GSK-5959

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GSK-5959  纯度: 98.29%

GSK-5959 是有效的、选择性的、细胞渗透性的 BRPF1 溴端结构域的抑制剂，其 IC50 值为 80 nM。

GSK-5959

GSK-5959 Chemical Structure

CAS No. : 901245-65-6

规格 价格 是否有货 数量
Free Sample (0.1-0.5 mg)   Apply now  
10 mM * 1 mL in DMSO ￥990 In-stock
5 mg ￥900 In-stock
10 mg ￥1500 In-stock
50 mg ￥4500 In-stock
100 mg   询价  
200 mg   询价  

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生物活性

GSK-5959 is a potent, selective and cell permeable BRPF1 bromodomain inhibitor with an IC50 of ~ 80 nM[1].

IC50 & Target

IC50: 80 nM (BRPF1)[1].
体外研究
(In Vitro)

GSK-5959 (3a) also displays selectivity over the closely related family members, BRPF2 (100-fold) and BRPF3 (>1000-fold)[2].
GSK-5959 (3a) exhibits an EC50 = 0.98 μM) in cellular NanoBRET assay[2].
GSK-5959 has no effect on TRIM24 SUMOylation[3].

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.
分子量

394.47

Formula

C22H26N4O3
CAS 号

901245-65-6
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 13 mg/mL (32.96 mM; Need ultrasonic and warming)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.5350 mL 12.6752 mL 25.3505 mL
5 mM 0.5070 mL 2.5350 mL 5.0701 mL
10 mM 0.2535 mL 1.2675 mL 2.5350 mL

*

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。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。
参考文献

  • [1]. Demont EH, et al. 1,3-Dimethyl Benzimidazolones Are Potent, Selective Inhibitors of the BRPF1 Bromodomain. (2014) ACS Med Chem Lett. 5(11):1190-1195.

    [2]. Wylie S.Palmer, et al. Development of small molecule inhibitors of BRPF1 and TRIM24 bromodomains Discovery Today: Technologies Volume 19, March 2016, Pages 65-71.

    [3]. Srikanth Appikonda, et al. Cross-talk between chromatin acetylation and SUMOylation of tripartite motif-containing protein 24 (TRIM24) impacts cell adhesionJ Biol Chem. 2018 May 11;293(19):7476-7485.

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