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HIV-1 integrase inhibitor

" in MedChemExpress (MCE) Product Catalog:

By Targets:	HIV (26) HIV Integrase (26) Endogenous Metabolite (1) GLUT (1) Isotope-Labeled Compounds (5) Tyrosinase (1)
By Research Areas:	Cancer (2) Infection (33) Inflammation/Immunology (2)
Click Chemistry:	Azide (1)

Inhibitors & Agonists

Natural
Products

Isotope-Labeled Compounds

Click Chemistry

Targets Recommended: HIV Integrase HIV HIV Protease

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-13025

**HIV-1 integrase inhibitor** 1 Publications Verification	HIV HIV Integrase	Infection
HIV-1 integrase inhibitor is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. Strain-promoted alkyne-azide cycloaddition (SPAAC) can also occur with molecules containing DBCO or BCN groups.

HY-107485

HIV-1 integrase inhibitor 8

HIV Integrase Infection

HIV-1 integrase inhibitor 8 is a HIV-1 integrase inhibitor, compound 8 .

HIV-1 integrase inhibitor 8	HIV Integrase	Infection
HIV-1 integrase inhibitor 8 is a **HIV-1 integrase** inhibitor, compound 8 .

HY-150079

HIV-1 integrase inhibitor 10	HIV Integrase	Infection
HIV-1 integrase inhibitor 10 is an orally active **HIV-1 allosteric integrase** inhibitor (ALLINI). HIV-1 integrase inhibitor 10 can inhibit viral outgrowth of the NLRepRluc virus in MT-2 cells with EC₅₀ values of 3-5 nM. HIV-1 integrase inhibitor 10 can be used for the research of Human immunodeficiency virus-1 (HIV-1) .

HY-130760

HIV-1 integrase inhibitor 7

HIV Integrase Infection

HIV-1 integrase inhibitor 7 is a potent HIV-1 integrase inhibitor, with an IC₅₀ of 33.3 nM .
HY-108817

HIV-1 integrase inhibitor 3

HIV Integrase HIV Infection

HIV-1 integrase inhibitor 3 is a HIV-1 integrase strand transfer (INST) inhibitor with an IC₅₀ of 2.7 nM.
HY-108820

HIV-1 integrase inhibitor 4

HIV Integrase HIV Infection

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 7	HIV Integrase	Infection
HIV-1 integrase inhibitor 7 is a potent **HIV-1 integrase** inhibitor, with an IC₅₀ of 33.3 nM .

HIV-1 integrase inhibitor 3	HIV Integrase HIV	Infection
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 4	HIV Integrase HIV	Infection
HIV-1 integrase inhibitor 4 is a HIV-1 integrase strand transfer (INST) inhibitor with an IC₅₀ of 3.7 nM.

HY-132572

HIV-1 integrase inhibitor 9	HIV	Infection
HIV-1 integrase inhibitor 9 (compound 8a) is a potent HIV-1 RNase H inhibitor with an IC₅₀ of 12.3 μM. HIV-1 integrase inhibitor 9 shows an antiviral activity .

HY-N7330

Integracin B	HIV Integrase HIV	Infection
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 .

HY-18595

BI 224436	HIV HIV Integrase	Infection
BI 224436 is a novel *HIV-1* noncatalytic site integrase inhibitor with EC₅₀ values of less than 15 nM against different HIV-1 laboratory strains.

HY-17605

Bictegravir

5+ Cited Publications

GS-9883
HIV HIV Integrase Infection

Bictegravir (GS-9883) is a potent inhibitor of HIV-1 integrase with an IC₅₀ of 7.5 nM.

Bictegravir 5+ Cited Publications GS-9883	HIV HIV Integrase	Infection
Bictegravir (GS-9883) is a potent inhibitor of **HIV-1 integrase with an IC₅₀** of 7.5 nM.

HY-163177

HIV-1 inhibitor-63	HIV	Infection
HIV-1 inhibitor-63 (compound S17) is a potent *HIV-1* inhibitor. HIV-1 inhibitor-63 inhibits integrase-Ku70 complex formation with an IC₅₀ value of 12 µM. HIV-1 inhibitor-63 inhibits HIV-1 post-integration DNA repair .

HY-147653

Integrase-LEDGF/p75 allosteric inhibitor 1	HIV Integrase	Infection
Integrase-LEDGF/p75 allosteric inhibitor 1 (Compound 31h) is an orally active integrase-LEDGF/p75 (IN-LEDGF/p75) allosteric inhibitor. Integrase-LEDGF/p75 allosteric inhibitor 1 inhibits HIV-1 DNA integration and shows antiviral activity with an EC₅₀ of 3.9 nM against HIV-1 recombinant molecular clone NL432 .

