2. Signaling Pathways
  3. Metabolic Enzyme/Protease
  4. HIV Integrase

HIV Integrase

HIV Integrase

Related Products

PDF 0.49 MB

HIV integrase is one of the three key enzymes of the pol gene of HIV. HIV integrase catalyzes the insertion into the genome of the infected human cell of viral DNA produced by the retrotranscription process. This unique step in the virus life cycle provides a variety of points for intervention and hence is an attractive target for the development of new therapeutics for the treatment of AIDS. HIV integrase includes HIV-1 and HIV-2 integrases.

HIV-1 integrase is a 32-kDa enzyme that carries out DNA integration in a two-step reaction. In the first step, called 3′ processing, two nucleotides are removed from each 3′ end of the viral DNA made by reverse transcription. In the next step, called DNA strand transfer, a pair of transesterification reactions integrates the ends of the viral DNA into the host genome. Integrase is comprised of three structurally and functionally distinct domains, and all three domains are required for each step of the integration reaction.

HIV Integrase Related Products (65):

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-13269
    BMS-707035
    		Inhibitor 99.99%
    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-18601
    (±)-BI-D
    		Inhibitor 98.06%
    (±)-BI-D is a potent ALLINI(An allosteric IN inhibitor) that binds integrase at the LEDGF/p75 binding site.
    (±)-BI-D
  • HY-153094
    BDM-2
    		Inhibitor 99.09%
    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-108935
    Lavendustin B
    		Inhibitor 98.02%
    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-130000
    Pirmitegravir
    		Inhibitor 99.76%
    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-108820
    HIV-1 integrase inhibitor 4
    		Inhibitor
    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-1 integrase inhibitor 3
    		Inhibitor
    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-15592S1
    Cabotegravir-d5
    		Inhibitor 99.31%
    Cabotegravir-d5 is deuterium labeled Cabotegravir.
    Cabotegravir-d<sub>5</sub>
  • HY-13305
    MK-2048
    		Inhibitor ≥98.0%
    MK-2048 is a potent inhibitor of integrase and INR263K with IC50 of 2.
    MK-2048
  • HY-10353B
    Raltegravir sodium
    		Inhibitor
    Raltegravir (MK 0518) sodium is a potent and orally active integrase (IN) inhibitor, used to treat HIV infection.
    Raltegravir sodium
  • HY-150080
    GSK3739936
    		Inhibitor
    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-10353AS
    Raltegravir-d3 potassium
    		Inhibitor
    Raltegravir-d3 (potassium) is the deuterium labeled Raltegravir potassium. Raltegravir (MK 0518) potassium is a potent integrase (IN) inhibitor, used to treat HIV infection[1][2].
    Raltegravir-d<sub>3</sub> potassium
  • HY-10353S
    Raltegravir-d4
    		Inhibitor
    Raltegravir-d4 is deuterium labeled Raltegravir. Raltegravir is a potent integrase (IN) inhibitor, used to treat HIV infection.
    Raltegravir-d<sub>4</sub>
  • HY-14740S
    Elvitegravir-d8
    		Inhibitor
    Elvitegravir-d8 is deuterium labeled Elvitegravir. 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-d<sub>8</sub>
  • HY-15592S2
    Cabotegravir-d3-1
    		Inhibitor
    Cabotegravir d3-1 (GSK-1265744-d3-1) is a deuterium substitute of Cabotegravir. Cabotegravir is a potent HIV integrase inhibitor used in AIDS research
    Cabotegravir-d<sub>3</sub>-1
  • HY-13238S2
    Dolutegravir-d5
    		Inhibitor
    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)[1][2].
    Dolutegravir-d<sub>5</sub>
  • HY-153247
    GSK3839919A
    		Inhibitor
    GSK3839919A is a potent and allosteric HIV-1integrase inhibitor.
    GSK3839919A
  • HY-N7330
    Integracin B
    		Inhibitor
    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-N0457AR
    L-Chicoric Acid (Standard)
    		Inhibitor
    L-Chicoric Acid (Standard) is the analytical standard of L-Chicoric Acid. This product is intended for research and analytical applications. 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 (Standard)
  • HY-17605S2
    Bictegravir-d4
    		Inhibitor
    Bictegravir-d4 is a deuterium of Bictegravir (HY-17605). Bictegravir (GS-9883) is a potent inhibitor of HIV-1 integrase with an IC50 of 7.5 nM.
    Bictegravir-d<sub>4</sub>