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 (apoptosis)，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。
货号:ajcx16842
CAS:1550053-02-5
分子式:C15H14FN3O2
分子量：287.29
溶解度:DMSO: 250 mg/mL (870.20 mM)
纯度：98%
存储：Store at -20°C
库存：现货

Background:

BRD3308 is a highly selective HDAC3 inhibitor with an IC50 of 54 nM. BRD3308 is 23-fold selectivity for HDAC3 over HDAC1 (IC50 of 1.26 μM) or HDAC2 (IC50 of 1.34 μM). BRD3308 suppresses pancreatic β-cell apoptosis induced by inflammatory cytokines or glucolipotoxic stress, and increases functional insulin release. BRD3308 activates HIV-1 transcription and disrupts HIV-1 latency[1][2][3].

[1]. Barton KM, et al. Selective HDAC inhibition for the disruption of latent HIV-1 infection. PLoS One. 2014 Aug 19;9(8):e102684. [2]. Lundh M, et al. Histone deacetylase 3 inhibition improves glycaemia and insulin secretion in obese diabetic rats. Diabetes Obes Metab. 2015 Jul;17(7):703-7. [3]. Wagner FF, et al. An Isochemogenic Set of Inhibitors To Define the Therapeutic Potential of Histone Deacetylases in β-Cell Protection. ACS Chem Biol. 2016 Feb 19;11(2):363-74.