Potent and selective pan-BD2 inhibitor; orally bioavailable
iBET-BD2 is a potent and selective pan-BD2 inhibitor (IC50 values are 49, 98, 214 and 264 nM for BRD4BD2, BRD3BD2, BRDTBD2 and BRD2BD2, respectively). iBET-BD2 is selective for BD2 over BD1 (IC50 values are 10965, 36317, 70558, and >50119 ?M for BRD2BD1, BRD3BD1, BRD4BD1, and BRDTBD1, respectively) in a time-resolved FRET (TR-FRET) assay. iBET-BD2 (1 μM) inhibits IFN-γ-induced protein expression of MHC class I in K562 cells. iBET-BD2 reduces the production of anti-KLH IgM antibodies in mice immunized with keyhole limpet hemocyanin (KLH). iBET-BD2 exhibits immunomodulatory activity. iBET-BD2 is orally bioavailable.
| Marque | Tocris Bioscience |
|---|---|
| Réf. B-LABO | BL-RE-151160 |
| Réf. fabricant | 18709756 |
| Nom chimique ou matériau | 4-(Acetylamino)-3-fluoro-N-(trans-4-hydroxycyclohexyl)-5-[(1 S)-1-phenylethoxy]benzamide |
| CAS | 2474876-09-8 |
| Quantité | 50 mg |
| Cible | Bromodomain Inhibitors |
| Formule moléculaire | C<sub>23</sub>H<sub>27</sub>FN<sub>2</sub>O<sub>4</sub> |
| Pureté | 0.98 |
