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HIV-1 integrase

" in MedChemExpress (MCE) Product Catalog:

83

Inhibitors & Agonists

1

Peptides

13

Natural
Products

10

Isotope-Labeled Compounds

1

Click Chemistry

2

Oligonucleotides

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-13238
    Dolutegravir
    Maximum Cited Publications
    32 Publications Verification

    S/GSK1349572

    HIV Integrase HIV Infection
    Dolutegravir (S/GSK1349572) is a highly potent and orally bioavailable HIV integrase strand transfer inhibitor with an IC50 of 2.7 nM for HIV-1 integrase-catalyzed strand transfer. Dolutegravir (S/GSK1349572) inhibits HIV-1 viral replication with an IC50 of 0.51 nM in peripheral blood mononuclear cells. Dolutegravir retains a high potency against the HIV-1 Y143R, N155H, and G140S/Q148H mutants (EC50=3.6-5.8 nM) .
    Dolutegravir
  • HY-14740
    Elvitegravir
    10+ Cited Publications

    GS-9137; JTK-303; D06677

    HIV Integrase HIV Infection
    Elvitegravir (GS-9137; JTK-303; D06677) is an HIV integrase inhibitor for HIV-1IIIB, HIV-2EHO and HIV-2ROD with IC50 of 0.7 nM, 2.8 nM and 1.4 nM, respectively.
    Elvitegravir
  • HY-17605
    Bictegravir
    15+ Cited Publications

    GS-9883

    HIV HIV Integrase Infection
    Bictegravir (GS-9883) is a potent inhibitor of HIV-1 integrase with an IC50 of 7.5 nM.
    Bictegravir
  • HY-13238A
    Dolutegravir sodium
    Maximum Cited Publications
    32 Publications Verification

    S/GSK1349572 sodium

    HIV Integrase HIV Infection
    Dolutegravir sodium (S/GSK1349572 sodium) is a highly potent and orally bioavailable HIV integrase strand transfer inhibitor with an IC50 of 2.7 nM for HIV-1 integrase-catalyzed strand transfer. Dolutegravir sodium (S/GSK1349572 sodium) inhibits HIV-1 viral replication with an IC50 of 0.51 nM in peripheral blood mononuclear cells. Dolutegravir sodium (S/GSK1349572 sodium) retains a high potency against the HIV-1 Y143R, N155H, and G140S/Q148H mutants (EC50=3.6-5.8 nM) .
    Dolutegravir sodium
  • HY-N0457A
    L-Chicoric Acid
    3 Publications Verification

    (-)-Chicoric acid; trans-Caffeoyltartaric acid

    HIV Integrase HIV Endogenous Metabolite Infection Cancer
    L-Chicoric Acid ((-)-Chicoric acid) is a dicaffeoyltartaric acid and a potent, selective and reversible HIV-1 integrase inhibitor with an IC50 of ~100 nM. L-Chicoric Acid inhibits HIV-1 replication in tissue culture .
    L-Chicoric Acid
  • HY-I0096

    iGluR HIV HIV Integrase Neurological Disease
    Indole-2-carboxylic acid (I2CA) is a competitive antagonist of the glycine site of the NMDA receptor (Ki=15 μM, 5-fluoro-I2CA) and an inhibitor of HIV-1 integrase. Indole-2-carboxylic acid is selective for the glycine site of the NMDA receptor and blocks the enhancement of NMDA receptor by competitively inhibiting the binding of glycine to the NMDA receptor. Indole-2-carboxylic acid can also inhibit the strand transfer activity of HIV-1 integrase by chelating Mg 2+ at the active site of integrase and interacting with the hydrophobic cavity. Indole-2-carboxylic acid can be used in the study of neurological diseases (such as stroke, epilepsy) and HIV-1 infection .
    Indole-2-carboxylic acid
  • HY-W010937

