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Targets Recommended: Reverse Transcriptase
Results for "

reverse

" in MCE Product Catalog:

156

Inhibitors & Agonists

2

Screening Libraries

2

Biochemical Assay Reagents

19

Peptides

4

MCE Kits

18

Natural
Products

12

Isotope-Labeled Compounds

Cat. No. Product Name Target Research Areas
  • 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 IIIB, E138K and K103N mutants, respectively. Reverse transcriptase-IN-1 also has an IC50of 13.7 nM against HIV-1 reverse transcriptase enzyme.
  • HY-135330
    Lamivudine 13C,15N2

    HIV Reverse Transcriptase Infection
    Lamivudine 13C,15N2 is a labelled impurity of Lamivudine (BCH-189). Lamivudine is a nucleoside reverse transcriptase inhibitors (NRTIs), and can inhibit HIV reverse transcriptase 1/2 and the reverse transcriptase of hepatitis B virus.
  • HY-138592
    7-Deaza-2',3'-dideoxyguanosine

    7-Deaza-ddG

    HIV Infection
    7-Deaza-2',3'-dideoxyguanosine (7-Deaza-ddG) is a 2′,3′-dideoxynucleoside 5′-triphosphate, which can inhibit HIV-1 reverse transcriptase with a Ki of 25 nM.
  • HY-122935
    Nigranoic acid

    HIV Reverse Transcriptase Infection
    Nigranoic acid is a triterpenoid separated from Schisandra chinensis. Nigranoic acid inhibits HIV-1 reverse transcriptase. Nigranoic acid exhibits protective effects on brain through PARP/AIF signaling pathway in cerebral ischemia-reperfusion animal model.
  • HY-P2039
    Retrobradykinin

    Bradykinin Receptor Endogenous Metabolite Endocrinology Cardiovascular Disease
    Retrobradykinin has the reverse sequence of Bradykinin (HY-P0206). Retrobradykinin exhibits no kinin activity and can be used as a negative control for Bradykinin.
  • HY-118423
    SJ-3366

    IQP-0410

    HIV Inflammation/Immunology
    SJ-3366 (IQP-0410) is a potent inhibitor of HIV nonnucleoside reverse transcriptase. SJ-3366 (IQP-0410) inhibits HIV at sub-nanomolar concentrations primarily through a typical non-nucleoside mechanism.
  • HY-136548
    Tenofovir diphosphate

    TFV-DP

    Reverse Transcriptase Infection Inflammation/Immunology
    Tenofovir diphosphate (TFV-DP) is a competitive DNA polymerases inhibitor (with respect to dATP) and a substrate of HIV type 1 (HIV-1) reverse transcriptase (RT).
  • HY-132291
    HIV-1 inhibitor-8

    HIV Infection
    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-136548A
    Tenofovir diphosphate triethylamine

    TFV-DP triethylamine

    Reverse Transcriptase Infection Inflammation/Immunology
    Tenofovir diphosphate triethylamine (TFV-DP triethylamine) is a competitive DNA polymerases inhibitor (with respect to dATP) and a substrate of HIV type 1 (HIV-1) reverse transcriptase (RT).
  • HY-105240
    Delparantag

    PMX-60056

    Factor Xa Cardiovascular Disease
    Delparantag (PMX-60056) is a salicylamide derivative and an effective unfractionated heparin (UFH) and low molecular weight heparin (LMWH) reversing agent. Delparantag shows ability to neutralize the anticoagulation and bleeding effects of UFH and LMWH.
  • HY-19509
    IQP-0528

    Reverse Transcriptase HIV Infection
    IQP-0528 is a highly potent nonnucleoside reverse transcriptase inhibitor (NNRTI). IQP-0528 shows nanomolar activity against both HIV-1 and HIV-2, with an HIV-1 EC50 of 0.2 nM and an HIV-2 EC50 of 100 nM.
  • HY-15353
    Emivirine

    MKC-442

    HIV Infection Inflammation/Immunology
    Emivirine (MKC-442) is a non-nucleoside reverse transcriptase inhibitors (NNRTIs) with Ki values of 0.20 and 0.01 μM for dTTP- and dGTP-dependent DNA or RNA polymerase activity, respectively. Emivirine displays potent and selective anti-human immunodeficiency virus type 1 (HIV-1) activity.
  • HY-145110
    IGF-1R inhibitor-2

    IGF-1R Cancer
    IGF-1R inhibitor-2 (example 121) is an insulin-like growth factor-1 receptor (IGF-1R) inhibitor. Downregulation of IGF-1R can reverse the transformed phenotype of tumor cells and potentially render them susceptible to apoptosis.
  • HY-14267
    Lersivirine

    UK-453061

    HIV Reverse Transcriptase Infection
    Lersivirine (UK-453061) is potent and selective non-nucleoside reverse transcription inhibitor (NNRTI; IC50=119 nM) with excellent efficacy against NNRTI-resistant viruses. Lersivirine exhibits potent antiretroviral activity against wild-type HIV virus and clinically relevant NNRTI-resistant strains.
  • HY-105268
    AzddMeC

    CS-92

    HIV Reverse Transcriptase Nucleoside Antimetabolite/Analog Infection
    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.
  • HY-122470
    Stampidine

    Reverse Transcriptase HIV Infection
    Stampidine is a nucleoside reverse transcriptase inhibitor (NRTI) with potent and broad-spectrum anti-HIV activity. Stampidine inhibits the laboratory HIV-1 strain HTLVIIIB (B-envelope subtype) and primary clinical isolates with IC50s of 1 nM and 2 nM, respectively. Stampidine also inhibits NRTI-resistant primary clinical isolates and NNRTI-resistant clinical isolates with IC50s of 8.7 nM and 11.2 nM, respectively.
  • HY-10574
    Rilpivirine

    R278474; TMC278; DB08864

    HIV Reverse Transcriptase Infection
    Rilpivirine (R278474) is a potent and specific diarylpyrimidine (DAPY) non-nucleoside reverse transcriptase inhibitor (NNRTI). Rilpivirine has high antiviral activity against wild-type HIV (EC50=0.4 nM) and mutant viruses (EC50=0.1-2.0 nM). Rilpivirine has a high genetic barrier to resistance development of HIV.
  • HY-B0250
    Lamivudine

    BCH-189

    HIV Reverse Transcriptase Infection
    Lamivudine (BCH-189) is a nucleoside reverse transcriptase inhibitors (NRTIs). Lamivudine (BCH-189) can inhibit HIV reverse transcriptase 1/2 and also the reverse transcriptase of hepatitis B virus.
  • HY-N0425
    Epoxylathyrol

    P-glycoprotein Cancer
    Epoxylathyrol, an epoxylathyrane derivative isolated from the Euphorbia boetica, is a P-glycoprotein (P-gp) inhibitor. Epoxylathyrol is a P-gp-mediated multidrug resistance (MDR) reverser.
  • HY-100079
    9-Propenyladenine

    Mutagenic Impurity of Tenofovir Disoproxil; Tenofovir Impurity 2

    HIV Infection
    9-Propenyladenine is a mutagenic impurity in tenofovir disoproxil fumarate. Tenofovir is an antiretroviral drug known as nucleotide analogue reverse transcriptase inhibitors, which block reverse transcriptase, a crucial virus enzyme in HIV-1 and HBV.
  • HY-17423
    Abacavir

    HIV Reverse Transcriptase Apoptosis Infection
    Abacavir is a potent nucleoside analog reverse-transcriptase inhibitor (NRTI).
  • HY-100079A
    (Z)-9-Propenyladenine

