S1208 |
Doxorubicin (DOX) HCl
|
ドキソルビチン塩酸塩 (Doxorubicin (Adriamycin, NSC 123127, DOX, Hydroxydaunorubicin) HCl) は抗生物質の一種であり、DNA トポイソメラーゼ (topoisomerase) II を阻害することで DNA 損傷を引き起こし、がん細胞中においてマイトファジー (mitophagy) およびアポトーシス (apoptosis) を誘導します。ドキソルビシンは AMPK の 基底状態におけるリン酸化を減弱します。また、ドキソルビシンは HIV 感染患者の併用療法において使用されますが、同時に HBV 再活性化のリスクを伴うことが分かっています。This product may precipitate when dissolved in PBS solution. It is recommended to prepare the stock solution in pure water and dilute with either pure water or saline to obtain the working solution. |
-
Cell Metab, 2024, S1550-4131(24)00371-1
-
Nat Cancer, 2024, 10.1038/s43018-024-00814-0
-
Nucleic Acids Res, 2024, gkae811
|
|
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. |
-
Nat Cell Biol, 2024, 10.1038/s41556-024-01473-0
-
J Clin Invest, 2024, 134(18)e179860
-
Haematologica, 2024, 109(6):1713-1725
|
|
S1209 |
5-FU (5-Fluorouracil)
|
5-FU (5-Fluorouracil) 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. |
-
Mol Cancer, 2024, 23(1):186
-
Cancer Discov, 2024, 10.1158/2159-8290.CD-24-0887
-
Nat Cell Biol, 2024, 10.1038/s41556-024-01473-0
|
|
S1230 |
Flavopiridol (Alvocidib)
|
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. |
-
Nat Commun, 2024, 15(1):8539
-
Nat Commun, 2024, 15(1):35
-
Cell Rep, 2024, 43(5):114176
|
|
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. |
-
Cell, 2024, 187(5):1223-1237.e16
-
Cell, 2024, 187(5):1223-1237.e16
-
Stem Cell Res Ther, 2024, 15(1):167
|
|
S1117 |
Triciribine (API-2)
|
Triciribine (API-2) 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. |
-
J Cell Sci, 2023, 136(4)jcs259788
-
Exp Gerontol, 2023, 173:112091
-
EJHaem, 2023, 4(3):631-638
|
|
S7015 |
Birinapant
|
Birinapant 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. |
-
Cell Death Differ, 2024, 10.1038/s41418-024-01316-3
-
Cancer Res, 2024, 84(15):2432-2449
-
Cell Death Dis, 2024, 15(4):255
|
|
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. |
-
Nat Commun, 2024, 15(1):830
-
Cell Death Dis, 2024, 15(5):363
-
Cell Death Discov, 2024, 10(1):125
|
|
S2679 |
Flavopiridol (Alvocidib) HCl
|
Flavopiridol (Alvocidib) HClcompetes 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
|
|
S2003 |
Maraviroc
|
Maraviroc 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. |
-
Commun Biol, 2024, 7(1):488
-
Commun Biol, 2024, 7(1):488
-
iScience, 2024, 27(7):110141
|
|
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. |
-
Sci Signal, 2024, 17(828):eabl3758
-
Cell Discov, 2023, 9(1):104
-
Cell Discov, 2023, 9(1):104
|
|
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. |
-
Cancer Cell Int, 2024, 24(1):303
-
Front Pharmacol, 2024, 15:1418902
-
PLoS Negl Trop Dis, 2024, 18(8):e0012428
|
|
S1896 |
Hydroxyurea
|
Hydroxyurea 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. |
-
Nat Commun, 2024, 15(1):7360
-
iScience, 2024, 27(4):109580
-
Sci Adv, 2024, 10(21):eadk8908
|
|
S1189 |
Aprepitant
|
Aprepitant 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. |
-
Br J Cancer, 2024, 10.1038/s41416-024-02608-8
-
Inflammation, 2023, 46(1):256-269
-
Nat Commun, 2022, 13(1):4995
|
|
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
-
Front Cell Infect Microbiol, 2024, 14:1334126
-
Viruses, 2024, 16(3)323
|
|
S1351 |
Ivermectin
|
Ivermectin 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 (MK-933) is a specific inhibitor of Impα/β1-mediated nuclear import and has potent antiviral activity towards both HIV-1 and dengue virus. Ivermectin induces autophagy through the AKT/mTOR signaling pathway and mitophagy. |
-
Viruses, 2024, 16(4)640
-
Life Sci Alliance, 2023, 6(8)e202302133
-
Cell Rep Methods, 2023, 3(10):100599
|
|
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. Intracellular half-life is 39 h. |
-
J Biomed Sci, 2024, 31(1):34
-
Clin Immunol, 2024, 260:109915
-
Sci Rep, 2024, 14(1):9167
|
|
S8512 |
Cenicriviroc
|
Cenicriviroc 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. |
-
Int J Biol Sci, 2023, 19(8):2572-2587
-
Stem Cells, 2023, 41(6):672-683
-
Life Science Alliance, 2023, 6(6)
|
|
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. |
-
Evid Based Complement Alternat Med, 2023, 2023:8378581
-
