生物活性 | |||
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描述 | Selective histone deacetylases (HDAC) are a family of enzymes that regulate the transcription of cellular and viral genes. HDAC inhibitors have emerged as anti-latency therapeutic options for persistent HIV-1 infection. BRD3308 is a highly selective, small-molecule inhibitor of HDAC3 with an IC50 value of 54nM. BRD3308 is 23-fold more selective for HDAC3 over HDAC1 (IC50=1.26μM) and HDAC2 (IC50=1.34μM). The IC50 values of BRD3308 for HDAC4–9 are above 33μM. Treatment of 2D10 cells with 10–30µM BRD3308 for 12 hours increased the expression of HIV-1. The overnight exposure of patients’ resting CD4+ T cells to 15µM BRD3308 induced viral outgrowth. Treatment of PBMCs with various concentrations of BRD3308 (5, 10, 15, or 30µM) for 24 hours did not significantly decrease cell viability compared with vehicle-treated controls[3]. In male ZDF rats, a model of type 2 diabetes, administration with BRD3308 (5mg/kg, i.p.) every second day starting from 7 weeks of age prior to the development of hyperglycemia significantly lowered glycemia by 61% and increased average steady-state glucose-infusion rate compared to vehicle-treated group. The plasma insulin concentration was 84% higher in BRD3308-treated rats. The pancreatic islet area in BRD3308-treated animals was also significantly larger than that in the control group[4]. |
实验方案 | |||
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1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
3.48mL 0.70mL 0.35mL |
17.40mL 3.48mL 1.74mL |
34.81mL 6.96mL 3.48mL |
参考文献 |
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