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HIV Integrase

Human immunodeficiency virus (HIV) integrase is a Mr 32000 protein encoded by the pol gene of HIV that catalyzes an essential step in the viral replicative cycle to integrate the viral DNA into the host DNA. HIV integrase catalyzes two temporally and spatially separated reactions, including process, where a CA dinucleotide from the 3’-ends of the double stranded viral DNA is cleaved by HIV integrase in cytoplasm generating a double-stranded DNA with a two-base overhang, and strand transfer, where the HIV integrase-and-DNA complex is transferred in to the nucleus. The most well studied HIV integrase is HIV-1 integrase characterized by containing three domains, including the N-terminal domain, the C-terminal domain and the core domain.

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  1. Cat.No. Product Name Information
  2. A4072 MK-2048 MK-2048 is a second generation inhibitor of HIV-1 integrase with IC50 values of 0.075 μM and 0.08 μM for subtype B and subtype C integrase, respectively.
  3. A4069 BMS-707035
  4. C4787 Equisetin
  5. B5856 GSK1349572 sodiuM salt
  6. B4851 (±)-BI-D
  7. B4845 BI 224436
  8. A8566 GSK744 (S/GSK1265744) GSK744 (S/GSK1265744) is a potential inhibitor of HIV integrase with IC50 value of 3 nM.
  9. A4070 Elvitegravir (GS-9137) Elvitegravir (also known as GS-9137 or JTK-303), a monoketo acid modified from the distinct diketo acid moiety (DKA) motif, is a potent inhibitor of human immunodeficiency virus type I (HIV-1) integrase, an enzyme integrating the viral DNA into the cellular DNA of the host during HIV replication.
  10. A4071 Fluorouracil (Adrucil) Fluorouracil (Adrucil), a heterocyclic aromatic organic compound, is a potent anticancer agent widely used for the treatment of solid tumors, including breast cancer, ovarian cancer, head and neck cancer, and colon cancer. As an analogue of uracil, fluorouracil has a fluorine atom replacing the hydrogen atom at the C-5 position.
  11. A4073 Raltegravir (MK-0518) Raltegravir, formerly named MK-0518, is an HIV-1 integrase strand transfer inhibitor which has been shown to have activity against multidrug-resistant HIV-1 and both CCR5-trophic and CXCR4-trophic HIV-1 in vitro.

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