inhibitor.
|
-
- HY-E70203
-
-
- HY-10300
-
SCH 900518
|
HCV
HCV Protease
SARS-CoV
|
Infection
|
Narlaprevir (SCH 900518) is a selective and orally bioavailable NS3 protease inhibitor with a Ki value of 6 nM and an EC90 value of 40 nM . Narlaprevir also inhibits the HCV nonstructural protein 3 serine protease . Narlaprevir is also a SARS-CoV 3CL pro inhibitor with an IC50 of 2.3 μM .
|
-
- HY-106188
-
|
HIV Protease
|
Infection
|
L 756423 is a potent HIV protease inhibitor. L 756423 has the potential for the research of HIV infection .
|
-
- HY-N2786
-
-
- HY-P1260
-
-
- HY-P4543
-
-
- HY-118057
-
-
- HY-N12384
-
|
SARS-CoV
|
Infection
|
Antcin-B is a potent inhibitor of 3CLPro with high affinity. Antcin-B can be used in study SARS-CoV-2 .
|
-
- HY-108285
-
|
Others
|
Inflammation/Immunology
|
(Rac)-Telmesteine is a protease inhibitor and is thus a suitable enzyme stabilizer extracted from patent WO 2017220302 A1, compound II-1. (Rac)-Telmesteine can be used as an enzyme stabilizer in protease-containing detergents and cleaning agents .
|
-
- HY-19135
-
|
HIV Protease
|
Infection
|
A-77003 is an inhibitor for HIV protease, with IC50 of 0.1 to 0.2 μg/ml, for HIV-1 and HIV-2 protease. A-77003 exhibits high levels of antiretroviral activity and low cytotoxicity in vitro .
|
-
- HY-P1260A
-
-
- HY-120880
-
-
- HY-125551
-
-
- HY-P10657
-
-
- HY-17367
-
BMS-232632
|
HIV
HIV Protease
SARS-CoV
Cytochrome P450
P-glycoprotein
Endogenous Metabolite
|
Infection
Cancer
|
Atazanavir (BMS-232632), a highly selective HIV-1 protease inhibitor, 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) . Atazanavir is also a SARS-CoV 3CL pro inhibitor with an IC50 of 3.49 μM .
|
-
- HY-17367A
-
BMS-232632 sulfate
|
HIV
HIV Protease
SARS-CoV
Cytochrome P450
P-glycoprotein
Endogenous Metabolite
|
Infection
Cancer
|
Atazanavir (BMS-232632) sulfate, a highly selective HIV-1 protease inhibitor, is the first protease inhibitor approved for once-daily administration . Atazanavir sulfate is a substrate and inhibitor of CYP3A4, and an inhibitor and inducer of P-glycoprotein (P-gp) . Atazanavir sulfate is also a SARS-CoV 3CL pro inhibitor with an IC50 of
3.49 μM .
|
-
- HY-126973
-
|
HCV Protease
|
Infection
|
BI-1230 is potent and digit nanomolar inhibitor of HCV NS3 protease and of viral replication. BI-1230 is also highly selective against other serine/cysteine proteases. BI-1230 shows good Pharmacokinetic(PK) activity .
|
-
- HY-19232
-
|
HIV Protease
|
Inflammation/Immunology
|
R-87366 is a water-soluble human immunodeficiency virus (HIV) protease inhibitor. R-87366 has potent inhibitory for HIV protease with a Ki value of 11 nM. R-87366 can be used for the research of anti-human immunodeficiency virus (HIV) .
|
-
- HY-152200
-
|
HIV Protease
Reverse Transcriptase
|
Infection
Inflammation/Immunology
|
HIV-1 inhibitor-53 is a dual HIV-1 protease and reverse transcriptase inhibitor. HIV-1 inhibitor-53 inhibits HIV-1 protease (PR) and reverse transcriptase (RT) activity with IC50 values of 1.93 nM and 2.35 μM, respectively. HIV-1 inhibitor-53 can be used for the research of acquired immune deficiency syndrome (AIDS) .
|
-
- HY-15148
-
PNU-140690
|
HIV Protease
HIV
SARS-CoV
|
Infection
|
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 . Tipranavir inhibits SARS-CoV-2 3CL pro activity .
|
-
- HY-15282
-
-
- HY-N2360
-
|
E1/E2/E3 Enzyme
Apoptosis
MMP
ClpP
|
Infection
Inflammation/Immunology
Cancer
|
Hinokiflavone is a novel modulator of pre-mRNA splicing activity extracted from plants with anti-inflammatory, anti-tumor and antiviral activities. Hinokiflavone is also a potent inhibitor for matrix metalloproteinases (MMPs). Hinokiflavone attenuates the virulence of Methicillin (HY-121544)-resistant staphylococcus aureus by inhibiting caseinolytic protease P (ClpP) with an IC50 value of 34.36 mg/mL. Hinokiflavone induces apoptosis via the reactive oxygen species-mitochondria-mediated apoptotic pathway and inhibits tumor cell migration and invasion. Hinokiflavone is a SUMO protease inhibitor against sentrin-specific protease 1 (SENP1) activity .
|
-
- HY-17540
-
|
Deubiquitinase
|
Cancer
|
HBX 19818 is a specific inhibitor of ubiquitin-specific protease 7 (USP7), with an IC50 of 28.1 μM.
|
-
- HY-10242
-
BILN 2061; BILN 2061ZW
|
HCV
HCV Protease
|
Infection
|
Ciluprevir(BILN 2061) is a specific and potent peptidomimetic inhibitor of the HCV NS3 protease with an IC50 of 3.0 nM.
|
-
- HY-145349
-
-
- HY-137565
-
|
Drug Metabolite
|
Others
|
Hydroxy ritonavir is a metabolite of Ritonavir. Ritonavir is an inhibitor of HIV protease used to treat HIV infection and AIDS .
|
-
- HY-19194
-
-
- HY-162981
-
|
SARS-CoV
|
Cancer
|
PLpro-IN-7 (compund 83) is a novel papain-like protease (PLpro) inhibitor with IC50 of 3 nM .
|
-
- HY-147020
-
NK01-63
|
SARS-CoV
|
Infection
|
Coronastat is a potent inhibitor of the SARS-CoV-2 3CL protease. The SARS-CoV-2 3CL protease is a critical agent target for small molecule COVID-19, given its likely agentgability and essentiality in the viral maturation and replication cycle .
