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[1].

Research Areas >> Infection

Signaling Pathways >> Metabolic Enzyme/Protease >> HIV Protease

IC50: 2.53 nM (HIV-1 protease)[1]

HIV-1 protease-IN-2 (compound 10e) (100 nM) shows a promising inhibition ratio of 68% at 100 nM for wild-type HIV-1[1]. HIV-1 protease-IN-2 (0-1000 nM) shows antiviral activity against DRV (Darunavir)-sensitive or resistant pseudotyped HIV-1 with EC50s of 0.27 µM and 0.59 µM for HIV-1NL4-3 and HIVRDRVS, respectively[1].

[1]. Zhu M, et al. Preliminary SAR and biological evaluation of potent HIV-1 protease inhibitors with pyrimidine bases as novel P2 ligands to enhance activity against DRV-resistant HIV-1 variants. Eur J Med Chem. 2020 Jan 1;185:111866.