GSK-J1
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货号：A773094
GSK-J1 is a H3K27 histone demethylase inhibitor with IC50 of 28 nM and 53 nM for JMJD3 (KDM6B) and UTX (KDM6A), respectively.
GSK-J1 化学结构
GSK-J1 3D分子结构
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GSK-J1 纯度/质量文件 产品仅供科研
货号：A773094
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GSK-J1 质控信息
GSK-J1 生物活性
靶点
描述
The Jumonji (JMJ) family of histone demethylases are Fe2+ - and α-ketoglutarate-dependent oxygenases implicated in chromatin modifications. GSK-J1 is a selective inhibitor of Jumonji H3K27 demethylase. The IC50 value of GSK-J1 for JMJD3 is 60nM.[3] [4] [5]
作用机制
GSK-J1 is a Jumonji H3K27 demethylase inhibitor. It is competitive with α-ketoglutarate but non-competitive with the peptide substrate. The propanoic acid of GSK-J1 mimics α-ketoglutarate binding by interacting with K1381, T1387, and N1480.[3]
GSK-J1 参考文献
[1] Yang D, Okamura H, et al. Histone demethylase Utx regulates differentiation and mineralization in osteoblasts. J Cell Biochem. 2015 Nov;116(11):2628-36.
[2] Kruidenier L, Chung CW, et al. A selective jumonji H3K27 demethylase inhibitor modulates the proinflammatory macrophage response. Nature. 2012 Aug 16;488(7411):404-8.
[3] Kruidenier L, Chung CW, Cheng Z, Liddle J, Che K, Joberty G, Bantscheff M, Bountra C, Bridges A, Diallo H, Eberhard D, Hutchinson S, Jones E, Katso R, Leveridge M, Mander PK, Mosley J, Ramirez-Molina C, Rowland P, Schofield CJ, Sheppard RJ, Smith JE, Swales C, Tanner R, Thomas P, Tumber A, Drewes G, Oppermann U, Patel DJ, Lee K, Wilson DM. A selective jumonji H3K27 demethylase inhibitor modulates the proinflammatory macrophage response. Nature. 2012 Aug 16;488(7411):404-8
[4] Horton JR, Engstrom A, Zoeller EL, Liu X, Shanks JR, Zhang X, Johns MA, Vertino PM, Fu H, Cheng X. Characterization of a Linked Jumonji Domain of the KDM5/JARID1 Family of Histone H3 Lysine 4 Demethylases. J Biol Chem. 2016 Feb 5;291(6):2631-46
[5] Raeisossadati R, Móvio MI, Walter LT, Takada SH, Del Debbio CB, Kihara AH. Small Molecule GSK-J1 Affects Differentiation of Specific Neuronal Subtypes in Developing Rat Retina. Mol Neurobiol. 2019 Mar;56(3):1972-1983
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GSK-J1 实验方案
计算器
摩尔计算器
总药量计算器
工作液计算器
存储液制备
1mg
5mg
10mg
1 mM
5 mM
10 mM
2.57mL
0.51mL
0.26mL
12.84mL
2.57mL
1.28mL
25.68mL
5.14mL
2.57mL
GSK-J1 技术信息
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