    (Z)-Mutagenic Impurity of Tenofovir Disoproxil

    HIV Infection
    (Z)-9-Propenyladenine is a mutagenic impurity in tenofovir disoproxil fumarate. Tenofovir is an antiretroviral drug known as nucleotide analogue reverse transcriptase (NtART) inhibitor, which blocks reverse transcriptase, a crucial virus enzyme in HIV-1 and HBV.
  • HY-B0249
    Didanosine

    2',3'-Dideoxyinosine; ddI

    HIV Reverse Transcriptase Infection
    Didanosine(Videx) is a reverse transcriptase inhibitor with an IC50 of 0.49 μM.
  • HY-13910A
    Tenofovir hydrate

    GS 1278 hydrate; PMPA hydrate

    HIV Reverse Transcriptase Infection
    Tenofovir hydrate is a nucleotide reverse transcriptase inhibitor to treat HIV and chronic Hepatitis B.
  • HY-90005
    Etravirine

    R165335; TMC125

    Reverse Transcriptase HIV Infection
    Etravirine is a non-nucleoside reverse transcriptase inhibitor (NNRTI) used for the treatment of HIV.
  • HY-17392
    Zalcitabine

    2',3'-Dideoxycytidine; ddC; Dideoxycytidine

    HIV Reverse Transcriptase Infection
    Zalcitabine is a potent nucleoside analogue reverse transcriptase inhibitor used in the treatment of HIV infection.
  • HY-13910B
    Tenofovir maleate

    GS 1278 maleate; PMPA maleate

    HIV Reverse Transcriptase Infection
    Tenofovir Disoproxil Fumarate is a nucleotide reverse transcriptase inhibitor to treat HIV and chronic Hepatitis B.
  • HY-100260
    beta-L-D4A

    2'3'-didehydro-2'3'-dideoxyadenosine

    HIV Infection
    beta-L-D4A is a nucleoside HIV-1 reverse transcriptase inhibitor.
  • HY-13782
    Tenofovir Disoproxil fumarate

    Tenofovir DF; Bis(POC)-PMPA fumarate; GS 4331 fumarate

    HIV Reverse Transcriptase HBV Infection
    Tenofovir Disoproxil fumarate is a nucleotide reverse transcriptase inhibitor used to treat HIV and chronic Hepatitis B.
  • HY-101791
    P-gp inhibitor 1

    P-glycoprotein Cancer
    P-gp inhibitor 1 is a novel inhibitor reversing P-glycoprotein-mediated multidrug resistance.
  • HY-16767
    Doravirine

    MK-1439

    HIV Reverse Transcriptase Infection
    Doravirine (MK-1439) is a highly specific HIV-1 nonnucleoside reverse transcriptase inhibitor with IC50s of 4.5 nM, 5.5 nM and 6.1 nM against the wild type and K103N and Y181C reverse transcriptase mutants, respectively.
  • HY-15355
    Loviride

    R 89439

    Reverse Transcriptase HIV Infection
    Loviride (R 89439) is a non-nucleoside reverse transcriptase inhibitor (NNRTI), with an IC50 of 0.3 µM for reverse transcriptase from HIV-1. Loviride (R 89439) inhibits HIV-1, HIV-2 and SIV replication in MT-4 cells.
  • HY-14266
    Dapivirine

    TMC120; R147681

    HIV Reverse Transcriptase Apoptosis Autophagy Infection
    Dapivirine (TMC120), the prototype of diarylpyrimidines (DAPY), is an orally active and nonnucleoside reverse transcriptase inhibitor (NRTI). Dapivirine (TMC120) binds directly to HIV-1 reverse transcriptase. Dapivirine (TMC120) regulates autophagy and induced Akt, Bad and SAPK/JNK activations.
  • HY-N0459
    3,5-O-Dicaffeoylquinic acid

    Others Neurological Disease
    3,5-O-Dicaffeoylquinic acid reverses Trimethyltin-induced learning and memory deficits.
  • HY-109056
    Elsulfavirine

    HIV Infection
    Elsulfavirine is a reverse transcriptase inhibitors for HIV-1 infection and is a new anti-HIV drug.
  • HY-13782A
    Tenofovir Disoproxil

    Bis(POC)-PMPA; GS 4331

    HIV Reverse Transcriptase HBV Cancer
    Tenofovir Disoproxil (Bis(POC)-PMPA) is a nucleotide reverse transcriptase inhibitor to treat HIV and chronic Hepatitis B.
  • HY-B1744
    Pyridoxal phosphate

    Pyridoxal 5′-phosphate; Pyridoxyl phosphate

    Reverse Transcriptase Endogenous Metabolite Neurological Disease
    Pyridoxal phosphate is the active form of vitamin B6, acts as an inhibitor of reverse transcriptases, and is used for the treatment of tardive dyskinesia.
  • HY-A0142A
    Dapiprazole hydrochloride

    Adrenergic Receptor Endocrinology
    Dapiprazole hydrochloride is a potent α-adrenergic blocking drug, which is used to reverse mydriasis after eye examination.
  • HY-17423A
    Abacavir sulfate

    Abacavir Hemisulfate; ABC sulfate

    Reverse Transcriptase Apoptosis Infection
    Abacavir sulfate (ABC) is a powerful nucleoside analog reverse transcriptase inhibitor (NRTI) used to treat HIV and AIDS.
  • HY-100298
    Caldaret

    MCC-135

    Na+/Ca2+ Exchanger Cardiovascular Disease
    Caldaret is an intracellular Ca 2+ handling modulator that acts through reverse mode Na +/Ca 2+ exchanger inhibition.
  • HY-13910
    Tenofovir

    GS 1278; PMPA

    Reverse Transcriptase HIV HBV Infection
    Tenofovir (GS 1278) is a nucleotide reverse transcriptase inhibitor to treat HIV and chronic Hepatitis B (HBV).
  • HY-N2571
    Corydine

    Reverse Transcriptase HIV Infection
    Corydine is a naturally occurring alkaloid which can be extracted from plants such as Croton echinocarpus leaves. Corydine is efficient on inhibiting reverse transcriptase (RT) activity with an IC50 of 356.8 μg/mL. Corydine displays significant in vitro anti-HIV potential, inhibiting 40% of the HIV-1 reverse transcriptase enzyme activity at a concentration of 450 μg/mL of Corydine.
  • HY-17013
    Dofequidar

    P-glycoprotein Cancer
    Dofequidar(MS-209) is a novel quinoline compound, which can reverse P-glycoprotein (P-gp)-mediated MDR.
  • HY-106268A
    Larazotide acetate

    Gap Junction Protein Inflammation/Immunology
    Larazotide acetate is a synthetic peptide. Larazotide acetate acts as a tight junction regulator and reverses leaky junctions to their normally closed state.
  • HY-17427
    Emtricitabine

    BW1592

    HIV Reverse Transcriptase Infection
    Emtricitabine is a nucleoside reverse transcriptase inhibitor (NRTI) with an EC50 of 0.01 µM in PBMC cell. It is an antiviral drug for the treatment of HIV infection.
  • HY-15232
    Tenofovir alafenamide

    GS-7340

    HIV Reverse Transcriptase Infection
    Tenofovir alafenamide (GS-7340) is an investigational oral prodrug of Tenofovir. Tenofovir is a HIV-1 nucleotide reverse transcriptase inhibitor.
  • HY-15232A
    Tenofovir alafenamide fumarate

    GS-7340 (fumarate)

    HIV Reverse Transcriptase Infection
    Tenofovir alafenamide fumarate (GS-7340 fumarate) is an investigational oral prodrug of Tenofovir. Tenofovir is a HIV-1 nucleotide reverse transcriptase inhibitor.
  • HY-103038
    ML327

    c-Myc Autophagy Cancer
    ML327 is a blocker of MYC which can also de-repress E-cadherin transcription and reverse Epithelial-to-Mesenchymal Transition (EMT).
  • HY-10570
    Nevirapine

