HIV-1 inhibitor-50 is a non-nucleoside reverse transcriptase inhibitor (NNRTI) that targets HIV-1 reverse transcriptase (IC50 = 50 nM). HIV-1 inhibitor-50 shows significant antiviral activity, with EC50s of 2.22-53.3nM against HIV-1 IIIB and its mutant strains.

HIV-1 Rev (34-50) (HIV-1 rev Protein (34-50)) is a 17 amino acid peptide with anti-HIV-1 activity. HIV-1 Rev (34-50) is derived from the Rev-responsive element-binding domains of Rev in HIV-1.

GW841819X is an analogue of (+)-JQ1 and a novel inhibitor of BET bromodomains. GW841819X was a single enantiomer but of undefined chirality at the 4-position of the benzodiazepine ring3. GW841819X and JQ1 were recently discovered that bind to the acetyl-lysine binding pocket of BET bromodomains with Kd ranges from 50 to 370 nM [1]. GW841819X bounded to both the individual BD1 and BD2 domains with affinities of 46 and 52.5 nM, respectively. GW841819X-Brd3 interaction was estimated to be around 70 nM4. GW841819X displayed activity in vivo against NUT-midline carcinoma, multiple myeloma, mixed-lineage leukemia, and acute myeloid leukemia1. It also potent induced the ApoA1 reporter gene with an EC50 of 440 nM. It had very little effect on LDL-R luciferase activity at the concentrations at which it induces ApoA1 expression, suggesting that the effect is indeed specific3. GW841819X competed directly with GATA1 site for BD1 binding and also specifically blocked the interaction between Brd3 and acetylated GATA14. Recent findings reported that GW841819X are chose as an interest compound to further develop into potential drugs against diseases including cancer, HIV infection and heart disease2.

HIV-1 Inhibitor-49, a HEPT analog, is an orally active non-nucleoside reverse transcriptase inhibitor with potent activity against HIV-1, demonstrating an IC 50 of 30 nM. It features an excellent pharmacokinetic profile and has shown to be potentially safe without acute toxicity in mouse models.

HIV-1 Inhibitor-57 (Compound 12g) is an antiviral agent that potently inhibits both wild-type and five common NNRTI-resistant strains of HIV-1, exhibiting EC50 values between 0.024 and 0.0010 μM. It achieves this efficacy by forming supplementary interactions with residues surrounding the binding site in the HIV-1 reverse transcriptase (RT) [1].

gp120-IN-1 (compound 4e) is a potent HIV-1 gp120 inhibitor with an CC 50 of 100.90 μM and IC 50 of 2.2 μM. gp120-IN-1 inhibitis gp120-mediated virus enter into cells. gp120-IN-1 has anti-HIV-1 activity. gp120-IN-1 has dose-dependent cytotoxicity in SUP-T1 cells [1].

DDX3-IN-1 is a DEAD-box polypeptide 3 (DDX3) inhibitor with CC50 of 50 and 36 μM for HIV and HCV, respectively. Antiviral activity.

Diphyllin could be characterized as a new V-ATPase inhibitor in treating gastric cancer and inhibiting the phosphorylation of LRP6 in Wnt/β-catenin signaling.

HIV-1 Inhibitor-58 (Compound 10c) is a non-nucleoside reverse transcriptase inhibitor with broad-spectrum antiviral properties, effective against both wild-type strain IIIB and NNRTI-resistant strains like K103N and E138K in MT-4 cells at an EC50 of less than 50 nM. Additionally, it inhibits CYP2C9 and CYP2C19 with IC50 values of 2.06 μM and 1.91 μM, respectively. This compound is utilized in HIV infection research [1].

Azvudine hydrochloride (RO-0622) is a potent nucleoside reverse transcriptase inhibitor (NRTI) that exhibits strong antiviral effects against HIV, HBV, and HCV. It demonstrates highly potent inhibition of HIV-1 (EC 50 ranging from 0.03 to 6.92 nM) and HIV-2 (EC 50 ranging from 0.018 to 0.025 nM). Additionally, Azvudine hydrochloride effectively inhibits NRTI-resistant viral strains.

