reverse transcriptase in 1

Reverse transcriptase-IN-1 is a diarylbenzopyrimidine (DABP) analogue and a potent inhibitor of HIV-1 nonnucleoside reverse transcriptase with an IC50of 13.7 nM.

Punicalin exerts anti-inflammatory, antioxidative, and anti-hepatotoxic activities, it shows inhibitory activity on HIV-1 reverse transcriptase in a dose-dependent manner, with an IC50 of 0.11 microg/ml (0.14 microM).

Apricitabine (SPD754) is a highly selective and orally active HIV-1 reverse transcriptase inhibitor (Ki=0.08 μM), the (-) enantiomer of 2′-deoxy-3′-oxy-4′-thiocytidine (dOTC) . Apricitabine inhibits DNA polymerase α, β and γ with Ki values of 300 μM, 12 μM and 112.25 μM, respectively. Apricitabine has shown good antiretroviral therapeutic efficacy in antiretroviral HIV-infected patients, with good tolerability and low selective resistance.

UC-781 (NSC-675186) is a potent and selective inhibitor of human immunodeficiency virus HIV-1 non-nucleoside reverse transcriptase (NNRTI) I with a C50 value of 5 nM.UC-781 exhibits both antiviral activity and drug resistance.UC-781 is in a stable state, and is unaffected by lower pH or varying temperatures.

Lamivudine (BCH-189) is a reverse transcriptase inhibitor and ZALCITABINE analog in which a sulfur atom replaces the 3' carbon of the pentose ring. It is used to treat HIV disease.

Nevirapine (NVP) is a benzodiazepine non-nucleoside reverse transcriptase inhibitor. In combination with other antiretroviral drugs, nevirapine reduces HIV viral loads and increases CD4 counts, thereby retarding or preventing the damage to the immune system and reducing the risk of developing AIDS.

Bavtavirine is a potent non-nucleoside reverse transcriptase inhibitor (NNRTIs) that inhibits HIV replication by inhibiting HIV-1 reverse transcriptase activity and preventing the transcription of viral RNA into DNA for use in Highly Active Antiretroviral Therapy (HAART) programs and HIV disease studies

beta-L-D4A, a nucleoside HIV-1 reverse transcriptase inhibitor, exhibits biological activity by terminating DNA chain synthesis in the 5'-3' direction.

4'-Ethynyl-2'-deoxyadenosine (4'-E-dA), a nucleoside reverse transcriptase (RT) inhibitor, demonstrates potent activity against drug-resistant HIV variants, with an EC50 of 98 nM in MT-4 cells for anti-HIV-1 activity.

Loviride is a non-nucleoside reverse transcriptase inhibitor (IC50: 0.3 µM). Loviride inhibits HIV-1, HIV-2 and SIV replication in MT-4 cells. It is used for reverse transcriptase from HIV-1.

HIV-1inhibitor-75 is a human immunodeficiency virus 1 (HIV-1) inhibitor with an EC50 range of 0.0039-0.338 μM. Its target is the reverse transcriptase, exhibiting an IC50 value of 0.055 μM. Additionally, HIV-1inhibitor-75 demonstrates good metabolic stability in vitro, presenting moderate clearance rates and an extended half-life in human plasma and liver microsomes.

HIV-1inhibitor-76 (compound 9t-2) is an inhibitor of the HIV-1 non-nucleoside reverse transcriptase. It is utilized in research aimed at combating HIV.

TAC (TERT activator compound) is a TERT (telomerase reverse transcriptase) activator that enhances TERT transcriptional activity through the MEK/ERK/AP-1 cascade pathway, promotes telomere synthesis in primary human cells and naturally aged mice, reduces cellular senescence and inflammatory cytokines, and alleviates neuroinflammation, among other effects.

NRTT-IN-1 (Compound 1) is an inhibitor of the nucleoside reverse transcriptase translocation (NRTT), effectively blocking HIV DNA synthesis and viral replication.

