HIV Protease

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HIV Proteaseシグナル伝達経路

HIV Protease製品

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  • HIV Protease阻害剤 (24)
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S1030 Panobinostat (LBH589) Panobinostat (LBH589, NVP-LBH589) is a novel broad-spectrum HDAC inhibitor with IC50 of 5 nM in a cell-free assay. Panobinostat (LBH589) induces autophagy and apoptosis. Panobinostat effectively disrupts HIV latency in vivo. Phase 3.
Cell Rep, 2024, 43(1):113575
Int J Mol Sci, 2024, 25(2)1278
Cancer Res Commun, 2024, 4(2):349-364
S6999 Chloroquine Chloroquine is an antimalarial drug and autophagy/lysosome inhibitor. Chloroquine also suppresses Toll-like receptor-9 (TLR9) protein expression. Chloroquine is highly effective agianst SARS-CoV-2 (COVID-19) infection with EC50 of 1.13 μM in Vero E6 cells. Chloroquine has anti-HIV-1 activity.
Bioact Mater, 2024, 32:277-291
Cancer Lett, 2024, 586:216695
Basic Res Cardiol, 2024, 119(1):113-131
S1380 Lopinavir (ABT-378) Lopinavir (ABT-378) is a potent HIV protease inhibitor with Ki of 1.3 pM in a cell-free assay.
Nat Commun, 2023, 14(1):5034
Nat Commun, 2023, 14(1):5034
Int J Mol Sci, 2023, 24(7)6062
S1185 Ritonavir Ritonavir is a Cytochrome P450 3A and Protease Inhibitor; Also inhibits Cytochrome P450 2D6, P-Glycoprotein and induces Cytochrome P450 2C19, Cytochrome P450 1A2, Cytochrome P450 2C9, Cytochrome P450 2B6 and UDP Glucuronosyltransferases. Ritonavir induces apoptosis.
Cancer Drug Resist, 2024, 7:3
Int. J. Mol. Sci, 2023, 10.3390/ijms24076062
Int J Mol Sci, 2023, 24(7)6062
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.
Anim Nutr, 2024, 20:16:409-421.
Int J Mol Sci, 2023, 24(2)1667
Biosensors (Basel), 2023, 13(7)682
S4282 Nelfinavir Mesylate Nelfinavir Mesylate is a potent HIV protease inhibitor with Ki of 2 nM.
Int J Mol Sci, 2023, 24(7)6062
Int. J. Mol. Sci, 2023, 10.3390/ijms24076062
mBio, 2022, 13(1):e0304421
S1457 Atazanavir (BMS-232632) Sulfate Atazanavir Sulfate (BMS-232632-05, Reyataz) is a HIV protease inhibitor with Ki of 2.66 nM in a cell-free assay.
J Pers Med, 2022, 12(2)258
Hum Cell, 2022, 10.1007/s13577-022-00671-y
Sci Rep, 2021, 11(1):19443
S4662 Atazanavir Atazanavir (Latazanavir, Zrivada, Reyataz, BMS-232632) is an azapeptide and HIV-protease inhibitor that is used in the treatment of HIV infections and AIDS in combination with other anti-HIV agents. Atazanavir is a substrate and inhibitor of cytochrome P450 isozyme 3A (CYP3A4) and an inhibitor and inducer of P-glycoprotein.
Int J Mol Sci, 2022, 23(23)15380
Chemistry, 2022, e202202798.
Sci Rep, 2021, 11(1):19443
S1620 Darunavir Ethanolate Darunavir Ethanolate (TMC-114, UIC 94017) is a nonpeptidic HIV protease inhibitor, used to treat HIV infection.
J Virol, 2022, JVI0173021
J Cell Biochem, 2022, 10.1002/jcb.30213
Sci Rep, 2021, 11(1):19443
S5250 Darunavir Darunavir (TMC114,DRV) is a nonpeptidic HIV protease inhibitor, used to treat HIV infection.
