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 (99):

Cat. No. Product Name Effect Purity Chemical Structure
  • 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.
    Raltegravir-d<sub>3</sub> potassium
  • HY-12108
    S 1360
    		Inhibitor
    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-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-159092
    HIV-1 integrase inhibitor 13
    		Inhibitor
    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-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-153247
    GSK3839919A
    		Inhibitor
    GSK3839919A is a potent and allosteric HIV-1integrase inhibitor.
    GSK3839919A
  • HY-16907
    GSK-364735
    		Inhibitor
    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-177098
    Lepetegravir
    		Inhibitor
    Lepetegravir (Example 24) is a HIV integrase inhibitor. Lepetegravir has antiviral effects (EC50: 0.98 nM in MT-4 cells).
    Lepetegravir
  • 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-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>
  • HY-10353AS1
    Raltegravir-13C,d3 potassium
    		Inhibitor
    Raltegravir-13C,d3 potassium is 13C labeled Raltegravir potassium (HY-10353A). Raltegravir (MK 0518) potassium is a potent integrase (IN) inhibitor, used to treat HIV infection.
    Raltegravir-<sup>13</sup>C,d<sub>3</sub> potassium
  • HY-15592AS
    Cabotegravir-d3 sodium
    Cabotegravir-d3 (sodium) is the deuterium labeled Cabotegravir sodium. Cabotegravir sodium is a highly potent HIV integrase inhibitor with an IC50 value of 2.5 nM for HIVADA. Cabotegravir sodium is primarily metabolized by uridine diphosphate glucuronosyltr
    Cabotegravir-d<sub>3</sub> sodium
  • HY-10353S1
    Raltegravir-d6
    		Inhibitor
    Raltegravir-d6 is a deuterated labeled Raltegravir. Raltegravir is a potent integrase (IN) inhibitor, used to treat HIV infection.
    Raltegravir-d<sub>6</sub>
  • HY-121096
    Funalenone
    		Inhibitor
    Funalenone (BMS-304245) is a MraY + MurG inhibitor with an IC50 of 25.5 μM in a MraY + MurG membrane plate assay. Funalenone inhibits Staphylococcus aureus (A15090) with an MIC of 64 μg/mL. Funalenone also inhibits MMP-1 with an IC50 of 170 μM.
    Funalenone
  • HY-P2379
    His-Cys-Lys-Phe-Trp-Trp
    		Inhibitor
    His-Cys-Lys-Phe-Trp-Trp is an inhibitor for the human immunodeficiency virus (HIV) integrase with an IC50 of 2 μM.
    His-Cys-Lys-Phe-Trp-Trp
  • HY-12210
    (S)-BI-1001
    		Inhibitor
    (S)-BI-1001 (Compound 11) is an active S-enantiomer of BI-1001. (S)-BI-1001 exhibits antiviral potency against HIV-1 integrase with an IC50 of 28 nM, an EC50 of 450 nM and a Kd of 4.7 μM.
    (S)-BI-1001
  • HY-N12036
    Dihydroobionin B
    		Inhibitor
    Dihydroobionin B is a potent
    Dihydroobionin B