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CAS No.: 1550053-02-5

BRD3308 Catalog No. CSN20569

Synonyms: Brd3308

BRD3308 is a highly selective inhibitor of histone deacetylase 3 (HDAC3) with an IC50 value of 65 nM for HDAC3 vs.

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技术信息

生物活性

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].
参考文献

[1] Dirice E, Ng R, et al. Isoform-selective inhibitor of histone deacetylase 3 (HDAC3) limits pancreatic islet infiltration and protects female nonobese diabetic mice from diabetes. J Biol Chem. 2017 Aug 31. pii: jbc.M117.804328.
[2] Wagner FF, Lundh M, 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.
[3] Barton KM, Archin NM, Keedy KS, Espeseth AS, Zhang YL, Gale J, Wagner FF, Holson EB, Margolis DM. Selective HDAC inhibition for the disruption of latent HIV-1 infection. PLoS One. 2014 Aug 19;9(8):e102684.
[4] Lundh M, Galbo T, Poulsen SS, Mandrup-Poulsen T. Histone deacetylase 3 inhibition improves glycaemia and insulin secretion in obese diabetic rats. Diabetes Obes Metab. 2015 Jul;17(7):703-7.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 3.4808 mL
- 17.4041 mL
- 34.8082 mL
- 5 mM
- 0.6962 mL
- 3.4808 mL
- 6.9616 mL
- 10 mM
- 0.3481 mL
- 1.7404 mL
- 3.4808 mL

技术信息

CAS号

1550053-02-5

储存条件

粉末: Keep in dark place,Inert atmosphere,Room temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C15H14FN3O2

运输

蓝冰

分子量

287.29

别名

Brd3308

溶解度

DMSO	57.0 mg/mL (198.4 mM)
Water	Insoluble
Ethanol	Insoluble

动物实验配方

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