化学性质:
规格 | 10mg 50mg 200mg |
CAS | 1373422-53-7 |
别名 |
|
化学名 | 3-[[2-pyridin-2-yl-6-(1,2,4,5-tetrahydro-3-benzazepin-3-yl)pyrimidin-4-yl]amino]propanoic acid |
分子式 | C22H23N5O2 |
分子量 | 389.45 |
溶解度 | ≥ 38.9 mg/mL in DMSO, ≥ 51.2 mg/mL in EtOH with ultrasonic |
储存条件 | Store at -20°C |
General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
Shipping Condition | Evaluation sample solution : ship with blue ice |
产品描述:
GSK J1 is a potent and selective inhibitor of the histone H3 lysine 27 (H3K27) demethylase JMJD3, a Fe2+- and α-ketoglutarate-dependent oxygenase involved in a variety of physiological functions including the inflammatory response, with the half maximal inhibition concentration IC50 value of 60 nM [1].
However, GSK J1 has restricted cellular permeability due to its highly polar carboxylate group, which plays a critical role in the binding of GSK J1 to JMJD3. In order to improve the cellular permeability, GSK J1 is esterified to mask the polarity generating an ethyl ester derivative that can be rapidly hydrolyzed to GSK J1 [1].
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