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HIV-1 reverse transcriptase inhibitory activity

" in MedChemExpress (MCE) Product Catalog:

19

Inhibitors & Agonists

5

Natural
Products

Targets Recommended:
Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-W719041
    1,6-Di-O-galloyl-β-D-glucose

    		HIV Reverse Transcriptase Infection
    1,6-Di-O-galloyl-β-D-glucose is a compound found in the fruit of Phyllanthus emblica. 1,6-Di-O-galloyl-β-D-glucose has HIV-1 reverse transcriptase (RT) inhibitory activity with an IC50 value of 270 μM. The inhibitory mechanism of 1,6-Di-O-galloyl-β-D-glucose is competitive inhibition of the template primer and non-competitive inhibition of the substrate (dTTP). 1,6-Di-O-galloyl-β-D-glucose can be used in anti-HIV research .
    1,6-Di-O-galloyl-β-D-glucose
  • HY-152161
    HIV-1 inhibitor-51

    		HIV Reverse Transcriptase Infection
    HIV-1 inhibitor-51, a non-nucleoside reverse transcriptase inhibitor (NNRTI), exhibits outstanding antiviral activity against WT HIV-1 (IIIB) and a panel of mutant strains. HIV-1 inhibitor-51 has high binding affinity (KD=2.50 μM) and inhibitory activity (IC50=0.03 μM) to WT HIV-1 RT. HIV-1 inhibitor-51 has EC50s of 2.22-53.3 nM for mutant strains (L100I, K103N, Y181C, Y188L, E138K, F227L + V106A, RES056) .
    HIV-1 inhibitor-51
  • HY-162461
    HIV-1 inhibitor-66

    		Reverse Transcriptase HIV Infection
    HIV-1 inhibitor-66 is an orally active non-nucleoside reverse transcription inhibitor (NNRTI). HIV-1 inhibitor-66 shows inhibitory activity against wild-type HIV-1 reverse transcriptase with an IC50 of 40 nM .
    HIV-1 inhibitor-66
  • HY-105249
    RDEA 806

    		HIV Reverse Transcriptase Infection
    RDEA 806 is an orally active non-nucleoside reverse transcriptase inhibitor (NNRTI) that exhibits potent in vitro inhibitory activity against both wild-type HIV-1 (EC50 = 3.05 nM) and NNRTI-resistant HIV-1 .
    RDEA 806
  • HY-N16422
    Mer-NF5003E

    		HIV HIV Protease Infection
    Mer-NF5003E is a non-nucleoside reverse transcriptase inhibitor targeting HIV-1 reverse transcriptase (RT) (EC50=50 μM). Mer-NF5003E exhibits inhibitory activity against wild-type HIV-1 and multiple NNRTI-resistant strains (e.g., K103N, Y181C). Mer-NF5003E is promising for research of HIV infections .
    Mer-NF5003E
  • HY-19869
    VRX-480773

    		HIV Reverse Transcriptase Infection
    VRX-480773 is an efficient non-nucleoside reverse transcriptase inhibitor (NNRTI), used for HIV infection. VRX-480773 has high specificity for HIV-1, with an EC50 for wild-type HIV-1 being 0.14 nM. VRX-480773 does not inhibit HIV-2, HBV or HCV, and has no effect on human DNA polymerase α/β. VRX-480773 retains inhibitory activity against Efavirenz (HY-10572) resistant strains, with EC50s mostly < 1 nM. VRX-480773 can be used for research on AIDS .
    VRX-480773
  • HY-150697
    HIV-1 inhibitor-44

    		HIV Others
    HIV-1 inhibitor-44 (compound 11l) is a HIV-1 reverse transcriptase inhibitor. HIV-1 inhibitor-44 shows inhibitory activity against wild-type HIV-1 strain with an EC50 value of 0.209 μM .
    HIV-1 inhibitor-44
  • HY-179348
    DPP9-IN-2

    		Dipeptidyl Peptidase HIV Pyroptosis Cancer
    DPP9-IN-2 is a selective, potent and orally active inhibitor of Dipeptidyl Peptidase 9 (DPP9 ) with an IC50 of 12.9 nM. DPP9-IN-2 shows a SI of 59 over DPP8, and shows no significant inhibitory activity against related peptidases including DPP2, DPP4, FAP, and PREP. DPP9-IN-2 can induce cancer cells pyroptosis and has weak synergistic anti-HIV-1 activity when combined with non-nucleoside reverse transcriptase inhibitor. DPP9-IN-2 can be used for the researches of cance rand infection .
    DPP9-IN-2
  • HY-N14666
    Agrocybin

    		Fungal HIV Reverse Transcriptase Infection
    Agrocybin is an antifungal peptide that exerts antifungal activity against several fungal species but lacks inhibitory activity against bacteria. Agrocybin attenuates the activity of HIV-1 reverse transcriptase .
    Agrocybin
  • HY-N17718
    Urushiol (15:3)

    3-[8'(Z), 11'(Z), 14'-Pentadecatrienyl] catechol

    		 HIV Reverse Transcriptase Infection Cancer
    Ursolic acid (15:3) (Compound 4) is a type of resiniferatoxin compound that can be found in the leaves of the tree Rhus verniciflua. Ursolic acid (15:3) exhibits moderate inhibitory activity against HIV-1 reverse transcriptase (b HIV-1 reverse transcriptase), with an IC50 value of 55.36 μM. Ursolic acid (15:3) shows strong cytotoxicity against both PC-3 and MRC-5 cells. Ursolic acid (15:3) can be used in the research of anti-HIV-1 infection and prostate cancer .
    Urushiol (15:3)
  • HY-151933
    HIV-1 inhibitor-49