|
-
- HY-P5062
-
Decanoyl-Arg-Val-Arg-Lys-chloromethylketone
|
Furin
|
Infection
|
DEC-RVRK-CMK (Decanoyl-Arg-Val-Arg-Lys-chloromethylketone) is a peptide-based CMK (chloromethylketone) inhibitor that targets and inactivates the secreted soluble kexin (Kex2) (Ki=8.45 μM). The yeast enzyme Kex2 (kexin, EC 3.4.21.61) is a calcium-dependent transmembrane protease and belongs to the mammalian protease family of the serine protease subtilisin family. The binding mechanism of Kex2 with different CMK inhibitors depends on substrate selectivity, particularly the selective differences between lysine and arginine at the P1 position .
|
-
- HY-13447A
-
-
- HY-13447
-
-
- HY-107468
-
|
HIV Protease
|
Infection
Inflammation/Immunology
|
PL-100 is a potent HIV-1 protease inhibitor with a Ki of 36 pM and an EC50 of 16 nM. PL-100 inhibits viral replication by suppressing HIV-1 protease activity and demonstrates excellent antiviral efficacy against drug-resistant HIV strains. PL-100 can be used in research on drug-resistant HIV disease .
|
-
- HY-149936
-
|
HIV Protease
|
Infection
|
HIV-1 protease-IN-8 (compound 34b) is a potent HIV-1 protease inhibitor with an IC50 value of 0.32 nM. HIV-1 protease-IN-8 displays IC50s of 0.29 μM and 1.90 μM for wild-type HIV-1 (HIV-1NL4-3) and drug-resistant variant (HIV-1MDR), respectively. HIV-1 protease-IN-8 displays robust antiviral activity against both wild-type HIV-1 and drug-resistant variant .
|
-
- HY-P5062A
-
Decanoyl-Arg-Val-Arg-Lys-chloromethylketone TFA
|
Furin
|
Infection
|
DEC-RVRK-CMK (Decanoyl-Arg-Val-Arg-Lys-chloromethylketone) TFA is a peptide-based CMK (chloromethylketone) inhibitor that targets and inactivates the secreted soluble kexin (Kex2) (Ki=8.45 μM). The yeast enzyme Kex2 (kexin, EC 3.4.21.61) is a calcium-dependent transmembrane protease and belongs to the mammalian protease family of the serine protease subtilisin family. The binding mechanism of Kex2 with different CMK inhibitors depends on substrate selectivity, particularly the selective differences between lysine and arginine at the P1 position .
|
-
- HY-162474
-
-
- HY-50736
-
|
Deubiquitinase
|
Cancer
|
DUB-IN-1 is an active inhibitor of ubiquitin-specific proteases (USPs), with an IC50 of 0.85 μM for USP8 .
|
-
- HY-126085
-
(±)-L-Alliin
|
SARS-CoV
|
Infection
|
(±)-Alliin is the main active component of garlic. (±)-Alliin is a putative inhibitor of the main protease of SARS-CoV-2 (Mpro) .
|
-
- HY-N7672
-
|
HCV Protease
|
Infection
|
Isoeuphorbetin, a dimeric coumarin isolated from Viola philippica, is a potent HCV protease inhibitor with an IC50 of 3.63 µg/mL .
|
-
- HY-I0179
-
|
HCV Protease
|
Infection
|
ITMN 4077 is a macrocyclic inhibitor against Hepatitis C Virus (HCV) NS3 protease (EC50: 2131 nM) .
|
-
- HY-154975
-
|
SARS-CoV
|
Others
|
SARS-CoV-2-IN-49 is an irreversible covalent inhibitor of SARS-CoV-2 main protease .
|
-
- HY-120712
-
|
HIV Protease
|
Infection
|
Ro 31-8588 is a HIV protease inhibitor with the Ki of 0.3 nM. Ro 31-8588 can be used for study of AIDS .
|
-
- HY-162984
-
|
SARS-CoV
|
Cancer
|
SARS-CoV-2-IN-99 (compund 58) is a SARS-CoV-2 main protease inhibitor .
|
-
- HY-125571
-
|
HIV Protease
|
Infection
|
A 74704 is a pseudo C2-symmetric inhibitor of HIV-1 protease and its diester analog .
|
-
- HY-17367S3
-
-
- HY-17367S2
-
-
- HY-17367R
-
|
HIV
HIV Protease
SARS-CoV
Cytochrome P450
P-glycoprotein
Endogenous Metabolite
|
Infection
Cancer
|
Atazanavir (Standard) is the analytical standard of Atazanavir. This product is intended for research and analytical applications. Atazanavir (BMS-232632), a highly selective HIV-1 protease inhibitor, 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) . Atazanavir is also a SARS-CoV 3CL pro inhibitor with an IC50 of 3.49 μM .
|
-
- HY-17367AR
-
|
HIV
HIV Protease
SARS-CoV
Cytochrome P450
P-glycoprotein
Endogenous Metabolite
|
Infection
Cancer
|
Atazanavir (sulfate) (Standard) is the analytical standard of Atazanavir (sulfate). This product is intended for research and analytical applications. Atazanavir (BMS-232632) sulfate, a highly selective HIV-1 protease inhibitor, is the first protease inhibitor approved for once-daily administration . Atazanavir sulfate is a substrate and inhibitor of CYP3A4, and an inhibitor and inducer of P-glycoprotein (P-gp) . Atazanavir sulfate is also a SARS-CoV 3CLpro inhibitor with an IC50 of
3.49 μM .
|
-
- HY-144742
-
|
Virus Protease
|
Infection
|
NS2B/NS3-IN-6 (Compound 1a) is an allosteric DENV and ZIKV NS2B/NS3 protease inhibitor with IC50 values of 2.23 µM and 25.2 µM against ZIKV and DENV proteases, respectively .
|
-
- HY-17431
-
GW433908G
|
HIV
Endogenous Metabolite
|
Infection
|
Fosamprenavir Calcium Salt (GW433908G) is a phosphate ester proagent of the antiretroviral protease inhibitor Amprenavir, with improved solubility . Anti-HIV infection .
|
-
- HY-78726
-
Amprenavir phosphate; GW 433908
|
HIV
Endogenous Metabolite
|
Infection
|
Fosamprenavir (Amprenavir phosphate;GW 433908) is a phosphate ester proagent of the antiretroviral protease inhibitor Amprenavir, with improved solubility . Anti-HIV infection .
