HIV

Inhibitory Selectivity

HIV Products

Catalog No. Information Product Use Citations Product Validations
S1009

Dactolisib (BEZ235)

Dactolisib (BEZ235, NVP-BEZ235) is a dual ATP-competitive PI3K and mTOR inhibitor for p110α/γ/δ/β and mTOR(p70S6K) with IC50 of 4 nM /5 nM /7 nM /75 nM /6 nM in cell-free assays, respectively. Inhibits ATR with IC50 of 21 nM in 3T3TopBP1-ER cell. Dactolisib induces autophagy and suppresses HIV-1 replication. Phase 2.

S1208

Doxorubicin (Adriamycin) HCl

Doxorubicin (Adriamycin, NSC 123127, DOX, Hydroxydaunorubicin) HCl is an antibiotic agent that inhibits DNA topoisomerase II and induces DNA damage, mitophagy and apoptosis in tumor cells. Doxorubicin reduces basal phosphorylation of AMPK. Doxorubicin is used in the concomitant treatment of HIV-infected patients but is found to be at high risk of HBV reactivation.

S1230

Flavopiridol (L86-8275)

Flavopiridol (L86-8275, Alvocidib, NSC 649890, HMR-1275) competes with ATP to inhibit CDKs including CDK1, CDK2, CDK4, CDK6, and CDK9 with IC50 values in the 20-100 nM range. It is more selective for CDK1, 2, 4, 6, 9 versus CDK7. Flavopiridol is initially found to inhibit EGFR and PKA. Flavopiridol induces autophagy and ER stress. Flavopiridol blocks HIV-1 replication. Phase 1/2.

S2003

Maraviroc (UK-427857)

Maraviroc (UK-427857) is a CCR5 antagonist for MIP-1α, MIP-1β and RANTES with IC50 of 3.3 nM, 7.2 nM and 5.2 nM in cell-free assays, respectively. Maraviroc is used in the treatment of HIV infection.

S2679

Flavopiridol (L86-8275) HCl

Flavopiridol HCl (L86-8275, NSC 649890, Alvocidib, HMR-1275, DSP-2033) competes with ATP to inhibit CDKs including CDK1, CDK2, CDK4 and CDK6 with IC50 of ~ 40 nM in cell-free assays. It is 7.5-fold more selective for CDK1/2/4/6 than CDK7. Flavopiridol is initially found to inhibit EGFR and PKA. Flavopiridol HCl induces autophagy and ER stress. Flavopiridol HCl blocks HIV-1 replication. Phase 1/2.

E0005New

Enfuvirtide Acetate

Enfuvirtide Acetate (T20 Acetate, DP178 Acetate) is an HIV fusion inhibitor with ic50s of 13.63  nM and 30.21  nM on infection by HIV-1IIIB in MT-2 cells and HIV-1Bal in M7 cells, respectively.

S5979New

2',3'-Dideoxyadenosine

2',3'-Dideoxyadenosine (ddA, ddAdo) is an anti-human immunodeficiency virus agent against human immunodeficiency virus (HIV) and human hepatitis B virus (HBV) replication.

S5959New

Tenofovir Disoproxil

Tenofovir Disoproxil (Bis(POC)-PMPA, GS 4331) is a prodrug of tenofovir, which is metabolised intracellularly to its active anabolite tenofovir diphosphate, a competitive inhibitor of HIV-1 reverse transcriptase and terminates the growing DNA chain.

S4446New

Dimercaprol

Dimercaprol (Bal, 2,3-Dimercapto-1-propanol, Dithioglycerol) is an acrolein scavenger that inhibits HIV-1 tat activity, viral production, and infectivity in vitro.

S3500New

Pentosan Polysulfate Sodium

Pentosan 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.

S1209

Fluorouracil (5-Fluorouracil, 5-FU)

Fluorouracil (5-Fluorouracil, 5-FU, NSC 19893) is a DNA/RNA synthesis inhibitor, which interrupts nucleotide synthetic by inhibiting thymidylate synthase (TS) in tumor cells. Fluorouracil induces apoptosis and can be used in the treatment of HIV.

