MM-102 - WDR5-MLL1 Antagonist. CAS# 1417329-24-8 418 Smiles: CCCOC1C=CC(CCC2=NC3=CC(=CC=C3N2CCN2CCOCC2)C2C(C)=NOC=2C)=CC=1

Smiles: CCCOC1C=CC(CCC2=NC3=CC(=CC=C3N2CCN2CCOCC2)C2C(C)=NOC=2C)=CC=1

It was identified by an imaging-based high throughput screening in human MSCs

InChi: InChI=1S/C21H19N5O2S/c1-3-28-18-12-8-7-11-16(18)23-24-19-14(2)25-26(20(19)27)21-22-17(13-29-21)15-9-5-4-6-10-15/h4-13

we monitored the auto-phosphorylation activity of Bcr-Abl and JAK2 in cells treated with GNF-2 and AKIs

Magnaghi P

MM-102 - WDR5-MLL1 Antagonist. CAS# 1417329-24-8 418 Smiles: CCCOC1C=CC(CCC2=NC3=CC(=CC=C3N2CCN2CCOCC2)C2C(C)=NOC=2C)=CC=1MM 102, CAS No. 1417329 24 8, is a highly potent and selective inhibitor of the MLL1 WDR5 interaction with an IC50 ~2. 9 nM binding affinity to WDR5. In the MLL1 AF9 transduced murine cells, MM 102 specifically reduces expression of two critical MLL1 target genes (HoxA9 and Meis 1), which are required for MLL1 mediated leukemogenesis. MM 102 also specifically inhibits cell growth and induces apoptosis in leukemia cells harboring MLL1 fusion proteins.