    BI-RG 587; NSC 641530; NVP

    HIV Reverse Transcriptase Infection Cancer
    Nevirapine is a non-nucleoside inhibitor of HIV-1 reverse transcriptase used to treat and prevent HIV/AIDS; with a Ki of 270 μM.
  • HY-138657
    NCGC00378430

    Phosphatase Cancer
    NCGC00378430 is a potent SIX1/EYA2 interaction inhibitor. NCGC00378430 partially reverses transcriptional and metabolic profiles mediated by SIX1 overexpression and reverses SIX1-induced TGF-β signaling and epithelial-mesenchymal transition (EMT). NCGC00378430 inhibits SIX1-mediated breast cancer metastasis in a mouse model.
  • HY-100096
    Emtricitabine S-oxide

    Emtricitabine sulfoxide; Emtricitabine Degradant-III

    HIV Reverse Transcriptase Infection
    Emtricitabine S-oxide (Emtricitabine sulfoxide) is a major degradation product of Emtricitabine. Emtricitabine is a potent nucleoside reverse transcriptase inhibitor used for the treatment of HIV infection.
  • HY-B1169
    Timonacic

    1,3-Thiazolidine-4-carboxylic acid

    Others Cancer Cardiovascular Disease
    Timonacic is used as an adjuvant in the treatment of acute and hepatic disorders. It has also been used for the treatment of some cases of cancer, through the induction of the reverse transformation.
  • HY-15232B
    Tenofovir alafenamide hemifumarate

    GS-7340 (hemifumarate)

    HIV Reverse Transcriptase Infection
    Tenofovir alafenamide hemifumarate (GS-7340 hemifumarate) is an investigational oral prodrug of Tenofovir. Tenofovir is a HIV-1 nucleotide reverse transcriptase inhibitor.
  • HY-139262
    FNC-TP

    Reverse Transcriptase HIV HBV HCV Infection
    FNC-TP is the intracellular active form of FNC. FNC is a potent nucleoside reverse transcriptase inhibitor (NRTI), with antiviral activity on HIV, HBV and HCV.
  • HY-12495
    ISRIB (trans-isomer)

    PERK Autophagy Apoptosis Neurological Disease
    ISRIB (trans-isomer) is a potent inhibitor of PERK with an IC50 of 5 nM. ISRIB potently reverses the effects of eIF2α phosphorylation (IC50=5 nM).
  • HY-90005S
    Etravirine D4

    TMC-125 D4; R-165335 D4

    Reverse Transcriptase HIV Infection
    Etravirine D4 (TMC-125 D4) is the deuterium labeled Etravirine. Etravirine is a non-nucleoside reverse transcriptase inhibitor (NNRTI) used for the treatment of HIV.
  • HY-B1408
    Salicylanilide

    2-Hydroxybenzanilide

    HIV Integrase HIV Infection
    Salicylanilide demonstrates a wide range of biological activities including antiviral potency which can inhibit HIV virus by targeting HIV-1 integrase or reverse transcriptase.
  • HY-139262A
    FNC-TP trisodium

    Reverse Transcriptase HIV HBV HCV Infection
    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.
  • HY-17413
    Zidovudine

    Azidothymidine; AZT; ZDV

    HIV CRISPR/Cas9 Infection
    Zidovudine is a nucleoside reverse transcriptase inhibitor (NRTI), widely used to treat HIV infection. Zidovudine increases CRISPR/Cas9-mediated editing frequency.
  • HY-112912
    P-gp modulator 1

    P-glycoprotein Cancer
    P-gp modulator 1 is a high affinity, orally available modulator of P-glycoprotein (Pgp), can reverse the Pgp-mediated multidrug resistance ((MDR).
  • HY-121793
    Roemerine

    (-)-Roemerine

    P-glycoprotein Cancer
    Roemerine, an aporphine alkaloid, isolated from the leaves of Annona senegalensis, functions by interacting with P-glycoprotein. Roemerine reverses the multidrug-resistance phenotype with cultured cells.
  • HY-10571A
    Delavirdine mesylate

    U 90152 mesylate; BHAP-U 90152 mesylate

    HIV Reverse Transcriptase Infection
    Delavirdine (U 90152) mesylate is a potent, highly specific and orally active non-nucleoside reverse transcriptase inhibitor (NNRTI). Delavirdine mesylate selectively inhibits HIV-1 reverse transcriptase (RT) (IC50=0.26 μM) over DNA polymerase α (IC50=440 μM) and polymerase δ (IC50>550 μM). Delavirdine mesylate is an inhibitor of HIV-1 replication and can can be used for the study of AIDs.
  • HY-10571
    Delavirdine

    U 90152; BHAP-U 90152

    HIV Reverse Transcriptase Infection
    Delavirdine (U 90152) is a potent, highly specific and orally active non-nucleoside reverse transcriptase inhibitor (NNRTI). Delavirdine selectively inhibits HIV-1 reverse transcriptase (RT) (IC50=0.26 μM) over DNA polymerase α (IC50=440 μM) and polymerase δ (IC50>550 μM). Delavirdine is an inhibitor of HIV-1 replication and can can be used for the study of AIDs.
  • HY-W074930
    (S)-Tenofovir

    (S)-GS 1278; (S)-PMPA; (S)-TDF

    HIV HBV Infection
    (S)-Tenofovir ((S)-GS 1278) is the less active S-enantiomer of Tenofovir. Tenofovir is a nucleotide reverse transcriptase inhibitor to treat HIV and chronic Hepatitis B (HBV).
  • HY-123785
    ORM-10962

    Na+/Ca2+ Exchanger Metabolic Disease
    ORM-10962 is a potent, highly selective sodium-calcium exchanger (NCX) inhibitor, with IC50 values of 67 and 55 nM for the reverse and forward mode inhibition, respectively.
  • HY-15884
    GSK2838232

    HIV Infection
    GSK2838232 inhibit HIV reverse transcriptase activity across a broad panel of HIV-1 isolates, extracted from patent WO/2013090664A1, compound51.
  • HY-W008661
    Deoxyguanosine triphosphate trisodium salt

    dGTP trisodium salt; 2'-Deoxyguanosine-5'-triphosphate trisodium salt

    DNA/RNA Synthesis Others
    Deoxyguanosine triphosphate (dGTP) trisodium salt is a nucleotide precursor in cells for DNA synthesis. Deoxyguanosine triphosphate trisodium salt is used in reverse transcription-polymerase chain reaction (RT-PCR) for DNA amplification.
  • HY-B0255
    Adefovir dipivoxil

    GS 0840

    HBV Reverse Transcriptase Infection Cancer
    Adefovir dipivoxil, an adenosine analogue, is an oral prodrug of the nucleoside reverse transcriptase inhibitor Adefovir. Adefovir dipivoxil inhibits both the wild type and HBV Lamivudine-resistant strains.
  • HY-N2103
    Tenacissoside G

    Others Cancer
    Tenacissoside G is a C21 steroid from the stems of Marsdenia tenacissima. Tenacissoside G reverses multidrug resistance in P-glycoprotein (Pgp)-overexpressing multidrug-resistant cancer cells.
  • HY-10570S
    Nevirapine-D4

    HIV Reverse Transcriptase Neurological Disease
    Nevirapine-D4 is deuterium labeled Nevirapine. Nevirapine is a non-nucleoside inhibitor of HIV-1 reverse transcriptase used to treat and prevent HIV/AIDS; with a Ki of 270 μM.
  • HY-120832
    Azt-pmap

