HIV-1

HIV-1 is a retrovirus whose replication relies on reverse transcription of viral RNA into DNA, integrating into host genomes to produce progeny virions^[1]. Viral entry is mediated by interactions between the envelope glycoprotein gp120 and the host CD4 receptor, along with chemokine co-receptors CXCR4 or CCR5, triggering membrane fusion and infection of target cells^[2]^[3]. Post-entry, reverse transcription and integration involve complex protein-nucleic acid interactions, with viral integrase and nucleocapsid proteins directing efficient DNA synthesis^[4]. The viral replication cycle engages host signaling pathways, including calcium-dependent activation cascades, nitric oxide signaling, and protein kinase C isoforms, which modulate viral transcription and assembly^[5]^[6]. HIV-1 accessory proteins, such as Nef and Vif, interact with host factors to enhance replication and evade immune detection, establishing persistent infection^[7]. Compared with related retroviruses, HIV-1 exhibits unique isoform-specific interactions of its envelope and regulatory proteins with host pathways, enabling differential cellular tropism and pathogenicity^[8]. Small molecule inhibitors and peptide agonists targeting gp120-CD4 binding, integrase activity, or host signaling components have been employed to dissect viral replication mechanisms in vitro and in vivo, providing tools for experimental modulation of viral processes^[9]^[10]. Mechanistically, selective modulation of these pathways has been used to evaluate antiviral efficacy and to define host determinants of infection, highlighting the functional distinctions among viral isoforms and their cellular interactions^[11]^[12].

References:

[1]. Downey GP, et al. Chemotactic peptide-induced activation of MEK-2, the predominant isoform in human neutrophils. Inhibition by wortmannin. J Biol Chem. 1996 Aug 30;271(35):21005-1011. [Content Brief]

[2]. Boyé K, et al. Ligand activation induces different conformational changes in CXCR3 receptor isoforms as evidenced by plasmon waveguide resonance (PWR). Sci Rep. 2017 Sep 6;7(1):10703. [Content Brief]

[3]. Karaś K, et al. The Dichotomous Nature of AZ5104 (an EGFR Inhibitor) Towards RORγ and RORγT. Int J Mol Sci. 2019 Nov 17;20(22):5780. [Content Brief]

[4]. Maroney SA, et al. New insights into the biology of tissue factor pathway inhibitor. J Thromb Haemost. 2015 Jun;13 Suppl 1(0 1):S200-7. [Content Brief]

[5]. Mourelle M, et al. The arginine/nitric oxide pathway modulates sphincter of Oddi motor activity in guinea pigs and rabbits. Gastroenterology. 1993 Nov;105(5):1299-305. [Content Brief]

[6]. Liang C, et al. Rosiglitazone via upregulation of Akt/eNOS pathways attenuates dysfunction of endothelial progenitor cells, induced by advanced glycation end products. Br J Pharmacol. 2009 Dec;158(8):1865-73. [Content Brief]

[7]. Kampa M, et al. Opioids are non-competitive inhibitors of nitric oxide synthase in T47D human breast cancer cells. Cell Death Differ. 2001 Sep;8(9):943-52. [Content Brief]

[8]. Jing Q, et al. In search of potent and selective inhibitors of neuronal nitric oxide synthase with more simple structures. Bioorg Med Chem. 2013 Sep 1;21(17):5323-31. [Content Brief]

[9]. Courilleau D, et al. The (R)-enantiomer of CE3F4 is a preferential inhibitor of human exchange protein directly activated by cyclic AMP isoform 1 (Epac1). Biochem Biophys Res Commun. 2013 Oct 25;440(3):443-8. [Content Brief]

[10]. Shih CD. Activation of estrogen receptor beta-dependent nitric oxide signaling mediates the hypotensive effects of estrogen in the rostral ventrolateral medulla of anesthetized rats. J Biomed Sci. 2009 Jul 7;16(1):60. doi: 10.1186/1423-0127-16-60. PMID: 19583861; PMCID: PMC2717931. et al. Activation of estrogen receptor beta-dependent nitric oxide signaling mediates the hypotensive effects of estrogen in the rostral ventrolateral medulla of anesthetized rats. J Biomed Sci. 2009 Jul 7;16(1):60. [Content Brief]

