ZL0580 是ZL0590 的结构类似物，通过选择性的结合到 BD1 的BRD4结构域来诱导HIV的表观抑制。ZL0580通过抑制Tat转录激活和转录延长以及在 HIV 启动子上诱导抑制染色质结构来诱导 HIV 的抑制。
| 生物活性 | ZL0580, a structurally close analog of ZL0590, induces epigenetic suppression ofHIVvia selectively binding toBD1domain ofBRD4. ZL0580 inducesHIVsuppression by inhibiting Tat transactivation and transcription elongation as well as by inducing repressive chromatin structure at theHIVpromoter[1][2][3]. |
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体外研究
(In Vitro) | ZL0580 (8 μM, 2 days, PBMCs of viremic HIV-infected individuals) induces HIV transcriptional suppression with low toxicity[1].
ZL0580 treatment (10 μM) suppresses both PMA-stimulated and basal HIV transcription[1].
Cell Viability Assay[1] | Cell 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.
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RT-PCR[1] | Cell 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 Assay[1] | Cell 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.
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | | Powder | -20°C | 3 years | | 4°C | 2 years | | In solvent | -80°C | 6 months | | -20°C | 1 month |
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| 溶解性数据 | In Vitro: DMSO : 250 mg/mL(469.46 mM;Need ultrasonic) 配制储备液 | 1 mM | 1.8778 mL | 9.3891 mL | 18.7783 mL | | 5 mM | 0.3756 mL | 1.8778 mL | 3.7557 mL | | 10 mM | 0.1878 mL | 0.9389 mL | 1.8778 mL |
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