|
-
- HY-153121
-
RAY1216
|
SARS-CoV
|
Infection
|
Leritrelvir (RAY1216) is an orally active SARS-CoV-2 main protease slow-tight inhibitor with a Ki of 8.6 nM .
|
-
- HY-155130
-
|
Parasite
|
Infection
|
Antimalarial agent 31 (compound 7k) is an orally active Plasmodium falciparum aspartic protease plasmepsin X (PMX) inhibitor .
|
-
- HY-139794
-
|
HIV
|
Infection
|
SDZ283-910 is a potent human immunodeficiency virus type-1 (HIV-1) protease inhibitor .
|
-
- HY-19840
-
GS-9857
|
HCV Protease
|
Infection
Cancer
|
Voxilaprevir (GS-9857) is a noncovalent, reversible inhibitor of HCV NS3/4A protease inhibitor (PI) with pangenotypic antiviral activity . Voxilaprevir inhibits genotype 1b and 3a wild-type NS3 proteases with Ki values of 0.038 nM and 0.066 nM, respectively . Voxilaprevir is an orally active direct-acting antiviral agent (DAA) and can be used for HCV infection research .
|
-
- HY-16511
-
WX-671
|
Ser/Thr Protease
PAI-1
|
Cancer
|
Upamostat (WX-671) is a serine protease inhibitor. Upamostat is the orally available prodrug of the WX-UK1, which is a urokinase plasminogen activator (uPA) inhibitor.
|
-
- HY-B0182
-
-
- HY-150784
-
|
SARS-CoV
|
Infection
|
XR8-89 is a potent papain-like protease (PL pro) inhibitor with an IC50 value of 0.1 μM. XR8-89 induces conformational changes in SARS-COV-2 papain-like protease, inhibiting SARS-CoV-2 replication. XR8-89 can be used for SARS-CoV-2 research .
|
-
- HY-150786
-
|
SARS-CoV
|
Infection
|
PLP_Snyder530 is a potent papain-like protease (PL pro) inhibitor with an IC50 value of 6.4 μM. PLP_Snyder530 induces conformational changes in SARS-COV-2 papain-like protease, inhibiting SARS-CoV-2 replication. PLP_Snyder530 can be used for SARS-CoV-2 research .
|
-
- HY-16121
-
|
Cathepsin
|
Others
|
CAA-0225 is a tissue protease L inhibitor that inhibits rat liver tissue protease L with a IC50 value of 1.9 nM. CAA-0225 can participate in the degradation of autophagosome membrane markers LC3-II and GABARAP (HY-P72639), improve cardiac function in mice with reperfusion injury, and kill and eliminate Trypanosoma brucei parasites [1][2][3].
|
-
- HY-15148R
-
|
HIV Protease
HIV
SARS-CoV
|
Infection
|
Tipranavir (Standard) is the analytical standard of Tipranavir. This product is intended for research and analytical applications. 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 . Tipranavir inhibits SARS-CoV-2 3CL pro activity .
|
-
- HY-15148S1
-
PNU-140690-d7
|
HIV Protease
HIV
SARS-CoV
Isotope-Labeled Compounds
|
Infection
|
Tipranavir-d7 is deuterated labeled Tipranavir (HY-15148). 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 . Tipranavir inhibits SARS-CoV-2 3CL pro activity .
|
-
- HY-19400
-
DPH-153893
|
HIV Protease
HIV
|
Infection
|
DPC-681 is a potent and selective inhibitor of HIV protease with IC90s for wild-type HIV-1 of 4 to 40 nM.
|
-
- HY-112716
-
|
Others
|
Cancer
|
N-alpha-Tosyl-L-lysine chloromethyl ketone (TLCK), a trypsin like protease inhibitor, sensitizes HeLa cells to Fas-mediated cell death.
|
-
- HY-U00346
-
-
- HY-P1436
-
|
HIV
|
Infection
|
Acetyl-pepstatin is a potent classical inhibitor of aspartic proteases (PRs) with XMRV PR and HIV-1 PR Ki values of 712 nM and 13 nM .
|
-
- HY-10243
-
MK-7009
|
HCV
HCV Protease
|
Infection
|
Vaniprevir (MK-7009) is a non-covalent competitive inhibitor of the hepatitis C virus (HCV) NS3/4A protease.
|
-
- HY-139732
-
|
SARS-CoV
|
Infection
|
SARS-CoV-2-IN-8 is a SARS-CoV-2 main protease inhibitor with an IC50 value of 0.75 μM.
|
-
- HY-146649
-
|
Parasite
Cathepsin
|
Infection
|
LmCPB-IN-1 (compound 35) is a potent and reversible covalent Leishmania mexicana cysteine protease B (LmCPB) inhibitor with a pKi of 9.7 .
|
-
- HY-137495
-
|
PAI-1
Ser/Thr Protease
|
Cancer
|
GGACK (H-Glu-Gly-Arg-CMK) is an irreversible substrate-like serine protease urokinase-type plasminogen activator (uPA) inhibitor .
|
-
- HY-168584
-
|
SARS-CoV
|
Infection
|
SARS-CoV-2-IN-102 (example 58) is a SARS-CoV papain-like protease (PLpro) inhibitor with an IC50 <100 nM .
|
-
- HY-17007
-
Ro 31-8959
|
HIV
HIV Protease
SARS-CoV
|
Infection
Cancer
|
Saquinavir(Ro 31-8959) is an HIV Protease inhibitor used in antiretroviral therapy. Saquinavir is also a SARS-CoV 3CL pro inhibitor with an IC50 of 1.36 μM.
|
-
- HY-100212
-
AG1776; KNI-764
|
HIV
HIV Protease
|
Infection
|
JE-2147 (AG1776) is a potent dipeptide protease inhibitor with a Ki of 0.33 nM for HIV-1 protease. JE-2147 has effective activities against a wide spectrum of HIV-1, HIV-2, simian immunodeficiency virus, and various clinical HIV-1 strains in vitro .