[11]. Larivière S, et al. Gonadotropin-releasing hormone inhibits pituitary adenylyl cyclase-activating polypeptide coupling to 3',5'-cyclic adenosine-5'-monophosphate pathway in LbetaT2 gonadotrope cells through novel protein kinase C isoforms and phosphorylation of pituitary adenylyl cyclase-activating polypeptide type I receptor. Endocrinology. 2008 Dec;149(12):6389-98. [Content Brief]

Productos relacionados con HIV-1 (391):

By Type:	Pan (105) Selective (63)
By Effects:	Inhibitors (357) Antagonists (2) Activators (10) Inducer (1)

Cat. No.	Nombre del producto	Efecto	Pureza

HY-122482

β-Rubromycin	Inhibitor
β-Rubromycin, a quinone antibacterial agent, is a selective HIV-1 reverse transcriptase inhibitor with a K_i of 0.27 μM. β-Rubromycin is a potent telomerase inhibitor with an IC₅₀ of 3 μM. β-Rubromycin inhibits the proliferation of both K-562 and HeLa cells with IC₅₀ values of 19.5 µM and 22.7 µM, respectively.

HY-P10310A

F9170 TFA	Inhibitor	99.70%
F9170 TFA is an amphipathic peptide with an activity of inactivate HIV-1 virions. F9170 TFA targets the conserved cytoplasmic tail of HIV-1 env and disrupts the integrity of the viral membrane. F9170 TFA is able to cross the blood-brain barrier (BBB).

HY-15142A

Doxorubicin	Inhibitor
Doxorubicin (Hydroxydaunorubicin), a cytotoxic anthracycline antibiotic, is an anti-cancer chemotherapy agent. Doxorubicin is a potent human DNA topoisomerase I and topoisomerase II inhibitor with IC₅₀s of 0.8 μM and 2.67 μM, respectively. Doxorubicin reduces basal phosphorylation of AMPK and its downstream target acetyl-CoA carboxylase. Doxorubicin induces apoptosis and autophagy.

HY-135858

SARS-CoV-IN-3	Inhibitor	99.36%
SARS-CoV-IN-3 is an effective inhibitor of SARS-CoV replication. SARS-CoV-IN-3 shows anti-Coronavirus activity with an EC₅₀ of 3.6 μM in Vero cells. SARS-CoV-IN-3 inhibits the 3D7 and W2 strains of P. falciparum with IC₅₀s of 11.7 and 20.4 nM; and IC₉₀s of 29.19 and 56 nM; respectively. SARS-CoV-IN-3 reduces HIV-1-induced cytopathic effect with an EC₅₀ of 10 μM in MT-4 cells.

HY-145569

Fipravirimat	Inhibitor
Fipravirimat is a potent HIV-1 inhibitor. Fipravirimat has the potential for HIV and AIDS research.

HY-19851

Rovafovir etalafenamide	Inhibitor	99.85%
Rovafovir etalafenamide (GS-9131), a proagent of the adenosine nucleotide analogue GS-9148, is an orally active nucleoside reverse transcriptase inhibitor (NRTI). Rovafovir etalafenamide is potent and active against a variety of NRTI mutants, and shows potent anti-HIV-1 activity.

HY-16134

Celgosivir	Inhibitor
Celgosivir (MBI 3253; MDL 28574; MX3253) is an α-glucosidase I inhibitor; inhibits bovine viral diarrhoea virus (BVDV) with an IC₅₀ of 1.27 μM in in vitro assay.

HY-135856

SARS-CoV-IN-2	Inhibitor	98.66%
SARS-CoV-IN-2 is an effective inhibitor of SARS-CoV replication. SARS-CoV-IN-2 shows anti-Coronavirus activity with an EC₅₀ of 1.9 μM in Vero cells. SARS-CoV-IN-2 inhibits the 3D7 and W2 strains of P. falciparum with IC₅₀s of 21.5 and 30 nM; and IC₉₀s of 51.0 and 99.9 nM; respectively. SARS-CoV-IN-2 reduces HIV-1-induced cytopathic effect with an EC₅₀ of 2.9 μM in MT-4 cells. Antimalarial and Antiviral Activities.

HY-139989

NBD-14270	Antagonist	99.53%
NBD-14270, a pyridine analogue, is a potent HIV-1 entry antagonist with an IC₅₀ of 180 nM against 50 HIV-1 Env-pseudotyped viruses. NBD-14270 binds to HIV-1 gp120 and shows potent antiviral activity. NBD-14270 shows low cytotoxicity (CC₅₀>100 μM).

