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 |
| S3013 | Plerixafor (AMD3100) 8HCl | 100 mg/mL | <1 mg/mL | <1 mg/mL |
| S1457 | Atazanavir (BMS-232632) Sulfate | <1 mg/mL | 104 mg/mL | '<1 mg/mL |
| S6999 | Chloroquine (NSC-187208) | <1 mg/mL | 64 mg/mL | ''''64 mg/mL |
| S3500 | Pentosan Polysulfate Sodium | 100 mg/mL | <1 mg/mL | '<1 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 |
| S1620 | Darunavir Ethanolate | <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 |
| S0076 | ABX464 | <1 mg/mL | 68 mg/mL | 68 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. |
(A) KMS11 and
(B) L363 cells were plated in 5mM glucose medium with ritonavir or DMSO (D) for 17 hours. Glucose consumption rates are normalized to untreated cells (not shown).
(C) KMS11 and (D) L363 cells were treated with ritonavir or DMSO for 72 hours. Relative viable cell numbers were determined by MTS assay and normalized to
untreated cells (not shown).
|
|
| 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.
|
|
| S3013 |
Plerixafor (AMD3100) 8HClPlerixafor (AMD3100, JM 3100) 8HCl is the hydrochloride of Plerixafor, a chemokine receptor antagonist for CXCR4 and CXCL12-mediated chemotaxis with IC50 of 44 nM and 5.7 nM in cell-free assays, respectively. Plerixafor can be used as an anti-HIV agent. |
BLI of NSG mice engrafted with BV173, treated with no therapy (control), plerixafor: 1 mg/kg IP daily, ESKM 100 ug twice weekly, and a combination of ESKM and plerixafor. (A) Logarithmic plot of BLI of leukemia growth measured weekly. Error bars are 5-95% confidence intervals. There was a small but not significant difference between ESKM and combination treated group. (B) End of therapy (day 34) BLI.
|
|
| 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.
|
|
| 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. |
||
| S3500新 |
Pentosan Polysulfate SodiumPentosan Polysulfate Sodium (PPS, Elmiron) is an orally bioavailable, semi-synthetic medication with anti-inflammatory and pro-chondrogenic properties. Pentosan Polysulfate Sodium also exhibits 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. |
||
| 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. |
|
| 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. |
||
| S0076 |
ABX464ABX464 (SPL-464) is a novel anti-HIV molecule that inhibits HIV-1 replication in stimulated peripheral blood mononuclear cells (PBMCs) from 5 different donors with IC50 ranging between 0.1 μM and 0.5 μM. |
||
| 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. |
(A) KMS11 and
(B) L363 cells were plated in 5mM glucose medium with ritonavir or DMSO (D) for 17 hours. Glucose consumption rates are normalized to untreated cells (not shown).
(C) KMS11 and (D) L363 cells were treated with ritonavir or DMSO for 72 hours. Relative viable cell numbers were determined by MTS assay and normalized to
untreated cells (not shown).
|
|
| 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.
|
|
| S3013 |
Plerixafor (AMD3100) 8HClPlerixafor (AMD3100, JM 3100) 8HCl is the hydrochloride of Plerixafor, a chemokine receptor antagonist for CXCR4 and CXCL12-mediated chemotaxis with IC50 of 44 nM and 5.7 nM in cell-free assays, respectively. Plerixafor can be used as an anti-HIV agent. |
BLI of NSG mice engrafted with BV173, treated with no therapy (control), plerixafor: 1 mg/kg IP daily, ESKM 100 ug twice weekly, and a combination of ESKM and plerixafor. (A) Logarithmic plot of BLI of leukemia growth measured weekly. Error bars are 5-95% confidence intervals. There was a small but not significant difference between ESKM and combination treated group. (B) End of therapy (day 34) BLI.
|
|
| 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.
|
|
| 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. |
||
| S3500新 |
Pentosan Polysulfate SodiumPentosan Polysulfate Sodium (PPS, Elmiron) is an orally bioavailable, semi-synthetic medication with anti-inflammatory and pro-chondrogenic properties. Pentosan Polysulfate Sodium also exhibits 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. |
||
| 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. |
|
| 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. |
||
| S0076 |
ABX464ABX464 (SPL-464) is a novel anti-HIV molecule that inhibits HIV-1 replication in stimulated peripheral blood mononuclear cells (PBMCs) from 5 different donors with IC50 ranging between 0.1 μM and 0.5 μM. |
||
| 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. |
