HIVプロテアーゼ
シグナル伝達経路
研究分野
阻害剤の選択性比較
| カタログ番号 | 製品カタログ | 溶解度(25°C) | ||
|---|---|---|---|---|
| 水 | DMSO | アルコール | ||
| S1030 | Panobinostat (LBH589) | <1 mg/mL | 69 mg/mL | <1 mg/mL |
| S1185 | Ritonavir (ABT-538) | <1 mg/mL | 100 mg/mL | '''3 mg/mL |
| S1380 | Lopinavir (ABT-378) | <1 mg/mL | 126 mg/mL | '126 mg/mL |
| S1457 | Atazanavir (BMS-232632) Sulfate | <1 mg/mL | 104 mg/mL | '<1 mg/mL |
| S1620 | Darunavir Ethanolate | <1 mg/mL | 100 mg/mL | <1 mg/mL |
| S6999 | Chloroquine (NSC-187208) | <1 mg/mL | 64 mg/mL | ''''64 mg/mL |
| S6929 | Dextran sulfate sodium (DSS) | 100 mg/mL | <1 mg/mL | <1 mg/mL |
| S3287 | Rosamultin | -1 mg/mL | 100 mg/mL | -1 mg/mL |
| S1639 | Amprenavir (VX-478) | <1 mg/mL | 16 mg/mL | '100 mg/mL |
| S6625 | Temsavir (BMS-626529) | <1 mg/mL | 95 mg/mL | <1 mg/mL |
| S5250 | Darunavir | <1 mg/mL | 100 mg/mL | 11 mg/mL |
| S9010 | Bevirimat | -1 mg/mL | 100 mg/mL | '-1 mg/mL |
| S6581 | Fosamprenavir calcium salt | <1 mg/mL | 100 mg/mL | 3 mg/mL |
| S2319 | Limonin | <1 mg/mL | 44 mg/mL | <1 mg/mL |
| S4662 | Atazanavir | <1 mg/mL | 71 mg/mL | 32 mg/mL |
| S9567 | Indinavir Sulfate | -1 mg/mL | 100 mg/mL | '-1 mg/mL |
| S4282 | Nelfinavir (AG 1343) Mesylate | <1 mg/mL | 100 mg/mL | ''100 mg/mL |
| S7381 | Pepstatin A | <1 mg/mL | 57 mg/mL | 1 mg/mL |
HIV Protease製品
| 製品コード | 製品説明 | 文献中Selleckの製品使用例 | お客様のフィードバック |
|---|---|---|---|
| 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. |
LSD1 and HDAC inhibitors exhibit synergistic growth inhibition. Cells were simultaneously treated with pargyline or HDAC inhibitors for 48 h.
|
|
| S1185 |
Ritonavir (ABT-538)Ritonavir (ABT-538, A 84538, RTV, Norvir, Norvir Softgel) 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. |
Primary myeloma cells were treated with DMSO or ritonavir for 72 hours before annexin V/DAPI staining. Values are normalized to DMSO-treated samples (n=1 for each
patient sample).
|
|
| S1380 |
Lopinavir (ABT-378)Lopinavir (ABT-378) is a potent HIV protease inhibitor with Ki of 1.3 pM in a cell-free assay. |
Low-micromolar amounts of chloroquine, chlorpromazine, loperamide, and lopinavir inhibit MERS-CoV-induced cytopathology. Huh7 cells in 96-well plates were infected with MERS-CoV isolate EMC/2012 (MOI, 0.005) in the presence of 0 to 20 uM LPV. Cells were incubated for 2 days, and cell viability was monitored using an MTS assay. In addition, the potential toxicity of compound treatment only was monitored in parallel mock-infected Huh7 cell cultures. Graphs show the results (averages and standard deviations [SD]) of a representative experiment that was performed in quadruplicate. All experiments were repeated at least twice. For each compound, the calculated EC50, CC50, and SI values are given.
|
|
| S1457 |
Atazanavir (BMS-232632) SulfateAtazanavir Sulfate (BMS-232632) is a HIV protease inhibitor with Ki of 2.66 nM in a cell-free assay. |
Protease inhibitors induce macroautophagy. JEG3 were seeded on glass chamber slides (1 x 104 cell per chamber; 8-well μ slides; Ibidi, Martinsried, Germany), grown for 24 h under cell culture conditions, and treated for 24 h with 0-10 ug/ml of either lopinavir/ritonavir or atazanavir. Cells were then incubated for 30 min with the blue-green fluorescent autophagy marker monodansylcadaverine and viewed under a fluorescence microscope.