Science, 2022, 375(6586):1254-1261
-
NPJ Digit Med, 2022, 5(1):83
|
|
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. |
-
Bone Res, 2022, 10(1):27
-
Cell Death Dis, 2022, 13(11):1000
-
iScience, 2022, 25(11):105394
|
|
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
|
|
S0958 |
Zingibroside R1
|
Zingibroside R1, isolated from rhizomes of Panax zingiberensis Wu et Feng (Araliaceae), has some anti-HIV-1 activity. Zingibroside R1 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. |
|
|
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. |
|
|
S3500 |
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. |
|
|
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. |
|
|
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. |
|
|
E4891New |
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. |
|
|
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. |
|
|
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. |
|
|
S9630New |
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. |
|
|
S1208 |
Doxorubicin (DOX) HCl
|
ドキソルビチン塩酸塩 (Doxorubicin (Adriamycin, NSC 123127, DOX, Hydroxydaunorubicin) HCl) は抗生物質の一種であり、DNA トポイソメラーゼ (topoisomerase) II を阻害することで DNA 損傷を引き起こし、がん細胞中においてマイトファジー (mitophagy) およびアポトーシス (apoptosis) を誘導します。ドキソルビシンは AMPK の 基底状態におけるリン酸化を減弱します。また、ドキソルビシンは HIV 感染患者の併用療法において使用されますが、同時に HBV 再活性化のリスクを伴うことが分かっています。This product may precipitate when dissolved in PBS solution. It is recommended to prepare the stock solution in pure water and dilute with either pure water or saline to obtain the working solution. |
- Cell Metab, 2024, S1550-4131(24)00371-1
- Nat Cancer, 2024, 10.1038/s43018-024-00814-0
- Nucleic Acids Res, 2024, gkae811
|
|
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. |
- Nat Cell Biol, 2024, 10.1038/s41556-024-01473-0
- J Clin Invest, 2024, 134(18)e179860
- Haematologica, 2024, 109(6):1713-1725
|
|
S1209 |
5-FU (5-Fluorouracil)
|
5-FU (5-Fluorouracil) 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. |
- Mol Cancer, 2024, 23(1):186
- Cancer Discov, 2024, 10.1158/2159-8290.CD-24-0887
- Nat Cell Biol, 2024, 10.1038/s41556-024-01473-0
|
|
S1230 |
Flavopiridol (Alvocidib)
|
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. |
- Nat Commun, 2024, 15(1):8539
- Nat Commun, 2024, 15(1):35
- Cell Rep, 2024, 43(5):114176
|
|
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. |
- Cell, 2024, 187(5):1223-1237.e16
- Cell, 2024, 187(5):1223-1237.e16
- Stem Cell Res Ther, 2024, 15(1):167
|
|
S1117 |
Triciribine (API-2)
|
Triciribine (API-2) 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. |
- J Cell Sci, 2023, 136(4)jcs259788
- Exp Gerontol, 2023, 173:112091
- EJHaem, 2023, 4(3):631-638
|
|
S7015 |
Birinapant
|
Birinapant 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. |
- Cell Death Differ, 2024, 10.1038/s41418-024-01316-3
- Cancer Res, 2024, 84(15):2432-2449
- Cell Death Dis, 2024, 15(4):255
|
|
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. |
- Nat Commun, 2024, 15(1):830
- Cell Death Dis, 2024, 15(5):363
- Cell Death Discov, 2024, 10(1):125
|
|
S2679 |
Flavopiridol (Alvocidib) HCl
|
Flavopiridol (Alvocidib) HClcompetes 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
|
|
S2003 |
Maraviroc
|
Maraviroc 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. |
- Commun Biol, 2024, 7(1):488
- Commun Biol, 2024, 7(1):488
- iScience, 2024, 27(7):110141
|
|
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. |
- Sci Signal, 2024, 17(828):eabl3758
- Cell Discov, 2023, 9(1):104
- Cell Discov, 2023, 9(1):104
|
|
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. |
- Cancer Cell Int, 2024, 24(1):303
- Front Pharmacol, 2024, 15:1418902
- PLoS Negl Trop Dis, 2024, 18(8):e0012428
|
|
S1896 |
Hydroxyurea
|
Hydroxyurea 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. |
- Nat Commun, 2024, 15(1):7360
- iScience, 2024, 27(4):109580
- Sci Adv, 2024, 10(21):eadk8908
|
|
S1189 |
Aprepitant
|
Aprepitant 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. |
- Br J Cancer, 2024, 10.1038/s41416-024-02608-8
- Inflammation, 2023, 46(1):256-269
- Nat Commun, 2022, 13(1):4995
|
|
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
