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GSK J1

Catalog No.
A4191
H3K27 demethylase JMJD3 inhibitor
Grouped product items
SizePriceStock Qty
10mg
$85.00
In stock
50mg
$245.00
In stock
200mg
$665.00
In stock

Tel: +1-832-696-8203

Email: [email protected]

Worldwide Distributors

Background

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 [1].

However, GSK J1 has restricted cellular permeability due to its highly polar carboxylate group, which plays a critical role in the binding of GSK J1 to JMJD3. In order to improve the cellular permeability, GSK J1 is esterified to mask the polarity generating an ethyl ester derivative that can be rapidly hydrolyzed to GSK J1 [1].

Reference

References:
[1] 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. doi: 10.1038/nature11262.

Chemical Properties

StorageStore at -20°C
M.Wt389.45
Cas No.1373422-53-7
FormulaC22H23N5O2
Solubility≥38.9 mg/mL in DMSO, ≥51.2 mg/mL in EtOH with ultrasonic,insoluble in H2O
Chemical Name3-[[2-pyridin-2-yl-6-(1,2,4,5-tetrahydro-3-benzazepin-3-yl)pyrimidin-4-yl]amino]propanoic acid
SDFDownload SDF
Canonical SMILESC1CN(CCC2=CC=CC=C21)C3=CC(=NC(=N3)C4=CC=CC=N4)NCCC(=O)O
Shipping ConditionEvaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

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