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首页-小分子抑制剂&激动剂-Wnt/Notch/Hedgehog-Casein Kinase-GO289
GO289

Chemical Structure : GO289

CAS No.: 694522-87-7

GO289 (GO-289;GO 289)

货号: PC-36021Not For Human Use, Lab Use Only.

GO289 (GO-289, GO 289) is a potent and selective inhibitor of casein kinase 2 (CK2) with IC50 of 7 nM in in vitro kinase assays, shows minor effects on CKIδ and CKIα activity in vitro.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

GO289 (GO-289, GO 289) is a potent and selective inhibitor of casein kinase 2 (CK2) with IC50 of 7 nM in in vitro kinase assays, shows minor effects on CKIδ and CKIα activity in vitro.
GO289 showed only a moderate or minor effect on the activity of 59 kinases from a variety of classes, the second most affected kinase was PIM2 with an IC50 of 13 nM.
GO289 caused dose-dependent lengthening of circadian period not only in Bmal1-dLuc reporter cells but also in Per2-dLuc reporter cells with a phase opposite to that of Bmal1-dLuc.
GO289 inhibits phosphorylation of clock protein PER2 S693 in cells; strongly inhibits Caki-2, A498, and 769-P cancer cells, significantly reduces growth of mouse MLL-AF9 leukemia cells without effect on hematopoietic progenitor cells.
GO289 shows effectivity on circadian period and reporter signal intensity in spleen explants of MLL-AF9 mice.

物理化学性质&存储条件

分子量 419.297
分子式 C17H15BrN4O2S
外观性状 Solid
CAS No.
储存条件
固体粉末
-20 °C 12 个月; 4°C 6 个月
配置液
-80 °C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

5-bromo-2-methoxy-4-(((3-(methylthio)-5-phenyl-4H-1,2,4-triazol-4-yl)imino)methyl)phenol

参考文献

1. Tsuyoshi Oshima, et al. Science Advances 23 Jan 2019: Vol. 5, no. 1, eaau9060. DOI: 10.1126/sciadv.aau9060.

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