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HIV-1 integrase inhibitor 2
Cat No.
CEI-1362
Description
HIV-1 integrase inhibitor 2 is an inhibitor of HIV-1 integrase used in the treatment of human immunodeficiency virus (HIV) infection
Product Overview
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.
CAS No.
957890-42-5
Molecular Weight
353.84
Purity
0.98
Storage
Store at -20°C
Targets
HIV-1
Molecular Formula
C21H20ClNO2
Chemical Name
2-(6-chloro-2-methyl-4-phenylquinolin-3-yl)pentanoic acid
Solubility
Soluble in DMSO
Shipping Conditions
Evaluation sample solution: ship with blue ice. All other available size: ship with RT, or blue ice upon request
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 inter¬ action 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.
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