|
|
| S1620 |
Darunavir EthanolateDarunavir Ethanolate (TMC-114, UIC 94017) is a nonpeptidic HIV protease inhibitor, used to treat HIV infection. |
HIV PIs variably alter intracellular HIV epitope stability. (A) HLA-A02–restricted SL9 epitope (SLYNTVATL, aa 77–85 in HIV-1 Gag p17) was degraded in PBMC extracts pretreated with DMSO (control, circles), 5 µM of Nelfinavir (triangles) or 5 µM of Saquinavir (squares). Remaining peptide was quantified by RP-HPLC analysis after 0, 10, 30 and 60 minutes. 100% represents the amount of peptide at time 0 calculated as the surface under the peptide peak detected by RP-HPLC (815.986, 821.569, and 813.118 for DMSO, Saquinavir, and Nelfinavir, respectively). Times at which 50% of the SL9 peptide remained correspond to peptide half-lives (37 min, 52 min and 24 min for Control, Saquinavir and Nelfinavir respectively). (B–F) HLA-A02–SL9, HLA-B57-KF11, HLAB57-ISW9, HLA-B57-TW10 and HLA-A11-ATK9 epitopes (from B to F respectively) were degraded in PBMC extracts pretreated with DMSO, 2 µM or 5 µM PI (Saquinavir, Ritonavir, Nelfinavir, Atazanavir or Darunavir). The cytosolic half-lives in control condition were 33.87, 25.66, 14.83, 119.4 and 37.21 minutes for SL9, KF11, ISW9, TW10 and ATK9 respectively. Fold differences of each epitope half-life upon treatment compared to control are presented in each panel. All data represent the average of 4 different experiments using 4 different PBMC extracts. *P < 0.05, **P < 0.01, ***P < 0.001, 1-way ANOVA with Dunnett’s post-test. |
|
| S6999新 |
Chloroquine (NSC-187208)Chloroquine (NSC-187208, Aralen, CHQ, CQ) 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. |
||
| S6929新 |
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. |
||
| S3287新 |
RosamultinRosamultin 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. |
||
| 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. |
||
| S6625 |
Temsavir (BMS-626529)Temsavir (BMS-626529) is a novel small-molecule HIV-1 attachment inhibitor active against both CCR5- and CXCR4-tropic viruses. |
||
| S5250 |
DarunavirDarunavir (TMC114) is a nonpeptidic HIV protease inhibitor, used to treat HIV infection. |
||
| S9010 |
BevirimatBevirimat (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. |
||
| S6581 |
Fosamprenavir calcium saltFosamprenavir is a pro-drug of the protease inhibitor and antiretroviral drug amprenavir. It is used for the treatment of HIV-1 infections. |
||
| S2319 |
LimoninLimonin is a triterpenoid enriched in citrus fruits, which has antivirus and antitumor ability. |
||
| S4662 |
AtazanavirAtazanavir (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. |
||
| S9567 |
Indinavir SulfateIndinavir 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. |
||
| S4282 |
Nelfinavir (AG 1343) MesylateNelfinavir Mesylate (Viracept, AG1343) is a potent HIV protease inhibitor with Ki of 2 nM. |
||
| S7381 |
Pepstatin APepstatin 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. |
| 製品コード | 製品説明 | 文献中Selleckの製品使用例 | お客様のフィードバック |
|---|---|---|---|
| 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. |
LSD1 and HDAC inhibitors exhibit synergistic growth inhibition. Cells were simultaneously treated with pargyline or HDAC inhibitors for 48 h.
|
|
| S1185 |
Ritonavir (ABT-538)Ritonavir (ABT-538, A 84538, RTV, Norvir, Norvir Softgel) 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. |
Primary myeloma cells were treated with DMSO or ritonavir for 72 hours before annexin V/DAPI staining. Values are normalized to DMSO-treated samples (n=1 for each
patient sample).