PNAS Nexus, 2024, 3(1):pgad446
Antimicrob Agents Chemother, 2023, 67(7):e0046223
J Cell Biochem, 2022, 10.1002/jcb.30213
S9567 Indinavir Sulfate Indinavir sulfate (Crixivan, L-735524, MK-639) is a specific and potent inhibitor of HIV-1 protease and is widely used in the treatment of AIDS.
Antimicrob Agents Chemother, 2023, 67(7):e0046223
J Cell Biochem, 2022, 10.1002/jcb.30213
Mol Metab, 2020, 29;101027
S1639 Amprenavir (VX-478) Amprenavir (VX-478, 141W94, KVX-478) is a potent PXR-selective agonist, and an HIV protease inhibitor, used to treat HIV.
Nat Commun, 2023, 14(1):5034
Nat Commun, 2023, 14(1):5034
Sci Rep, 2021, 11(1):19443
S2319 Limonin Limonin is a triterpenoid enriched in citrus fruits, which has antivirus and antitumor ability.
Int J Biol Sci, 2019, 15(11):2497-2508
Biomed Pharmacother, 2019, 118:109366
Food Chem Toxicol, 2019, 125:621-628
S6625 Temsavir (BMS-626529) Temsavir (BMS-626529) is a novel small-molecule HIV-1 attachment inhibitor active against both CCR5- and CXCR4-tropic viruses.
J Virol, 2023, 97(10):e0115423
S3494 Vicriviroc maleate Vicriviroc maleate(SCH-417690 maleate,SCH-D maleate) is a potent, selective, oral bioavailable and CNS penetrated antagonist of CCR5, with a Ki of 2.5 nM, and also inhibits HIV-1 in PBMC cells.
Breast Cancer Res, 2021, 23(1):11
S6581 Fosamprenavir calcium salt Fosamprenavir(GW433908G) is a pro-drug of the protease inhibitor and antiretroviral drug amprenavir. It is used for the treatment of HIV-1 infections.
Antimicrob Agents Chemother, 2020, AAC.00872-20
S3287 Rosamultin Rosamultin is a 19 α-hydroxyursane-type triterpenoid isolated from Potentilla anserina L. that inhibits HIV-1 protease. Rosamultin has protective effects on H2O2-induced oxidative damage and apoptosis.
S9010 Bevirimat Bevirimat (MPC-4326, PA-457, YK-FH312), the prototype Human Immunodeficiency Virus type 1 (HIV-1) maturation inhibitor, is highly potent in cell culture and efficacious in HIV-1 infected patients.
S9625 Saquinavir (Ro 31-8959) Saquinavir (Ro 31-8959,SAQ) is a potent and selective inhibitor of HIV proteinase with a mean IC50 of 2.7 nM in JM cells.
S6929 Dextran sulfate sodium (DSS) Dextran sulfate sodium (DSS) is a potent and selective inhibitor of human immunodeficiency virus type 1 (HIV-1) in vitro that inhibits virus adsorption to the host cells.
E0943 NBD-556 NBD-556 is a novel human immunodeficiency virus type 1 (HIV-1) entry inhibitor that block the gp120-CD4 interaction.
S9633New GS-6207 GS-6207 (Lenacapavir) is a HIV-1 capsid inhibitor. It shows anti-HIV activity with an EC50 of 0.1 nM in MT-4 cells.
E4466New Saquinavir Mesylate Saquinavir mesylate (Ro 31-8959/003) is a potent inhibitor of HIV Protease used in antiretroviral therapy. It blocks proteolysis of polyproteins containing either wild-type or single-chain dimer retroviral proteinase (PR).
E1243 Azvudine Azvudine (RO-0622) is a novel nucleoside reverse transcriptase inhibitor with antiviral activity against human immunodeficiency virus (HIV), hepatitis B virus (HBV) and hepatitis C virus (HCV), potently inhibits HIV-1 (EC50 range 0.03 to 6.92 nM) and HIV-2 (EC50s ranging from 0.018 to 0.025 nM).
S1030 Panobinostat (LBH589) Panobinostat (LBH589, NVP-LBH589) is a novel broad-spectrum HDAC inhibitor with IC50 of 5 nM in a cell-free assay. Panobinostat (LBH589) induces autophagy and apoptosis. Panobinostat effectively disrupts HIV latency in vivo. Phase 3.