|
-
- HY-10235
-
VX-950
|
HCV Protease
HCV
SARS-CoV
|
Infection
|
Telaprevir (VX-950) is a highly selective, reversible, and potent peptidomimetic inhibitor of the HCV NS3-4A protease, the steady-state inhibitory constant (Ki) of Telaprevir is 7 nM against a genotype 1 (H strain) NS3 protease domain plus a NS4A cofactor peptide . Telaprevir inhibits SARS-CoV-2 3CL pro activity .
|
-
- HY-14588
-
ABT-378
|
HIV
HIV Protease
SARS-CoV
|
Infection
Cancer
|
Lopinavir (ABT-378) is a highly potent, selective peptidomimetic inhibitor of the HIV-1 protease, with Kis of 1.3 to 3.6 pM for wild-type and mutant HIV protease. Lopinavir acts by arresting maturation of HIV-1 thereby blocking its infectivity . Lopinavir is also a SARS-CoV 3CL pro inhibitor with an IC50 of 14.2 μM .
|
-
- HY-150783
-
|
SARS-CoV
|
Infection
|
SARS-CoV-2-IN-24 (compound 7) is a potent papain-like protease (PL pro) inhibitor. SARS-CoV-2-IN-24 induces conformational changes in SARS-COV-2 papain-like protease, inhibiting SARS-CoV-2 replication. SARS-CoV-2-IN-24 can be used for SARS-CoV-2 research .
|
-
- HY-118355
-
Calpain inhibitor II
|
Proteasome
Cathepsin
|
Neurological Disease
|
ALLM (Calpain inhibitor II) is a potent inhibitor of calpain and cathepsin proteases. ALLM inhibits neuronal cell death and improves chronic neurological function after spinal cord injury (SCI) .
|
-
- HY-115753
-
|
Proteasome
|
Neurological Disease
|
Calpain Inhibitor-1 (compound 36) is a potent and selective cysteine protease calpain 1 (Cal1) inhibitor (IC50=100 nM; Ki=2.89 μM) .
|
-
- HY-90001
-
-
- HY-163109
-
|
Carbonic Anhydrase
|
Infection
|
Carbonic anhydrase inhibitor 16 (compound 1) is a dengue protease inhibitor with inhibitory activity against carbonic anhydrase hCA I and hCA II (Ki: 28.5 nM, 2.2 nM) .
|
-
- HY-129678
-
|
Others
|
Infection
|
UK-88947 hydrochloride is a protease inhibitor with activity in inhibiting the replication of human immunodeficiency virus HIV-1. UK-88947 hydrochloride can be added to cells before infection to block the early steps of HIV-1 replication. The use of UK-88947 hydrochloride shows its specific inhibitory effect on HIV-1. At the same time, when the virus infects cells, it inhibits the action of viral protease and affects the virus replication process .
|
-
- HY-Y0241
-
|
Cathepsin
|
Metabolic Disease
|
2-Cyanopyrimidine is a potent and non-selective cysteine protease cathepsin K inhibitor with an IC50 of 170 nM. 2-Cyanopyrimidine is used for osteoporos .
|
-
- HY-N8205
-
-
- HY-139866
-
|
SARS-CoV
|
Infection
|
SARS-CoV-2-IN-9 is an inhibitor binding to subsites S1 and S2 in SARS-CoV-2 main protease.
|
-
- HY-147845
-
|
SARS-CoV
|
Infection
|
F8-S40 is an inhibitor of SARS-CoV-2 main protease, with an IC50 of 10.88 μM .
|
-
- HY-16593
-
|
HCV Protease
|
Infection
|
GS-9256 is a selective HCV NS3 protease inhibitor. GS-9256 has good pharmacokinetic properties and antiviral activity .
|
-
- HY-148481
-
|
Deubiquitinase
|
Cancer
|
USP7-IN-10 (compound 1) is a potent ubiquitin-specific protease 7 (USP7) inhibitor, with an IC50 of 13.39 nM .
|
-
- HY-148481A
-
|
Deubiquitinase
|
Cancer
|
USP7-IN-10 hydrochloride (compound 1) is a potent ubiquitin-specific protease 7 (USP7) inhibitor, with an IC50 of 13.39 nM .
|
-
- HY-17367S
-
-
- HY-17367S1
-
-
- HY-161365
-
|
SARS-CoV
|
Infection
|
PLpro-IN-2 (Compound 16) is an inhibitor for SARS-CoV-2 papain-like protease (PLpro), with an IC50 of 0.25 μM .
|
-
- HY-120863
-
|
Virus Protease
|
Infection
|
(Rac)-PD 135390 is a dipeptide and an HIV-1 protease inhibitor with an IC50 of 2 nM. (Rac)-PD 135390 can be utilized in antiviral research .
|
-
- HY-137038
-
TLCK hydrochloride
|
Caspase
Ser/Thr Protease
|
Cancer
|
N-a-Tosyl-L-lysinyl-chloromethylketone hydrochloride (TLCK hydrochloride) is an irreversible inhibitor for serine protease, which inhibits trypsin and trypsin-like protease by alkylating histidine residues in their active site. N-a-Tosyl-L-lysinyl-chloromethylketone hydrochloride inhibits caspase-3, caspase-6 and caspase-7, with IC50s of 12.0, 54.5 and 19.3 μM, respectively. N-a-Tosyl-L-lysinyl-chloromethylketone hydrochloride induces apoptosis in cell HL-60, and inhibits the decrease in mitochondrial transmembrane potential during apoptosis .
|
-
- HY-162471
-
|
Others
|
Cancer
|
GSK_WRN3 is a selective inhibitor of WRN protease (IC50 = 8.6 μM). GSK_WRN3 displays a high degree of selectivity by forming a covalent binding to the Cys727 residue of the WRN protein. GSK_WRN3 reduces growth support for MSI tumor cells by inhibiting WRN protease activity, resulting in increased DNA double-strand breaks and cell growth inhibition .
|
-
- HY-122542
-
|
PAI-1
|
Cardiovascular Disease
|
PPACK is a plasminogen activator (rt-PA) inhibitor. PPACK can inhibit changes in fibrin degradation products, plasminogen and alpha 2-antiplasmin. PPACK also inhibits the binding of rt-PA to plasma protease inhibitors .
|
-
- HY-122542A
-
Pebac; D-Phenylalanyl-prolyl-arginyl Chloromethyl Ketone; D-Phe-Pro-Arg-CH2Cl
|
PAI-1
|
Cardiovascular Disease
|
PPACK dihydrochloride is a plasminogen activator (rt-PA) inhibitor. PPACK dihydrochloride can inhibit changes in fibrin degradation products, plasminogen and alpha 2-antiplasmin. PPACK dihydrochloride also inhibits the binding of rt-PA to plasma protease inhibitors .
