OICR 9429

• Supplier: Tocris Bioscience
• Catalog: 2710
• Prices: $195.00, $805.00
• Sizes: 10 mg, 50 mg
• Function Type: Antagonist
• Cas Number: 1801787-56-3
• Chemical Name: N-[2-(4-Methylpiperazin-1-yl)-5-[3-(morpholin-4-ylmethyl)phenyl]phenyl]-6-oxo-4-(trifluoromethyl)-1,6-dihydropyridine-3-carboxamide
• Formula: C29H32F3N5O3
• Molecular Weight: 555.59
• Purity: >98 %
• Description: High affinity WDR5 antagonist (K d = 93 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.

Product References

Pharmacological targeting of the Wdr5-MLL interaction in C/EBPalpha N-terminal - Pharmacological targeting of the Wdr5-MLL interaction in C/EBPalpha N-terminal

Grebien F, Vedadi M, Getlik M, Giambruno R, Grover A, Avellino R, Skucha A, Vittori S, Kuznetsova E, Smil D, Barsyte-Lovejoy D, Li F, Poda G, Schapira M, Wu H, Dong A, Senisterra G, Stukalov A, Huber KV, Schonegger A, Marcellus R, Bilban M, Bock C, Brown PJ, Zuber J, Bennett KL, Al-Awar R, Delwel R, Nerlov C, Arrowsmith CH, Superti-Furga G. Nat Chem Biol. 2015 Aug;11(8):571-8.