Cell Rep, 2024, 43(1):113575
Int J Mol Sci, 2024, 25(2)1278
Cancer Res Commun, 2024, 4(2):349-364
S6999 Chloroquine Chloroquine is an antimalarial drug and autophagy/lysosome inhibitor. Chloroquine also suppresses Toll-like receptor-9 (TLR9) protein expression. Chloroquine is highly effective agianst SARS-CoV-2 (COVID-19) infection with EC50 of 1.13 μM in Vero E6 cells. Chloroquine has anti-HIV-1 activity.
Bioact Mater, 2024, 32:277-291
Cancer Lett, 2024, 586:216695
Basic Res Cardiol, 2024, 119(1):113-131
S1380 Lopinavir (ABT-378) Lopinavir (ABT-378) is a potent HIV protease inhibitor with Ki of 1.3 pM in a cell-free assay.
Nat Commun, 2023, 14(1):5034
Nat Commun, 2023, 14(1):5034
Int J Mol Sci, 2023, 24(7)6062
S1185 Ritonavir Ritonavir is a Cytochrome P450 3A and Protease Inhibitor; Also inhibits Cytochrome P450 2D6, P-Glycoprotein and induces Cytochrome P450 2C19, Cytochrome P450 1A2, Cytochrome P450 2C9, Cytochrome P450 2B6 and UDP Glucuronosyltransferases. Ritonavir induces apoptosis.
Cancer Drug Resist, 2024, 7:3
Int. J. Mol. Sci, 2023, 10.3390/ijms24076062
Int J Mol Sci, 2023, 24(7)6062
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.
Anim Nutr, 2024, 20:16:409-421.
Int J Mol Sci, 2023, 24(2)1667
Biosensors (Basel), 2023, 13(7)682
S4282 Nelfinavir Mesylate Nelfinavir Mesylate is a potent HIV protease inhibitor with Ki of 2 nM.
Int J Mol Sci, 2023, 24(7)6062
Int. J. Mol. Sci, 2023, 10.3390/ijms24076062
mBio, 2022, 13(1):e0304421
S1457 Atazanavir (BMS-232632) Sulfate Atazanavir Sulfate (BMS-232632-05, Reyataz) is a HIV protease inhibitor with Ki of 2.66 nM in a cell-free assay.
J Pers Med, 2022, 12(2)258
Hum Cell, 2022, 10.1007/s13577-022-00671-y
Sci Rep, 2021, 11(1):19443
S4662 Atazanavir Atazanavir (Latazanavir, Zrivada, Reyataz, BMS-232632) is an azapeptide and HIV-protease inhibitor that is used in the treatment of HIV infections and AIDS in combination with other anti-HIV agents. Atazanavir is a substrate and inhibitor of cytochrome P450 isozyme 3A (CYP3A4) and an inhibitor and inducer of P-glycoprotein.
Int J Mol Sci, 2022, 23(23)15380
Chemistry, 2022, e202202798.
Sci Rep, 2021, 11(1):19443
S1620 Darunavir Ethanolate Darunavir Ethanolate (TMC-114, UIC 94017) is a nonpeptidic HIV protease inhibitor, used to treat HIV infection.
J Virol, 2022, JVI0173021
J Cell Biochem, 2022, 10.1002/jcb.30213
Sci Rep, 2021, 11(1):19443
S5250 Darunavir Darunavir (TMC114,DRV) is a nonpeptidic HIV protease inhibitor, used to treat HIV infection.
PNAS Nexus, 2024, 3(1):pgad446
Antimicrob Agents Chemother, 2023, 67(7):e0046223
J Cell Biochem, 2022, 10.1002/jcb.30213
S9567 Indinavir Sulfate Indinavir sulfate (Crixivan, L-735524, MK-639) is a specific and potent inhibitor of HIV-1 protease and is widely used in the treatment of AIDS.
Antimicrob Agents Chemother, 2023, 67(7):e0046223
J Cell Biochem, 2022, 10.1002/jcb.30213
Mol Metab, 2020, 29;101027
S1639 Amprenavir (VX-478) Amprenavir (VX-478, 141W94, KVX-478) is a potent PXR-selective agonist, and an HIV protease inhibitor, used to treat HIV.