    BMIM-TFSI; BMI-TFSI

    HIV HIV Integrase Infection
    1-Butyl-3-methylimidazolium bis(trifluoromethylsulfonyl)imide (BMIM-TFSI; BMI-TFSI) is an HIV-1 integrase inhibitor. 1-Butyl-3-methylimidazolium bis(trifluoromethylsulfonyl)imide weakly inhibits recombinant HIV-1 integrase 3'-processing or strand transfer activity. 1-Butyl-3-methylimidazolium bis(trifluoromethylsulfonyl)imide can be used for the research of HIV-1 .
    1-Butyl-3-methylimidazolium bis(trifluoromethylsulfonyl)imide
  • HY-130000

    STP0404

    HIV Integrase HIV Infection
    Pirmitegravir is a potent and first-in-class inhibitor of allosteric integrase (ALLINI) that targets LEDGF/p75 binding site. Pirmitegravir displays picomolar IC50 in human PBMCs with a >24,000 therapeutic index against HIV-1. Pirmitegravir harbors outstanding anti-virus and safety properties .
    Pirmitegravir
  • HY-B1408
    Salicylanilide
    5 Publications Verification

    2-Hydroxybenzanilide

    Environmental Pollutants 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.
    Salicylanilide
  • HY-100083

    HIV Drug Intermediate Infection
    Dolutegravir intermediate-1 (Compound 11) is a synthetic intermediate. Dolutegravir intermediate-1 can be used to synthesize Dolutegravir (HY-13238). Dolutegravir is an Integrase inhibitor with potential applications in HIV-1 infection research .
    Dolutegravir intermediate-1
  • HY-18257

    Antibiotic Bacterial Dengue Virus Amyloid-β HIV Integrase Infection Neurological Disease Inflammation/Immunology
    Rolitetracycline is a highly soluble, broad-spectrum antibiotic derived from tetracycline. Rolitetracycline binds to and stabilizes bovine serum albumin, and also inhibits HIV-1 integrase, blocks Aβ fibril formation and suppresses dengue virus proliferation. Rolitetracycline mediates the inhibition of Aβ fibrils via a specific three-dimensional pharmacophore conformation, and exerts bacteriostatic and bactericidal activities. Rolitetracycline acts synergistically with Penicillin G (HY-N7139) or Cephalothin (HY-B1275A) to alter the effects on microbial growth. Rolitetracycline serves as an important tool compound for the study of bacterial infections (urinary tract infections, sepsis), HIV-1 and dengue virus infections, as well as Alzheimer's disease .
    Rolitetracycline
  • HY-13269
    BMS-707035
    1 Publications Verification

    HIV HIV Integrase Infection Inflammation/Immunology
    BMS-707035 is a potent orally active HIV-1 integrase strand transfer inhibitor (INSTI). BMS-707035 has enzyme inhibitory with an IC50 value of 3 nM. BMS-707035 also has weak CYP inhibiton and antiviral activity. BMS-707035 can be used for the research of human immunodeficiency virus-1 (HIV-1) .
    BMS-707035
  • HY-18595
    BI 224436
    5+ Cited Publications

    HIV HIV Integrase Infection
    BI 224436 is a novel HIV-1 noncatalytic site integrase inhibitor with EC50 values of less than 15 nM against different HIV-1 laboratory strains.
    BI 224436
  • HY-17605A
    Bictegravir sodium
    15+ Cited Publications

    GS-9883 sodium

    HIV Integrase HIV Infection
    Bictegravir sodium is a potent inhibitor of HIV-1 integrase, with an IC50 of 7.5 nM. Bictegravir sodium exhibits potent and selective anti-HIV activity and low cytotoxicity .
    Bictegravir sodium
  • HY-107485

    HIV Integrase Infection
    HIV-1 integrase inhibitor 8 is a HIV-1 integrase inhibitor, compound 8 .
    HIV-1 integrase inhibitor 8
  • HY-N6711

