AMD 3465 hexahydrobromide is a potent antagonist of CXCR4, inhibits binding of 12G5 mAb and CXCL12AF647 to CXCR4, with IC50s of 0.75 nM and 18 nM in SupT1 cells; AMD 3465 also potently inhibits the replication of X4 HIV strains (IC50: 1-10 nM), but has no effect on CCR5-using (R5) viruses.
Darunavir ethanolate (TMC114 ethanolate) is a potent HIV protease inhibitor used to treat and prevent HIV/AIDS. Darunavir has a Ki of 1 nM for wild type HIV-1 protease.
Triptonine B, a sesquiterpene pyridine alkaloid that isolated from Tripterygium hypoglaucum and Tripterygium wilfordii, inhibits HIV replication in H9 lymphocytes with an EC50 value of <0.10 μg/mL[1].
Cabotegravir is a potent HIV integrase inhibitor as an oral lead-in tablet and long-acting injectable for the treatment and prevention of HIV infection. Cabotegravir is an inhibitor of OAT1 (IC50 0.81 μM) and OAT3 (IC50 0.41 μM).IC50 value: 0.81 μM (OAT1), 0.41 μM (OAT3) [1]Target: OAT1, OAT3Cabotegravir is a potent HIV integrase inhibitor in clinical development as an oral lead-in tablet and long-acting injectable for the treatment and prevention of HIV infection.[2] Cabotegravir is an HIV-1 integrase inhibitor under development as a tablet for both oral lead-in therapy and long-acting (LA) injectable for intramuscular dosing.[3]
3'-Azido-3'-deoxy-5-methylcytidine (CS-92) is a potent xenotropic murine leukemia-related retrovirus (XMRV) inhibitor with a CC50 of 43.5 μM in MCF-7 cells. 3'-Azido-3'-deoxy-5-methylcytidine also inhibits HIV-1 reverse transcriptase with an EC50 of 0.06 μM in peripheral blood mononuclear (PBM) cells[1].
PF-232798 is an orally active CCR5 antagonist with anti-HIV effects[1].
Influenza antiviral conjugate-1 (INT-2) is a HIV inhibitor, shows potent cell fusion inhibition[1].
HIV-1 inhibitor-60 (compound 45) is an HIV inhibitor with the potential for the research of infection diseases[1].
HIV-1 capsid inhibitor 1 is a potent HIV-1 Capsid inhibitor with an EC50 value of 3.13 µM. HIV-1 capsid inhibitor 1 shows antiviral activities[1].
Tenofovir is a nucleotide reverse transcriptase inhibitor to treat HIV and chronic Hepatitis B.
Apricitabine (SPD754; AVX754), the (-) enantiomer of 2′-deoxy-3′-oxa-4′-thiocytidine (dOTC), is a highly selective and orally active HIV-1 reverse transcriptase (RT) inhibitor (Ki=0.08 μM), as well as inhibits DNA polymerases α, β, and γ with Ki value of 300 μM, 12 μM, and 112.25 μM, respectively[1]. Apricitabine (SPD754; AVX754) shows promising antiretroviral efficacy, good tolerability and a low propensity for resistance selection in antiretroviral-naive HIV infection[2].
HIV-1 inhibitor-37 (Compound 83) is a potent HIV-1. HIV-1 inhibitor-37 has the potential for further development as novel latency reversing agents[1].
(+)-Dihydrocalanolide A (DHCal A; NSC 678323) is an orally active nonnucleoside inhibitor of Reverse Transcriptase. (+)-Dihydrocalanolide A can be used to HIV infection research[1].
Thiamine disulfide, a vitamin B1 derivative, is an oxidized dimer of Thiamine. Thiamine disulfide is a potent HIV-1 inhibitor. Thiamine disulfide significantly depresses HIV-1 transactivator (Tat) activity[1][2].
HIV-1 Rev (34-50) is a 17-aa peptide derived from the Rev-responsive element (RRE)-binding domains of Rev in HIV-1, with anti-HIV-1 activity.
BNM-III-170 TFA salt is a small-molecule CD4-mimetic compound that enhances vaccine efficacy against HIV-1 challenge in vivo; binds the HIV-1 gp120 Env and promotes conformational changes similar to those induced by CD4, exposing conserved Env elements to antibodies; synergizes with antibodies elicited by monomeric HIV-1 gp120 to protect monkeys from multiple high-dose intrarectal challenges with a heterologous simian-human immunodeficiency virus (SHIV).
Interiotherin A is a lignan with a dibenzocyclooctadiene skeleton isolated from Kadsura interior. Interiotherin A inhibits HIV replication to exhibit anti-HIV activity, it has a role as a metabolite and an anti-HIV agent[1].
Inosine pranobex is a potent, broad-spectrum antiviral compound for HIV infection. Inosine pranobex is an immunopotentiator[1].