HY-N0457A

L-Chicoric Acid 1 Publications Verification (-)-Chicoric acid; trans-Caffeoyltartaric acid	HIV Integrase HIV Endogenous Metabolite	Infection Cancer
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 .

HY-17605A

Bictegravir sodium 5+ Cited Publications GS-9883 sodium	HIV Integrase HIV	Infection
Bictegravir sodium is a potent inhibitor of **HIV-1 integrase, with an IC₅₀** of 7.5 nM. Bictegravir sodium exhibits potent and selective anti-HIV activity and low cytotoxicity .

HY-N11288

Methyl salvionolate A	HIV	Infection
Methyl salvionolate A is a potent inhibitor of *HIV-1. Methyl salvionolate A inhibits* P24 antigen in HIV-1 infected MT-4 cell with an EC₅₀ of 1.62 μg/ml. Methyl salvionolate A also inhibits HIV-1 reverse transcriptase, protease and integrase with IC₅₀s of 50.58, 10.73 and 7.58 μg/ml, respectively .

HY-B1408

Salicylanilide 2 Publications Verification 2-Hydroxybenzanilide	HIV Integrase HIV	Infection
Salicylanilide demonstrates a wide range of biological activities including antiviral potency which can inhibit HIV virus by targeting **HIV-1 integrase or reverse transcriptase**.

HY-W751039

Bictegravir-d4 GS-9883-d₄	Isotope-Labeled Compounds	Infection
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 .

HY-13238

Dolutegravir Maximum Cited Publications 18 Publications Verification S/GSK1349572	HIV Integrase HIV	Infection
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) .

HY-13238A

Dolutegravir sodium Maximum Cited Publications 18 Publications Verification S/GSK1349572 sodium	HIV Integrase HIV	Infection
Dolutegravir sodium (S/GSK1349572 sodium) 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 sodium (S/GSK1349572 sodium) inhibits HIV-1 viral replication with an IC₅₀ of 0.51 nM in peripheral blood mononuclear cells. Dolutegravir sodium (S/GSK1349572 sodium) retains a high potency against the HIV-1 Y143R, N155H, and G140S/Q148H mutants (EC₅₀=3.6-5.8 nM) .

HY-100083

Dolutegravir intermediate-1	HIV	Others
Dolutegravir intermediate-1 is a synthetic intermediate of Dolutegravir extracted from patent WO 2016125192 A2. Dolutegravir is an integrase inhibitor developed for the treatment of human immunodeficiency virus (HIV)-1 infection.

HY-13238S1

Dolutegravir-d3 S/GSK1349572-d₃	Isotope-Labeled Compounds HIV Integrase HIV	Infection
Dolutegravir-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)[1][2].

HY-13238S2

Dolutegravir-d5 S/GSK1349572-d₅	Isotope-Labeled Compounds HIV Integrase HIV	Infection
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].

HY-134851

HIV-1 inhibitor-6	HIV	Infection
HIV-1 inhibitor-6 (compound 9), a diheteroarylamide-based compound, is a potent HIV-1 pre-mRNA alternative splicing inhibitor. HIV-1 inhibitor-6 blocks HIV replication. HIV-1 inhibitor-6 is active against wild-type HIV-1IIIB (subtype B, X4-tropic) and HIV-1 97USSN54 (subtype A, R5-tropic) with EC₅₀s of 0.6 μM and 0.9 μM, respectively. HIV-1 inhibitor-6 inhibits HIV strains resistant to agents targeting HIV reverse transcriptase, protease, integrase, and coreceptor CCR5 with EC₅₀s ranging from 0.9 to 1.5 μM .

HY-13269

BMS-707035 1 Publications Verification	HIV HIV Integrase	Infection Inflammation/Immunology
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) .

HY-108935

Lavendustin B	HIV Integrase GLUT Tyrosinase	Cancer
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 K_i of 15 µM. Lavendustin B is also a weak inhibitor of tyrosine kinases .

HY-122229

GS-9822	HIV	Infection
GS-9822 is a potent antivira agent with nanomolar activity against wild-type *HIV-1* viruses. GS-9822 potently inhibits the *LEDGF/p75-integrase* interaction with an IC₅₀ of 0.07 μM. GS-9822 has high in vitro metabolic stability and favorable oral pharmacokinetic profiles with low systemic clearance in rats, dogs, and monkeys .

HY-130000

Pirmitegravir STP0404	HIV Integrase HIV	Infection
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 .

HY-153094

BDM-2	HIV HIV Integrase	Infection
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 .

HY-153247

GSK3839919A

HIV Integrase Infection Inflammation/Immunology

GSK3839919A is a potent and allosteric HIV-1integrase inhibitor .

GSK3839919A	HIV Integrase	Infection Inflammation/Immunology
GSK3839919A is a potent and allosteric *HIV-1integrase* inhibitor .

