High affinity and selective WDR5 antagonist
OICR 9429 is a high affinity WDR5 antagonist (Kd = 93 nM; IC50 = 64 nM); disrupts WDR5-MLL interaction. Exhibits selectivity for WDR5 over 22 methyltransferases and a panel of kinases, GPCRs, ion channels, and transporters. Reduces viability of acute myeloid leukemia cells
in vitro
. Also disrupts MLL1-RbBP5 interaction.
To request the negative control for OICR 9429, please fill out the OICR 0547 request form on the SGC website.
| Marque | Tocris Bioscience |
|---|---|
| Réf. B-LABO | BL-RE-124663 |
| Réf. fabricant | 18756386 |
| Nom chimique ou matériau | OICR 9429 |
| Synonyme | N-[2-(4-Methylpiperazin-1-yl)-5-[3-(morpholin-4-ylmethyl)phenyl]phenyl]-6-oxo-4-(trifluoromethyl)-1,6-dihydropyridine-3-carboxamide |
| Quantité | 10 mg |
| Solubilité | Soluble to 50mM in DMSO |
| Cible | Additional Lysine Methyltransferase Compounds |
| Formule moléculaire | C<sub>2</sub><sub>9</sub>H<sub>3</sub><sub>2</sub>F<sub>3</sub>N<sub>5</sub>O<sub>3</sub> |
| Poids de la formule | 555.59 |
| Forme physique | Solid |
| Type de produit | Bioactive Small Molecule |
| Pureté | >98% |