- Front Cell Infect Microbiol, 2024, 14:1334126
- Viruses, 2024, 16(3)323
|
|
S1351 |
Ivermectin
|
Ivermectin 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 (MK-933) is a specific inhibitor of Impα/β1-mediated nuclear import and has potent antiviral activity towards both HIV-1 and dengue virus. Ivermectin induces autophagy through the AKT/mTOR signaling pathway and mitophagy. |
- Viruses, 2024, 16(4)640
- Life Sci Alliance, 2023, 6(8)e202302133
- Cell Rep Methods, 2023, 3(10):100599
|
|
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. Intracellular half-life is 39 h. |
- J Biomed Sci, 2024, 31(1):34
- Clin Immunol, 2024, 260:109915
- Sci Rep, 2024, 14(1):9167
|
|
S8512 |
Cenicriviroc
|
Cenicriviroc 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. |
- Int J Biol Sci, 2023, 19(8):2572-2587
- Stem Cells, 2023, 41(6):672-683
- Life Science Alliance, 2023, 6(6)
|
|
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. |
- Evid Based Complement Alternat Med, 2023, 2023:8378581
- Science, 2022, 375(6586):1254-1261
- NPJ Digit Med, 2022, 5(1):83
|
|
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. |
- Bone Res, 2022, 10(1):27
- Cell Death Dis, 2022, 13(11):1000
- iScience, 2022, 25(11):105394
|
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S5959 |
Tenofovir Disoproxil
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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
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S0958 |
Zingibroside R1
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Zingibroside R1, isolated from rhizomes of Panax zingiberensis Wu et Feng (Araliaceae), has some anti-HIV-1 activity. Zingibroside R1 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. |
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E0005 |
Enfuvirtide Acetate
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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. |
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S0076 |
ABX464
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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. |
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S4861 |
Oxindole
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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. |
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S3500 |
Pentosan Polysulfate Sodium
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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. |
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S6848 |
3'-Fluoro-3'-deoxythymidine (Alovudine)
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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. |
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E0797 |
WAY-383487
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WAY-383487 is one of the Tat peptide derivatives and inhibits HIV-1 long terminal repeat-activated transcription. |
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S5979 |
2',3'-Dideoxyadenosine
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2',3'-Dideoxyadenosine (ddA, ddAdo) is an anti-human immunodeficiency virus agent against human immunodeficiency virus (HIV) and human hepatitis B virus (HBV) replication. |
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E4891New |
Fostemsavir Tris
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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. |
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S9064 |
Trilobatin
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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. |
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S4446 |
Dimercaprol
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Dimercaprol (Bal, 2,3-Dimercapto-1-propanol, Dithioglycerol) is an acrolein scavenger that inhibits HIV-1 tat activity, viral production, and infectivity in vitro. |
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S9630New |
Tipranavir
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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. |
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