    		HIV Reverse Transcriptase Infection
    HIV-1 inhibitor-49 is an orally active HIV-1 inhibitor, is a HEPT analog. HIV-1 inhibitor-49 possesses great pharmacokinetics profiles and potent non-nucleoside reverse transcriptase inhibitory activity (IC50=30 nM). HIV-1 inhibitor-49 exerts potential safety without acute toxicity in mouse model .
    HIV-1 inhibitor-49
  • HY-144113
    HIV-1 inhibitor-14

    		HIV Infection
    HIV-1 inhibitor-14 (compound 14b) is a highly potent and broad-spectrum HIV-1 non-nucleoside reverse transcriptase (RT) inhibitor with an EC50 of 0.14 μM for HIV-1 RT. HIV-1 inhibitor-14 has inhibitory activity against HIV-1 WT and resistant strains with EC50s of 5.79 ~ 28.3 nM .
    HIV-1 inhibitor-14
  • HY-146746
    HIV-1 inhibitor-19

    		HIV Infection
    HIV-1 inhibitor-19 is a potent HIV-1 non-nucleoside reverse transcriptase inhibitor (NNRTI). HIV-1 inhibitor-19 maintains its inhibitory activity against L100I, K103N and V106A/ F227L mutant strains with EC50s of 7.3 nM, 9.2 nM and 21.0 nM, respectively.
    HIV-1 inhibitor-19
  • HY-169920
    HIV-1 inhibitor-79

    		HIV Reverse Transcriptase Infection
    HIV-1 inhibitor-79 (Compound 3k) is an HIV inhibitor that exhibits significant inhibitory activity against HIV-1 and its common mutant strains (with IC50 values of 1.9, 1.9, 8.7, and 11 nM against HIV-1, K103, L100I, and E138K, respectively), and has low cytotoxicity and a high selectivity index (CC50 = 21.95 μM, SI = 11478). Additionally, HIV-1 inhibitor-79 also shows antiviral activity against HIV-2, with an EC50 value of 6.14 μM, and significantly inhibits the activity of HIV-1 reverse transcriptase (IC50 = 25 nM) .
    HIV-1 inhibitor-79
  • HY-146019A
    HIV-1 inhibitor-25

    		HIV Infection
    HIV-1 inhibitor-25 (compound R-12a) is a highly potent HIV-1 reverse transcriptase, with an IC50 value of 0.1061 μM. HIV-1 inhibitor-25 has high antiretroviral activity against WT HIV-1 with an EC50 of 13.6 nM, and exhibits relatively low cytotoxicity with a CC50 of 33.13 μM in MT-4 cells. HIV-1 inhibitor-25 also has inhibitory activity against HIV-1 mutant strains (L100I, K103N, Y181C, Y188L, E138K, F227L+V106A) with EC50 of 0.1961 ~ 5.8136 μM. HIV-1 inhibitor-25 can be used for researching AIDS .
    HIV-1 inhibitor-25
  • HY-162720
    NNRT-IN-4

    		HIV Potassium Channel Reverse Transcriptase Infection
    NNRT-IN-4 (Compound 10p) is an inhibitor for non-nucleoside reverse transcriptase (NNRT) with an IC50 of 0.713 µM for HIV-1 RT. NNRT-IN-4 exhibits antiviral efficacy, inhibits HIV-1 wildtype and mutant strains with EC50 of 6-63 nM. NNRT-IN-4 exhibits a slight inhibitory activities against hERG (IC50=25.9 µM) and CYP enzymes (IC50>50 µM). NNRT-IN-4 exhibits good tolerability and safety in mice (2 g/kg) .
    NNRT-IN-4
  • HY-14266A
    Dapivirine hydrochloride

    		Apoptosis Reverse Transcriptase Autophagy HIV Infection
    Dapivirine hydrochloride is a non-nucleoside reverse transcriptase inhibitor with antitumor activity. Dapivirine hydrochloride attenuates the proliferation of glioblastoma cells and induces apoptosis. Dapivirine hydrochloride modulates autophagy and activates Akt, Bad, and SAPK/JNK signaling pathways. Dapivirine hydrochloride has shown inhibitory effects on glioma cell growth both in vitro and in vivo. Dapivirine hydrochloride is also a promising drug candidate for topical microbial agents for the prevention of sexual transmission of HIV-1 .
    Dapivirine hydrochloride
  • HY-116973
    L 738372

    		HIV Infection
    L-738372 is a non-competitive reversible inhibitor of HIV-1 reverse transcriptase (RT) with an inhibition constant (Ki) of 140 nM against dTTP. When combined with any nucleoside analogs (such as azidothymidine triphosphate, didexoyinosine triphosphate, or didexoycytidine triphosphate), L-738372 exhibits synergistic inhibition of RT activity. L-738372 has 2-3 times more inhibitory potency against the azidothymidine-resistant RT (D67N, K70R, T215Y, K219Q) compared to the wild-type RT. L-738372 holds promise for research in the field of HIV virus treatment .
    L 738372
  • HY-N16888
    Peruvianoside II

    		HIV Integrase Reverse Transcriptase Infection
    Peruvianoside II is a flavanone glucoside compound. Peruvianoside II shows no inhibitory activity against both HIV-1 reverse transcriptase and HIV-1 integrase at concentrations below 100 μM. Peruvianoside II can be extracted from the leaves of Thevetia peruviana .
    Peruvianoside II

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