Efavirenz

Efavirenz is a non-nucleoside reverse transcriptase inhibitor (NNRTI) that exhibits antiviral and anticancer activities. Efavirenz binds to wild-type and mutant HIV-1 RTs (Ki= 2.93nM and 3.85-56.5nM, respectively). It inhibits wild-type and mutant HIV-1 viral replication in MT-4 human T lymphoid cells (IC95s = 1.5-1,500 nM). Efavirenz also prevents RNA plus-strand initiation with an IC50 value of 17nM. Efavirenz is an anti-HIV drug, commonly used in combination therapy for AIDS treatment. It is part of highly active antiretroviral therapy (HAART) for the treatment of a human immunodeficiency virus (HIV) type 1. In various cancer cell lines, Efavirenz inhibits cellular proliferation and increases activation of p53. CARD8 inflammasome senses HIV-1 protease activity. In HIV-infected cells, CARD8 cannot detect the virus because the viral protease remains inactive as a subunit of unprocessed Gag-Pol polyprotein. HIV-1-specific non-nucleoside reverse transcriptase inhibitors (NNRTIs), such us Efavirenz, can trigger CARD8 sensing because they bind to HIV-1 Pol and enhance intracellular Gag-Pol polyprotein dimerization, which causes premature viral protease activation. Treating HIV-1-infected macrophages and CD4+ T cells with NNRTIs leads to CARD8-mediated caspase-1 activation and pyroptotic cell death. Induction of the CARD8 inflammasome activation has led to rapid clearance of latent HIV-1 in patient CD4+ T cells after virus reactivation. Appearance: White to off-white solid. Solubility: Soluble in DMSO (10mg/ml), DMF (20mg/ml) or ethanol (10mg/ml). Insoluble in water. InChi Key: XPOQHMRABVBWPR-UHFFFAOYSA-N Smiles: ClC1=CC=C2C([C@@](C#CC3CC3)(C(F)(F)F)OC(N2)=O)=C1