    HIV Integrase Bacterial Antibiotic Reactive Oxygen Species (ROS) STAT AMPK 11β-HSD Infection Metabolic Disease
    Equisetin is an N-methylserine-derived acyl tetramic acid, quorum sensing inhibitor (QSI), herbicides and antibiotics. Equisetin specifically inhibits the anionic carriers of substrates in the inner mitochondrial membrane. Equisetin inhibits the activity of HIV-1 integrase, 11β-HSD1, and 2,4-dinitrophenol (Dnp)-stimulated ATPase (IC50 = ~8 nmol per mg of protein). Equisetin exhibits growth inhibition of bacteria, anti-inflammatory, amelioration of lipid-associated disorders, and cytotoxic effects .
    Equisetin
  • HY-108935

    HIV Integrase GLUT Tyrosinase Cancer
    Lavendustin B is an inhibitor of HIV-1 integrase interaction with LEDGF/p75 with an IC50 of 94.07 μM. Lavendustin B is an ATP-competitive GLUT1 inhibitor with a Ki of 15 μM. Lavendustin B is also a weak inhibitor of tyrosine kinases .
    Lavendustin B
  • HY-13305

    HIV HIV Integrase Apoptosis PARP Infection
    MK-2048 is a HIV-1 and HIV-1 integrase inhibitor. MK-2048 shows selective activity against HTLV-1-infected cells and retained potency against HIV-1 variants. MK-2048 induces apoptosis, inhibits cell growth, reduces proviral loads, and blocks HTLV-1 transmission and immortalization. MK-2048 can be used for the research of HIV-1 infection .
    MK-2048
  • HY-13025
    HIV-1 integrase inhibitor
    1 Publications Verification

    HIV HIV Integrase Infection
    HIV-1 integrase inhibitor 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.
    HIV-1 integrase inhibitor
  • HY-134851
    HIV-1 inhibitor-6
    1 Publications Verification

    HIV Infection
    HIV-1 inhibitor-6 (compound 9), a diheteroarylamide-based compound, is a potent HIV-1 pre-mRNA alternative splicing inhibitor. HIV-1 inhibitor-6 blocks HIV replication. HIV-1 inhibitor-6 is active against wild-type HIV-1IIIB (subtype B, X4-tropic) and HIV-1 97USSN54 (subtype A, R5-tropic) with EC50s of 0.6 μM and 0.9 μM, respectively. HIV-1 inhibitor-6 inhibits HIV strains resistant to agents targeting HIV reverse transcriptase, protease, integrase, and coreceptor CCR5 with EC50s ranging from 0.9 to 1.5 μM .
    HIV-1 inhibitor-6
  • HY-N16050

    Ethyl salvionolate A

    HIV Reverse Transcriptase HIV Integrase HIV Protease Infection
    Ethyl salvianolate A (Ethyl salvionolate A) is an anti-HIV-1 compound that can be extracted from the roots of Salvia yunnanensis. Ethyl salvianolate A inhibits P24 antigen in HIV-1 infected MT-4 cell cultures (EC50: 1.44 μg/mL). Ethyl salvianolate A inhibits HIV-1 replicative enzymes, with IC50s of 56.38 μM (Reverse transcriptase), 12.03 μM (Protease), 14.54 μM (Integrase), respectively .
    Ethyl salvianolate A
  • HY-17605S

    Isotope-Labeled Compounds Infection
    Bictegravir- 15N,d2 (GS-9883- 15N,d2) is the 15N and deuterium labeled Bictegravir (HY-17605) . Bictegravir (GS-9883) is a potent inhibitor of HIV-1 integrase with an IC50 of 7.5 nM .
    Bictegravir-15N,d2
  • HY-150079

    HIV Integrase Infection
    HIV-1 integrase inhibitor 10 is an orally active HIV-1 allosteric integrase inhibitor (ALLINI). HIV-1 integrase inhibitor 10 can inhibit viral outgrowth of the NLRepRluc virus in MT-2 cells with EC50 values of 3-5 nM. HIV-1 integrase inhibitor 10 can be used for the research of Human immunodeficiency virus-1 (HIV-1) .
    HIV-1 integrase inhibitor 10
  • HY-159092