|
|
| S1380 |
Lopinavir (ABT-378)Lopinavir (ABT-378) is a potent HIV protease inhibitor with Ki of 1.3 pM in a cell-free assay. |
Low-micromolar amounts of chloroquine, chlorpromazine, loperamide, and lopinavir inhibit MERS-CoV-induced cytopathology. Huh7 cells in 96-well plates were infected with MERS-CoV isolate EMC/2012 (MOI, 0.005) in the presence of 0 to 20 uM LPV. Cells were incubated for 2 days, and cell viability was monitored using an MTS assay. In addition, the potential toxicity of compound treatment only was monitored in parallel mock-infected Huh7 cell cultures. Graphs show the results (averages and standard deviations [SD]) of a representative experiment that was performed in quadruplicate. All experiments were repeated at least twice. For each compound, the calculated EC50, CC50, and SI values are given.
|
|
| S1457 |
Atazanavir (BMS-232632) SulfateAtazanavir Sulfate (BMS-232632) is a HIV protease inhibitor with Ki of 2.66 nM in a cell-free assay. |
Protease inhibitors induce macroautophagy. JEG3 were seeded on glass chamber slides (1 x 104 cell per chamber; 8-well μ slides; Ibidi, Martinsried, Germany), grown for 24 h under cell culture conditions, and treated for 24 h with 0-10 ug/ml of either lopinavir/ritonavir or atazanavir. Cells were then incubated for 30 min with the blue-green fluorescent autophagy marker monodansylcadaverine and viewed under a fluorescence microscope.
|
|
| S1620 |
Darunavir EthanolateDarunavir Ethanolate (TMC-114, UIC 94017) is a nonpeptidic HIV protease inhibitor, used to treat HIV infection. |
HIV PIs variably alter intracellular HIV epitope stability. (A) HLA-A02–restricted SL9 epitope (SLYNTVATL, aa 77–85 in HIV-1 Gag p17) was degraded in PBMC extracts pretreated with DMSO (control, circles), 5 µM of Nelfinavir (triangles) or 5 µM of Saquinavir (squares). Remaining peptide was quantified by RP-HPLC analysis after 0, 10, 30 and 60 minutes. 100% represents the amount of peptide at time 0 calculated as the surface under the peptide peak detected by RP-HPLC (815.986, 821.569, and 813.118 for DMSO, Saquinavir, and Nelfinavir, respectively). Times at which 50% of the SL9 peptide remained correspond to peptide half-lives (37 min, 52 min and 24 min for Control, Saquinavir and Nelfinavir respectively). (B–F) HLA-A02–SL9, HLA-B57-KF11, HLAB57-ISW9, HLA-B57-TW10 and HLA-A11-ATK9 epitopes (from B to F respectively) were degraded in PBMC extracts pretreated with DMSO, 2 µM or 5 µM PI (Saquinavir, Ritonavir, Nelfinavir, Atazanavir or Darunavir). The cytosolic half-lives in control condition were 33.87, 25.66, 14.83, 119.4 and 37.21 minutes for SL9, KF11, ISW9, TW10 and ATK9 respectively. Fold differences of each epitope half-life upon treatment compared to control are presented in each panel. All data represent the average of 4 different experiments using 4 different PBMC extracts. *P < 0.05, **P < 0.01, ***P < 0.001, 1-way ANOVA with Dunnett’s post-test. |
|
| S6999新 |
Chloroquine (NSC-187208)Chloroquine (NSC-187208, Aralen, CHQ, CQ) 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. |
||
| S6929新 |
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. |
||
| S3287新 |
RosamultinRosamultin 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. |
||
| 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. |
||
| S6625 |
Temsavir (BMS-626529)Temsavir (BMS-626529) is a novel small-molecule HIV-1 attachment inhibitor active against both CCR5- and CXCR4-tropic viruses. |
||
| S5250 |
DarunavirDarunavir (TMC114) is a nonpeptidic HIV protease inhibitor, used to treat HIV infection. |
||
| S9010 |
BevirimatBevirimat (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. |
||
| S6581 |
Fosamprenavir calcium saltFosamprenavir is a pro-drug of the protease inhibitor and antiretroviral drug amprenavir. It is used for the treatment of HIV-1 infections. |
||
| S2319 |
LimoninLimonin is a triterpenoid enriched in citrus fruits, which has antivirus and antitumor ability. |
||
| S4662 |
AtazanavirAtazanavir (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. |
||
| S9567 |
Indinavir SulfateIndinavir 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. |
||
| S4282 |
Nelfinavir (AG 1343) MesylateNelfinavir Mesylate (Viracept, AG1343) is a potent HIV protease inhibitor with Ki of 2 nM. |
||
| S7381 |
Pepstatin APepstatin 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. |