NNRT-IN-6 (Compound 13a) is a non-nucleoside reverse transcriptase inhibitor (NNRT) used to inhibit HIV-1 reverse transcriptase (HIV-1RT), with an IC50 of 0.41 μM. It effectively suppresses both wild-type HIV-1 and mutants L100I, K103N, Y181C, Y188L, E138K, F227L/V106A, and RES056, with an EC50 range of 6.2-250 nM.

NNRT-IN-4 (Compound 10p) is an inhibitor of non-nucleoside reverse transcriptase (NNRT) with an IC50 of 0.713 µM for HIV-1RT. It exhibits antiviral activity against both wild-type and mutant strains of HIV-1, with an EC50 ranging from 6 to 63 nM. NNRT-IN-4 shows weak inhibitory activity on hERG (IC50=25.9 µM) and CYP enzymes (IC50>50 µM). In mice, NNRT-IN-4 demonstrates good tolerance and safety at 2 g/kg.

NNRT-IN-10 is a potent, selective, and orally bioavailable non-nucleoside reverse transcriptase inhibitor (NNRTI) for HIV-1. The compound exhibits EC50 values ranging from 1.16 to 18.3 nM against HIV and its variants. NNRT-IN-10 has favorable pharmacokinetic properties and safety profile, making it suitable for research on AIDS caused by HIV-1.

NNRT-IN-9 (Compound EG28) is a non-nucleoside reverse transcriptase inhibitor (NNRT). It demonstrates strong antiviral and resistance-fighting activity against wild-type (WT) and various clinically relevant mutant strains (E138K and K103N + Y181C) of HIV-1, with EC50 values of 55 nM, 67 nM, and 3910 nM, respectively. NNRT-IN-9 is applicable in acquired immunodeficiency syndrome (AIDS) research.

isoGTP (Isoguanosine-5'-O-triphosphate) sodium is an isomer of guanosine 5'-triphosphate and a phosphorylated form of Crotonoside. In reverse transcriptase assays, isoGTP sodium inhibits transcription and induces T-to-C mutations. It holds potential for research on substrate specificity of fructose phosphate kinase and mutT homolog 1 (MTH1).

HIV-1-IN-84 (Compound 9) is a potent inhibitor of the HIV-1 non-nucleoside reverse transcriptase (HIV-1RT), with an IC50 of 33.89 μM and an EC50 of 540 nM. It shows promise for use in HIV infection research.

HIV-1-IN-83 (Compound 18E) is a non-nucleoside reverse transcriptase inhibitor targeting HIV-1. It demonstrates an IC50 of 0.45 μM against wild-type HIV-1 reverse transcriptase. HIV-1-IN-83 exhibits potent antiviral activity against both wild-type and mutant HIV-1 strains and enhances drug resistance in Y188L and RES056 mutants. The compound is non-toxic up to a concentration of 11.088 μM.

HIV-IN-12 (Compound A1) is a dual inhibitor targeting both HIV-1 Vif and reverse transcriptase (RT). It shows potential for use in HIV infection research.

HIV-1-IN-85 is an orally active HIV-1 inhibitor with an IC50 of 72 nM. It exhibits potent inhibitory activity against wild-type (WT) HIV-1 and single mutant strains resistant to non-nucleoside reverse transcriptase inhibitors (NNRTIs), such as L100I, K103N, Y181C, Y188L, and E138K. Additionally, it shows moderate inhibitory activity against double mutant strains (F227L+V106A, RES056). In ICR mice, HIV-1-IN-85 demonstrates good in vivo safety and is suitable for research on HIV-1 infection.

NNRT-IN-11 (14l) is a potent non-nucleoside reverse transcriptase (NNRT) inhibitor, exhibiting EC50 values ranging from 6.50 to 52.9 nM against both wild-type (WT) and a range of HIV-1 mutant strains. NNRT-IN-11 demonstrates antiviral properties.