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GSK2801

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Chemical Structure| 1619994-68-1 同义名 : -
CAS号 : 1619994-68-1
货号 : A884058
分子式 : C20H21NO4S
纯度 : 99%+
分子量 : 371.45
MDL号 : MFCD26142953
存储条件：

粉末 Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 50 mg/mL(134.61 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：

0.5% CMC+1% Tween 80+water 30 mg/mL suspension

生物活性
靶点

  • bromodomain

    BAZ2B, Kd:136 nM

    BAZ2A, Kd:257 nM
描述 BAZ2A and BAZ2B are bromodomain-containing proteins that constitute the central scaffolding protein of the nucleolar remodeling complex (NoRC). GSK2801 is a potent, selective, cell-active inhibitor of BAZ2A and BAZ2B bromodomains. It binds to the BAZ2 bromodomains of BAZ2A and BAZ2B with KD values of 257 and 136nM, respectively. GSK2801 at a concentration of 10μM led to a temperature shift of 4.1 and 2.7°C for BAZ2A and BAZ2B, respectively. An isothermal titration calorimetry binding experiment showed that GSK2801 bound to TAF1L(2) with a binding enthalpy change ΔH of −8.6(±0.02)kcal/mol and a KD value of 3.2μM. A chemoproteomic competition binding assay showed that GSK2801 bound to endogenous BAZ2 proteins with a pKd value of 5.5. In male CD1 mice, GSK2801 exhibited reasonable in vivo exposure, modest clearance, and reasonable plasma stability after an oral dosing of 30mg/kg (Tmax=1.0h; Cmax=435ng/mL; Terminal t1/2=1.5h)[2].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.69mL

0.54mL

0.27mL

13.46mL

2.69mL

1.35mL

26.92mL

5.38mL

2.69mL
参考文献

[1]Chen P, Chaikuad A, et al. Discovery and Characterization of GSK2801, a Selective Chemical Probe for the Bromodomains BAZ2A and BAZ2B. J Med Chem. 2015 Apr 6.

[2]Chen P, Chaikuad A, Bamborough P, et al. Discovery and Characterization of GSK2801, a Selective Chemical Probe for the Bromodomains BAZ2A and BAZ2B. J Med Chem. 2016;59(4):1410-1424. doi:10.1021/acs.jmedchem.5b00209