    HIV Infection
    Azt-pmap, a nucleoside analogue, is an aryl phosphate derivative of AZT. Azt-pmap shows anti-HIV activity. AZT is a nucleoside reverse transcriptase inhibitor (NRTI) for HIV infection.
  • HY-W013715A
    Deoxythymidine-5'-triphosphate trisodium salt

    dTTP trisodium salt

    DNA/RNA Synthesis Others
    Deoxythymidine-5'-triphosphate (dTTP) trisodium salt is one of the four natural deoxynucleotides. Deoxythymidine-5'-triphosphate trisodium salt is used for the biosynthesis of deoxyribonucleic acid by DNA polymerase and reverse transcriptase.
  • HY-111414
    Hsp90-Cdc37-IN-1

    HSP Cancer
    Hsp90-Cdc37-IN-1 is an Hsp90-Cdc37 interaction disruptor that inhibit cell migration and reverse drug resistance, with an IC50 of 140 nM.
  • HY-136978
    OP-5244

    CD73 Cancer Inflammation/Immunology
    OP-5244 is a potent and orally active inhibitor of CD73, with an IC50 of 0.25 nM. OP-5244 reverses immunosuppression through blocking of adenosine production, and has the potential for the cancer research.
  • HY-136978A
    OP-5244 sodium

    CD73 Cancer Inflammation/Immunology
    OP-5244 sodium is a potent and orally active inhibitor of CD73, with an IC50 of 0.25 nM. OP-5244 sodium reverses immunosuppression through blocking of adenosine production, and has the potential for the cancer research.
  • HY-N1916
    Coniferyl ferulate

    Gutathione S-transferase P-glycoprotein Cancer
    Coniferyl ferulate, a strong inhibitor of glutathione S-transferase (GST), reverses multidrug resistance and downregulates P-glycoprotein. Coniferyl ferulate shows strong inhibition of human placental GST with an IC50 of 0.3 μM.
  • HY-N3312
    Matairesinol

    Endogenous Metabolite Others Infection
    Matairesinol confers anti-allergic effects in an allergic dermatitis mouse model. DfE-induced changes in IL-4 and IFN-γ mRNA expression in the ears of NC/Nga mice were reversed by matairesinol application.
  • HY-10572
    Efavirenz

    DMP 266; EFV; L-743726

    Reverse Transcriptase HIV Autophagy Infection Cancer
    Efavirenz (DMP 266) is a potent inhibitor of the wild-type HIV-1 reverse transcriptase with a Ki of 2.93 nM and exhibits an IC95 of 1.5 nM for the inhibition of HIV-1 replicative spread in cell culture.
  • HY-132508S
    Etravirine-d8

    Reverse Transcriptase HIV Infection
    Etravirine-d8 (R165335-d8) is the deuterium labeled Etravirine. Etravirine (R165335) is a non-nucleoside reverse transcriptase inhibitor (NNRTI) used for the treatment of HIV.
  • HY-N0691
    Schisandrin

    Schizandrin; Schizandrol; Schizandrol-A

    Autophagy Inflammation/Immunology Cancer
    Schisandrin (Schizandrin), a dibenzocyclooctadiene lignan, is isolated from the fruit of Schisandra chinensis Baill. Schisandrin exhibits antioxidant, hepatoprotective, anti-cancer and anti-inflammatory activities. Schisandrin also can reverses memory impairment in rats.
  • HY-B1238
    Pronethalol

    (±)-Pronethalo

    Adrenergic Receptor Neurological Disease Cardiovascular Disease
    Pronethalol ((±)-Pronethalo) is a non-selective β-adrenergic antagonist. Pronethalol is a potent inhibitor of Sox2 expression. Pronethalol protects against and to reverse Digitalis-induced ventricular arrhythmias and limits the cerebral arteriovenous malformation (AVMs).
  • HY-113904S
    (Rac)-Tenofovir-d6

    Reverse Transcriptase HIV HBV Infection
    (Rac)-Tenofovir-d6 ((Rac)-GS 1278-d6) is a labelled racemic Tenofovir. Tenofovir (GS 1278) is a nucleotide reverse transcriptase inhibitor to treat HIV and chronic Hepatitis B (HBV).
  • HY-B1238A
    Pronethalol hydrochloride

    (±)-Pronethalo hydrochloride

    Adrenergic Receptor Neurological Disease Cardiovascular Disease
    Pronethalol ((±)-Pronethalo) is a non-selective β-adrenergic antagonist. Pronethalol is a potent inhibitor of Sox2 expression. Pronethalol protects against and to reverse Digitalis-induced ventricular arrhythmias, and limits the cerebral arteriovenous malformation (AVMs).
  • HY-106841
    Draflazine

    R-75231; R88021

    Others Inflammation/Immunology
    Draflazine (R-75231) is a ENT1 inhibitor. Draflazine (R-75231) completely reverses the hypersensitivity in the complete Freund’s adjuvant (CFA) model of mechanical hyperalgesia and the carrageenan inflammation model of thermal and mechanical hyperalgesia.
  • HY-19378
    MIV-150

    PC 815

    HIV Infection
    MIV-150 is a nonnucleoside reverse transcriptase (NNRT) inhibitor, blocking HIV-1 and HIV-2 infections, with an EC50<1 nM against HIV-1/HIV-2MN.
  • HY-13580
    Budesonide

    Glucocorticoid Receptor Cancer Inflammation/Immunology
    Budesonide, an inhaled glucocortical steroid, is an orally active glucocorticoid receptor agonist. Budesonide decreases the size of lung tumors, reverses DNA hypomethylation and modulates mRNA expression of genes. Budesonide is an anti-inflammatory agent used for asthma.
  • HY-B1744S
    Pyridoxal phosphate-d5

    Reverse Transcriptase Endogenous Metabolite Neurological Disease
    Pyridoxal phosphate-d5 (Pyridoxal 5′-phosphate-d5) is the deuterium labeled Pyridoxal phosphate. Pyridoxal phosphate is the active form of vitamin B6, acts as an inhibitor of reverse transcriptases, and is used for the treatment of tardive dyskinesia.
  • HY-P1290
    PKA Inhibitor Fragment (6-22) amide

    PKI-(6-22)-amide

    PKA Neurological Disease
    PKA Inhibitor Fragment (6-22) amide is an inhibitor of cAMP-dependent protein kinase A (PKA), with a Ki of 2.8 nM. PKA Inhibitor Fragment (6-22) amide can significantly reverse low-level morphine antinociceptive tolerance in mice.
  • HY-10570S1
    Nevirapine-d3

    HIV Reverse Transcriptase Infection Cancer
    Nevirapine-d3 (BI-RG 587-d3) is the deuterium labeled Nevirapine. Nevirapine is a non-nucleoside inhibitor of HIV-1 reverse transcriptase used to treat and prevent HIV/AIDS; with a Ki of 270 μM.
  • HY-124047
    RX 67668

    AChE Neurological Disease
    RX 67668 is a potent cholinesterase inhibitor with an IC50 of 5 μM for both acetylcholinesterase (AChE) and butyrylcholinesterase. RX 67668 can reverse the neuromuscular blockade induced by D-tubocurarine. RX 67668 is a muscle relaxant used to relieve skeletal muscle fatigue.
  • HY-138561
    EFdA-TP

    Reverse Transcriptase DNA/RNA Synthesis HIV Infection
    EFdA-TP is a potent nucleoside reverse transcriptase (RT) inhibitor. EFdA-TP inhibits RT-catalyzed DNA synthesis as an effective immediate or delayed chain terminator (ICT or DCT). EFdA-TP inhibits HIV-1 RT with multiple mechanisms.
  • HY-137522
    Zidovudine O-β-D-glucuronide sodium

    3'-Azido-3'-deoxythymidine β-D-glucuronide sodium

    Drug Metabolite Others
    Zidovudine O-β-D-glucuronide (3'-Azido-3'-deoxythymidine β-D-glucuronide) sodium is the major metabolite of Zidovudine. Zidovudine is a nucleoside reverse transcriptase inhibitor (NRTI), widely used to treat HIV infection.
  • HY-B1826
    Adefovir

