For research use only. Not for therapeutic Use.
The histone H3 lysine 27 (H3K27) demethylase JMJD3 plays important roles in the transcriptional regulation of cell differentiation, development, the inflammatory response, and cancer. GSK-<wbr></wbr>J4 (Item No. <span class=/itemid/>12073</span>) is a cell-<wbr></wbr>permeable prodrug which is modified by intracellular esterases to give GSK-<wbr></wbr>J1 (Item No. <span class=/itemid/>12054</span>), an inhibitor of JMJD3. GSK-<wbr></wbr>J5 is a pyridine regio-<wbr></wbr>isomer of GSK-<wbr></wbr>J4. Like GSK-<wbr></wbr>J4, this isomer is cell-<wbr></wbr>permeable and hydrolyzed to a free base. However, the free base is a weak inhibitor of JMJD3 (IC<sub>50</sub> > 100 μM), making it an ideal inactive control molecule for elucidating the functional role of JMJD3 inhibition.
| Catalog Number | R062466 |
| CAS Number | 1797983-32-4 |
| Synonyms | N-[2-(3-pyridinyl)-6-(1,2,4,5-tetrahydro-3H-3-benzazepin-3-yl)-4-pyrimidinyl]-β-alanine, ethyl ester, monohydrochoride |
| Molecular Formula | C24H27N5O2 • HCl |
| Purity | ≥95% |
| Storage | -20°C |
| InChI | InChI=1S/C24H27N5O2.ClH/c1-2-31-23(30)9-13-26-21-16-22(28-24(27-21)20-8-5-12-25-17-20)29-14-10-18-6-3-4-7-19(18)11-15-29;/h3-8,12,16-17H,2,9-11,13-15H2,1H3,(H,26,27,28);1H |
| InChIKey | QQHQMHJAOKADED-UHFFFAOYSA-N |
| SMILES | O=C(OCC)CCNC1=CC(N2CCC(C=CC=C3)=C3CC2)=NC(C4=CC=CN=C4)=N1.Cl |
| Reference | 1.Agger, K.,Cloos, P.A.C.,Christensen, J., et al. UTX and JMJD3 are histone H3K27 demethylases involved in HOX gene regulation and development. Nat.Lett. 449(7163), 731-734 (2011). |
