For research use only. Not for therapeutic Use.
DN02 is a potent, selective BRD8 bromodomain probe. DN02 has exhibits high affinity for the BRD8(1) (Ki=32 nM), which is 30-fold more affinity than BRD8 (2) (Ki＞1000 nM)[1].
DN02 has (1 nM-100 μM) low nM AlphaScreen with IC50 value of 48 nM, with high selectivity over BRD9 and BRD4 in biochemical AlphaScreen assays[1].
DN02 (32 nM) has minimal off-target engagement across the bromodomain family, with modest activity against CBP/P300[1].
| Catalog Number | I042836 |
| Synonyms | 4-[4-[(3-aminoazetidin-1-yl)methyl]-2,6-dimethoxyphenyl]-7-fluoro-2-methylisoquinolin-1-one |
| Molecular Formula | C22H24FN3O3 |
| Purity | ≥95% |
| InChI | InChI=1S/C22H24FN3O3/c1-25-12-18(16-5-4-14(23)8-17(16)22(25)27)21-19(28-2)6-13(7-20(21)29-3)9-26-10-15(24)11-26/h4-8,12,15H,9-11,24H2,1-3H3 |
| InChIKey | CFUSHHQUUUZFAG-UHFFFAOYSA-N |
| SMILES | CN1C=C(C2=C(C1=O)C=C(C=C2)F)C3=C(C=C(C=C3OC)CN4CC(C4)N)OC |
| Reference | [1]. Remillard D, et, al. Chemoproteomics Enabled Discovery of Selective Probes for NuA4 Factor BRD8. ACS Chem Biol. 2021 Nov 19;16(11):2185-2192. |