    GS-0393; PMEA

    HBV Reverse Transcriptase Infection
    Adefovir (GS-0393) is an adenosine monophosphate analog antiviral agent that after intracellular conversion to Adefovir diphosphate inhibits HBV DNA polymerase. Adefovir has an IC50 of 0.7 μM against HBV in the HepG2.2.15 cell line. Adefovir has good antiviral activity against several viruses, including HBV and herpesviruses.
  • HY-P1290A
    PKA Inhibitor Fragment (6-22) amide TFA

    PKI-(6-22)-amide TFA

    PKA Neurological Disease
    PKA Inhibitor Fragment (6-22) amide TFA is an inhibitor of cAMP-dependent protein kinase A (PKA), with a Ki of 2.8 nM. PKA Inhibitor Fragment (6-22) amide TFA can significantly reverse low-level morphine antinociceptive tolerance in mice.
  • HY-16776
    Censavudine

    OBP-601; BMS-986001

    HIV Reverse Transcriptase Nucleoside Antimetabolite/Analog Infection
    Censavudine (OBP-601; BMS-986001), a nucleoside analog, is a nucleoside reverse transcriptase inhibitor. Censavudine is a potent HIV inhibitor with EC50 ranges from 30 nM to 81 nM and 450 nM to 890 nM for HIV-2 and HIV-1, respectively.
  • HY-N6608
    Physostigmine

    Eserine

    AChE Neurological Disease
    Physostigmine (Eserine) is a reversible acetylcholinesterase (AChE) inhibitor. Physostigmine can crosses the blood-brain barrier and stimulates central cholinergic neurotransmission. Physostigmine can reverse memory deficits in transgenic mice with Alzheimer's disease. Physostigmine is also an antidote for anticholinergic poisoning.
  • HY-111791
    ACY-1083

    HDAC Cancer
    ACY-1083 is a selective and brain-penetrating HDAC6 inhibitor with an IC50 of 3 nM and is 260-fold more selective for HDAC6 than all other classes of HDAC isoforms. ACY-1083 effectively reverses chemotherapy-induced peripheral neuropathy.
  • HY-132268
    Cav 2.2 blocker 2

    Calcium Channel Neurological Disease
    Cav 2.2 blocker 2 is a Cav2.2 calcium channel blocker extracted from patent WO2017046581A1, compound 1. Cav 2.2 blocker 2 can reverses hyperalgesia associated with an injury or inflammation in conjunction with the opioid.
  • HY-120504
    N-Acetyltyramine

    Bacterial Cancer Infection
    N-Acetyltyramine is a quorum-sensing inhibitor (QSI) compound produced by V. alginolyticus M3-10. N-Acetyltyramine is capable of inhibiting the QS of C. violaceum ATCC 12472. N-acetyltyramine reverses resistance in Doxorubicin-resistant leukemia P388 cells.
  • HY-13053
    Ro-0335

    Reverse Transcriptase Cancer
    RO-0335 is a novel and potent diphenylether nonnucleoside reverse transcriptase inhibitor(NNRTI). RO-0335 inhibits Wt HIV-1 with an IC50 of 1.1 nM and retained activity (IC50< 100 nM) against 92% of a large number of NNRTI-resistant clinical isolates.
  • HY-15415
    KB-R7943 mesylate

    Na+/Ca2+ Exchanger Autophagy Cancer
    KB-R7943 mesylate is a widely used inhibitor of the reverse Na +/Ca 2+ exchanger (NCXrev) with IC50 of 5.7±2.1 µM. KB-R7943 mesylate induces cancer cell death via activating the JNK pathway and blocking autophagic flux.
  • HY-141510
    myo-Inositol trispyrophosphate hexasodium

    ITPP hexasodium

    Others Cancer
    myo-Inositol trispyrophosphate (ITPP) hexasodium, a modifier of haemoglobin, is an allosteric effector that reduces the oxygen‐binding affinity of haemoglobin and facilitates the release of oxygen by red blood cells. myo-Inositol trispyrophosphate can reverse hypoxia, control tumor growth and improve chemotherapy response.
  • HY-138561A
    EFdA-TP tetraammonium

    Reverse Transcriptase DNA/RNA Synthesis HIV Infection
    EFdA-TP tetraammonium is a potent nucleoside reverse transcriptase (RT) inhibitor. EFdA-TP tetraammonium inhibits RT-catalyzed DNA synthesis as an effective immediate or delayed chain terminator (ICT or DCT). EFdA-TP tetraammonium inhibits HIV-1 RT with multiple mechanisms.
  • HY-138561B
    EFdA-TP tetrasodium

    Reverse Transcriptase DNA/RNA Synthesis HIV Infection
    EFdA-TP tetrasodium is a potent nucleoside reverse transcriptase (RT) inhibitor. EFdA-TP tetrasodium inhibits RT-catalyzed DNA synthesis as an effective immediate or delayed chain terminator (ICT or DCT). EFdA-TP tetrasodium inhibits HIV-1 RT with multiple mechanisms.
  • HY-136541
    YB-0158

    Wnt pathway inhibitor 2

    Wnt Apoptosis Cancer
    YB-0158 (Wnt pathway inhibitor 2) is a reverse-turn peptidomimetic and a potent colorectal cancer stem cell (CSC) targeting agent. YB-0158 disrupts Sam68-Src interactions and induces apoptosis in CRC cells. Anti-cancer activities.
  • HY-P1346
    APETx2

    Sodium Channel Inflammation/Immunology Neurological Disease
    APETx2, a sea anemone peptide from Anthopleura elegantissima, is a selective and reversible ASIC3 inhibitor, with an IC50 of 63 nM. APETx2 directly inhibits the ASIC3 channel by acting at its external side. APETx2 could reverses acid‐induced and inflammatory pain.
  • HY-19851
    Rovafovir etalafenamide

    GS-9131

    Reverse Transcriptase HIV Cancer
    Rovafovir etalafenamide (GS-9131), a prodrug 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-113986
    (R)-Fadrozole

    (R)-CGS 16949A free base; FAD286

    Others Cardiovascular Disease
    (R)-Fadrozole ((R)-CGS 16949A; FAD286) is a potent nonsteroidal inhibitor. (R)-Fadrozole also inhibits human placental aromatase (pIC50 = 6.17) and aldosterone biosynthesis. (R)-Fadrozole reverses cardiac fibrosis in spontaneously hypertensive heart failure rats..
  • HY-P1346A
    APETx2 TFA

    Sodium Channel Inflammation/Immunology Neurological Disease
    APETx2 TFA, a sea anemone peptide from Anthopleura elegantissima, is a selective and reversible ASIC3 inhibitor, with an IC50 of 63 nM. APETx2 directly inhibits the ASIC3 channel by acting at its external side. APETx2 could reverses acid‐induced and inflammatory pain.
  • HY-125810
    4'-Ethynyl-2'-deoxyadenosine

    HIV Reverse Transcriptase Infection Inflammation/Immunology
    4'-Ethynyl-2'-deoxyadenosine (4'-E-dA), a nucleoside reverse transcriptase (RT) inhibitor, is an antiretroviral agent which is potent against drug-resistant HIV variants, with an EC50 of 98 nM in MT-4 cells for anti-HIV-1 activity.
  • HY-N0462
    Corilagin

    Reverse Transcriptase Bacterial Cancer Infection Inflammation/Immunology
    Corilagin, a gallotannin, inhibits activity of reverse transcriptase of RNA tumor viruses. Corilagin inhibits the growth of Staphylococcus aureus with a MIC of 25 μg/mL. Corilagin shows good anti-tumor activity on hepatocellular carcinoma and ovarian cancer. Corilagin shows a low level of toxicity toward normal cells and tissues.
  • HY-13580S
    Budesonide-d8

