| Name | GSK J1 |
|---|---|
| Supplier | Tocris Bioscience |
| Catalog | 4116 |
| Prices | $199.00, $825.00 |
| Sizes | 10 mg, 50 mg |
| Function Type | Inhibitor |
| Cas Number | 1373422-53-7 |
| Chemical Name | N-[2-(2-Pyridinyl)-6-(1,2,4,5-tetrahydro-3H-3-benzazepin-3-yl)-4-pyrimidinyl]-β-alanine |
| Formula | C22H23N5O2 |
| Molecular Weight | 389.45 |
| Purity | >99 % |
| Description | Potent inhibitor of the H3K27 histone demethylases JMJD3 (KDM6B) and UTX (KDM6A) (IC 50 values are 28 and 53 nM respectively). Also inhibits KDM5B, KDM5C and KDM5A (IC 50 values are 170, 550 and 6,800 nM respectively). Exhibits no activity against a panel of other histone demethylases (IC 50 >20 μ M), and displays no significant inhibitory activity against 100 protein kinases at a concentration of 30 μ M. Ethyl ester derivative also available. |
| Supplier Page | Shop |
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. Nature. 2012 Aug 16;488(7411):404-8.
Heinemann B, Nielsen JM, Hudlebusch HR, Lees MJ, Larsen DV, Boesen T, Labelle M, Gerlach LO, Birk P, Helin K. Nature. 2014 Oct 2;514(7520):E1-2.