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nonnucleoside compounds

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Cytochrome P450 (2) DNA/RNA Synthesis (1) HCV (1) Histone Methyltransferase (2) HIV (25) HIV Protease (1) Potassium Channel (1) Reverse Transcriptase (11)
By Research Areas:	Cancer (3) Infection (26) Inflammation/Immunology (1)
Click Chemistry:	Azide (1)

Inhibitors & Agonists

Click Chemistry

Targets Recommended: Isotope-Labeled Compounds ATTECs

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-W325699

HIV-1 inhibitor-48	HIV Reverse Transcriptase	Infection
HIV-1 inhibitor-48 (compound 13o) is a novel non-nucleoside reverse transcriptase inhibitor (NNRTI) and exhibits anti-HIV-1 activity .

HY-117725

S-2720	HIV Reverse Transcriptase	Infection
S-2720 is a potent inhibitor of both immunodeficiency virus type 1 reverse transcriptase (HIV-1 RT) and HIV-1 replication. The binding sites of S-2720 and the nonnucleoside compounds overlap. The small pocket in the p66 subunit-BI-RG-587 (HY-10570) complex is most likely the target of S-2720. S-2720 is a quinoxaline derivative, which is promising for research of HIV-1 infection .

HY-111204

MK3281	HCV	Infection
MK3281 (Compound 33) is a non-nucleoside hepatitis C virus (HCV) NS5B polymerase inhibitor, with an EC₅₀ of 28 nM for gt1a .

HY-149338

NNRT-IN-3	HIV Protease	Infection
NNRT-IN-3 (compound 8) is an HIV-1 non-nucleoside reverse transcriptase inhibitor (EC₅₀=0.01 μM) .

HY-126900

HI-253	HIV Reverse Transcriptase	Others
HI-253 is a non-nucleoside inhibitor of HIV-1 reverse transcriptase that has demonstrated greater activity than multiple anti-HIV compounds against both resistant and sensitive HIV-1 strains.

HY-168189

HIV-1 inhibitor-76	HIV	Infection
HIV-1 inhibitor-76 (compound 9t-2) is a non-nucleoside reverse transcriptase inhibitor of HIV-1. HIV-1 inhibitor-76 can be used in anti-HIV research .

HY-172996

NNRT-IN-8	HIV Reverse Transcriptase	Infection
NNRT-IN-8 (compound 9K) is a potent non-nucleoside reverse transcriptase inhibitor with EC₅₀ values of 0.0014, 0.0041, 0.0077 µM for WT HIV-1, K103N, E138K, respectively .

HY-174849

TdT-IN-1	DNA/RNA Synthesis	Cancer
TdT-IN-1 (Compound 8c) is a selective and non-nucleoside terminal deoxynucleotidyl transferase (TdT) inhibitor with IC₅₀s of 0.11 and 0.19 μM for Mg ²⁺ and Mn ²⁺. TdT-IN-1 can be used for leukaemias and skin cancer research .

HY-147370

HIV-1 inhibitor-46	HIV	Infection
HIV-1 inhibitor-46 (compound 13d) is a potent HIV-1 non-nucleoside reverse transcriptase inhibitor with an EC₅₀ value of 1.425 μM. HIV-1 inhibitor-46 can be used for the research of AIDS .

HY-159984

HIV-1 inhibitor-78	HIV	Infection
HIV-1 inhibitor-78 (compound 15f) is a potent and broad-spectrum non-nucleoside reverse transcriptase inhibitor, with an EC₅₀ of 3 nM for wild-type HIV-1. HIV-1 inhibitor-78 can be used for the research of HIV infection .

HY-176534

PRMT5-IN-52	Histone Methyltransferase	Cancer
PRMT5-IN-52 (Compound 17) is a non-nucleoside Protein Arginine Methyltransferase 5 (PRMT5) inhibitor with inhibitory rates of 20.2% at 10 μM. PRMT5-IN-52 has potent antitumor activity, promising for research of cancers, including lung, prostate cancer, and colorectal carcinoma .

HY-149928

NNRT-IN-1	HIV	Infection
NNRT-IN-1 (compound 8r) is a potent non-nucleoside reverse transcriptase (NNRT) inhibitor featuring significantly anti-resistance efficacy. NNRT-IN-1 inhibits the wild-type HIV-1 and five mutant strains with EC₅₀s in the nanomolar range. NNRT-IN-1 displays favorable pharmacokinetic properties .