    Glucocorticoid Receptor Cancer Inflammation/Immunology
    Budesonide-d8 is the deuterium labeled Budesonide. Budesonide, an inhaled glucocortical steroid, is an orally active glucocorticoid receptor agonist. Budesonide decreases the size of lung tumors, reverses DNA hypomethylation and modulates mRNA expression of genes. Budesonide is an anti-inflammatory agent used for asthma.
  • HY-10586
    5-Azacytidine

    Azacitidine; 5-AzaC; Ladakamycin

    Nucleoside Antimetabolite/Analog DNA Methyltransferase Bacterial Autophagy Antibiotic Cancer Infection
    5-Azacytidine (Azacitidine; 5-AzaC; Ladakamycin) is a nucleoside analogue of cytidine that specifically inhibits DNA methylation. 5-Azacytidine is incorporated into DNA to covalently trap DNA methyltransferases and contributes to reverse epigenetic changes. 5-Azacytidine induces cell autophagy.
  • HY-B1266
    Physostigmine salicylate

    Eserine salicylate

    AChE Neurological Disease
    Physostigmine salicylate (Eserine salicylate) is a reversible acetylcholinesterase (AChE) inhibitor. Physostigmine salicylate crosses the blood-brain barrier and stimulates central cholinergic neurotransmission. Physostigmine salicylate can reverse memory deficits in transgenic mice with Alzheimer's disease. Physostigmine salicylate is also an antidote for anticholinergic poisoning.
  • HY-104012
    Islatravir

    MK-8591

    HIV Reverse Transcriptase Infection
    Islatravir (MK-8591) is a potent anti-HIV-1 agent, acting as a nucleoside reverse transcriptase inhibitor, with EC50s of 0.068 nM, 3.1 nM and 0.15 nM for HIV-1 (WT), HIV-1 (M184V), HIV-1 (MDR), respectively.
  • HY-17427S
    Emtricitabine-15N,D2

    BW1592-15N,D2

    HIV Reverse Transcriptase Endogenous Metabolite Infection
    Emtricitabine-15N,D2 (BW1592-15N,D2) is a 15N-labeled and deuterium labeled Emtricitabine. Emtricitabine is a nucleoside reverse transcriptase inhibitor (NRTI) with an EC50 of 0.01 µM in PBMC cell. It is an antiviral drug for the treatment of HIV infection.
  • HY-N7135
    Tropolone

    Tyrosinase Others
    Tropolone, a  tropone derivative with a hydroxyl group in the 2-position, is a precursor of manyazulene derivatives such as methyl 2-methylazulene-1-carboxylate. Tropolone is a potent inhibitor of mushroom tyrosinase with a IC50 of 0.4 μM, and the inhibition can be reversed by dialysis or by excess CU 2+.
  • HY-130613
    MAC-545496

    Bacterial Infection
    MAC-545496 is a nanomolar inhibitor of glycopeptide-resistance-associated protein R (GraR). MAC-545496 displays strong binding affinity to the full-length GraR protein (Kd ≤ 0.1 nM). MAC-545496 is an antivirulence agent that reverses β-lactam resistance in Methicillin-resistant strains (MRSA).
  • HY-116999
    IR415

    HBV Infection
    IR415 is a potent anti-HBV agent and inhibits HBV replication by blocking the HBx activity. IR415 selectively interacts with HBx (Kd=2 nM) and blocks HBV-mediated RNAi suppression, reverses the inhibitory effect of HBx protein on the activity of the dicer endoribonuclease. HBx: hepatitis B virus X protein.
  • HY-N2320
    Physostigmine hemisulfate

    Eserine hemisulfate

    AChE Neurological Disease
    Physostigmine hemisulfate (Eserine hemisulfate) is a reversible acetylcholinesterase (AChE) inhibitor. Physostigmine hemisulfate can crosses the blood-brain barrier and stimulates central cholinergic neurotransmission. Physostigmine hemisulfate can reverse memory deficits in transgenic mice with Alzheimer's disease. Physostigmine hemisulfate is also an antidote for anticholinergic poisoning.
  • HY-112210
    Shield-1

    FKBP Others
    Shield-1 is a specific, cell-permeant and high-affinity ligand of FK506-binding protein-12 (FKBP), and reverses the instability by binding to mutated FKBP (mtFKBP), allowing conditional expression of mtFKBP-fused proteins. Shield-1 can stabilize the entire fusion protein.
  • HY-W010041
    Scyllo-Inositol

    Amyloid-β Endogenous Metabolite Neurological Disease
    Scyllo-Inositol, an amyloid inhibitor, potentialy inhibits α-synuclein aggregation. Scyllo-Inositol stabilizes a non-fibrillar non-toxic form of amyloid-β peptide (Aβ42) in vitro, reverses cognitive deficits, and reduces synaptic toxicity and lowers amyloid plaques in an Alzheimer's disease mouse model.
  • HY-B1238S
    Pronethalol-d6

    Adrenergic Receptor Neurological Disease Cardiovascular Disease
    Pronethalol-d6 ((±)-Pronethalo-d6) is the deuterium labeled Pronethalol. Pronethalol ((±)-Pronethalo) is a non-selective β-adrenergic antagonist. Pronethalol is a potent inhibitor of Sox2 expression. Pronethalol protects against and to reverse Digitalis-induced ventricular arrhythmias and limits the cerebral arteriovenous malformation (AVMs).
  • HY-114268
    BRD-K98645985

    HIV Infection
    BRD-K98645985 is a BAF (mammalian SWI/SNF) transcriptional repression inhibitor with an EC50 of ~2.37 µM. BRD-K98645985 binds ARID1A-specific BAF complexes, prevents nucleosomal positioning, and potently reverses HIV-1 latency, without T cell activation or toxicity.
  • HY-139848
    WS-898

    P-glycoprotein Cancer
    WS-898 is a highly effective ABCB1 inhibitor capable of reversing paclitaxel (PTX) resistance in drug-resistant SW620/Ad300, KB-C2, and HEK293/ABCB1 cells (IC50 = 5.0, 3.67, and 3.68 nM, respectively).
  • HY-126781
    Fozivudine tidoxil

    BM-211290

    HIV DNA/RNA Synthesis Infection
    Fozivudine tidoxil (BM-211290) is an orally active thioether lipid-zidovudine (ZDV) conjugate with anti-HIV activity. Fozivudine tidoxil, a member of the NRTI family of drug, is incorporated into the newly synthesized strand of DNA during intracellular viral replication and irreversibly binds viral RT which disrupts viral reverse-transcription.
  • HY-10572S
    Efavirenz-d5

    Reverse Transcriptase HIV Autophagy Infection Cancer
    Efavirenz-d5 (DMP 266-d5) is the deuterium labeled Efavirenz. Efavirenz (DMP 266) is a potent inhibitor of the wild-type HIV-1 reverse transcriptase with a Ki of 2.93 nM and exhibits an IC95 of 1.5 nM for the inhibition of HIV-1 replicative spread in cell culture.
  • HY-116686
    Inz-1

    Cytochrome P450 Fungal Infection
    Inz-1 is a potent and selective mitochondrial cytochrome bc1 inhibitor for yeast (IC50=8.092 μM) over humans (IC50=45.320 μM). Inz-1 reverses Fluconazole (HY-B0101) or other triazole antifungals’ resistance in the pathogenic fungus Candida albicans.
  • HY-10572BS
    (Rac)-Efavirenz-d4