S1117

Triciribine (NSC 154020)

Triciribine (NSC 154020, VD-0002, vqd-002, API-2, TCN) is a DNA synthesis inhibitor, also inhibits Akt in PC3 cell line and HIV-1 in CEM-SS, H9, H9IIIB, U1 cells with IC50 of 130 nM and 20 nM, respectively; does not inhibit PI3K/PDK1; 5000-fold less active in cells lacking adenosine kinase. Phase 1/2.

S3013

Plerixafor (AMD3100) 8HCl

Plerixafor (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.

S1189

Aprepitant (MK-0869)

Aprepitant (MK-0869, L-754030) is a potent and selective neurokinin-1 receptor antagonist with IC50 of 0.1 nM. Aprepitant reduces levels of pro-inflammatory cytokines including G-CSF, IL-6, IL-8 and TNFα. Aprepitant inhibits HIV infection of human macrophages.

S7015

Birinapant (TL32711)

Birinapant (TL32711) is a SMAC mimetic antagonist, mostly to cIAP1 with Kd of <1 nM in a cell-free assay, less potent to XIAP. Birinapant helps to induce apoptosis in latent HIV-1-infected cells. Phase 2.

S1400

Tenofovir (GS 1278) Disoproxil Fumarate

Tenofovir Disoproxil Fumarate (GS-1278, Tenofovir DF) belongs to a class of antiretroviral drugs, it inhibits the activity of HIV reverse transcriptase by competing with the natural substrate deoxyadenosine 5’-triphosphate and, after incorporation into DNA, by DNA chain termination.

S1704

Emtricitabine (BW 1592)

Emtricitabine (BW1592, FTC) is a new nucleoside agent that has activity against both human immunodeficiency virus (HIV) and hepatitis B virus. It is a reverse transcriptase inhibitor. Intracellular half-life is 39 h.

S8030

Plerixafor (AMD3100)

Plerixafor (AMD3100, JM 3100, SID791) is 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 inhibits human immunodeficiency virus (HIV) replication.

S1896

Hydroxyurea (NSC-32065)

Hydroxyurea (NSC-32065, NCI-C04831, Hydroxycarbamide) is an antineoplastic agent that inhibits DNA synthesis through the inhibition of ribonucleoside diphosphate reductase. Hydroxyurea activates apoptosis and autophagy. Hydroxyurea is used to treat HIV infection.

S1848

Curcumin

Curcumin (Diferuloylmethane, Natural Yellow 3, Turmeric yellow) is the principal curcuminoid of the popular Indian spice turmeric, which is a member of the ginger family (Zingiberaceae). It is an inhibitor of p300 histone acetylatransferase(IC50~25 μM)and Histone deacetylase (HDAC); activates Nrf2 pathway and supresses the activation of NF-κB. Curcumin induces mitophagy, autophagy, apoptosis, and cell cycle arrest with antitumor activity. Curcumin reduces renal damage associated with rhabdomyolysis by decreasing ferroptosis-mediated cell death. Curcumin exhibits anti-infective properties against various human pathogens like the influenza virus, hepatitis C virus, HIV and so on.

S1351

Ivermectin (MK-933)

Ivermectin (MK-933, IVM) is a glutamate-gated chloride channel (GluCls) activator, used as a broad-spectrum antiparasitic drug. Ivermectin (MK-933, IVM) is a specific positive allosteric effector of P2X4 and α7 nicotinic acetylcholine receptors (nAChRs). Ivermectin has potent antiviral activity towards both HIV-1 and dengue virus. Ivermectin induces autophagy through the AKT/mTOR signaling pathway and mitophagy.

S5144

Neferine

Neferine ((R)-1,2-Dimethoxyaporphine), a natural component of Nelumbo nucifera, has antitumor efficiency. Neferine induces apoptosis in renal cancer cells. Neferine prevents autophagy through activation of Akt/mTOR pathway and Nrf2 in muscle cells. Neferine strongly inhibits NF-κB activation. Neferine possesses a number of therapeutic effects such as anti-diabetic, anti-aging, anti-microbial, anti-thrombotic, anti-arrhythmic, anti-inflammatory and even anti-HIV.

