| S0958 |
Zingibroside R1
|
Zingibroside R1, isolated from rhizomes of Panax zingiberensis Wu et Feng (Araliaceae), has some anti-HIV-1 activity. This compound shows the inhibitory effects on the 2-deoxy-D-glucose (2-DG) uptake by EAT cells with IC50 of 91.3 µM and the growth of MT-4 cells with CC50 of 46.2 µM.
|
|
|
| E0005 |
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.Solutions are unstable and should be fresh-prepared.
|
|
|
| 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. This compound has anti-cancer, anti-HIV, anti-diabetic, antibacterial and other pharmacological activities.
|
|
|
| S9626 |
Nelfinavir
|
Nelfinavir (AG-1341) is a potent inhibitor of HIV protease and induces endoplasmic reticulum (ER) stress, autophagy, and apoptosis in vitro and in vivo. It also inhibits Streptolysin S (SLS) production, a key virulence factor of Streptococcus pyogenes, with IC50 of 6 µM.
|
|
|
| E0797 |
WAY-383487
|
WAY-383487 is one of the Tat peptide derivatives and inhibits HIV-1 long terminal repeat-activated transcription.
|
|
|
| S5979 |
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.
|
|
|
| E4891 |
Fostemsavir Tris
|
Fostemsavir Tris(BMS-663068 Tris) is a phosphonooxymethyl prodrug of BMS-626529, formulated as a tris(hydroxymethyl)aminomethane salt. It inhibits human immunodeficiency virus type 1 (HIV-1) by binding to the gp120 protein, preventing the virus from attaching to CD4+ T-cells.
|
|
|
| E1138 |
CQ31
|
CQ31, a small molecule, selectively activates caspase activation and recruitment domain-containing 8 (CARD8).
|
|
|
| S4446 |
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.
|
|
|
| S9630 |
Tipranavir
|
Tipranavir(PNU-140690) is a nonpeptidyl inhibitor of HIV protease with high potency Ki of 0.008 nM and IC50 of 0.03 μM, it also inhibited HIV-2 protease with Ki of < 1 nM. It is administered in combination antiretroviral therapy to treat HIV-1 infection and AIDS.
|
|
|
| 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. It inhibits ATR with IC50 of 21 nM in 3T3TopBP1-ER cell, induces autophagy, and suppresses HIV-1 replication. Phase 2.
|
-
Adv Mater, 2025, e12810.
-
Nat Commun, 2025, 16(1):8189
-
Nat Commun, 2025, 16(1):4502
|
|
| S1230 |
Flavopiridol (Alvocidib, HMR-1275)
|
Flavopiridol (Alvocidib) 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.
|
-
Mol Cell, 2025, S1097-2765(25)00042-5
-
Cell Rep Med, 2025, S2666-3791(25)00231-9
-
Dev Cell, 2025, S1534-5807(25)00537-4
|
|
| S1117 |
Triciribine (API-2)
|
Triciribine (API-2) is a DNA synthesis inhibitor that 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; it does not inhibit PI3K/PDK1 and is 5000-fold less active in cells lacking adenosine kinase. Phase 1/2.
|
-
Mol Psychiatry, 2025, 10.1038/s41380-025-02917-1
-
Transl Oncol, 2025, 58:102434
-
J Cell Sci, 2023, 136(4)jcs259788
|
|
| S7015 |
Birinapant (TL32711)
|
Birinapant is a SMAC mimetic antagonist, mostly to cIAP1 with Kd of <1 nM in a cell-free assay, less potent to XIAP. This compound helps to induce apoptosis in latent HIV-1-infected cells. Phase 2.
|
-
Cell, 2025, S0092-8674(25)01233-4
-
Nat Commun, 2025, 16(1):7360
-
EMBO Mol Med, 2025, 10.1038/s44321-025-00201-x
|
|
| S2679 |
Flavopiridol (Alvocidib) HCl
|
Flavopiridol (Alvocidib) HCl 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.
