ZL0580

ZL0580, a structurally close analog of ZL0590, induces epigenetic suppression of HIV via selectively binding to BD1 domain of BRD4 . ZL0580 induces HIV suppression by inhibiting Tat transactivation and transcription elongation as well as by inducing repressive chromatin structure at the HIV promoter In Vitro ZL0580 (8 μM, 2 days, PBMCs of viremic HIV-infected individuals) induces HIV transcriptional suppression with low toxicity. ZL0580 treatment (10 μM) suppresses both PMA-stimulated and basal HIV transcription. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Viability AssayCell Line: HIV-infected human CD4+ T cells. Concentration: 0-8 μM. Incubation Time: 2 days. Result: Suppress HIV in primary CD4+ T cell. Single treatment (8 μM) led to almost completed loss of productive HIV infection in CD4+ T cells. RT-PCRCell Line: PBMCs of viremic HIV-infected individuals. Concentration: 8 μM. Incubation Time: 2 days. Result: Suppresses HIV transcription ex vivo in PBMCs of viremic HIV-infected individuals. Cell Cytotoxicity AssayCell Line: J-Lat cells. Concentration: 0-80 μM. Incubation Time: 1 and 3 days. Result: Did not cause significant cell death at concentrations below 40 μM. Treatment of J-Lat cells with ZL0580 (10 μM) also did not cause significant cell death on days 2, 7, and 14 compared with NC in both PMA-activated and unstimulated cells. Form:Solid IC50& Target:BRD4 (BD1)

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