HY-132291

HIV-1 inhibitor-8	Inhibitor	98.03%
HIV-1 inhibitor-8 is an orally active, low-toxicity and potent HIV‑1 non-nucleoside reverse transcriptase inhibitor (NNRTI). HIV-1 inhibitor-8 yields exceptionally potent antiviral activities (EC₅₀=4.44~54.5 nM) against various HIV‑1 strains. The IC₅₀ of HIV-1 inhibitor-8 against WT HIV-1 reverse transcriptase is 0.081 μM.

HY-112714

GSK3532795	Inhibitor	99.59%
GSK3532795 (BMS-955176) is a potent, orally active, second-generation HIV-1 maturation inhibitor, with EC₅₀s of 1.9, 10.2, 2.7 and 13 nM for HIV-1 WT, HIV-1 WT(human serum), HIV-1 V370A, and HIV-1 ΔV370, respectively.

HY-130241

Reverse transcriptase-IN-1	Inhibitor	98.08%
Reverse transcriptase-IN-1 (Compound 12z), a diarylbenzopyrimidine (DABP) analogue, is a potent, orally active HIV-1 nonnucleoside reverse transcriptase inhibitor. Reverse transcriptase-IN-1 has antiviral activity with EC₅₀ values of 3.4 nM, 4.3 nM and 3.6 nM for HIV-1 III_B, E138K and K103N mutants, respectively. Reverse transcriptase-IN-1 also has an IC₅₀of 13.7 nM against HIV-1 reverse transcriptase enzyme.

HY-101458

IT1t	Inhibitor
IT1t is a potent CXCR4 antagonist; inhibits CXCL12/CXCR4 interaction with an IC₅₀ of 2.1 nM.

HY-14891

Fosdevirine	Inhibitor	98.96%
Fosdevirine (GSK2248761) is is a potent, selective, non-nucleoside reverse transcriptase inhibitor (NNRTI) of human immunodeficiency virus type 1 (HIV-1) replication with low nanomolar activity in vitro. Fosdevirine shows good activity against a broad range of HIV-1 strains, including efavirenz (HY-10572)-resistant clinical isolates.

HY-115488A

BNM-III-170	Inhibitor	98.48%
BNM-III-170, CD4-mimeticcompound, is an anti-HIV-1 agent. BNM-III-170 binds to the Phe43 cavity of HIV 1 gp120. BNM-III-170 can inhibits HIV-1 viral entry into target cells. BNM-III-170 can be used for the research of HIV-1 infection.

HY-P2988B

Neuraminidase, arthrobacter ureafaciens	Activator
Neuraminidase, arthrobacter ureafaciens is a neuraminidase derived from Arthrobacter ureafaciens. Neuraminidase, arthrobacter ureafaciens catalyzes the removal of sialic acid residues from cell surfaces and viral glycoconjugates. Neuraminidase, arthrobacter ureafaciens enhances HIV-1-mediated syncytium formation and promotes the viral binding and entry steps in the HIV-1 replication cycle.

HY-P1064A

Apelin-36(human) TFA	Inhibitor	99.42%
Apelin-36(human) TFA is an endogenous orphan G protein-coupled receptor APJ agonist, with an EC₅₀ of 20 nM. Apelin-36(human) TFA shows high affinity to human APJ receptors expressed in HEK 293 cells (pIC5₅₀=8.61). Apelin-36(human) TFA has been linked to two major types of biological activities: cardiovascular and metabolic. Apelin-36(human) TFA inhibits the entry of some HIV-1 and HIV-2 into the NP2/CD4 cells expressing APJ.

HY-17450

Aplaviroc	Inhibitor
Aplaviroc (AK 602), a SDP derivative, is a CCR5 antagonist, with IC₅₀s of 0.1-0.4 nM for HIV-1_Ba-L, HIV-1_JRFL and HIV-1_MOKW.

HY-139262A

FNC-TP trisodium	Inhibitor
FNC-TP trisodium is the intracellular active form of FNC. FNC is a potent nucleoside reverse transcriptase inhibitor (NRTI), with antiviral activity on HIV, HBV and HCV. FNC-TP (trisodium) is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.

HY-105268

AzddMeC	Inhibitor	98.96%
AzddMeC (CS-92) is an antiviral nucleoside analogue and a potent potent, selective and orally active HIV-1 reverse transcriptase and HIV-1 replication inhibitor. In HIV-1-infected human PBM cells and HIV-1-infected human macrophages, the EC₅₀ values of AzddMeC are 9 nM and 6 nM, respectively. AzddMeC is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.

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