HIV Protease
HIV Protease产品
目录号 | 产品描述 | 文献引用 | 实验数据 |
---|---|---|---|
S1030 |
Panobinostat (LBH589)Panobinostat (LBH589, NVP-LBH589)是一种新型的,广谱HDAC抑制剂,无细胞试验中IC50为5 nM。Panobinostat (LBH589) 可诱导自噬和凋亡。Panobinostat 可以有效地破坏体内 HIV 的潜伏期。Phase 3。 |
![]() ![]() LSD1 and HDAC inhibitors exhibit synergistic growth inhibition. Cells were simultaneously treated with pargyline or HDAC inhibitors for 48 h.
|
|
S1185 |
RitonavirRitonavir (ABT-538, A 84538) 是Cytochrome P450 3A和HIV蛋白酶抑制剂,用于治疗HIV感染和AIDS。抑制Cytochrome P450 2D6, P-Glycoprotein,诱导Cytochrome P450 2C19, Cytochrome P450 1A2, Cytochrome P450 2C9, Cytochrome P450 2B6和UDP Glucuronosyltransferases。Ritonavir 可诱导凋亡。 |
![]() ![]() (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 |
LopinavirLopinavir (ABT-378) 是一种有效的HIV protease抑制剂,无细胞试验中Ki为1.3 pM。 |
![]() ![]() 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 是Plerixafor的盐酸盐,是CXCR4趋化因子受体拮抗剂,作用于CXCR4和CXCL12介导调节的趋化性,IC50分别为44 nM和5.7 nM。Plerixafor 可应用为抗HIV的药物。 |
![]() ![]() 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 SulfateAtazanavir Sulfate (BMS-232632) 是一种HIV protease抑制剂,无细胞试验中Ki值为2.66 nM。 |
![]() ![]() 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.
|
|
S6999New |
ChloroquineChloroquine (Aralen, CHQ, CQ) 是抗疟药和自噬及溶酶体 autophagy/lysosome 的抑制剂。Chloroquine 还可抑制 Toll-like receptor-9 (TLR9) 蛋白的表达。Chloroquine 是非常有效的抗SARS-CoV-2 (COVID-19)侵染剂,在Vero E6细胞中的EC50值为1.13 μM。Chloroquine 也具有抗HIV-1活性。 |
||
S3500New |
Pentosan Polysulfate SodiumPentosan Polysulfate Sodium (PPS, Elmiron) 是一种口服生物可利用的半合成药物,具有抗炎和促软骨形成的特性。Pentosan Polysulfate Sodium 也具有抗 HIV-1 的活性。 |
||
S6929New |
Dextran sulfate sodium (DSS)Dextran sulfate sodium (DSS) 是一种有效的、选择性的 human immunodeficiency virus type 1 (HIV-1) 抑制剂,可抑制病毒吸附到宿主细胞中。 |
||
S3287New |
RosamultinRosamultin 是一种从 Potentilla anserina L. 分离的19 α-hydroxyursane-type三萜,可抑制 HIV-1 protease。Rosamultin 对H2O2诱导的氧化损伤和细胞凋亡具有保护作用。 |
||
S0076New |
ABX464ABX464 (SPL-464)是一种新型的抗HIV的分子,可抑制 HIV-1 的复制,对来自5个不同供体的受刺激的外周血单个核细胞(PBMCs)中的IC50范围为0.1 μM至0.5 μM。 |
||
S1620 |
Darunavir EthanolateDarunavir Ethanolate (TMC-114, UIC 94017)是一种人类免疫缺陷病毒(HIV)蛋白酶抑制剂。 |
![]() ![]() 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 |
AmprenavirAmprenavir (141W94, VX-478, KVX-478) 是一种人类免疫缺陷病毒(HIV)蛋白酶抑制剂,作用于野生型HIV分离株,IC50为14.6 ng/ml。 |
||
S6625 |
Temsavir (BMS-626529)Temsavir (BMS-626529)是一种新型的HIV-1粘附抑制剂。 |
||
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是amprenavir的前体药物。Amprenavir是蛋白酶体抑制剂和抗逆转录病毒药物。Fosamprenavir可用于治疗HIV-1感染。 |
||
S2319 |
LimoninLimonin又称Limonoate D-ring-lactone 和 Limonoic acid di-delta-lactone,化学上属于Furanolactone类化合物。 |
||
S4662 |
AtazanavirAtazanavir (Latazanavir, Zrivada, Reyataz, BMS-232632) 是一种氮杂肽及HIV-蛋白酶抑制剂,常与其他抗HIV药物结合,用于治疗HIV感染以及获得性免疫缺乏综合征。Atazanavir 是 cytochrome P450 isozyme 3A (CYP3A4) 的底物和抑制剂,也是 P-glycoprotein 的抑制剂和诱导剂。 |
||
S9567 |
Indinavir SulfateIndinavir sulfate (Crixivan, L-735524, MK-639)是一种有效的、特异的HIV-1 protease抑制剂,广泛用于艾滋病的治疗。 |
||
S4282 |
Nelfinavir MesylateNelfinavir Mesylate (Viracept, AG1343) 是强效的HIV protease抑制剂,Ki为2 nM。 |
||
S7381 |
Pepstatin APepstatin A (Pepstatin) 是一种强效的aspartic protease抑制剂, 并可抑制HIV的复制。Pepstatin A 也是 cathepsins D 和 cathepsins E 的抑制剂。Pepstatin A 通过抑制溶酶体蛋白酶来抑制自噬。 |
目录号 | 产品描述 | 文献引用 | 实验数据 |
---|---|---|---|
S1030 |
Panobinostat (LBH589)Panobinostat (LBH589, NVP-LBH589)是一种新型的,广谱HDAC抑制剂,无细胞试验中IC50为5 nM。Panobinostat (LBH589) 可诱导自噬和凋亡。Panobinostat 可以有效地破坏体内 HIV 的潜伏期。Phase 3。 |
![]() ![]() LSD1 and HDAC inhibitors exhibit synergistic growth inhibition. Cells were simultaneously treated with pargyline or HDAC inhibitors for 48 h.
