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GSK2801

GSK2801 是一种有口服活性的和细胞活性的乙酰赖氨酸竞争性BAZ2A 和BAZ2B 溴结构域选择性抑制剂，Kd 值分别为 136 nM 和 257 nM。

CAS号

1619994-68-1

分子式

C20H21NO4S

主要靶点

Epigenetic Reader Domain|Apoptosis

仅限科研使用

Cat No : CM03969

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Synonyms

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  • CAS No.: 1619994-68-1

    GSK2801
    CAS#: 1619994-68-1

产品信息

GSK2801 is an effective, specific and cell active acetyl-lysine competitive inhibitor of BAZ2A(Kd: 136 nM) and BAZ2B(Kd: 257 nM) bromodomains.

CAS号 1619994-68-1
分子式 C20H21NO4S
主要靶点 Epigenetic Reader Domain|Apoptosis
主要通路 凋亡|表观遗传
分子量 371.45
纯度 99.50%， 此纯度可做参考，具体纯度与批次有关系，可咨询客服
储存条件 Powder: -20°C for 3 years | In solvent: -80°C for 1 year
别名

靶点活性

BAZ2B:136 nM(Kd)|BAZ2A:257 nM(Kd)

体内活性

In male CD1 mice, GSK2801 (30 mg/kg, p.o. and i.p.) has reasonable in vivo exposure after oral dosing, modest clearance, and reasonable plasma stability. [1]

体外活性

In U2OS cells transfected with mutant BAZ2A (N1873F), GSK2801 (1 μM) accelerates FRAP half-recovery time by displacing BAZ2A from chromatin. [1]

溶解度

DMSO:18.6 mg/mL (50 mM)

参考文献

1.Chen P, et al. 2015. DOI: 10.1021/acs.jmedchem.5b00209

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
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C1   V1   C2   V2