HY-147904

HIV-IN-5	HIV	Infection
HIV-IN-5 (compound 5r) is a potent HIV-1 inhibitor, with an IC₅₀ of 0.16 μM. HIV-IN-5 shows inhibition of HIV DNA-dependent DNA polymerization activity, with an IC₅₀ of 2.18 μM. HIV-IN-5 can bind to NNIBP (NNRTIs (non-nucleoside reverse transcriptase inhibitors) binding pocket) .

HY-163110

NNRT-IN-2	HIV Reverse Transcriptase	Infection
NNRT-IN-2 (compound 7w) is an orally available non-nucleoside reverse transcriptase inhibitor (NNRTI) with broad inhibitory effects on wild-type HIV-1 and mutant strains. NNRT-IN-2 inhibits HIV-1 reverse transcriptase with an EC₅₀ of 22 nM. NNRT-IN-2 is insensitive to CYP and hERG and has good safety and pharmacokinetic characteristics .

HY-149991

HIV-1 inhibitor-56	HIV	Infection
HIV-1 inhibitor-56 (compound 12126065) is a potent *HIV-1 non-nucleoside* reverse transcriptase inhibitor. HIV-1 inhibitor-56 has antiviral activity against wild-type HIV-1 in TZM cells with an EC₅₀** value of 0.24 nM. HIV-1 inhibitor-56 penetrates the blood-brain barrier .

HY-144112

HIV-1 inhibitor-13	HIV	Infection
HIV-1 inhibitor-13 (compound 16c) is a orally active and potent HIV-1 non-nucleoside reverse transcriptase inhibitor (NNRTI), with IC₅₀ of 0.14 μM (HIV-1 RT). HIV-1 inhibitor-13 shows activity against a panel of HIV-1 resistant strains, with EC₅₀ values of 2.85-18.0 nM .

HY-147841

HIV-1 inhibitor-41	HIV Reverse Transcriptase	Infection
HIV-1 inhibitor-41 (Compound B23) is an orally active non-nucleoside HIV-1 reverse transcriptase inhibitor with EC₅₀ values of 20.8 nM and 50 nM against HIV-1 WT and mutant E138K strain, respectively. HIV-1 inhibitor-41 shows low hERG, no apparent CYP enzymatic inhibition and no acute toxicity .

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 .

HY-146018

HIV-1 inhibitor-23	HIV	Infection
HIV-1 inhibitor-23 (compound 12a) is a highly potent HIV-1 non-nucleoside reverse transcriptase inhibitor, with EC₅₀s of 24.9 nM and 10.4 nM for HIV-1 WT and HIV-1 K103N, respectively. HIV-1 inhibitor-23 has low cytotoxicity (CC₅₀ > 221 μM) and a favorable in vitro microsomal stability .

HY-174303

NNRT-IN-9	HIV Reverse Transcriptase	Infection
NNRT-IN-9 (Compound EG28) is a non-nucleoside reverse transcriptase (NNRT) inhibitor. NNRT-IN-9 has potent antiviral and anti-resistance activity against wild-type (WT) HIV-1 and various clinically relevant mutations (E138K and K103N + Y181C) with EC₅₀s of 55, 67 and 3910 nM, respectively. NNRT-IN-9 can be used for acquired immune deficiency syndrome (AIDS) research .

HY-147807

HIV-1 inhibitor-40	HIV Cytochrome P450	Infection
HIV-1 inhibitor-40 (Compound 4ab) is a non-nucleoside reverse transcriptase inhibitor (NNRTI) of HIV-1 with an EC₅₀ of 1.9 nM. HIV-1 inhibitor-40 displays weak CYP sensitivity with IC₅₀ values of 5.16 μM and 4.51 μM against CYP2C9 and CYP2C19, respectively. HIV-1 inhibitor-40 has no apparent in vivo acute toxicity .

HY-172408

NNRT-IN-6	Reverse Transcriptase HIV	Infection
NNRT-IN-6 (Compound 13a) is the non-nucleoside reverse transcriptase inhibitor (NNRT) for HIV-1 reverse transcriptase (HIV-1 RT) with IC₅₀ of 0.41 μM. NNRT-IN-6 inhibits HIV-1 wildtype and mutant strains L100I, K103N, Y181C, Y188L, E138K, F227L/V106A and RES056 with EC₅₀ of 6.2-250 nM .

HY-149005

PRMT5-IN-19	Histone Methyltransferase	Cancer
PRMT5-IN-19 (Compound 41) is an selective orally active non-nucleoside PRMT5 inhibitor with IC₅₀ values of 23.9 nM (radioactive biochemical assay) and 47 nM (AlphaLISA assay). PRMT5-IN-19 can occupy the SAM-binding pocket in PRMT5 and block methyltransferase activity, which displays good selectivity over other PRMTs and PKMTs. PRMT5-IN-19 inhibits cell proliferation by inducing cell apoptosis, and can be used for cancer-related research .

