HIV Integrase

all Inhibitors (28)

CAS No.	Product Name	Inquiry
	Dolutegravir-d3 Dolutegravir-d3 (S/GSK1349572-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).
1051375-13-3	Cabotegravir-sodium Cabotegravir (GSK-1265744) sodium is a orally active and long-acting HIV integrase inhibitor and organic anion transporter 1/3 (OAT1/OAT3) inhibitor with IC50 values of 2.5 nM, 0.41 μM and 0.81 μM for HIVADA, OAT3 and OAT1, respectively.
1155419-89-8	BI 224436 BI 224436 is a novel HIV-1 non-catalytic-site integrase inhibitor; has antiviral EC50s of <15 nM against different HIV-1 laboratory strains and cellular cytotoxicity of >90 μM.
1246816-98-7	Raltegravir-[d3] Potassium Salt Labelled Raltegravir K salt. Raltegravir is a potent, selective, and orally bioavailable inhibitor of HIV integrase (IC50 = 15 nM). It is metabolized primarily by uridine diphosphate glucuronosyltransferase 1A. Raltegravir has long-term efficacy and safety in managing HIV-1 infection in adults, children, and adolescents.
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.
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).
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-[methyl-d3] Cabotegravir-[methyl-d3] is the labelled analogue of Cabotegravir. Cabotegravir is a long-acting HIV integrase inhibitor against a broad range of HIV subtypes, and inhibits the HIV-1 integrase catalyzed strand transfer reaction with an IC50 of 3.0 nM.
2750534-77-9	Cabotegravir-[d5] Cabotegravir-[d5] is the labelled analogue of Cabotegravir. Cabotegravir is a long-acting HIV integrase inhibitor against a broad range of HIV subtypes, and inhibits the HIV-1 integrase catalyzed strand transfer reaction with an IC50 of 3.0 nM.
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.
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.

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.

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