    Reverse Transcriptase HIV Autophagy Infection Cancer
    (Rac)-Efavirenz-d4 ((Rac)-DMP 266-d4) is a labelled racemic Efavirenz. Efavirenz (DMP 266) is a potent inhibitor of the wild-type HIV-1 reverse transcriptase with a Ki of 2.93 nM and exhibits an IC95 of 1.5 nM for the inhibition of HIV-1 replicative spread in cell culture.
  • HY-103157
    PD146176

    NSC168807

    Autophagy Ferroptosis Cardiovascular Disease
    PD146176 (NSC168807), a 15-Lipoxygenase (15-LO) inhibitor, inhibits rabbit reticulocyte 15-LO (Ki=197 nM, IC50=0.54 μM). PD146176 reverses cognitive impairment, brain amyloidosis, and tau pathology by stimulating autophagy in aged triple transgenic mice.
  • HY-103442
    CGP52411

    DAPH

    EGFR Amyloid-β Cancer Neurological Disease
    CGP52411 (DAPH) is a high selective, potent, orally active and ATP-competitive EGFR inhibitor with an IC50 of 0.3 μM. CGP52411 blocks the toxic influx of Ca 2+ ions into neuronal cells, and dramatic inhibits and reverses the formation of β-amyloid (Aβ42) fibril aggregates associated with Alzheimer's disease.
  • HY-B0116
    Stavudine

    d4T

    Reverse Transcriptase HIV Nucleoside Antimetabolite/Analog NOD-like Receptor (NLR) Autophagy Apoptosis Infection
    Stavudine (d4T) is an orally active nucleoside reverse transcriptase inhibitor (NRTI). Stavudine has activity against HIV-1 and HIV-2. Stavudine also inhibits the replication of mitochondrial DNA (mtDNA). Stavudine reduces NLRP3 inflammasome activation and modulates Amyloid-β autophagy. Stavudine induces apoptosis.
  • HY-B0116A
    Stavudine sodium

    d4T sodium

    Reverse Transcriptase HIV Nucleoside Antimetabolite/Analog NOD-like Receptor (NLR) Autophagy Apoptosis Infection
    Stavudine (d4T) sodium is an orally active nucleoside reverse transcriptase inhibitor (NRTI). Stavudine sodium has activity against HIV-1 and HIV-2. Stavudine sodium also inhibits the replication of mitochondrial DNA (mtDNA). Stavudine sodium reduces NLRP3 inflammasome activation and modulates Amyloid-β autophagy. Stavudine sodium induces apoptosis.
  • HY-117147A
    GSK2945 hydrochloride

    Cytochrome P450 Metabolic Disease
    GSK2945 hydrochloride is a class of tertiary amine, and is a highly specific Rev-erbα/REV-ERBα (mouse/human reverse erythroblastosis virus α) antagonist with EC50s of 21.5 μM and 20.8 μM, respectively. GSK2945 hydrochloride enhances cholesterol 7α-hydroxylase (CYP7A1) level and cholesterol metabolism.
  • HY-117147
    GSK2945

    Cytochrome P450 Metabolic Disease
    GSK2945 is a class of tertiary amine, and is a highly specific Rev-erbα/REV-ERBα (mouse/human reverse erythroblastosis virus α) antagonist with EC50s of 21.5 μM and 20.8 μM, respectively. GSK2945 enhances cholesterol 7α-hydroxylase (CYP7A1) level and cholesterol metabolism.
  • HY-101511
    TTT-28

    P-glycoprotein Cancer
    TTT-28 is a synthesized thiazole-valine peptidomimetic, a novel selective inhibitor of ABCB1 (P-gp/MDR1) with high efficacy and low toxicity, which reverses the ATP-binding cassette sub-family B member 1 (ABCB1)-mediated Multidrug resistance (MDR) by selectively blocking the efflux function of ABCB1.
  • HY-N1457
    Chrysosplenetin

    P-glycoprotein Cytochrome P450 Ferroptosis Metabolic Disease
    Chrysosplenetin is one of the polymethoxylated flavonoids in Artemisia annua L. (Compositae) and other several Chinese herbs. Chrysosplenetin inhibits P-gp activity and reverses the up-regulated P-gp and MDR1 levels induced by artemisinin (ART). Chrysosplenetin significantly augments the rat plasma level and anti-malarial efficacy of ART, partially due to the uncompetitive inhibition effect of Chrysosplenetin on rat CYP3A.
  • HY-139467
    PF-04577806

    PKC Metabolic Disease
    PF-04577806 is a potent, selective and ATP competitive PKC inhibitor. PF-04577806 shows potent inhibitory activity towards PKCα, PKCβI, PKCβII, PKCγ, and PKCθ with IC50s of 2.4 nM, 8.1 nM, 6.9 nM, 45.9 nM, and 29.5 nM, respectively. PF-04577806 can reverse retinal vascular leakage in diabetic rats.
  • HY-19314A
    Azvudine hydrochloride

    RO-0622 hydrochloride; FNC hydrochloride

    Reverse Transcriptase HIV HBV HCV Infection
    Azvudine (RO-0622) hydrochloride is a potent nucleoside reverse transcriptase inhibitor (NRTI), with antiviral activity on HIV, HBV and HCV. Azvudine hydrochloride exerts highly potent inhibition on HIV-1 (EC50s ranging from 0.03 to 6.92 nM) and HIV-2 (EC50s ranging from 0.018 to 0.025 nM). Azvudine hydrochloride inhibits NRTI-resistant viral strains.
  • HY-19314
    Azvudine

    RO-0622; FNC

    Reverse Transcriptase HIV HBV HCV Infection
    Azvudine (RO-0622) is a potent nucleoside reverse transcriptase inhibitor (NRTI), with antiviral activity on HIV, HBV and HCV. Azvudine exerts highly potent inhibition on HIV-1 (EC50s ranging from 0.03 to 6.92 nM) and HIV-2 (EC50s ranging from 0.018 to 0.025 nM). Azvudine inhibits NRTI-resistant viral strains.
  • HY-P1726A
    MSG606 TFA

    Melanocortin Receptor
    MSG606 TFA is a potent human MC1 receptor antagonist (IC50=17 nM). MSG606 TFA also partial agonist at human MC3 and MC5 receptors (EC50 values are 59 and 1300 nM, respectively). MSG606 TFA exhibits binding affinity for A375 melanoma cells in vitro. MSG606 TFA reverses morphine-induced hyperalgesia in female mice, with no effect in male mice.
  • HY-P1208
    PG-931

    Melanocortin Receptor Inflammation/Immunology
    PG-931, an analog of SHU 9119 (HY-P0227), is a potent melanocortin 4 (MC4) receptor (IC50=0.58 nM) agonist and is more selective than for the hMC3R (IC50=55 nM) or the hMC5R (IC50=2.4 nM). PG-931 can reverse haemorrhagic shock and prevent multiple organ damage in vivo.
  • HY-117626
    LP-935509

    Others Inflammation/Immunology Neurological Disease
    LP-935509 is a selective, ATP-competitive and brain-penetrant inhibitor of adapter protein-2 associated kinase 1 (AAK1) with an IC50 and a Ki of 3.3 nM and 0.9 nM, respectively. LP-935509 is also a potent inhibitor of BIKE (IC50=14 nM) and a modest inhibitor of GAK (IC50=320 nM). LP-935509 is highly brain-penetrant and reverses fully established pain behavior following the SNL procedure.
  • HY-12614
    AMG-1694

    Glucokinase Metabolic Disease
    AMG-1694 is a potent glucokinase–glucokinase regulatory protein (GK-GKRP) disruptors and promotes the dissociation of the GK-GKRP complex with an IC50 of 7 nM, indirectly increasing GK enzymatic activity. AMG-1694 potently reverses the inhibitory effect of GKRP on GK activity and promotes GK translocation. AMG-1694 normalizes blood glucose levels in several rodent models of diabetes and lowes blood glucose restricted to diabetic and not normoglycaemic animals.
  • HY-P1208A
    PG-931 TFA

