生物活性分子抑制剂 特异性抑制剂 激动剂 化合物库 重组蛋白 GSK2801 纯度: 99.93%
GSK2801 是一种有效的,选择性的,口服活性的和细胞活性的乙酰赖氨酸竞争性 BAZ2A 和 BAZ2B 溴结构域抑制剂,Kd 值分别为 136 nM 和 257 nM。GSK2801 对 BAZ2A/B 的选择性是 BRD4 的 50 倍以上。
GSK2801 Chemical Structure
CAS No. : 1619994-68-1
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Free Sample (0.1-0.5 mg) | Apply now | ||
10 mM * 1 mL in DMSO | ¥715 | In-stock | |
5 mg | ¥650 | In-stock | |
10 mg | ¥870 | In-stock | |
50 mg | ¥3500 | In-stock | |
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200 mg | 询价 |
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GSK2801 相关产品
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生物活性 |
GSK2801 is a potent, selective, orally active and cell active acetyl-lysine competitive BAZ2A and BAZ2B bromodomains inhibitor with Kd values of 136 nM and 257 nM, respectively. GSK2801 shows >50-fold selectivity for BAZ2A/B over BRD4[1]. |
IC50 & Target |
Kd: 136 nM (BAZ2A) and 257 nM (BAZ2B)[1] |
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体外研究 (In Vitro) |
GSK2801 binds TAF1L(2) with an affinity KB of 0.31μM (KD: 3.2 μM) and a binding enthalpy change ΔH of −8.6 kcal/mol. ITC experiments using the bromodomain of BRD9 results in the determination of an affinity KB of 0.826 μM (KD: 1.1 μM) and ΔH of −9.8 kcal/mol[1]. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only. |
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体内研究 (In Vivo) |
In order to determine the suitability of GSK2801 for in vivo experiments, pharmacokinetic parameters after intraperitoneal and oral dosing to male CD1 mice is measured. GSK2801 has reasonable in vivo exposure after oral dosing, modest clearance, and reasonable plasma stability[1]. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only. |
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分子量 |
371.45 |
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Formula |
C20H21NO4S |
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CAS 号 |
1619994-68-1 |
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运输条件 |
Room temperature in continental US; may vary elsewhere. |
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储存方式 |
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溶解性数据 |
In Vitro:
DMSO : 50 mg/mL (134.61 mM; Need ultrasonic) 配制储备液
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请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 In Vivo:
请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
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参考文献 |
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