For research use only. Not for therapeutic Use.
GSK4028 is the enantiomeric negative control of GSK4027, which is a PCAF/GCN5 bromodomain chemical probe, the pIC50 of GSK4028 is 4.9 in a time-resolved fluorescence resonance energy transfer (TR-FRET) assay.
GSK4028 is the enantiomeric negative control of GSK4027, which is a PCAF/GCN5 bromodomain chemical probe, the pIC50 of GSK4028 is 4.9. GSK4028 also demonstrates potency toward BRD4 BD1 and BRD9 inTR-FRET assay with pIC50s of <4.3 and 4.5±0.13, respectively[1].
| Catalog Number | I019776 |
| CAS Number | 2079886-19-2 |
| Synonyms | 4-bromo-2-methyl-5-[[(3S,5S)-1-methyl-5-phenylpiperidin-3-yl]amino]pyridazin-3-one |
| Molecular Formula | C17H21BrN4O |
| Purity | ≥95% |
| InChI | InChI=1S/C17H21BrN4O/c1-21-10-13(12-6-4-3-5-7-12)8-14(11-21)20-15-9-19-22(2)17(23)16(15)18/h3-7,9,13-14,20H,8,10-11H2,1-2H3/t13-,14+/m1/s1 |
| InChIKey | VZAFGXCWAWRULT-KGLIPLIRSA-N |
| SMILES | CN1CC(CC(C1)NC2=C(C(=O)N(N=C2)C)Br)C3=CC=CC=C3 |
| Reference | [1]. Humphreys PG, et al. Discovery of a Potent, Cell Penetrant, and Selective p300/CBP-Associated Factor (PCAF)/General Control Nonderepressible 5 (GCN5) Bromodomain Chemical Probe. J Med Chem. 2017 Jan 26;60(2):695-709. |