S7311

Q-VD-Oph

Q-VD-Oph (Quinoline-Val-Asp-Difluorophenoxymethylketone) is a potent pan-caspase inhibitor with IC50 ranged from 25 to 400 nM for caspases 1,3,8, and 9. Q-VD-OPh can inhibits HIV infection.

S0076

ABX464

ABX464 (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.

S4861

Oxindole

Oxindole (2-indolone, 2-Oxindole, Indolin-2-one) is an aromatic heterocyclic organic compound which causes sedation, muscle weakness, hypotension, and coma when dosed in excess. Oxindole has anti-cancer, anti-HIV, anti-diabetic, antibacterial and other pharmacological activities.

S6676

Ebselen

Ebselen (DR 3305, SPI-1005, PZ-51, CCG-39161) is a small-molecule capsid inhibitor of HIV-1 Replication with IC50 of 46.1 nM in TR-FRET assay.

S6848

3'-Fluoro-3'-deoxythymidine (Alovudine)

3'-Fluoro-3'-deoxythymidine (Alovudine, CL 184824, FddThd, FLT, MIV-310) is a potent inhibitor of polymerase γ and reverse transcriptase that can be used in the treatment of HIV infection. 3'-Fluoro-3'-deoxythymidine (Alovudine) is also a marker of DNA synthesis that can be used as an early response biomarker in the chemotherapy of pancreatic cancer.

S9064

Trilobatin

Trilobatin (P-Phlorizin), a natural flavonoid lipid molecule, is an HIV-1 entry inhibitor targeting the HIV-1 Gp41 envelope and exihibits anti-oxidant and anti-inflammatory effect.

S8512

Cenicriviroc (TAK-652)

Cenicriviroc (CVC, TAK-652, TBR-652) is a potent, orally active dual inhibitor of CC chemokine receptor 2 (CCR2) and CCR5. Cenicriviroc also inhibits HIV-1 and HIV-2 with potent anti-inflammatory and antiinfective activity.

Catalog No. Information Product Use Citations Product Validations
S1009

Dactolisib (BEZ235)

Dactolisib (BEZ235, NVP-BEZ235) is a dual ATP-competitive PI3K and mTOR inhibitor for p110α/γ/δ/β and mTOR(p70S6K) with IC50 of 4 nM /5 nM /7 nM /75 nM /6 nM in cell-free assays, respectively. Inhibits ATR with IC50 of 21 nM in 3T3TopBP1-ER cell. Dactolisib induces autophagy and suppresses HIV-1 replication. Phase 2.

S1208

Doxorubicin (Adriamycin) HCl

Doxorubicin (Adriamycin, NSC 123127, DOX, Hydroxydaunorubicin) HCl is an antibiotic agent that inhibits DNA topoisomerase II and induces DNA damage, mitophagy and apoptosis in tumor cells. Doxorubicin reduces basal phosphorylation of AMPK. Doxorubicin is used in the concomitant treatment of HIV-infected patients but is found to be at high risk of HBV reactivation.

S1230

Flavopiridol (L86-8275)

Flavopiridol (L86-8275, Alvocidib, NSC 649890, HMR-1275) competes with ATP to inhibit CDKs including CDK1, CDK2, CDK4, CDK6, and CDK9 with IC50 values in the 20-100 nM range. It is more selective for CDK1, 2, 4, 6, 9 versus CDK7. Flavopiridol is initially found to inhibit EGFR and PKA. Flavopiridol induces autophagy and ER stress. Flavopiridol blocks HIV-1 replication. Phase 1/2.

S2003

Maraviroc (UK-427857)

Maraviroc (UK-427857) is a CCR5 antagonist for MIP-1α, MIP-1β and RANTES with IC50 of 3.3 nM, 7.2 nM and 5.2 nM in cell-free assays, respectively. Maraviroc is used in the treatment of HIV infection.

