货号	规格	价格	上海	北京	珠海	重庆	武汉
S81376-2mg买3赠1	99.70%	￥255.00 S81376-2mg ￥255.00 现货（买3赠1）	5 5	-	-	-	-
S81376-5mg买3赠1	99.70%	￥370.00 S81376-5mg ￥370.00 现货（买3赠1）	5 5	-	-	-	-
S81376-10mg买3赠1	99.70%	￥495.00 S81376-10mg ￥495.00 现货（买3赠1）	5 5	-	-	-	-
S81376-25mg买3赠1	99.70%	￥990.00 S81376-25mg ￥990.00 现货（买3赠1）	5 0 5	-	-	-	-
S81376-50mg	≥98%	￥1590.00 S81376-50mg ￥1590.00 2-3天	0 货期：2-3天	-	-	-	-
S81376-100mg	≥98%	￥2500.00 S81376-100mg ￥2500.00 2-3天	0 货期：2-3天	-	-	-	-

大包装询价收藏产品

加入购物车

产品描述：

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

靶点：

Kd: 136 nM (BAZ2A) and 257 nM (BAZ2B);Apoptosis; EpigeneticReaderDomain

体外研究：

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. GSK2801 or RNAi knockdown of BAZ2A/B with JQ1 selectively displaced BRD2 at promoters/enhancers of ETS-regulated genes. In 2D cultures, enhances displacement of BRD2 from chromatin by combination drug treatment induced senescence. In spheroid cultures, combination treatment induces cleaved caspase-3 and cleaved PARP characteristic of apoptosis in tumor cells. Thus, GSK2801 blocks BRD2-driven transcription in combination with BET inhibitor and induces apoptosis of TNBC

体内研究：

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

参考文献：

1. Chen P, et al. Discovery and Characterization of GSK2801, a Selective Chemical Probe for the Bromodomains BAZ2A and BAZ2B. J Med Chem. 2016 Feb 25;59(4):1410-24. 2. Bevill SM, et al. GSK2801, a BAZ2/BRD9 Bromodomain Inhibitor, Synergizes with BET Inhibitors to Induce Apoptosis in Triple-Negative Breast Cancer. Mol Cancer Res. 2019 Jul;17(7):1503-1518.

溶解性：

soluble in DMSO

保存条件：

-20℃

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	2.692 ml	13.461 ml	26.922 ml
5 mM	0.538 ml	2.692 ml	5.384 ml
10 mM	0.269 ml	1.346 ml	2.692 ml
50 mM	0.054 ml	0.269 ml	0.538 ml

注意：

部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

参考文献

质检证书(COA)

输入产品批号：

如何获取质检证书(COA)?

请输入货号和一个与之匹配的批号。
例如:
批号：JS298415 货号：S20001-25g
在货品标签上如何找到货号和批号?

摩尔浓度计算器

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)

质量

浓度

体积

分子摩尔量

计算重置