GSK-3β inhibitor 8

Names

[ Name ]:
GSK-3β inhibitor 8

[Synonym ]:
GSK3Î² Inhibitor XVIII
(2-Chloro-4-{[4-(2-thienyl)-2-pyrimidinyl]amino}phenyl)(4-methyl-1-piperazinyl)methanone
Methanone, [2-chloro-4-[[4-(2-thienyl)-2-pyrimidinyl]amino]phenyl](4-methyl-1-piperazinyl)-

Biological Activity

[Description]:

GSK-3β inhibitor 8, a thiophenacil derivative, is an effective and selective inhibitor of GSK-3β (IC50=64 nM). GSK-3β inhibitor 8 negatively regulated Wnt signaling pathway and stimulated β cell proliferation[1][2].

[Related Catalog]:

Signaling Pathways >> Stem Cell/Wnt >> GSK-3

Research Areas >> Inflammation/Immunology

Signaling Pathways >> PI3K/Akt/mTOR >> GSK-3

[Target]

GSK-3β:64 nM (IC50)

[In Vitro]

GSK-3β inhibitor 8 (化合物 1a) (1 nM-100 μM; 7 d) 剂量依赖性地刺激 β 细胞增殖，EC50 值为 1.41 μM。GSK-3β inhibitor 8 (2 μM; 72 h) 使复制 R7T1 β 细胞增加约 2 倍[1]。 GSK-3β inhibitor 8 (1 nM-100 μM; 24 h) 诱导 Super (8X) TOPFlash 报告晶活化，EC50 值为 1.25 μM[1]。 GSK-3β inhibitor 8 (2 μM; 72 h) 刺激 HEK293 细胞 β-catenin 转位进入细胞核[1]。

[References]

[1]. Wang W, et al. Identification of small-molecule inducers of pancreatic beta-cell expansion. Proc Natl Acad Sci U S A. 2009 Feb 3;106(5):1427-32.

Chemical & Physical Properties

[ Density]:
1.4±0.1 g/cm3

[ Boiling Point ]:
632.3±65.0 °C at 760 mmHg

[ Molecular Formula ]:
C₂₀H₂₀ClN₅OS

[ Molecular Weight ]:
413.924

[ Flash Point ]:
336.2±34.3 °C

[ Exact Mass ]:
413.107697

[ LogP ]:
3.59

[ Vapour Pressure ]:
0.0±1.9 mmHg at 25°C

[ Index of Refraction ]:
1.666

Related Compounds

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