S2679

Flavopiridol (L86-8275) HCl

Flavopiridol HCl (L86-8275, NSC 649890, Alvocidib, HMR-1275, DSP-2033) competes with ATP to inhibit CDKs including CDK1, CDK2, CDK4 and CDK6 with IC50 of ~ 40 nM in cell-free assays. It is 7.5-fold more selective for CDK1/2/4/6 than CDK7. Flavopiridol is initially found to inhibit EGFR and PKA. Flavopiridol HCl induces autophagy and ER stress. Flavopiridol HCl blocks HIV-1 replication. Phase 1/2.

E0005New

Enfuvirtide Acetate

Enfuvirtide Acetate (T20 Acetate, DP178 Acetate) is an HIV fusion inhibitor with ic50s of 13.63  nM and 30.21  nM on infection by HIV-1IIIB in MT-2 cells and HIV-1Bal in M7 cells, respectively.

S5979New

2',3'-Dideoxyadenosine

2',3'-Dideoxyadenosine (ddA, ddAdo) is an anti-human immunodeficiency virus agent against human immunodeficiency virus (HIV) and human hepatitis B virus (HBV) replication.

S5959New

Tenofovir Disoproxil

Tenofovir Disoproxil (Bis(POC)-PMPA, GS 4331) is a prodrug of tenofovir, which is metabolised intracellularly to its active anabolite tenofovir diphosphate, a competitive inhibitor of HIV-1 reverse transcriptase and terminates the growing DNA chain.

S4446New

Dimercaprol

Dimercaprol (Bal, 2,3-Dimercapto-1-propanol, Dithioglycerol) is an acrolein scavenger that inhibits HIV-1 tat activity, viral production, and infectivity in vitro.

S3500New

Pentosan Polysulfate Sodium

Pentosan 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.

S1209

Fluorouracil (5-Fluorouracil, 5-FU)

Fluorouracil (5-Fluorouracil, 5-FU, NSC 19893) is a DNA/RNA synthesis inhibitor, which interrupts nucleotide synthetic by inhibiting thymidylate synthase (TS) in tumor cells. Fluorouracil induces apoptosis and can be used in the treatment of HIV.

S1117

Triciribine (NSC 154020)

Triciribine (NSC 154020, VD-0002, vqd-002, API-2, TCN) is a DNA synthesis inhibitor, also inhibits Akt in PC3 cell line and HIV-1 in CEM-SS, H9, H9IIIB, U1 cells with IC50 of 130 nM and 20 nM, respectively; does not inhibit PI3K/PDK1; 5000-fold less active in cells lacking adenosine kinase. Phase 1/2.

S3013

Plerixafor (AMD3100) 8HCl

Plerixafor (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.

S1189

Aprepitant (MK-0869)

Aprepitant (MK-0869, L-754030) is a potent and selective neurokinin-1 receptor antagonist with IC50 of 0.1 nM. Aprepitant reduces levels of pro-inflammatory cytokines including G-CSF, IL-6, IL-8 and TNFα. Aprepitant inhibits HIV infection of human macrophages.

S7015

Birinapant (TL32711)

Birinapant (TL32711) is a SMAC mimetic antagonist, mostly to cIAP1 with Kd of <1 nM in a cell-free assay, less potent to XIAP. Birinapant helps to induce apoptosis in latent HIV-1-infected cells. Phase 2.

S1400

Tenofovir (GS 1278) Disoproxil Fumarate

Tenofovir Disoproxil Fumarate (GS-1278, Tenofovir DF) belongs to a class of antiretroviral drugs, it inhibits the activity of HIV reverse transcriptase by competing with the natural substrate deoxyadenosine 5’-triphosphate and, after incorporation into DNA, by DNA chain termination.

S1704

Emtricitabine (BW 1592)

Emtricitabine (BW1592, FTC) is a new nucleoside agent that has activity against both human immunodeficiency virus (HIV) and hepatitis B virus. It is a reverse transcriptase inhibitor. Intracellular half-life is 39 h.

S8030

Plerixafor (AMD3100)

Plerixafor (AMD3100, JM 3100, SID791) is 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 inhibits human immunodeficiency virus (HIV) replication.