|
-
- HY-15667
-
P5091
|
Deubiquitinase
|
Cancer
|
P005091 is a selective and potent inhibitor of ubiquitin-specific protease 7 (USP7) with an EC50 of 4.2 μM.
|
-
- HY-138558
-
-
- HY-120390
-
|
HIV Protease
HIV
|
Infection
|
L 694746 is the metabolite of L-689502 (HY-U00261). L 694746 is an inhibitor for HIV-1 protease with an IC50 of 1 nM and a Ki of 0.34 nM .
|
-
- HY-159655
-
-
- HY-169256
-
|
SARS-CoV
|
Infection
|
ZINC4497834 is an inhibitor of SARS-CoV-2 major protease Mpro. ZINC4497834 can be used in anti-COVID19 research .
|
-
- HY-116815
-
|
Beta-lactamase
Bacterial
|
Infection
Neurological Disease
|
Lalistat 1 is a potent, selective, and competitive inhibitor of lysosomal acid lipase (LAL) and against purified human LAL (phLAL) with an IC50 of 68 nM. Lalistat 1 is a inhibitor of immunoglobulin A1 protease (IgA1P) proteases for H. influenzae, has less effects on other serine hydrolases (trypsin or β-lactamase, etc.). Lalistat 1 can be used for the research of niemann-pick type C (NPC) disease .
|
-
- HY-13865
-
|
Deubiquitinase
|
Cancer
|
P 22077 is a cell-permeable ubiquitin-specific protease 7 (USP7) inhibitor with an EC50 of 8.01 μM. P 22077 also inhibits USP47 with an EC50 of 8.74 μM.
|
-
- HY-33900
-
3-Oxotetrahydrofuran
|
Others
|
Others
|
Dihydrofuran-3(2H)-one (3-Oxotetrahydrofuran) can be used to synthesize cyclic ketone inhibitors that inhibit the serine protease plasmin and increase its inhibitory activity .
|
-
- HY-10241
-
TMC435; TMC435350
|
HCV
HCV Protease
SARS-CoV
DNA/RNA Synthesis
|
Infection
|
Simeprevir (TMC435; TMC435350) is an oral, potent and highly specific hepatitis C virus (HCV) NS3/4A protease inhibitor with a Ki of 0.36 nM. Simeprevir inhibits HCV replication with an EC50 of 7.8 nM. Simeprevir also potently suppresses SARS-CoV-2 replication and synergizes with Remdesivir. Simeprevir inhibits the main protease (M pro) and the RNA-dependent RNA polymerase (RdRp) of SARS-CoV-2, and also modulates host immune responses .
|
-
- HY-10241A
-
TMC435 sodium; TMC435350 sodium
|
HCV
HCV Protease
SARS-CoV
DNA/RNA Synthesis
|
Infection
|
Simeprevir (TMC435; TMC435350) sodium is an oral, potent and highly specific hepatitis C virus (HCV) NS3/4A protease inhibitor with a Ki of 0.36 nM. Simeprevir sodium inhibits HCV replication with an EC50 of 7.8 nM. Simeprevir sodium also potently suppresses SARS-CoV-2 replication and synergizes with Remdesivir. Simeprevir sodium inhibits the main protease (M pro) and the RNA-dependent RNA polymerase (RdRp) of SARS-CoV-2, and also modulates host immune responses .
|
-
- HY-119293
-
K777
1 Publications Verification
|
Cathepsin
CCR
Cytochrome P450
Parasite
SARS-CoV
Filovirus
|
Infection
Cancer
|
K777 is a potent, orally active and irreversible cysteine protease inhibitor. K777 is also a potent CYP3A4 inhibitor with an IC50 of 60 nM and a selective CCR4 antagonist featuring the potent chemotaxis inhibition. K777 irreversibly inhibits Cruzain, the major cysteine protease of Trypansoma cruzi, and cathepsins B and L. K777 is a broad-spectrum antiviral by targeting cathepsin-mediated cell entry. K777 inhibits SARS-CoV and EBOV pseudovirus entry with IC50 values of 0.68 nM and 0.87 nM, respectively .
|
-
- HY-119293A
-
|
Cathepsin
CCR
Cytochrome P450
Parasite
SARS-CoV
Filovirus
|
Infection
Cancer
|
K777 tosylate is a potent, orally active and irreversible cysteine protease inhibitor. K777 tosylate is also a potent CYP3A4 inhibitor with an IC50 of 60 nM and a selective CCR4 antagonist featuring the potent chemotaxis inhibition. K777 tosylate irreversibly inhibits Cruzain, the major cysteine protease of Trypansoma cruzi, and cathepsins B and L. K777 tosylate is a broad-spectrum antiviral by targeting cathepsin-mediated cell entry. K777 tosylate inhibits SARS-CoV and EBOV pseudovirus entry with IC50 values of 0.68 nM and 0.87 nM, respectively .
|
-
- HY-16709
-
|
Deubiquitinase
|
Cancer
|
USP7-IN-1 is a selective and reversible inhibitor of ubiquitin-specific protease 7 (USP7), with an IC50 of 77 μM, and can be used for the research of cancer.
|
-
- HY-125169
-
|
Autophagy
Atg4
|
Cancer
|
NSC 185058 is an inhibitor of ATG4B, a major cysteine protease. Inhibition of ATG4B using NSC 185058 markedly attenuates autophagic activity .
|
-
- HY-N4330
-
|
Ser/Thr Protease
|
Metabolic Disease
|
Rivulariapeptolides 1155 is a potent serine protease inhibitor with IC50s of 41.84, 4.94, 56.54 nM for chymotrypsin, elastase, prpteinase K, respectively .
|
-
- HY-151611
-
-
- HY-148310
-
|
Virus Protease
|
Infection
|
Flaviviruses-IN-2 (compound 78) is a potent flaviviruses inhibitor. Flaviviruses-IN-2 reduces the WNV (West Nile virus) protease activity, with inhibition of 56% .