HY-17605S

Bictegravir-15N,d2	Isotope-Labeled Compounds	Infection
Bictegravir- ¹⁵N,d₂ (GS-9883- ¹⁵N,d₂) is the ¹⁵N and deuterium labeled Bictegravir (HY-17605) . Bictegravir (GS-9883) is a potent inhibitor of **HIV-1 integrase with an IC₅₀** of 7.5 nM .

HY-150080

GSK3739936 BMS-986180	HIV HIV Integrase	Infection
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 .

HY-N6711

Equisetin	HIV Integrase	Infection
Equisetin is an N-methylserine-derived acyl tetramic acid isolated from a terrestrial fungus Fusarium equiseti NRRL 5537 . Equisetin is a tetramate-containing natural product with antibiotic and cytotoxic activity . Equisetin inhibits the growth of Gram-positive bacteria and *HIV-1* integrase activity but shows no activity against Gram-negative bacteria . Equisetin is a Quorum-sensing inhibitor (QSI) that attenuates QS-regulated virulence phenotypes in P. aeruginosa without affecting the growth of bacterias, serves as a leading compound for the treatment of P. aeruginosa infections .

HY-18666

D77	HIV	Infection
D77 is anti-HIV-1 inhibitor targeting the interaction between integrase and cellular LEDGF/p75. D77 inhibits HIV-1(IIIB) replication by EC50 value of 23.8 μg/ml in MT-4 cell (5.03 μg/ml for C8166 cells).

HY-14740

Elvitegravir 5+ Cited Publications GS-9137; JTK-303; D06677	HIV Integrase HIV	Infection
Elvitegravir (GS-9137; JTK-303; D06677) is an HIV integrase inhibitor for HIV-1_IIIB, HIV-2_EHO and HIV-2_ROD with IC₅₀ of 0.7 nM, 2.8 nM and 1.4 nM, respectively.

HY-14740S

Elvitegravir-d8 GS-9137-d₈; JTK-303-d₈; D06677-d₈	Isotope-Labeled Compounds HIV Integrase HIV	Infection
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.

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-N0457A

L-Chicoric Acid 1 Publications Verification (-)-Chicoric acid; trans-Caffeoyltartaric acid	Structural Classification other families Classification of Application Fields Simple Phenylpropanols Source classification Phenols Polyphenols Phenylpropanoids Plants Disease Research Fields Cancer	HIV Integrase HIV Endogenous Metabolite
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 .

HY-N6711

Equisetin	Infection Structural Classification Microorganisms Classification of Application Fields Antibiotics Source classification Antibacterial Disease Research Disease Research Fields Other Antibiotics	HIV Integrase
Equisetin is an N-methylserine-derived acyl tetramic acid isolated from a terrestrial fungus Fusarium equiseti NRRL 5537 . Equisetin is a tetramate-containing natural product with antibiotic and cytotoxic activity . Equisetin inhibits the growth of Gram-positive bacteria and *HIV-1* integrase activity but shows no activity against Gram-negative bacteria . Equisetin is a Quorum-sensing inhibitor (QSI) that attenuates QS-regulated virulence phenotypes in P. aeruginosa without affecting the growth of bacterias, serves as a leading compound for the treatment of P. aeruginosa infections .

HY-N7330

Integracin B	Infection Microorganisms Classification of Application Fields Source classification Phenols Polyphenols Disease Research Fields	HIV Integrase HIV
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 .

HY-N11288

Methyl salvionolate A	Structural Classification Labiatae Source classification Phenols Polyphenols Salvia yunnanensis C. H. Wright Plants	HIV
Methyl salvionolate A is a potent inhibitor of *HIV-1. Methyl salvionolate A inhibits* P24 antigen in HIV-1 infected MT-4 cell with an EC₅₀ of 1.62 μg/ml. Methyl salvionolate A also inhibits HIV-1 reverse transcriptase, protease and integrase with IC₅₀s of 50.58, 10.73 and 7.58 μg/ml, respectively .

Cat. No.	Product Name	Chemical Structure

HY-13238S1

Dolutegravir-d3
Dolutegravir-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)[1][2].

Dolutegravir-d3

Dolutegravir-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)[1][2].

HY-W751039

Bictegravir-d4

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-d4
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 .

HY-13238S2

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)[1][2].

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)[1][2].

HY-17605S

Bictegravir-15N,d2
Bictegravir- ¹⁵N,d₂ (GS-9883- ¹⁵N,d₂) is the ¹⁵N and deuterium labeled Bictegravir (HY-17605) . Bictegravir (GS-9883) is a potent inhibitor of **HIV-1 integrase with an IC₅₀** of 7.5 nM .

HY-14740S

Elvitegravir-d8
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.

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