Acriflavine

Acriflavine (Acriflavinium chloride) is a fluorescent acridine dye that can be used to label nucleic acid. Acriflavine is an antiseptic agent. Acriflavine is a potent HIF-1 inhibitor that prevents the dimerization of HIF-1α and HIF-1β subunits. Acriflavine inhibits the interaction between monocarboxylate transporter 4 (MCT4) and Basigin. Acriflavine is used in cancer research, such as breast cancer, brain tumor and chronic myeloid leukemia. Acriflavine is a potent papain-like protease (PLpro) inhibitor, which inhibits SARS-CoV-2^{[1][2][3][4][5][6]}. In Vitro: Acriflavine inhibits MCT4-Basigin dependent Rluc activity in a dose-dependent fashion with an IC₅₀ of 4.6 μM. The IC₅₀ for Acriflavine inhibiting NhRL-MCT1/ Basigin-ChRL interaction is calculated to be ~19.5 μM^[3].
Acriflavine (5 μM; treatment for 24 hours) does not significantly affect hypoxia-induced lactate production and secretion in HSR-GBM1 cells^[3].
Acriflavine (1-25 μM; treatment for 72 hours) reduces the clonogenic potential of several neurosphere-derived cells and is more obvious under hypoxic conditions^[3].
Acriflavine (1-10 μM; treatment for 24 hours) inhibits the replication of SARS-CoV-2 in Vero and A549ACE2⁺ cells and has low cytotoxicity^[6]. In Vivo: Acriflavine (8 mg/kg; intraperitoneal injection; once a day; 13 administrations) inhibits tumor growth and angiogenesis in NOG mice bearing large HSR-GBM1-Luc cell-derived xenografts^[3].
Acriflavine (8 mg/kg; intraperitoneal injection; once a day; 15 administrations) inhibits tumor growth in NOG mice bearing small HSR-GBM1-Luc cell-derived xenografts^[3].
Acriflavine (8 mg/kg; intraperitoneal injection; once a day; 10 days of administration) reduces the development of chronic myeloid leukemia and the maintenance of leukemia stem cells in C57BL/6J-CD45.1 mice transplanted with BCR/abl-transduced bone marrow cells^[5].
Acriflavine (100 mg/kg orally; 5-15 mg/kg intramuscularly; once a day orally, twice a day intramuscularly; 6 days of administration) inhibits the replication of SARS-CoV-2 in the brain and lungs of K18-ACE2 transgenic mice^[6].