S1896

Hydroxyurea (NSC-32065)

Hydroxyurea (NSC-32065, NCI-C04831, Hydroxycarbamide) is an antineoplastic agent that inhibits DNA synthesis through the inhibition of ribonucleoside diphosphate reductase. Hydroxyurea activates apoptosis and autophagy. Hydroxyurea is used to treat HIV infection.

S1848

Curcumin

Curcumin (Diferuloylmethane, Natural Yellow 3, Turmeric yellow) is the principal curcuminoid of the popular Indian spice turmeric, which is a member of the ginger family (Zingiberaceae). It is an inhibitor of p300 histone acetylatransferase(IC50~25 μM)and Histone deacetylase (HDAC); activates Nrf2 pathway and supresses the activation of NF-κB. Curcumin induces mitophagy, autophagy, apoptosis, and cell cycle arrest with antitumor activity. Curcumin reduces renal damage associated with rhabdomyolysis by decreasing ferroptosis-mediated cell death. Curcumin exhibits anti-infective properties against various human pathogens like the influenza virus, hepatitis C virus, HIV and so on.

S1351

Ivermectin (MK-933)

Ivermectin (MK-933, IVM) is a glutamate-gated chloride channel (GluCls) activator, used as a broad-spectrum antiparasitic drug. Ivermectin (MK-933, IVM) is a specific positive allosteric effector of P2X4 and α7 nicotinic acetylcholine receptors (nAChRs). Ivermectin has potent antiviral activity towards both HIV-1 and dengue virus. Ivermectin induces autophagy through the AKT/mTOR signaling pathway and mitophagy.

S5144

Neferine

Neferine ((R)-1,2-Dimethoxyaporphine), a natural component of Nelumbo nucifera, has antitumor efficiency. Neferine induces apoptosis in renal cancer cells. Neferine prevents autophagy through activation of Akt/mTOR pathway and Nrf2 in muscle cells. Neferine strongly inhibits NF-κB activation. Neferine possesses a number of therapeutic effects such as anti-diabetic, anti-aging, anti-microbial, anti-thrombotic, anti-arrhythmic, anti-inflammatory and even anti-HIV.

S7311

Q-VD-Oph

Q-VD-Oph (Quinoline-Val-Asp-Difluorophenoxymethylketone) is a potent pan-caspase inhibitor with IC50 ranged from 25 to 400 nM for caspases 1,3,8, and 9. Q-VD-OPh can inhibits HIV infection.

S0076

ABX464

ABX464 (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.

S4861

Oxindole

Oxindole (2-indolone, 2-Oxindole, Indolin-2-one) is an aromatic heterocyclic organic compound which causes sedation, muscle weakness, hypotension, and coma when dosed in excess. Oxindole has anti-cancer, anti-HIV, anti-diabetic, antibacterial and other pharmacological activities.

S6676

Ebselen

Ebselen (DR 3305, SPI-1005, PZ-51, CCG-39161) is a small-molecule capsid inhibitor of HIV-1 Replication with IC50 of 46.1 nM in TR-FRET assay.

S6848

3'-Fluoro-3'-deoxythymidine (Alovudine)

3'-Fluoro-3'-deoxythymidine (Alovudine, CL 184824, FddThd, FLT, MIV-310) is a potent inhibitor of polymerase γ and reverse transcriptase that can be used in the treatment of HIV infection. 3'-Fluoro-3'-deoxythymidine (Alovudine) is also a marker of DNA synthesis that can be used as an early response biomarker in the chemotherapy of pancreatic cancer.

S9064

Trilobatin

Trilobatin (P-Phlorizin), a natural flavonoid lipid molecule, is an HIV-1 entry inhibitor targeting the HIV-1 Gp41 envelope and exihibits anti-oxidant and anti-inflammatory effect.

S8512

Cenicriviroc (TAK-652)

Cenicriviroc (CVC, TAK-652, TBR-652) is a potent, orally active dual inhibitor of CC chemokine receptor 2 (CCR2) and CCR5. Cenicriviroc also inhibits HIV-1 and HIV-2 with potent anti-inflammatory and antiinfective activity.