GSK6853
| 规格 | 价格 | 货期 | 数量 |
|---|---|---|---|
| 1mL(10 mM in DMSO) | ￥656.00 | 10-15工作日发货 | |
| 5mg | ￥711.00 | 10-15工作日发货 | |
| 10mg | ￥1260.00 | 10-15工作日发货 | |
| 50mg | ￥4536.00 | 10-15工作日发货 | |
| 100mg | ￥7257.00 | 10-15工作日发货 |
特色产品
- 适用于流式细胞仪和荧光显微镜检测
- 准确区分活细胞/凋亡细胞/坏死细胞
- 用于免疫印迹和质谱分析等后续操作
- 适用于30 KDa-130 KDa大小的蛋白
- 对细胞无毒性
- 步骤更简单，无需有机溶剂
- 可将信号灵敏度提高100倍
- 同时保持稳定的特异性和分辨率
- 提供更高的转录效率并抑制免疫激活
- 使用5-moUTP和Cy5-utp修饰
- 优异的扩增效率、可重复性和稳定性
- 卓越的灵敏度和准确性，操作简单
- 优化的缓冲液和T7 RNA聚合酶混合物
- 20 μL反应体系可获得更高的RNA产量
产品描述
pIC50: 8.1
GSK6853 is a BRPF1 inhibitor.
The BRPF (Bromodomain and PHD Fingercontaining) protein family are key scaffolding proteins for assembly of MYST histone acetyltransferase complexes.
In vitro: In previous study, GSK6853 was tested in the BROMOscan panel of bromodomain binding assays and the results showed that consistent with the previous findings, it showed excellent BRPF1 potency (pKd 9.5) and greater than 1600-fold selectivity over all other bromodomains tested. In addition, screening GSK6853 against a panel of 48 unrelated assays revealed only off-target activities that were relatively weak compared to its high BRPF1 potency [1].
In vivo: To assess the suitability of GSK6853 for in vivo studies, its DMPK characteristics were studied in male CD1 mice by i.v., po, and i.p. administration. The results indicated that the i.p. route of administration would be suitable for dosing this molecule in further PK/PD models. Moreover, in order to be able to compare biochemical potency measurements to free blood concentrations, the fraction unbound in the CD1 mouse was also tested with a resulting value of 7.9% [1].
Clinical trial: So far, no clinical study has been conducted.
Reference:
[1] Bamborough, P. ,Barnett, H.A.,Becher, I., et al. GSK6853, a chemical probe for inhibition of the BRPF1 bromodomain. ACS Med. Chem. Lett. 7(6), 552-557 (2016).
产品性质
| 物理外观 | A crystalline solid |
| CAS号 | 1910124-24-1 |
| 分子式 | C22H27N5O3 |
| 分子量 | 409.5 |
| 化学名称 | N-[2,3-dihydro-1,3-dimethyl-6-[(2R)-2-methyl-1-piperazinyl]-2-oxo-1H-benzimidazol-5-yl]-2-methoxy-benzamide |
| 溶解度 | ≤30mg/ml in ethanol;25mg/ml in DMSO;30mg/ml in dimethyl formamide |
| SMILES | C[C@H](CNCC1)N1c(c(NC(c(cccc1)c1OC)=O)c1)cc(N2C)c1N(C)C2=O |
| 存储条件 | -20°C |
| 运输条件 | 蓝冰 |
产品应用 (实验数据来自文献，APExBIO并未验证，仅供参考)
IC50和靶点
| 生物活性描述 | GSK6853 是 BRPF1 溴odomain 的强效选择性抑制剂。GSK6853 具有出色的 BRPF1 效用（pKd=9.5），其选择性超过所有其他溴域的 1600 倍。 |
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