Nat Commun, 2023, 14(1):5034
Nat Commun, 2023, 14(1):5034
Sci Rep, 2021, 11(1):19443
S2319 Limonin Limonin is a triterpenoid enriched in citrus fruits, which has antivirus and antitumor ability.
Int J Biol Sci, 2019, 15(11):2497-2508
Biomed Pharmacother, 2019, 118:109366
Food Chem Toxicol, 2019, 125:621-628
S6625 Temsavir (BMS-626529) Temsavir (BMS-626529) is a novel small-molecule HIV-1 attachment inhibitor active against both CCR5- and CXCR4-tropic viruses.
J Virol, 2023, 97(10):e0115423
S3494 Vicriviroc maleate Vicriviroc maleate(SCH-417690 maleate,SCH-D maleate) is a potent, selective, oral bioavailable and CNS penetrated antagonist of CCR5, with a Ki of 2.5 nM, and also inhibits HIV-1 in PBMC cells.
Breast Cancer Res, 2021, 23(1):11
S6581 Fosamprenavir calcium salt Fosamprenavir(GW433908G) is a pro-drug of the protease inhibitor and antiretroviral drug amprenavir. It is used for the treatment of HIV-1 infections.
Antimicrob Agents Chemother, 2020, AAC.00872-20
S3287 Rosamultin Rosamultin is a 19 α-hydroxyursane-type triterpenoid isolated from Potentilla anserina L. that inhibits HIV-1 protease. Rosamultin has protective effects on H2O2-induced oxidative damage and apoptosis.
S9010 Bevirimat Bevirimat (MPC-4326, PA-457, YK-FH312), the prototype Human Immunodeficiency Virus type 1 (HIV-1) maturation inhibitor, is highly potent in cell culture and efficacious in HIV-1 infected patients.
S9625 Saquinavir (Ro 31-8959) Saquinavir (Ro 31-8959,SAQ) is a potent and selective inhibitor of HIV proteinase with a mean IC50 of 2.7 nM in JM cells.
S6929 Dextran sulfate sodium (DSS) Dextran sulfate sodium (DSS) is a potent and selective inhibitor of human immunodeficiency virus type 1 (HIV-1) in vitro that inhibits virus adsorption to the host cells.
E0943 NBD-556 NBD-556 is a novel human immunodeficiency virus type 1 (HIV-1) entry inhibitor that block the gp120-CD4 interaction.
S9633New GS-6207 GS-6207 (Lenacapavir) is a HIV-1 capsid inhibitor. It shows anti-HIV activity with an EC50 of 0.1 nM in MT-4 cells.
E4466New Saquinavir Mesylate Saquinavir mesylate (Ro 31-8959/003) is a potent inhibitor of HIV Protease used in antiretroviral therapy. It blocks proteolysis of polyproteins containing either wild-type or single-chain dimer retroviral proteinase (PR).
E1243 Azvudine Azvudine (RO-0622) is a novel nucleoside reverse transcriptase inhibitor with antiviral activity against human immunodeficiency virus (HIV), hepatitis B virus (HBV) and hepatitis C virus (HCV), potently inhibits HIV-1 (EC50 range 0.03 to 6.92 nM) and HIV-2 (EC50s ranging from 0.018 to 0.025 nM).
S9633New GS-6207 GS-6207 (Lenacapavir) is a HIV-1 capsid inhibitor. It shows anti-HIV activity with an EC50 of 0.1 nM in MT-4 cells.
E4466New Saquinavir Mesylate Saquinavir mesylate (Ro 31-8959/003) is a potent inhibitor of HIV Protease used in antiretroviral therapy. It blocks proteolysis of polyproteins containing either wild-type or single-chain dimer retroviral proteinase (PR).

HIV Protease阻害剤の選択性比較

Tags: HIV Protease inhibitor|HIV Protease agonist|HIV Protease activator|HIV Protease inducer|HIV Protease antagonist|HIV Protease signaling pathway|HIV Protease assay kit