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CAS No.: 1619994-68-1

GSK2801 Catalog No. CSN13657

Synonyms: GSK2801

GSK2801 inhibits BAZ2 family of bromodomain-containing proteins BAZ2A (Kd = 260 nM) and BAZ2B (Kd= 140 nM, IC50 = 9-350 nM).

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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 K_D 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 K_D value of 3.2μM. A chemoproteomic competition binding assay showed that GSK2801 bound to endogenous BAZ2 proteins with a pK_d 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 (T_max=1.0h; C_max=435ng/mL; Terminal _t1/2=1.5h)^[2].
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

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
- 2.6922 mL
- 13.4608 mL
- 26.9215 mL
- 5 mM
- 0.5384 mL
- 2.6922 mL
- 5.3843 mL
- 10 mM
- 0.2692 mL
- 1.3461 mL
- 2.6922 mL

技术信息

CAS号

1619994-68-1

储存条件

粉末: Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C20H21NO4S

运输

蓝冰

分子量

371.45

别名

GSK2801

溶解度

DMSO	72.0 mg/mL (193.8 mM) warming
Water	Insoluble
Ethanol	7.0 mg/mL (18.8 mM) warming

动物实验配方

0.5% CMC+1% Tween 80+water

30 mg/mL

suspension

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GSK2801 Catalog No. CSN13657

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