|
-
- HY-153076
-
|
Virus Protease
|
Infection
|
Flaviviruses-IN-3 (compound 87) is a potent flaviviruse inhibitor. Flaviviruses-IN-3 reduces the WNV (West Nile virus) protease activity, with a inhibition of 54% .
|
-
- HY-156459
-
|
SARS-CoV
|
Infection
|
SARS-CoV-2 Mpro-IN-12 (compound D026) is a SARS-CoV-2 main protease (Mpro) inhibitor with antiviral activities .
|
-
- HY-17003R
-
Ro 31-8959/003 (Standard)
|
HIV
HIV Protease
Autophagy
|
Infection
Cancer
|
Saquinavir (mesylate) (Standard) is the analytical standard of Saquinavir (mesylate). This product is intended for research and analytical applications. Saquinavir Mesylate (Ro 31-8959/003) is an HIV protease inhibitor used in retrovirus research.
|
-
- HY-10235S
-
VX-950-d4
|
Isotope-Labeled Compounds
HCV Protease
HCV
SARS-CoV
|
Infection
|
Telaprevir-d4 is the deuterium labeled Telaprevir. Telaprevir (VX-950) is a highly selective, reversible, and potent peptidomimetic inhibitor of the HCV NS3-4A protease, the steady-state inhibitory constant (Ki) of Telaprevir is 7 nM against a genotype 1 (H strain) NS3 protease domain plus a NS4A cofactor peptide[1][2][3]. Telaprevir inhibits SARS-CoV-2 3CLpro activity[4].
|
-
- HY-B0182R
-
|
Nucleoside Antimetabolite/Analog
SARS-CoV
Virus Protease
FAAH
Ceramidase
Glutathione Peroxidase
|
Infection
Inflammation/Immunology
Cancer
|
Carmofur (Standard) is the analytical standard of Carmofur. This product is intended for research and analytical applications. Carmofur (HCFU) is a rat recombinant acid ceramidase inhibitor with an IC50 of 29 nM. Carmofur is also a protease inhibitor of SARS-CoV-2 main protease (Mpro), fatty acid amide hydrolase (FAAH) and N-acylethanolamine acid amidase (NAAA). Carmofur has anti-cancer, anti-inflammatory and anti-virus activities, and can be used for the study of COVID-19 and acute lung injury (ALI) .
|
-
- HY-144812
-
|
Cathepsin
|
Inflammation/Immunology
Cancer
|
Gü1303 is a potent, reversible, slow-binding cathepsin K (CatK) inhibitor with a Ki of 0.91 nM for mature CatK (mCatK). Gü1303 suppresses the autocatalytic activation of the cathepsin K zymogen .
|
-
- HY-144813
-
|
Cathepsin
|
Inflammation/Immunology
Cancer
|
Gü2602 is a potent, reversible cathepsin K (CatK) inhibitor with a Ki of 0.013 nM for mature CatK (mCatK). Gü2602 suppresses the autocatalytic activation of the cathepsin K zymogen .
|
-
- HY-17542
-
|
SARS-CoV
|
Infection
|
PLpro inhibitor is a potent inhibitor of papain-like protease (PLpro) with an IC50 of 2.6 µM . PLpro inhibitor inhibits SARS-CoV-2 PLpro with an IC50 of 5.0 µM and an EC50 of 21.0 µM .
|
-
- HY-N10076
-
-
- HY-145263
-
|
Ser/Thr Protease
|
Cancer
|
VD2173 is a side chain cyclized macrocyclic peptide inhibitor of HGF-activating serine proteases. VD2173 potently inhibits matriptase and hepsin. VD2173 can be used for the research of lung cancer .
|
-
- HY-100229
-
E64d; E64c ethyl ester
|
Cathepsin
SARS-CoV
|
Neurological Disease
|
Aloxistatin (E64d) is a cell-permeable and irreversible broad-spectrum cysteine protease inhibitor. Aloxistatin (E64d) exhibits entry-blocking effect for MERS-CoV.
|
-
- HY-112818
-
-
- HY-N9366
-
|
Others
|
Inflammation/Immunology
|
Tumulosic acid, a triterpenoid, inhibits KLK5 protease activity (IC50= 14.84 μM). Tumulosic acid suppresses the proteolytic processing of LL-37 in keratinocytes at ≤10 μM .
|
-
- HY-143470
-
|
SARS-CoV
|
Infection
|
SARS-CoV-2-IN-18 (Compound 26) is a potent SARS-CoV-2 3C-like protease inhibitor with an IC50 of 45 nM .
|
-
- HY-143423
-
|
MALT1
|
Cancer
|
MALT1-IN-5 (compound 1) is a potent MALT1 protease inhibitor. MALT1-IN-5 can be used for cancer research .
|
-
- HY-N4331
-
|
Ser/Thr Protease
|
Infection
Cancer
|
Rivulariapeptolides 1185 is a high potent and selective serine protease inhibitor with IC50 values of 13.17 nM, 23.59 nM and 55.26 nM for chymotrypsin, elastase and proteinase K, respectively .
|
-
- HY-N4332
-
|
Ser/Thr Protease
|
Infection
Cancer
|
Rivulariapeptolides 1121 is a high potent and selective serine protease inhibitor with IC50 values of 35.52 nM, 13.24 nM and 48.05 nM for chymotrypsin, elastase and proteinase K, respectively .
|
-
- HY-N4333
-
|
Ser/Thr Protease
|
Infection
Cancer
|
Rivulariapeptolides 988 is a high potent and selective serine protease inhibitor with IC50 values of 95.46 nM, 15.29 nM and 85.50 nM for chymotrypsin, elastase and proteinase K, respectively .
|
-
- HY-122542B
-
|
PAI-1
|
Cardiovascular Disease
|
PPACK TFA is a plasminogen activator (rt-PA) inhibitor. PPACK TFA can inhibit changes in fibrin degradation products, plasminogen and alpha 2-antiplasmin. PPACK TFA also inhibits the binding of rt-PA to plasma protease inhibitors .
|
-
- HY-P4284
-
|
ClpP
Proteasome
|
Others
|
Z-GGF-CMK is a protease inhibitor, inhibits ClpP1P2 and proteasome. Z-GGF-CMK exhibits cytotoxic activity against HepG2 cells with a CC50 value of 125 μM .
