首页Chromatin/EpigeneticEpigenetic Reader DomainGSK6853
GSK6853
编号 T3311    
CAS 1910124-24-1     分子式 C22H27N5O3     分子量 409.21
靶点: BRPF1; BRPF2; BRPF3;
GSK6853 is a potent, soluble, cell-active, and highly selective inhibitor of the BRPF1 bromodomain.
纯度:99.11%
规格 库存 单价 数量
2 mg 上海现货 442.00
5 mg 上海现货 717.00
10 mg 上海现货 1297.00
50 mg 上海现货 4907.00
100 mg 上海现货 8327.00
1 mL * 10 mM (in DMSO) 上海现货 717.00
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生物活性

产品描述

GSK6853 is a potent, soluble, cell-active, and highly selective inhibitor of the BRPF1 bromodomain.

靶点活性

BRPF1,8.1(pIC50)

BRPF2,5.1(pIC50)

BRPF3,4.8(pIC50)

体外活性

Screening GSK6853 against a panel of 48 unrelated assays reveals only off-target activities that are relatively weak compared to the BRPF1 potency. However, to minimize the chance of off-target effects , the recommended concentration is no higher than 1 μM in cell-based assays[1].

体内活性

In male CD1 mouse, following IV administration (1 mg/kg), GSK6853 demonstrates a high blood clearance of 107 mL/min/kg, a moderate volume of distribution (5.5 L/kg) and a moderate terminal half-life of 1.7 h. Oral administration (PO, 3 mg/kg) achieves a moderate systemic exposure, with a Cmax of 42 ng/mL and Tmax of 1.5 h, resulting in a bioavailability of 22%. The intraperitoneal route of administration (IP, 3 mg/kg) reaches a Cmax of 469 ng/mL and Tmax of 0.25 h, resulting in a bioavailability of 85%. The results indicate that the IP route of administration would be suitable for dosing this molecule in potential PKPD models[1].

动物实验

动物模型:CD1 mice

化学信息

分子量

409.21

分子式

C22H27N5O3

CAS

1910124-24-1

溶解度

DMSO: ≥29 mg/mL

Ethanol: 81 mg/mL (197.81 mM)

( < 1 mg/ml refers to the product slightly soluble or insoluble )

储存条件

store at -80°C

备注

For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

配制溶液

1 mg 5 mg 10 mg
1 mM 2.444 ml 12.219 ml 24.437 ml
5 mM 0.489 ml 2.444 ml 4.887 ml
10 mM 0.244 ml 1.222 ml 2.444 ml
50 mM 0.049 ml 0.244 ml 0.489 ml
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