Uses
(±)-BI-D is a potent ALLINI(An allosteric IN inhibitor) that binds integrase at the LEDGF/p75 binding site.
IC50 value: 2.4–2.9 μM(HIV-Luc infection of WT and Hdgfrp2 KO cells) [1]
Target: integrase inhibitor
in vitro: Approximately 2.4–2.9 μM of BI-D was required to inhibit 50% of HIV-Luc infection of WT and Hdgfrp2 KO cells, while the IC50 decreased dramatically, to 160–200 nM, in Psip1 and double-KO cells [1].
References
[1] Wang H, et al. HRP2 determines the efficiency and specificity of HIV-1 integration in LEDGF/p75 knockout cells but does not contribute to the antiviral activity of a potent LEDGF/p75-binding site integrase inhibitor. Nucleic Acids Res. 2012 Dec;40(22):11518-30. DOI:
10.1093/nar/gks913[2] Fader LD, et al. Minimizing the Contribution of Enterohepatic Recirculation to Clearance in Rat for the NCINI Class of Inhibitors of HIV. ACS Med Chem Lett. 2014 Apr 16;5(6):711-6. DOI:
10.1021/ml500110j
