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You are here:Home-Inhibitors & Agonists-Antibiotics and Antivirals-HIV

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HIV (Human immunodeficiency virus) is a lentivirus (a subgroup of retrovirus) that causes the acquired immunodeficiency syndrome (AIDS), a condition in humans in which progressive failure of the immune system allows life-threatening opportunistic infections and cancers to thrive. Infection with HIV occurs by the transfer of blood, semen, vaginal fluid, pre-ejaculate, or breast milk. Within these bodily fluids, HIV is present as both free virus particles and virus within infected immune cells.

   

HIV infects vital cells in the human immune system such as helper T cells (specifically CD4+ T cells), macrophages, and dendritic cells. HIV infection leads to low levels of CD4+ T cells through a number of mechanisms, including apoptosis of uninfected bystander cells, direct viral killing of infected cells, and killing of infected CD4+ T cells by CD8 cytotoxic lymphocytes that recognize infected cells. When CD4+ T cell numbers decline below a critical level, cell-mediated immunity is lost, and the body becomes progressively more susceptible to opportunistic infections.

Cat. No. Product Name CAS No. Information
GY04324

Rilpivirine

500287-72-9

A highly potent nonnucleoside inhibitor (NNRTI) of HIV-1 reverse trK7912:M7912anscriptase with IC50 of 0.4 nM for WT HIV-1 in cell-based assay; shows activity against a panel of single and double HIV-1 site-directed mutant (IC50=0.3-2 nM); orally active.

GY03964

YYA-021

144217-65-2

A small-molecule CD4 mimic that acts as a highly potent HIV entry inhibitor with IC50 of 9 uM against YTA48P virus with no significant cytotoxicity; shows wide tissue distribution and relatively high distribution volumes, and has promise for intravenous administration.

GY03882

RN-18

431980-38-0

RN-18 is a small molecule that antagonizes HIV-1 Vif function and inhibits HIV-1 replication only in the presence of A3G; increases cellular A3G levels in a Vif-dependent manner and increases A3G incorporation into virions without inhibiting general proteasome-mediated protein degradation; enhances Vif degradation, reduces viral infectivity by increasing A3G incorporation into virions and enhances cytidine deamination of the viral genome.

GY07070

PD 404182

72596-74-8

PD 404182 (PD404182, PD-404182) is a heterocyclic iminobenzothiazine derivative with antimicrobial and anti-inflammatory properties, a potent inhibitor of human DDAH1 activity (IC50=9 uM) and elevates cellular ADMA levels; significantly increases intracellular levels of ADMA and reduces LPS-induced NO production in cultured primary human vascular endothelial cells (ECs), abrogates the formation of tube-like structures by ECs in in vitro angiogenesis assay; also shows anti-HIV and anti-HSV activites.

GY10167

NSC260594

906718-66-9

NSC260594 (NSC 260594) is a specific inhibitor of HIV-1 RNA packaging, which involves preventing the interaction of Gag with SL3 by stabilizing this small RNA stem-loop which then leads to stabilization of the global packaging signal region (psi or ψ); specifically blocks HIV-1 RNA encapsidation, binds to HIV-1 gRNA and exhibits potent antiviral activity; NSC260594 also is a small molecule inhibitor of the Escherichia coli condensin MukBEF, affects MukB directly.

GY10351

BMS-818251

BMS-818251 (BMS818251) is a novel potent, small-molecule inhibitor of HIV-1 entry with EC50 of 0.019 nM against e laboratory-adapted HIV-1 strain NL4-3; displays >10-fold more potent than temsavir on a cross-clade panel of 208-HIV-1 strains, interacts with gp120 residues from the conserved β20-β21 hairpin to improve potency.

GY10471

ABX464

1258453-75-6

ABX464 (ABX-464, ABX 464) is a novel class of anti-HIV small molecule targeting Rev-mediated viral RNA biogenesis, shows dose dependent inhibition of HIV-1 replication in stimulated PBMCs with IC50 of 0.1-0.5 uM; ABX464 inhibits different HIV-1 clades, resistant viruses and did not select for resistance; increases the levels of spliced HIV RNA, influences REV-mediated HIV RNA biogenesis and export, and interacts with the CBC complex; inhibit viral replication in humanized mice.

GY10529

ZBMA-1

1975145-64-2

ZBMA-1 is a potent HIV-1 replication inhibitor (IC50=1.01 uM) that efficiently protects APOBEC3G protein by targeting Vif-APOBEC3G complex; protected APOBEC3G from Vif-mediated degradation in a dose-dependent manner and induced nonfunctional proviruses, blocked Vif binding to Elongin C, does not affect the interactions between Vif and APOBEC3G or CBF-β.

GY10574

HIV-1 inhibitor 5b

HIV-1 inhibitor 5b is a novel anti-HIV-1 compound that inhibits HIV-1 JR-CSF with EC50 of 1 nM without significant cytotoxicity (CC50>20 uM), also shows potency against NRTI- and NNRTI-resistant HIV-1 (EC50=1-3 nM); shows a chemical backbone similar to the clinically used integrase (IN) strand transfer inhibitor (INSTI) elvitegravir, but has no detectable INSTI activity; various drug-resistant HIV-1 strains did not display cross resistance to HIV-1 inhibitor 5b; remains its anti-HIV-1 activity even after the viral integration stage, significantly suppresses p24 antigen production in HIV-1 latently infected cells exposed with TNF-alpha; demonstrates favorable pharmacokinetic profiles in mice.

GY05021

(±)-BI-D

1416258-16-6

A potent, allosteric HIV integrase inhibitor (Kd=34 nM) that binds the LEDGF/p75 binding site on integrase; inhibits the replication of NL4.3 virus (T124/T125) with EC50 of 51 nM.

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