Ro24-7429 is a potent and orally active HIV-1 transactivator protein Tat antagonist. Ro24-7429 is also a runt-related transcription factor 1 (RUNX1) inhibitor. Ro24-7429 has anti-HIV, antifibrotic and anti-inflammatory effects[1][2].
Ro 24-7429 (0.1-5 μM; 3 days) induces apoptosis of cultured PBMCs in a dose-dependent manner[1].Ro 24-7429 (1-25 μM) also induces apoptosis and inhibits antigen-induced lymphocyte proliferation[1].Ro24-7429 (50-200 μM; 24-72 hours) strongly inhibits the proliferation of A549 and HLF cells in a dose-dependent manner. Ro24-7429 treatment (75 μM) significantly reduces TNF-α-induced up-regulation of RUNX1 mRNA by 50% at 48 hours[2].
Ro24-7429 (17.5-70 mg/kg; i.p.; daily; for 14 or 21 days) treatment robustly ameliorates lung fibrosis and inflammation in the Bleomycin-induced pulmonary fibrosis (PF) mouse model. Ro24-7429 curbs expression of fibrosis markers in injured mouse lungs[2].
[1]. A H Patki, et al. HIV-1 Tat protein and its inhibitor Ro 24-7429 inhibit lymphocyte proliferation and induce apoptosis in peripheral blood mononuclear cells from healthy donors. Cell Immunol. 1996 Apr 10;169(1):40-6.
[2]. Michael O’Hare, et al. Targeting Runt-Related Transcription Factor 1 Prevents Pulmonary Fibrosis and Reduces Expression of Severe Acute Respiratory Syndrome Coronavirus 2 Host Mediators. Am J Pathol. 2021 Jul;191(7):1193-1208.