    Melanocortin Receptor Inflammation/Immunology
    PG-931 TFA, an analog of SHU 9119 (HY-P0227), is a potent melanocortin 4 (MC4) receptor (IC50=0.58 nM) agonist and is more selective than for the hMC3R (IC50=55 nM) or the hMC5R(IC50=2.4 nM). PG-931 TFA can reverse haemorrhagic shock and prevent multiple organ damage in vivo.
  • HY-W014421
    AP-18

    TRP Channel Neurological Disease
    AP-18, a potent and selective TRPA1 inhibitor, blocks activation of TRPA1 by 50 μM Cinnamaldehyde with an IC50 of 3.1 μM and 4.5 μM for human and mouse TRPA1, respectively. AP-18 reverses complete Freund's adjuvant (CFA)-induced mechanical hyperalgesia in mice. AP-18 attenuated 30 μM AITC-induced Yo-Pro uptake in a concentration-dependent manner, with an IC50 of 10.3 μM.
  • HY-111640
    3'-Azido-3'-deoxy-5-methylcytidine

    HIV Reverse Transcriptase Infection
    3'-Azido-3'-deoxy-5-methylcytidine (CS-92) is a potent xenotropic murine leukemia-related retrovirus (XMRV) inhibitor with a CC50 of 43.5 μM in MCF-7 cells. 3'-Azido-3'-deoxy-5-methylcytidine also inhibits HIV-1 reverse transcriptase with an EC50 of 0.06 μM in peripheral blood mononuclear (PBM) cells.
  • HY-110155
    LM11A-31 dihydrochloride

    Others Neurological Disease
    LM11A-31 dihydrochloride, a non-peptide p75 NTR (neurotrophin receptor p75) modulator, is an orally active and potent proNGF (nerve growth factor) antagonist. LM11A-31 dihydrochloride is an amino acid derivative with high blood-brain barrier permeability and blocks p75-mediated cell death. M11A-31 dihydrochloride reverses cholinergic neurite dystrophy in Alzheimer's disease mouse models with mid- to late-stage disease progression.
  • HY-128851
    Coenzyme A

    Endogenous Metabolite Cancer Neurological Disease
    Coenzyme A is is an obligatory cofactor in all living cells synthesised from pantothenate (Vitamin B5), adenosine triphosphate (ATP) and cysteine. Covalent binding of Coenzyme A to Peroxiredoxin 5 (Prdx5) results in complete inhibition of its peroxidase activity, which is reversed by reduction with DTT.Coenzyme A and its thioester derivatives are key players in major catabolic and anabolic pathways and the regulation of gene expression. Many human pathologies, including cancer, diabetes and neurodegeneration, have been associated with abnormal biosynthesis and homeostasis of CoA and its derivatives.
  • HY-14565
    Pozanicline

    ABT-089

    nAChR Neurological Disease
    Pozanicline (ABT-089) selectively activate neuronal nicotinic acetylcholine receptor (nAChR) subtypes, is a novel cholinergic agent that is a partial agonist at α4β2* nAChRs (Ki=16 nM) and shows high selectivity for α6β2* and α4α5β2 nAChR subtypes, the binding affinity (Ki, rat) for Pozanicline to [ 3H] cytisine sites is 16.7 nM. Pozanicline reverses nicotine withdrawal-induced cognitive deficits, may be an effective component of novel therapeutic strategies for nicotine addiction.
  • HY-101044
    PPADS tetrasodium

    P2X Receptor Na+/Ca2+ Exchanger Neurological Disease
    PPADS tetrasodiuma is a non-selective P2X receptor antagonist. PPADS tetrasodiuma blocks recombinant P2X1, -2, -3, -5 with IC50s ranging from 1 to 2.6 μM. PPADS tetrasodiuma blocks native P2Y2-like (IC50~0.9 mM) and recombinant P2Y4 (IC50~15 mM) receptors. PPADS tetrasodiuma is an inhibitor of the reverse mode of the Na/Ca 2+ exchanger in guinea pig airway smooth muscle.
  • HY-14913
    Apricitabine

    SPD754; AVX754

    Nucleoside Antimetabolite/Analog HIV DNA/RNA Synthesis Infection
    Apricitabine (SPD754; AVX754), the (-) enantiomer of 2′-deoxy-3′-oxa-4′-thiocytidine (dOTC), is a highly selective and orally active HIV-1 reverse transcriptase (RT) inhibitor (Ki=0.08 μM), as well as inhibits DNA polymerases α, β, and γ with Ki value of 300 μM, 12 μM, and 112.25 μM, respectively. Apricitabine (SPD754; AVX754) shows promising antiretroviral efficacy, good tolerability and a low propensity for resistance selection in antiretroviral-naive HIV infection[2].
  • HY-120072
    PF-3450074

    PF-74

    HIV Infection
    PF-3450074 (PF-74) is a specifical inhibitor of HIV-1 capsid protein (CA) and displays a broad-spectrum inhibition of HIV isolates with submicromolar potency (EC50=8-640 nM). PF-3450074 (PF-74) acts at an early stage of HIV-1 infection, inhibits viral replication by directly competing with the binding of CPSF6 and NUP153, and blocks the uncoating, assembly, and the reverse transcription steps of the viral life cycle. CPSF6: nuclear host factors cleavage and polyadenylation specific factor 6; NUP153: nucleoporin 153.
  • HY-103142
    AS19

    5-HT Receptor Neurological Disease
    AS19 is a potent, selective 5-HT7 receptor agonist with an IC50 value of 0.83 nM and a Ki of 0.6 nM. AS19 is selective for 5-HT7 over 5-HT1A, 5-HT1B, 5-HT1D, and 5-HT5A receptors (Kis = 89.7 nM, 490 nM, 6.6 nM and 98.5 nM, respectively). AS19 enhances memory consolidation and reverses Scopolamine- or Dizocilpine-induced amnesia.
  • HY-B0879A
    Suramin sodium salt

    Suramin hexasodium salt

    Phosphatase Sirtuin Reverse Transcriptase Topoisomerase SARS-CoV Parasite Apoptosis Cancer Infection Cardiovascular Disease
    Suramin sodium salt (Suramin hexasodium salt) is a reversible and competitive protein-tyrosine phosphatases (PTPases) inhibitor. Suramin sodium salt is a potent inhibitor of sirtuins: SirT1 (IC50=297 nM), SirT2 (IC50=1.15 μM), and SirT5 (IC50=22 μM). Suramin sodium salt is a competitive inhibitor of reverse transcriptase (DNA topoisomerase II: IC50=5 μM). Suramin sodium salt is a potent SARS-CoV-2 RNA-dependent RNA polymerase (RdRp) inhibitor. Suramin sodium salt efficiently inhibits IP5K and is an antiparasitic, anti-neoplastic and anti-angiogenic agent.
  • HY-B0879
    Suramin

    Phosphatase Sirtuin Reverse Transcriptase Topoisomerase SARS-CoV Parasite Apoptosis Cancer Infection Cardiovascular Disease
    Suramin is a reversible and competitive protein-tyrosine phosphatases (PTPases) inhibitor. Suramin is a potent inhibitor of sirtuins: SirT1 (IC50=297 nM), SirT2 (IC50=1.15 μM), and SirT5 (IC50=22 μM). Suramin is a competitive inhibitor of reverse transcriptase (DNA topoisomerase II: IC50=5 μM). Suramin is a potent SARS-CoV-2 RNA-dependent RNA polymerase (RdRp) inhibitor.Suramin efficiently inhibits IP5K and is an antiparasitic, anti-neoplastic and anti-angiogenic agent.