|
-
- HY-17430
-
VX-478
|
HIV
HIV Protease
SARS-CoV
|
Infection
Cancer
|
Amprenavir (VX-478) is a HIV protease inhibitor (Ki=0.6 nM) used to treat HIV infection. Amprenavir is also a SARS-CoV 3CL pro inhibitor with an IC50 of 1.09 μM.
|
-
- HY-128971
-
|
Cathepsin
Parasite
|
Infection
Neurological Disease
|
LHVS is a potent, non-selective, irreversible, cell-permeable cysteine protease and cathepsin inhibitor. LHVS decreases actin ring formation. LHVS inhibits T. gondii invasion with an IC50 of 10 μM .
|
-
- HY-156655A
-
STI-1558 sodium
|
SARS-CoV
Cathepsin
|
Infection
|
Olgotrelvir sodium is an orally active dual inhibitor of coronavirus main protease (Mpro) and human cell cathepsin (Cathepsin L). Olgotrelvir sodium can effectively inhibit both SARS-CoV-2 replication and entry into host cells .
|
-
- HY-144736
-
|
Virus Protease
|
Infection
|
NS2B/NS3-IN-4 (Compound 34e) is an allosteric DENV2 and ZIKV NS2B/NS3 protease inhibitor with IC50 values of 0.69 µM and 1.04 µM against DENV2 and ZIKV NS2B/NS3 proteases, respectively .
|
-
- HY-144740
-
|
Virus Protease
|
Infection
|
NS2B/NS3-IN-5 (Compound 25b) is an allosteric DENV2 and ZIKV NS2B/NS3 protease inhibitor with IC50 values of 0.67 µM and 4.38 µM against ZIKV and DENV2 NS2B/NS3 proteases, respectively .
|
-
- HY-B0689S
-
-
- HY-143425
-
|
MALT1
|
Cancer
|
MALT1-IN-7 (compound 142b) is a potent MALT1 protease inhibitor. MALT1-IN-7 has the potential for cancer research .
|
-
- HY-147844
-
|
SARS-CoV
|
Infection
|
F8-S43-S3 is an inhibitor of SARS-CoV-2 main protease, with an IC50 of 9.69 μM .
|
-
- HY-148099
-
|
Deubiquitinase
|
Cancer
|
USP1-IN-2 (Compound I-193) is a potent ubiquitin-specific protease 1 (USP1) inhibitor with an IC50 of less than about 50 nM .
|
-
- HY-144644A
-
-
- HY-100472
-
|
Caspase
|
Cancer
|
ZYZ-488 is a competitive apoptotic protease activating factor-1 (Apaf-1) inhibitor. ZYZ-488 inhibits the activation of binding protein procaspase-9 and procaspase-3 .
|
-
- HY-152222
-
|
SARS-CoV
Cathepsin
|
Infection
|
SPR38 is a potent SARS-CoV-2 main protease inhibitor, with a Ki of 0.260 μM. SPR38 also inhibits hCatL and hCatB, with Ki values of 1.92 μM and 11.1 μM, respectively .
|
-
- HY-14588R
-
ABT-378 (Standard)
|
HIV
HIV Protease
SARS-CoV
|
Infection
Cancer
|
Lopinavir (Standard) is the analytical standard of Lopinavir. This product is intended for research and analytical applications. Lopinavir (ABT-378) is a highly potent, selective peptidomimetic inhibitor of the HIV-1 protease, with Kis of 1.3 to 3.6 pM for wild-type and mutant HIV protease. Lopinavir acts by arresting maturation of HIV-1 thereby blocking its infectivity . Lopinavir is also a SARS-CoV 3CL pro inhibitor with an IC50 of 14.2 μM .
|
-
- HY-14588S2
-
ABT-378-d7
|
HIV
SARS-CoV
HIV Protease
Isotope-Labeled Compounds
|
Infection
Cancer
|
Lopinavir-d7 is deuterated labeled Lopinavir (HY-14588). Lopinavir (ABT-378) is a highly potent, selective peptidomimetic inhibitor of the HIV-1 protease, with Kis of 1.3 to 3.6 pM for wild-type and mutant HIV protease. Lopinavir acts by arresting maturation of HIV-1 thereby blocking its infectivity . Lopinavir is also a SARS-CoV 3CL pro inhibitor with an IC50 of 14.2 μM .
|
-
- HY-P1998
-
|
Others
|
Others
|
Pepsinostreptin is an enzyme inhibitor with the activity of inhibiting pepsin. Pepsinostreptin can form a 1:1 complex with pepsin and significantly inhibit its activity. The activity of pepsinostreptin makes it have important application potential in the study of protease inhibition and related biological processes .
|
-
- HY-139399
-
JNJ-67856633
|
MALT1
|
Cancer
|
Safimaltib (JNJ-67856633) is an orally active, first-in-class, potent, selective and allosteric MALT1 protease inhibitor. Safimaltib in some cases lead to tumor stasis .
|
-
- HY-143425A
-
|
MALT1
|
Cancer
|
(R)-MALT1-IN-7 (compound 142a) is a potent MALT1 protease inhibitor. (R)-MALT1-IN-7 has the potential for cancer research .
|
-
- HY-144644
-
-
- HY-111074
-
MK-0767 analog
|
SARS-CoV
|
Infection
Metabolic Disease
|
DB12055 (MK-0767 analog) is a covalent SARS-CoV-2 3CL protease inhibitor. DB12055 has the potential for the study of dyslipidemia and diabetes mellitus .
|
-
- HY-100397
-
|
Elastase
|
Inflammation/Immunology
|
Elastatinal is a potent and competitive inhibitor of elastase, with a Ki of 0.21 μM. Elastatinal more potently inhibits pancreatic elastase versus leucocyte elastase. Elastatinal shows no activity on human leucocyte chymotrypsin-like protease .
|
-
- HY-10241S
-
TMC435-13C,d3; TMC435350-13C,d3
|
Isotope-Labeled Compounds
HCV
HCV Protease
SARS-CoV
DNA/RNA Synthesis
|
Infection
|
Simeprevir- 13C,d3 is the 13C- and deuterium labeled Simeprevir. Simeprevir is an oral, potent and highly specific hepatitis C virus (HCV) NS3/4A protease inhibitor with a Ki of 0.36 nM. Simeprevir inhibits HCV replication with an EC50 of 7.8 nM. Simeprevir also potently suppresses SARS-CoV-2 replication and synergizes with Remdesivir. Simeprevir inhibits the main protease (Mpro) and the RNA-dependent RNA polymerase (RdRp) of SARS-CoV-2, and also modulates host immune responses[1][2][5].
