GSK-J1 - ≥99%, high purity , CAS No.1373422-53-7, Inhibitor of lysine demethylase 5A;Inhibitor of lysine demethylase 5B;Inhibitor of lysine demethylase 5C;Inhibitor of lysine demethylase 6A;Inhibitor of lysine demethylase 6B
GSK-J1 - ≥99%, high purity , CAS No.1373422-53-7, Inhibitor of lysine demethylase 5A;Inhibitor of lysine demethylase 5B;Inhibitor of lysine demethylase 5C;Inhibitor of lysine demethylase 6A;Inhibitor of lysine demethylase 6B
GSK-J1 is also termed as 3-((6-(4,5-Dihydro-1H-benzo[d]azepin-3(2H)-yl)-2-(pyridin-2-yl)pyrimidin-4-yl)amino)propanoate. It may disturb the differentiation of specific neuronal subtypes in growing rat retina.
GSK-J1 is a potent selective jumonji H3K27 dem
Storage Temp
Store at -20°C,Desiccated
Shipped In
Ice chest + Ice pads
Grade
Moligand™
Action Type
INHIBITOR
Mechanism of action
Inhibitor of lysine demethylase 5A;Inhibitor of lysine demethylase 5B;Inhibitor of lysine demethylase 5C;Inhibitor of lysine demethylase 6A;Inhibitor of lysine demethylase 6B
Note
Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20°C. Generally, these will be useable for up to one month. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour. Need more advice on solubility, usage and handling? Please visit our frequently asked questions (FAQ) page for more details.
Product Description
Product introduction
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 .
Application
GSK-J1 has been used in formaldehyde dehydrogenase (FDH)-coupled demethylase assay.
1.Sakurai M, Rose NR, Schultz L, Quinn AM, Jadhav A, Ng SS, Oppermann U, Schofield CJ, Simeonov A. (2010) A miniaturized screen for inhibitors of Jumonji histone demethylases.. Mol Biosyst, 6 (2):(357-64). [PMID:20094655]
2.Mackeen MM, Kramer HB, Chang KH, Coleman ML, Hopkinson RJ, Schofield CJ, Kessler BM. (2010) Small-molecule-based inhibition of histone demethylation in cells assessed by quantitative mass spectrometry.. J Proteome Res, 9 (8):(4082-92). [PMID:20583823]
3.Kruidenier L, Chung CW, Cheng Z, Liddle J, Che K, Joberty G, Bantscheff M, Bountra C, Bridges A, Diallo H et al.. (2012) A selective jumonji H3K27 demethylase inhibitor modulates the proinflammatory macrophage response.. Nature, 488 (7411):(404-8). [PMID:22842901]
4.Heinemann B, Nielsen JM, Hudlebusch HR, Lees MJ, Larsen DV, Boesen T, Labelle M, Gerlach LO, Birk P, Helin K. (2014) Inhibition of demethylases by GSK-J1/J4.. Nature, 514 (7520):(E1-2). [PMID:25279926]
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H2206417