HY-146017

HIV-1 inhibitor-22	HIV	Infection
HIV-1 inhibitor-22 (compound 11a) is a potent HIV-1 non-nucleoside reverse transcriptase (RT) inhibitor, with an IC₅₀ value of 3.63 μM for HIV-1 RT. HIV-1 inhibitor-22 has antiretroviral activity against HIV-1 WT and K103N strains with EC₅₀s of 0.304 μM and 0.201 μM, also has low cytotoxicity (CC₅₀ > 227 μM)

HY-130241

Reverse transcriptase-IN-1	HIV	Infection
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-146015

HIV-1 inhibitor-21	HIV	Infection
HIV-1 inhibitor-21 (compound 9b) is a potent HIV-1 non-nucleoside reverse transcriptase (RT) inhibitor, with an IC₅₀ value of 0.55 μM for HIV-1 RT. HIV-1 inhibitor-21 has antiretroviral activity against HIV-1 WT and K103N strains with EC₅₀s of 12.7 nM and 10.4 nM, and has relatively low cytotoxicity (MT-4 cells CC₅₀ =10.2 μM) .

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) .

HY-15350

Trovirdine hydrochloride LY 300046 hydrochloride	Reverse Transcriptase	Others
Trovirdine hydrochloride, a phenethylthiazolylthiourea (PETT) derivative, is an HIV reverse transcriptase (RT) non-nucleoside inhibitor (NNI). A novel computer model of the RT/NNI binding pocket revealed spatial gaps around Trovirdine hydrochloride's pyridyl ring. Docking studies suggested that replacing this planar ring with a nonplanar piperidinyl or piperazinyl ring could better occupy the binding pocket, enhancing anti-HIV activity. Synthesized heterocyclic compounds based on this modification demonstrated greater potency than Trovirdine hydrochloride, effectively inhibiting HIV replication at nanomolar concentrations without cytotoxicity in infected peripheral blood mononuclear cells .

HY-152233

Reverse transcriptase-IN-4	HIV	Infection
Reverse transcriptase-IN-4 (compound F10) is a potent and selective non-nucleoside reverse transcriptase (NNRT) inhibitor with an EC₅₀ value of 0.053 μM for wild-type HIV-1 and an EC₅₀ value of 0.26 μM for HIV-1 mutant E138K . Reverse transcriptase-IN-4 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-149866

HIV-1 inhibitor-58	Cytochrome P450 HIV Reverse Transcriptase	Infection
HIV-1 inhibitor-58 (Compound 10c) is a broad-spectrum antiviral agent. HIV-1 inhibitor-58 is a non-nucleoside reverse transcriptase inhibitor. HIV-1 inhibitor-58 inhibits WT strain IIIB, NNRTI-resistant strains (such as K103N and E138K) in MT-4 cells, with EC₅₀ less than 50 nM. HIV-1 inhibitor-58 also inhibits CYP2C9 and CYP2C19 (IC₅₀: 2.06 μM, 1.91 μM). HIV-1 inhibitor-58 can be used for HIV infection reserch .

HY-146365

HIV-1 inhibitor-30	HIV	Infection Inflammation/Immunology
HIV-1 inhibitor-30 (compound 10i) is a potent HIV-1 inhibitor with an EC₅₀ value of 40 nM and an IC₅₀ value of 80 nM for HIV-1 RT DNA polymerase. HIV-1 inhibitor-30 has highly antiretroviral activity against seven non-nucleoside reverse transcriptase inhibitor (NNRTI)-resistant HIV-1 strains (RT-K103N; RT-Y181C; RT-K103N,Y181C; RT-L100I,K103N; RT-Y188L; RT-K103N,G190A; RT-K103N,V108I) with IC₅₀s of 0.04~1.42 μM. HIV-1 inhibitor-30 can be used for researching AIDS .

Cat. No.	Product Name		Classification

HY-152233

Reverse transcriptase-IN-4		Azide
Reverse transcriptase-IN-4 (compound F10) is a potent and selective non-nucleoside reverse transcriptase (NNRT) inhibitor with an EC₅₀ value of 0.053 μM for wild-type HIV-1 and an EC₅₀ value of 0.26 μM for HIV-1 mutant E138K . Reverse transcriptase-IN-4 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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