1910124-24-1|GSK6853|CsnPharm

CAS No.: 1910124-24-1

GSK6853 Catalog No. CSN18953

Synonyms: GSK6853

GSK6853 selectively inhibits the BRPF1 bromodomain with the pKd value of 9.5.

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400-920-2911

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靶点选择性

生物活性

实验方案

技术信息

生物活性

描述The bromodomain and PHD finger-containing (BRPF) family of BRPF1 is essential for the assembly of MYST histone acetyltransferase complexes. GSK6853 is a potent, selective, soluble, and cell-active inhibitor of the BRPF1 bromodomain (TR-FRET pIC50=8.1; NanoFRET pIC50=7.7). In the BROMOscan panel of bromodomain binding assay, GSK6853 exhibited potent inhibition towards BRPF1 with a pK_d value of 9.5 and >1600-fold selectivity over other bromodomains. In male CD1 mice, GSK6853 showed a high blood clearance (107mL/min/kg), a moderate volume of distribution (5.5L/kg) and a moderate terminal half-life (1.7h) following intravenous injection (1mg/kg). Via oral administration (3 mg/kg), GSK6853 demonstrated a moderate systemic exposure (Cmax=42ng/mL; Tmax=1.5h) and a bioavailability of 22%. Intraperitoneal administration (3 mg/kg) achieved a Cmax of 469ng/mL, Tmax of 0.25h, and a bioavailability of 85%^[2].
参考文献

[1] Bamborough P, Barnett HA, et al. GSK6853, a Chemical Probe for Inhibition of the BRPF1 Bromodomain. ACS Med Chem Lett. 2016 May 9;7(6):552-7.
[2] Bamborough P, Barnett HA, Becher I, et al. GSK6853, a Chemical Probe for Inhibition of the BRPF1 Bromodomain. ACS Med Chem Lett. 2016;7(6):552-557.

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
- 2.4421 mL
- 12.2106 mL
- 24.4211 mL
- 5 mM
- 0.4884 mL
- 2.4421 mL
- 4.8842 mL
- 10 mM
- 0.2442 mL
- 1.2211 mL
- 2.4421 mL

技术信息

CAS号

1910124-24-1

储存条件

粉末: Sealed in dry,Store in freezer, under -20°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C22H27N5O3

运输

蓝冰

分子量

409.48

别名

GSK6853

溶解度

DMSO	112.0 mg/mL (273.5 mM)
Water	insoluble

动物实验配方

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