|
-
- HY-15287
-
AG1341
|
HIV Protease
HIV
|
Infection
Cancer
|
Nelfinavir (AG-1341) is a potent and orally bioavailable HIV-1 protease inhibitor (Ki=2 nM) for HIV infection. Nelfinavir is a broad-spectrum, anticancer agent .
|
-
- HY-136703
-
|
HIV Protease
|
Infection
|
Lopinavir Metabolite M-1, an active metabolite of Lopinavir, inhibits HIV protease with a Ki of 0.7 pM. Lopinavir Metabolite M-1 has antiviral activities in vitro .
|
-
- HY-143216
-
S-217622
|
SARS-CoV
Virus Protease
|
Infection
|
Ensitrelvir (S-217622) is the first orally active non-covalent, non-peptidic, SARS-CoV-2 3CL protease inhibitor (IC50=13 nM) .
|
-
- HY-143216A
-
S-217622 fumarate
|
SARS-CoV
Virus Protease
|
Infection
|
Ensitrelvir (S-217622) fumarate is the first orally active non-covalent, non-peptidic, SARS-CoV-2 3CL protease inhibitor (IC50=13 nM) .
|
-
- HY-143424
-
|
MALT1
|
Cancer
|
MALT1-IN-6 is a potent MALT1 protease inhibitor with a Ki of 9 nM. MALT1-IN-6 has anticancer effects (WO2018226150A1; Compound 4) .
|
-
- HY-150789
-
|
SARS-CoV
|
Infection
|
SARS-CoV-2-IN-23 (compound GRL-0617) is a SARS-COV-2 papain-like protease (PLpro) inhibitor with an IC50 value of 2.3 μM .
|
-
- HY-152009
-
|
SARS-CoV
|
Infection
|
SARS-CoV-2 3CLpro-IN-7 is a reversible covalent SARS-CoV-2 3CL protease inhibitor with an IC50 value of 1.4 µM .
|
-
- HY-157439
-
|
SARS-CoV
|
Infection
|
SARS-CoV-2-IN-72 (compound 12) is a potent allosteric inhibitor of the SARS-COV-2 papain-like protease domain that can trigger the degradation of NSP3 .
|
-
- HY-10756
-
|
Factor Xa
|
Cardiovascular Disease
|
BMS-740808 is a potent, selective and orally active factor Xa inhibitor with a Ki of 30 pM. BMS-740808 shows >1000-fold for factor Xa than other proteases .
|
-
- HY-126046
-
|
ClpP
Bacterial
|
Infection
|
ACP1b is an activator for ClpP protease with Kd of 3.2 μM, and exhibits antibacterial activity. ACP1b inhibits N. meningitidis and H. influenzae with MBC of 16 and 8 μg/mL .
|
-
- HY-126822
-
|
Elastase
|
Others
|
MDL27324 is an inhibitor of neutrophil proteases. MDL27324 can be taken up by the cell and has a modest inhibitory effect on the proteolysis of ingested fluoresceinated immune complexes (200 μM, 20% inhibition) .
|
-
- HY-114080B
-
E-3123 hydrochloride
|
Ser/Thr Protease
|
Inflammation/Immunology
|
Patamostat hydrochloride is a potent protease inhibitor. Patamostat hydrochloride potently inhibits trypsin, plasmin and thrombin with IC50s of 39 nM, 950 nM and 1.9 μM, respectively. Patamostat hydrochloride may possess suppressing effects on pathogenesis and development of acute pancreatitis .
|
-
- HY-P3026
-
|
Others
|
Cancer
|
The Bowman-Birk inhibitor, a highly cross-linked protein featuring seven disulfide bridges, possesses spatially distinct domains specifically designed for the inhibition of both trypsin and chymotrypsin, showcasing its significant role as a plant protease inhibitor with anticarcinogenic properties.
|
-
- HY-13512
-
Camostat mesilate; FOY305; FOY-S980
|
Ser/Thr Protease
SARS-CoV
|
Infection
Inflammation/Immunology
|
Camostat mesylate (Camostat mesilate) is an orally active, synthetic serine protease inhibitor for chronic pancreatitis. Camostat mesylate, an inhibitor of TMPRSS2, shows antiviral activity against SARS-CoV-2. Camostat mesylate also inhibits the activity of prostasin, trypsin, and matriptase .
|
-
- HY-14588S1
-
|
HIV
HIV Protease
SARS-CoV
|
Infection
|
Lopinavir-d8 (ABT-378-d8) is the deuterium labeled Lopinavir. Lopinavir (ABT-378) is a highly potent, selective peptidomimetic inhibitor of the HIV-1 protease, with Kis of 1.3 to 3.6 pM for wild-type and mutant HIV protease. Lopinavir acts by arresting maturation of HIV-1 thereby blocking its infectivity[1][2]. Lopinavir is also a SARS-CoV 3CLpro inhibitor with an IC50 of 14.2 μM[3].
|
-
- HY-17634
-
ABT-493
|
HCV
HCV Protease
SARS-CoV
|
Infection
|
Glecaprevir is a novel HCV NS3/4A protease inhibitor, with IC50 values ranging from 3.5 to 11.3 nM. Glecaprevir is also a SARS-CoV 3CL pro inhibitor with an IC50 of 4.09 μM .
|
-
- HY-17007S
-
-
- HY-127039
-
|
Ser/Thr Protease
DNA/RNA Synthesis
|
Metabolic Disease
Cancer
|
Antipain is a protease inhibitor isolated from Actinomycetes. Antipain inhibits N-methyl-N'-nitro-N-nitrosoguanidine (MNNG)-induced transformation and increases chromosomal aberrations. Antipain restricts uterine DNA synthesis and function in mice .
|
-
- HY-127034
-
|
Ser/Thr Protease
DNA/RNA Synthesis
|
Metabolic Disease
Cancer
|
Antipain dihydrochloride is a protease inhibitor isolated from Actinomycetes. Antipain dihydrochloride inhibits N-methyl-N'-nitro-N-nitrosoguanidine (MNNG)-induced transformation and increases chromosomal aberrations. Antipain dihydrochloride restricts uterine DNA synthesis and function in mice .
|
-
- HY-147031
-