    HIV Integrase Infection
    HIV-1 integrase inhibitor 13 (Compound 15) is an inhibitor for HIV-1 integrase with an IC50 of 1.8 nM. HIV-1 integrase inhibitor 13 inhibits the HIV-1 WT and HIV-1 T125A, with IC50 of 21 and 580 nM, respectively .
    HIV-1 integrase inhibitor 13
  • HY-130760

    HIV Integrase Infection
    HIV-1 integrase inhibitor 7 is a potent HIV-1 integrase inhibitor, with an IC50 of 33.3 nM .
    HIV-1 integrase inhibitor 7
  • HY-108820

    HIV Integrase HIV Infection
    HIV-1 integrase inhibitor 4 is a HIV-1 integrase strand transfer (INST) inhibitor with an IC50 of 3.7 nM.
    HIV-1 integrase inhibitor 4
  • HY-108817

    HIV Integrase HIV Infection
    HIV-1 integrase inhibitor 3 is a HIV-1 integrase strand transfer (INST) inhibitor with an IC50 of 2.7 nM.
    HIV-1 integrase inhibitor 3
  • HY-W507252

    HIV Integrase Infection
    HIV-1 integrase inhibitor 11 (compound 5) is a potent inhibitor of HIV-1 integrase, with the IC50 of 125 μM .
    HIV-1 integrase inhibitor 11
  • HY-159091

    HIV Integrase Infection
    HIV-1 integrase inhibitor 12 (Compound 17) is an inhibitor for HIV-1 integrase with an IC50 of 1.4 nM. HIV-1 integrase inhibitor 12 inhibits the HIV-1 WT and HIV-1 T125A, with IC50 of 7.4 and 120 nM, respectively. HIV-1 integrase inhibitor 12 exhibits metabolic stability and Caco-2 permeability, and good pharmacokinetic characteristics with good bioavailability (64%) and low clearance (0.16 L/hr/kg) in rats .
    HIV-1 integrase inhibitor 12
  • HY-132572

    HIV Infection
    HIV-1 integrase inhibitor 9 (compound 8a) is a potent HIV-1 RNase H inhibitor with an IC50 of 12.3 μM. HIV-1 integrase inhibitor 9 shows an antiviral activity .
    HIV-1 integrase inhibitor 9
  • HY-17605AR

    GS-9883 sodium (Standard)

    Reference Standards HIV Integrase HIV Infection
    Bictegravir (sodium) (Standard) is the analytical standard of Bictegravir (sodium). This product is intended for research and analytical applications. Bictegravir sodium is a potent inhibitor of HIV-1 integrase, with an IC50 of 7.5 nM. Bictegravir sodium exhibits potent and selective anti-HIV activity and low cytotoxicity .
    Bictegravir sodium (Standard)
  • HY-153094

    HIV HIV Integrase Infection
    BDM-2 is an IN-LEDGF allosteric inhibitor (INLAI) of HIV-1 integrase (IN refers to integrase) (IC50=47 nM) with potent anti-Retroviral (ARV) activity. BDM-2 shows IN multimerization activation effect with an AC50 value of 20 nM. BDM-2 blocks the interaction between the catalytic core domain of IN (IN-CCD) and the Integrase binding domain of LEDGF/p75 (IBD), with an IC50 value of 0.15 μM. BDM-2 exhibits highly selective and favorable cytotoxicity .
    BDM-2
  • HY-N7330

    HIV Integrase HIV Infection
    Integracin B is a potent dimeric alkyl aromatic inhibitor of HIV-1 integrase discovered from the screening of fungal extracts using an in vitro assay. Integracin B inhibits both coupled and strand transfer activity of HIV-1 integrase .
    Integracin B
  • HY-12108