MC1742 is an inhibitor of class I histone deacetylases (HDACs; IC50s = 0.1, 0.11, 0.02, and 0.61 μM for HDAC1, -2, -3, and -8, respectively) and class IIb HDACs (IC50s = 7 and 40 nM for HDAC6 and HDAC10, respectively).1 It is selective for class I and class IIb over class IIa HDACs (IC50s = >50 μM for HDAC4, -5, -7, and -9). MC1742 reduces proliferation of HOS, MG-63, RD, A204, SK-ES-1, and A673 sarcoma cancer stem cells (CSCs). It increases levels of acetylated histone H3 and acetylated tubulin and induces apoptosis in MG-63 CSCs when used at a concentration of 2 μM. MC1742 also reactivates HIV-1 in JLAT 10.6 latently infected cells (EC50 = 350 nM).2 |1. Di Pompo, G., Salerno, M., Rotili, D., et al. Novel histone deacetylase inhibitors induce growth arrest, apoptosis, and differentiation in sarcoma cancer stem cells. J. Med. Chem. 58(9), 4073-4079 (2015).|2. Heffern, E.F.W., Ramani, R., Marshall, G., et al. Identification of isoform-selective hydroxamic acid derivatives that potently reactivate HIV from latency. J. Virus Erad. 5(2), 84-91 (2019).

HIV-IN petide is a competitive inhibitor of HIV-1 protease (K i =50 nM) [1] .

gp120-IN-2 (compound 4i) exhibits anti-HIV-1 activity which is a potent inhibitor of HIV-1 gp120 with an IC 50 of 7.5 μM and CC 50 of 112.93 μM. gp120-IN-2 dose-dependently shows cytotoxicity in SUP-T1 cells [1].

HIV-1 inhibitor-30 (compound 10i) is a potent inhibitor of HIV-1, specifically targeting the RT DNA polymerase enzyme. It exhibits strong antiretroviral activity, with an EC 50 value of 40 nM and an IC 50 value of 80 nM. Furthermore, HIV-1 inhibitor-30 demonstrates significant effectiveness against seven NNRTI-resistant strains of HIV-1 (RT-K103N; RT-Y181C; RT-K103N, Y181C; RT-L100I, K103N; RT-Y188L; RT-K103N, G190A; RT-K103N, V108I), with IC 50 values ranging from 0.04 to 1.42 μM. This compound holds potential for AIDS research [1].

Ganoderiol F has anti-inflammatory, cytotoxic and anti-HIV activity, it inhibits activity of topoisomerases in vitro, and it inhibits human immunodeficiency virus-1 protease with IC(50) values of 20-40 microM. It induced HO-1 expression, activation of the mitogen-activated protein kinase EKR and up-regulation of cyclin-dependent kinase inhibitor p16 and suppressed lipopolysaccharide (LPS)-induced nitric oxide (NO) production.

HIV-1 inhibitor-12 is a potent inhibitor that targets the HIV-1 capsid protein, effectively preventing its polymerization with an inhibition concentration (IC 50) of 9 nM.

HIV-1 inhibitor-41 (Compound B23) is an orally active inhibitor of non-nucleoside HIV-1 reverse transcriptase with EC 50 values of 50 nM and 20.8 nM against mutant E138K strain and HIV-1 WT, respectively. HIV-1 inhibitor-41 exhibits low hERG inhibition, no apparent CYP enzymatic inhibition as well as no acute toxicity [1].

KRH-3955 hydrochloride is a CXCR4 antagonist with oral bioavailability. It effectively inhibits the binding of SDF-1α to CXCR4, exhibiting an IC 50 of 0.61 nM. Additionally, KRH-3955 hydrochloride displays high potency and selectivity as an inhibitor of X4 HIV-1, with an EC 50 ranging from 0.3 to 1.0 nM.