HIV Integrase

Current antiviral strategies against HIV rely on structure-function analysis of HIV reverse transcriptase (RT) and protease (PR). In addition, HIV integrase (IN) is also a good target for drug discovery because IN is essential for retroviral replication and, in addition, it has no obvious functional analog in the host. The development of new anti-HIV drugs targeting HIV integrase has become a hot spot for new drug development nowadays, and these drugs can be added to the anti-RT and anti-PR drug libraries.

HIV integrase consists of three structural domains which have been individually determined by X-ray crystallography or nuclear magnetic resonance spectroscopy. It can bind to the ends of viral DNA and to target DNA. Currently, integrase strand transfer inhibitors (INSTI) have been shown to significantly improve the treatment of human immunodeficiency virus (HIV). Four drugs are currently approved for the treatment of treatment-naive HIV-infected patients; these include first-generation Raltegravir, elvitegravir, and second-generation dolutegravir and bictegravir. The benefits of these INSTIs include their high genetic barrier to resistance, limited drug-drug interactions, good virologic suppression rates, and excellent tolerability.

CAS No.	Product Name	Inquiry
125697-91-8	Lavendustin B Lavendustin B is a competitive inhibitor of glucose transporter 1 (Glut1), and also an inhibitor of the interaction between HIV-1 integrase and LEDGF/p75. It can be used as a negative control of Lavendustin A.
1292804-07-9	Raltegravir-sodium Raltegravir (MK 0518) sodium is a potent and orally active integrase (IN) inhibitor, used to treat HIV infection.
1638504-56-9	HIV-1 integrase inhibitor 3 HIV-1 integrase inhibitor 3 is an HIV-1 integrase strand transfer (INST) inhibitor with an IC50 of 2.7 nM.
1638504-66-1	HIV-1 integrase inhibitor 4 HIV-1 integrase inhibitor 4 is an HIV-1 integrase strand transfer (INST) inhibitor with an IC50 of 3.7 nM.
1803444-21-4	GSK3739936 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.
223769-59-3	HIV-Protease-Substrate-1 HIV Protease Substrate 1, a fiuorogenic HIV protease substrate, can be used to study enzymatic activity of HIV protease.
2245231-10-9	Pirmitegravir Pirmitegravir is a potent and first-in-class allosteric integrase (ALLINI) inhibitor that targets LEDGF/p75 binding site, and has excellent antiviral and safety properties. It shows picomolar IC50 in human PBMCs with a therapeutic index of >24000 for HIV-1.
2248124-46-9	HIV-1-protease-IN-2 HIV-1 protease-IN-2 is a potent HIV-1 protease inhibitor with an IC50 of 2.53 nM. HIV-1 protease-IN-2 shows antiviral activity against DRV (Darunavir)-sensitive or DRV-resistant HIV-1 variants.
2249814-82-0	Dolutegravir-d5 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).
2511547-82-1	HIV-protease-IN-1 HIV protease-IN-1 (compound 1·succinate) is a potent HIV protease non-peptidic inhibitor, can be used to research AIDS.
2525173-96-8	HIV-1-protease-IN-5 HIV-1 protease-IN-5 (Compound 13c) is a HIV-1 protease inhibitor with an IC50 of 1.64 nM. HIV-1 protease-IN-5 shows remarkable activity against wild-type and DRV-resistant HIV-1 variants.
2712343-38-7	Raltegravir-d4 Raltegravir-d4 is deuterium labeled Raltegravir. Raltegravir is a potent integrase (IN) inhibitor, used to treat HIV infection.
2734920-43-3	Cabotegravir-d3 Cabotegravir-d3 (GSK-1265744-d3) is the deuterium labeled Cabotegravir. Cabotegravir is a potent HIV integrase inhibitor as an oral lead-in tablet and long-acting injectable for the treatment and prevention of HIV infection. Cabotegravir is an inhibitor of OAT1 (IC50 0.81 μM) and OAT3 (IC50 0.41 μM)
2750534-77-9	Cabotegravir-d5 Cabotegravir-d5 is deuterium labeled Cabotegravir.
284661-68-3	DPC-681 DPC-681, sulfonamide derivatives, is an extremely potent and selective inhibitor of HIV protease. IC90s: wild-type HIV-1=4-40 nM
490-31-3	Robinetin Robinetin is from the leaves of Robinia pseudacacia. It inhibits EYPC membrane lipid peroxidation and HbA glycosylation with high efficiency. It could lead to the occurrence of positive induced circular dichroism (ICD) bands in the near ultra-violet (UV) region.
70831-56-0	L-Chicoric acid Cichoric acid, that can be isolated from the herbs of Echinacea purpurea, has been shown to inhibit hyaluronidase and HIV-1 integrase, and to possess phagoeytosis stimulatory activity in vitro and in vivo and antiviral acitivy. Chicoric acid may reduce acute alcohol-induced steatosis in mice through interfering with the induction of iNOS and iNOS-dependent signaling cascades in the liver. Chicoric acid also inhibited cell viability and induced apoptosis in 3T3-L1 preadipocytes which was characterized by chromatin condensation and poly ADP-ribose-polymerase (PARP) cleavage.
729607-74-3	BMS-707035 BMS-707035 is a specific HIV-I integrase (IN) inhibitor with IC50 of 15 nM.
87-17-2	Salicylanilide Salicylanilide has a wide range of biological activities, including antiviral, anti-inflammatory, antibacterial and so on. It inhibits HIV virus by targeting HIV-1 integrase or reverse transcriptase. It inhibits mycobacterial isocitrate lyase (ICL) and has a significant antimycobacterial effect. It can be used as an antiseptic.
957890-42-5	HIV-1 integrase inhibitor 2 HIV-1 integrase inhibitor 2 is useful for anti-HIV, which can target HIV-1 integrase and depress the activity in the treatment of HIV infection, AIDS, and other similar diseases characterized by integration of a retroviral genome into a host chromosome. It did not affect integrase-DNA binding and only weakly inhibited the catalytic activities of integrase.

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