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BRD3308

CAS No. : 1550053-02-5

MCE 国际站：BRD3308

产品活性：BRD3308 是一种高选择性的 HDAC3 抑制剂，IC₅₀ 为 54 nM。BRD3308 对 HDAC3 的选择性是 HDAC1 (IC₅₀ 为 1.26 μM) 或 HDAC2 (IC₅₀ 为 1.34 μM) 的 23 倍。BRD3308 抑制由炎性细胞因子或糖脂毒性应激诱导的胰腺 β 细胞凋亡，并增加功能性胰岛素释放。BRD3308 还可激活 HIV-1 转录并破坏 HIV-1 潜伏期。

研究领域：Cell Cycle/DNA Damage  |  Epigenetics  |  Anti-infection  |  Apoptosis

作用靶点：HDAC  |  HIV  |  Apoptosis

In Vitro: BRD3308 (5-30 µM; 6-24 hours) treatment increases HIV-1 expression in the 2D10 cell line.
BRD3308 (15 µM; overnight) is able to induce outgrowth of HIV-1 from latently infected cells ex vivo in resting CD4+ T cells.BRD3308 inhibits HDAC1, HDAC2 and HDAC3 with K_i values of 5.1 μM, 6.3 μM and 29 nM, respectively.

In Vivo: BRD3308 (5 mg/kg; intraperitoneal injection; every second day; male Zucker Diabetic Fatty rats) treatment reduces hyperglycaemia and increases insulin secretion in a rat model of type 2 diabetes. At the end of the hyperglycaemic clamp, circulating insulin levels are significantly higher in BRD3308-treated rats. Pancreatic insulin staining and contents are also significantly higher. BRD3308 preserves the functional β-cell mass against glucolipotoxicity in vivo.

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