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GSK J1
- Soluble in 0.1N HCl(aq) and DMSO
- MF: C22H23N5O2
- MW: 389.45
Description
GSK J1 is a selective and potent KDM6 histone demethylase inhibitor targeting JMJD3/KDM6B and UTX/KDM6A, thereby blocking H3K27 demethylation.
JMJD3 and UTX remove repressive H3K27 methyl marks and regulate inflammatory, developmental and differentiation-associated gene programs. GSK J1 is a key epigenetic probe for studying KDM6-dependent chromatin regulation; the cell-permeable ethyl ester derivative is GSK J4 (Axon 1933).
Key Features
- Selective JMJD3/UTX histone demethylase inhibitor
- Blocks demethylation of H3K27 methyl marks
- Shows strong selectivity over other JmjC demethylases and kinase panels in reported profiling
- Parent acid of the cell-permeable prodrug GSK J4
Applications
- KDM6/JMJD3/UTX enzyme assays
- H3K27 methylation and chromatin regulation studies
- Inflammatory gene-expression research
- Epigenetic probe and prodrug comparison studies
More Information
| Parent CAS No. | 1373422-53-7 |
|---|---|
| Chemical Name | 3-(6-(4,5-dihydro-1H-benzo[d]azepin-3(2H)-yl)-2-(pyridin-2-yl)pyrimidin-4-ylamino)propanoic acid |
| SMILES | C(O)(=O)CCNC1C=C(N2CCC3=CC=CC=C3CC2)N=C(C2=NC=CC=C2)N=1 |
| MFCD | N.A. |
| InChi | InChI=1S/C22H23N5O2/c28-21(29)8-12-24-19-15-20(26-22(25-19)18-7-3-4-11-23-18)27-13-9-16-5-1-2-6-17(16)10-14-27/h1-7,11,15H,8-10,12-14H2,(H,28,29)(H,24,25,26) |
| InChiKey | AVZCPICCWKMZDT-UHFFFAOYSA-N |
| CID | 56963315 |
| Short Description | JMJD3/UTX inhibitor |
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