    HIV Integrase HIV Infection
    S 1360 is a potent and selective inhibitor of HIV-1 integrase. S 1360 inhibits the catalytic activity of purified integrase ( IC50: 20 nM). The EC50, and CC50 of S 1360 in MTT assay (MT-4 cells infected with HIV-1 IIIB) are 200 nM and 12 μM, respectively. S 1360 has antiviral activity against both X4 tropic and R5 tropic strains, as well as NRTI, NNRTI and PI drug-resistant variants .
    S 1360
  • HY-16907

    S/GSK-364735

    HIV HIV Integrase Infection
    GSK-364735 is a potent antiretroviral agent against human immunodeficiency virus type 1 (HIV-1) and serves as an integrase inhibitor with an IC50 of 8 ± 2 nM. GSK-364735 can be utilized in antiviral research .
    GSK-364735
  • HY-107485R

    Reference Standards HIV Integrase Infection
    HIV-1 integrase inhibitor 8 (Standard) is the analytical standard of HIV-1 integrase inhibitor 8 (HY-107485). This product is intended for research and analytical applications. HIV-1 integrase inhibitor 8 is a HIV-1 integrase inhibitor, compound 8 .
    HIV-1 integrase inhibitor 8 (Standard)
  • HY-177670A

    AR177 sodium; T30177 sodium

    HIV Infection
    Zintevir sodium is an antisense oligonucleotide that targets HIV-1 integrase.
    Zintevir sodium
  • HY-177670

    AR177; T30177

    HIV Infection
    Zintevir is an antisense oligonucleotide that targets HIV-1 integrase.
    Zintevir
  • HY-147653

    HIV Integrase Infection
    Integrase-LEDGF/p75 allosteric inhibitor 1 (Compound 31h) is an orally active integrase-LEDGF/p75 (IN-LEDGF/p75) allosteric inhibitor. Integrase-LEDGF/p75 allosteric inhibitor 1 inhibits HIV-1 DNA integration and shows antiviral activity with an EC50 of 3.9 nM against HIV-1 recombinant molecular clone NL432 .
    Integrase-LEDGF/p75 allosteric inhibitor 1
  • HY-N15327

    HIV HIV Integrase Infection
    Hyrtiosal, found in the marine sponge Hyrtios erectus, is an inhibitor of the N-terminal domain (NTD) of HIV-1 integrase (HIV-1 IN) with an IC50 value of 9.60-0.86 μM. Hyrtiosal binds to the Ser17, Trp19, and Lys34 sites on the NTD of HIV-1 IN, inhibiting the binding of HIV-1 viral DNA to integrase and interfering with the formation of the pre-integrated complex of HIV-1. Hyrtiosal is promising for research of anti-HIV agents .
    Hyrtiosal
  • HY-17605S1

    GS-9883-d5

    HIV HIV Integrase Isotope-Labeled Compounds Infection
    Bictegravir-d5 is deuterated labeled Bictegravir (HY-17605). Bictegravir (GS-9883) is a potent inhibitor of HIV-1 integrase with an IC50 of 7.5 nM.
    Bictegravir-d5
  • HY-17605R

    GS-9883 (Standard)

    Reference Standards HIV HIV Integrase Infection
    Bictegravir (Standard) is the analytical standard of Bictegravir. This product is intended for research and analytical applications. Bictegravir (GS-9883) is a potent inhibitor of HIV-1 integrase with an IC50 of 7.5 nM.
    Bictegravir (Standard)
  • HY-13238S1

    S/GSK1349572-d3

    Isotope-Labeled Compounds HIV Integrase HIV Infection
    Dolutegravir-d3 is the deuterium labeled Dolutegravir. Dolutegravir (S/GSK1349572) is a highly potent and orally bioavailable HIV integrase strand transfer inhibitor with an IC50 of 2.7 nM for HIV-1 integrase-catalyzed strand transfer. Dolutegravir (S/GSK1349572) inhibits HIV-1 viral replication with an IC50 of 0.51 nM in peripheral blood mononuclear cells. Dolutegravir retains a high potency against the HIV-1 Y143R, N155H, and G140S/Q148H mutants (EC50=3.6-5.8 nM) .
    Dolutegravir-d3
  • HY-13238S2

