HIV-1 integrase inhibitor 2

Short Summary : HIV-1 integrase inhibitor

Category : Microbiology & Virology|HIV

Purity : 0.98

CAS Number : 957890-42-5

Formula : C21H20ClNO2

Molecular Weight : 353.84

SMILE : CCCC(C1=C(N=C2C=CC(=CC2=C1C3=CC=CC=C3)Cl)C)C(=O)O

Solubility : Soluble in DMSO

Storage : Store at -20°C

Description : The human immunodeficiency virus (HIV) is the causative agent for the acquired immunodeficiency syndrome (AIDS), then HIV integrase is an attractive target for new anti-HIV drugs. HIV-1 integrase inhibitor 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.In vitro: On the basis of the available information, the authors synthesized several close analogs and discovered three new compounds with increased activity in vitro and in cell culture, thereby achieving an approximately tenfold increase of activity in AlphaScreen (IC50 = 1.37 ± 0.36 μM) and a nearly 20-fold increase in antiviral activity (EC50 = 2.35 ± 0.28 μM) for the most active compound, HIV-1 integrase inhibitor 2. The interaction of LEDGF/p75 with neither JPO2 nor PogZ (cellular binding partners of LEDGF/p7527–29) was inhibited, suggesting binding of the compound to integrase and not to LEDGF/p75. HIV-1 integrase inhibitor 2 did not affect integrase-DNA binding and only weakly inhibited the catalytic activities of integrase. These findings point to a different mechanism of action than that observed for the strand-transfer inhibitors raltegravir and elvitegravir. No inhibitory activity of HIV-1 integrase inhibitor 2 was detected against HIV-1 reverse transcriptase [1]. In vivo: Currently no in-vivo data available. Clinical trial: Currently no clinical data available.Reference:[1] Christ F, Voet A, Marchand A, Nicolet S, Desimmie BA, Marchand D, Bardiot D, Van der Veken NJ, Van Remoortel B, Strelkov SV, De Maeyer M, Chaltin P, Debyser Z. Rational design of small-molecule inhibitors of the LEDGF/p75-integrase interaction and HIV replication. Nat Chem Biol. 2010;6(6):442-8.

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