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GSK6853

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Chemical Structure| 1910124-24-1 同义名 : -
CAS号 : 1910124-24-1
货号 : A181180
分子式 : C22H27N5O3
纯度 : 99%+
分子量 : 409.481
MDL号 : MFCD30489734
存储条件：

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

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 25 mg/mL(61.05 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
靶点

  • BRPF

    BRPF1, pIC50:8.1
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 pKd 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].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.44mL

0.49mL

0.24mL

12.21mL

2.44mL

1.22mL

24.42mL

4.88mL

2.44mL
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.