1-Deoxymannojirimycin hydrochloride is a selective class I α1,2-mannosidase inhibitor with an IC50 of 20 μM. 1-Deoxymannojirimycin hydrochloride is also a N-linked glycosylation inhibitor and inhibits HIV‐1 strains. 1-Deoxymannojirimycin hydrochloride has antiviral activity[1][2].
Tipranavir-d4 (PNU-140690-d4) is the deuterium labeled Tipranavir. Tipranavir (PNU-140690) inhibits the enzymatic activity and dimerization of HIV-1 protease, exerts potent activity against multi-protease inhibitor (PI)-resistant HIV-1 isolates with IC50s of 66-410 nM[1][2]. Tipranavir inhibits SARS-CoV-2 3CLpro activity[3].
Azt-pmap, a nucleoside analogue, is an aryl phosphate derivative of AZT. Azt-pmap shows anti-HIV activity[1]. AZT is a nucleoside reverse transcriptase inhibitor (NRTI) for HIV infection[2].
Sparstolonin B acts as a selective TLR2 and TLR4 antagonist and selectively blocks TLR2- and TLR4-mediated inflammatory signaling. Sparstolonin B has anti-HIV and anticancer activities[1][2].
Nelfinavir(AG-1341) is a potent and orally bioavailable human immunodeficiency virus HIV-1 protease inhibitor (Ki=2 nM) and is widely prescribed in combination with HIV reverse transcriptase inhibitors for the treatment of HIV infection. IC50 Valur: 2 nM (Ki for HIV-1 protease) [2]Target: HIV Proteasein vitro: In vitro exposure (72 hours) of HAECs to NEL (0.25-2 μg/mL) decreased both basal (2.5-fold) and insulin-induced NO production (4- to 5-fold). NEL suppressed insulin-induced phosphorylation of both Akt and eNOS at serine residues 473 and 1177, respectively. NEL decreased tyrosine phosphorylation of IR-β, IRS-1, and PI3K. Coexposure to troglitazone (TRO; 250 nM) ameliorated the suppressive effects of NEL on insulin signaling and NO production. Coexposure to TRO also increased eNOS expression in NEL-treated HAECs [1]. AG1343 is a potent enzyme inhibitor (Ki = 2 nM) and antiviral agent (HIV-1 ED50 = 14 nM). An X-ray cocrystal structure of the enzyme-AG1343 complex reveals how the novel thiophenyl ether and phenol-amide substituents of the inhibitor interact with the S1 and S2 subsites of HIV-1 protease, respectively [2].in vivo: In vivo studies indicate that AG1343 is well absorbed orally in a variety of species and possesses favorable pharmacokinetic properties in humans [2].
L-739594 is a HIV-1 protease inhibitor, with an IC50 of 1.8 nM[1].
BMS-707035 is an HIV-1 integrase (IN) inhibitor with an IC50 value of 15 nM. IC50 Value: 15 nMTarget: HIV IntegraseBMS-707035 was scheduled to be evaluated in a Phase II study to assess the antiretroviral activity, safety, pharmacodynamics, and pharmacokinetics in 50 HIV-infected subjects using a 10-day randomized, double-blind, placebo-controlled, ascending multiple-dose study design.
D77 is anti-HIV-1 inhibitor targeting the interaction between integrase and cellular LEDGF/p75. D77 inhibits HIV-1(IIIB) replication by EC50 value of 23.8 μg/ml in MT-4 cell (5.03 μg/ml for C8166 cells).IC50 value: 23.8 μg/ml (EC50, in MT-4 cell ), 5.03 μg/ml (EC50, in C8166 cell)Target: HIV-1in vitro: D77 exhibits a highly specific binding affinity to HIV-1 integrase catalytic core domain.D77 induces a dramatic concentration-dependent decrease of α-galactosidase activity compared to the D77-untreated cells. D77 reveals a significant inhibition activity against the interaction of IN with IBD.
LJ 001 ((LJ-001, LJ001) is a broad-spectrum antiviral agent targeting entry of enveloped viruses, including influenza A, filoviruses, poxviruses, arenaviruses, bunyaviruses, paramyxoviruses, flaviviruses, and HIV-1; specifically intercalates into viral membranes, irreversibly inactivates virions while leaving functionally intact envelope proteins, and inhibits viral entry at a step after virus binding but before virus-cell fusion; specifically inhibits virus-cell but not cell-cell fusion
Elipovimab is a potent broadly neutralizing HIV-1 antibody for the targeted elimination of HIV-infected cells[1]
TAT (47-57), FAM-labeled is a cell-penetrating peptide (CPP). TAT (47-57), FAM-labeled has the potential for intracellular drug delivery research[1].
Amprenavir-d4-1 is deuterium labeled Amprenavir. Amprenavir (VX-478) is a HIV protease inhibitor (Ki=0.6 nM) used to treat HIV infection. Amprenavir is also a SARS-CoV 3CLpro inhibitor with an IC50 of 1.09 μM.