|
-
Elife, 2024, 13e80684
-
Int J Biol Macromol, 2023, 258(Pt 1):128776
-
Mol Cell Biol, 2023, 43(1):1-21
|
|
| S3013 |
Plerixafor (AMD3100) 8HCl
|
Plerixafor (AMD3100, JM 3100,Plerixafor Octahydrochloride,AMD3100 octahydrochloride,SID791 octahydrochloride) 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.
|
-
Angiogenesis, 2025, 28(3):26
-
bioRxiv, 2025, 2025.08.29.673113
-
bioRxiv, 2025, 2025.05.28.656643
|
|
| 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.
|
-
J Biol Chem, 2025, 301(7):110305
-
Mol Pain, 2025, 21:17448069251323668
-
BMC Immunol, 2025, 26(1):67
|
|
| S1400 |
Tenofovir Disoproxil Fumarate
|
Tenofovir Disoproxil Fumarate 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.
|
-
Clin Immunol, 2024, 260:109915
-
Antiviral Res, 2024, 231:106010
-
Front Cell Infect Microbiol, 2024, 14:1334126
|
|
| S1351 |
Ivermectin
|
Ivermectin is a glutamate-gated chloride channel (GluCls) activator, used as a broad-spectrum antiparasitic drug. This compound is a specific positive allosteric effector of P2X4 and α7 nicotinic acetylcholine receptors (nAChRs). It is a specific inhibitor of Impα/β1-mediated nuclear import and has potent antiviral activity towards both HIV-1 and dengue virus. This chemical induces autophagy through the AKT/mTOR signaling pathway and mitophagy.
|
-
Nat Commun, 2025, 16(1):7156
-
J Adv Res, 2025, S2090-1232(25)00874-4
-
Biomed Pharmacother, 2025, 189:118248
|
|
| S1704 |
Emtricitabine (FTC)
|
Emtricitabine (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, and its intracellular half-life is 39 h.
|
-
Cancer Discov, 2025, 10.1158/2159-8290.CD-24-1317
-
HIV Med, 2025, 26(2):285-294
-
Immunity, 2024, 57(12):2928-2944.e6
|
|
| S8512 |
Cenicriviroc
|
Cenicriviroc is a potent, orally active dual inhibitor of CC chemokine receptor 2 (CCR2) and CCR5. This compound also inhibits HIV-1 and HIV-2 with potent anti-inflammatory and antiinfective activity.
|
-
Nature, 2025, 10.1038/s41586-024-08535-1
-
Int J Biol Sci, 2023, 19(8):2572-2587
-
Stem Cells, 2023, 41(6):672-683
|
|
| S5144 |
Neferine
|
Neferine ((R)-1,2-Dimethoxyaporphine), a natural component of Nelumbo nucifera, has antitumor efficiency. It induces apoptosis in renal cancer cells. This compound prevents autophagy through activation of Akt/mTOR pathway and Nrf2 in muscle cells. It strongly inhibits NF-κB activation. It possesses a number of therapeutic effects such as anti-diabetic, anti-aging, anti-microbial, anti-thrombotic, anti-arrhythmic, anti-inflammatory and even anti-HIV.
|
-
J Cosmet Dermatol, 2024, 10.1111/jocd.16587
-
Bone Res, 2022, 10(1):27
-
Cell Death Dis, 2022, 13(11):1000
|
|
| S5959 |
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.
|
-
J Virol, 2022, JVI0173021
-
Front Microbiol, 2018, 9:278
|
|
| 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. It is also a marker of DNA synthesis that can be used as an early response biomarker in the chemotherapy of pancreatic cancer.
|
-
Toxicol Lett, 2025, 406:31-37
|
|
| S3500 |
Pentosan Polysulfate Sodium
|
Pentosan Polysulfate Sodium (PPS, Elmiron) is an orally bioavailable, semi-synthetic medication with anti-inflammatory and pro-chondrogenic properties. This compound also exhibits anti-HIV-1 activity.
|
|
|
| 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.
|
|
|