|
|
S1185 |
RitonavirRitonavir (ABT-538, A 84538) 是Cytochrome P450 3A和HIV蛋白酶抑制剂,用于治疗HIV感染和AIDS。抑制Cytochrome P450 2D6, P-Glycoprotein,诱导Cytochrome P450 2C19, Cytochrome P450 1A2, Cytochrome P450 2C9, Cytochrome P450 2B6和UDP Glucuronosyltransferases。Ritonavir 可诱导凋亡。 |
![]() ![]() (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 |
LopinavirLopinavir (ABT-378) 是一种有效的HIV protease抑制剂,无细胞试验中Ki为1.3 pM。 |
![]() ![]() 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 是Plerixafor的盐酸盐,是CXCR4趋化因子受体拮抗剂,作用于CXCR4和CXCL12介导调节的趋化性,IC50分别为44 nM和5.7 nM。Plerixafor 可应用为抗HIV的药物。 |
![]() ![]() 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 SulfateAtazanavir Sulfate (BMS-232632) 是一种HIV protease抑制剂,无细胞试验中Ki值为2.66 nM。 |
![]() ![]() 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.
|
|
S6999New |
ChloroquineChloroquine (Aralen, CHQ, CQ) 是抗疟药和自噬及溶酶体 autophagy/lysosome 的抑制剂。Chloroquine 还可抑制 Toll-like receptor-9 (TLR9) 蛋白的表达。Chloroquine 是非常有效的抗SARS-CoV-2 (COVID-19)侵染剂,在Vero E6细胞中的EC50值为1.13 μM。Chloroquine 也具有抗HIV-1活性。 |
||
S3500New |
Pentosan Polysulfate SodiumPentosan Polysulfate Sodium (PPS, Elmiron) 是一种口服生物可利用的半合成药物,具有抗炎和促软骨形成的特性。Pentosan Polysulfate Sodium 也具有抗 HIV-1 的活性。 |
||
S6929New |
Dextran sulfate sodium (DSS)Dextran sulfate sodium (DSS) 是一种有效的、选择性的 human immunodeficiency virus type 1 (HIV-1) 抑制剂,可抑制病毒吸附到宿主细胞中。 |
||
S3287New |
RosamultinRosamultin 是一种从 Potentilla anserina L. 分离的19 α-hydroxyursane-type三萜,可抑制 HIV-1 protease。Rosamultin 对H2O2诱导的氧化损伤和细胞凋亡具有保护作用。 |
||
S0076New |
ABX464ABX464 (SPL-464)是一种新型的抗HIV的分子,可抑制 HIV-1 的复制,对来自5个不同供体的受刺激的外周血单个核细胞(PBMCs)中的IC50范围为0.1 μM至0.5 μM。 |
||
S1620 |
Darunavir EthanolateDarunavir Ethanolate (TMC-114, UIC 94017)是一种人类免疫缺陷病毒(HIV)蛋白酶抑制剂。 |
![]() ![]() 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 |
AmprenavirAmprenavir (141W94, VX-478, KVX-478) 是一种人类免疫缺陷病毒(HIV)蛋白酶抑制剂,作用于野生型HIV分离株,IC50为14.6 ng/ml。 |
||
S6625 |
Temsavir (BMS-626529)Temsavir (BMS-626529)是一种新型的HIV-1粘附抑制剂。 |
||
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是amprenavir的前体药物。Amprenavir是蛋白酶体抑制剂和抗逆转录病毒药物。Fosamprenavir可用于治疗HIV-1感染。 |
||
S2319 |
LimoninLimonin又称Limonoate D-ring-lactone 和 Limonoic acid di-delta-lactone,化学上属于Furanolactone类化合物。 |
||
S4662 |
AtazanavirAtazanavir (Latazanavir, Zrivada, Reyataz, BMS-232632) 是一种氮杂肽及HIV-蛋白酶抑制剂,常与其他抗HIV药物结合,用于治疗HIV感染以及获得性免疫缺乏综合征。Atazanavir 是 cytochrome P450 isozyme 3A (CYP3A4) 的底物和抑制剂,也是 P-glycoprotein 的抑制剂和诱导剂。 |
||
S9567 |
Indinavir SulfateIndinavir sulfate (Crixivan, L-735524, MK-639)是一种有效的、特异的HIV-1 protease抑制剂,广泛用于艾滋病的治疗。 |
||
S4282 |
Nelfinavir MesylateNelfinavir Mesylate (Viracept, AG1343) 是强效的HIV protease抑制剂,Ki为2 nM。 |
||
S7381 |
Pepstatin APepstatin A (Pepstatin) 是一种强效的aspartic protease抑制剂, 并可抑制HIV的复制。Pepstatin A 也是 cathepsins D 和 cathepsins E 的抑制剂。Pepstatin A 通过抑制溶酶体蛋白酶来抑制自噬。 |