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GSK-J1

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Chemical Structure| 1373422-53-7 同义名 : -
CAS号 : 1373422-53-7
货号 : A773094
分子式 : C22H23N5O2
纯度 : 99%+
分子量 : 389.45
MDL号 : MFCD22683851
存储条件：

粉末 Keep in dark place,Inert atmosphere,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 50 mg/mL(128.39 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
靶点

  • KDM6

    JMJD3, IC50:60 nM
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] GSK-J1 inhibited the demethylase activity of KDM5C and KDM5B with IC50 values of ~11 and ~94μM, respectively.[4] Subretinal injection of P0 rats with GSK-J1 (1mM) enhanced the accumulation of cell cycle marker Ki67 and cell proliferation, and affected apoptosis and neuronal maturation in developing retina.[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]
实验方案
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
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