GSK J1
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.
| Storage | Store at -20°C |
| M.Wt | 389.45 |
| Cas No. | 1373422-53-7 |
| Formula | C22H23N5O2 |
| Solubility | ≥38.9 mg/mL in DMSO; insoluble in H2O; ≥51.2 mg/mL in EtOH with ultrasonic |
| Chemical Name | 3-[[2-pyridin-2-yl-6-(1,2,4,5-tetrahydro-3-benzazepin-3-yl)pyrimidin-4-yl]amino]propanoic acid |
| SDF | Download SDF |
| Canonical SMILES | C1CN(CCC2=CC=CC=C21)C3=CC(=NC(=N3)C4=CC=CC=N4)NCCC(=O)O |
| Shipping Condition | Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice. |
| General tips | We do not recommend long-term storage for the solution, please use it up soon. |
Quality Control & MSDS
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Chemical structure