    S/GSK1349572-d5

    Isotope-Labeled Compounds HIV Integrase HIV Infection
    Dolutegravir-d5 is deuterium labeled Dolutegravir. Dolutegravir (S/GSK1349572) is a highly potent and orally bioavailable HIV integrase strand transfer inhibitor with an IC50 of 2.7 nM for HIV-1 integrase-catalyzed strand transfer. Dolutegravir (S/GSK1349572) inhibits HIV-1 viral replication with an IC50 of 0.51 nM in peripheral blood mononuclear cells. Dolutegravir retains a high potency against the HIV-1 Y143R, N155H, and G140S/Q148H mutants (EC50=3.6-5.8 nM) .
    Dolutegravir-d5
  • HY-13238R

    S/GSK1349572 (Standard)

    Reference Standards HIV Integrase HIV Infection
    Dolutegravir (Standard) is the analytical standard of Dolutegravir. This product is intended for research and analytical applications. Dolutegravir (S/GSK1349572) is a highly potent and orally bioavailable HIV integrase strand transfer inhibitor with an IC50 of 2.7 nM for HIV-1 integrase-catalyzed strand transfer. Dolutegravir (S/GSK1349572) inhibits HIV-1 viral replication with an IC50 of 0.51 nM in peripheral blood mononuclear cells. Dolutegravir retains a high potency against the HIV-1 Y143R, N155H, and G140S/Q148H mutants (EC50=3.6-5.8 nM) .
    Dolutegravir (Standard)
  • HY-B1408R

    2-Hydroxybenzanilide (Standard)

    HIV Integrase HIV Reference Standards Infection
    Salicylanilide (Standard) is the analytical standard of Salicylanilide. This product is intended for research and analytical applications. Salicylanilide demonstrates a wide range of biological activities including antiviral potency which can inhibit HIV virus by targeting HIV-1 integrase or reverse transcriptase.
    Salicylanilide (Standard)
  • HY-150080

    BMS-986180

    HIV HIV Integrase Infection
    GSK3739936 (BMS-986180) is a potent HIV-1 allosteric integrase inhibitor with an IC50 value of 11.1 nM and an EC50 value of 1.7 nM. GSK3739936 is also a weak CYP inhibitor (IC50>24.3 μM). GSK3739936 shows favorable pharmacokinetic property in preclinical species with rapid absorption, low to moderate clearance and excellent oral bioavailability .
    GSK3739936
  • HY-W103287

    HIV Integrase Infection
    Hydroxyisoquinoline-1,3(2H,4H)-dione (compound 6a) is a HIV-1 integrase (IN) and HIV-1 reverse transcriptase (RT) ribonuclease H (RNase H) inhibitor with an IC50 value of 6.32, 5.9 µM, respectively .
    2-Hydroxyisoquinoline-1,3(2H,4H)-dione
  • HY-122256

    HIV Integrase Infection
    L-870812 is a HIV-1 integration with integrase strand transfer inhibitor. L-870812 consistently blocks cell-free and cell-associated HIV-1 infection. L-870812 blocks subtype C and CRFO2_AG primary isolates. L-870812 can be used for the study of replication-deficient HIV-1 Ba-L (env) pseudovirus .
    L-870812
  • HY-18666

    HIV Infection
    D77 is anti-HIV-1 inhibitor targeting the interaction between integrase and cellular LEDGF/p75. D77 inhibits HIV-1(IIIB) replication by EC50 value of 23.8 μg/ml in MT-4 cell (5.03 μg/ml for C8166 cells).
    D77

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