MM-102 Inhibitor – TFA

Solid. Powder

99.40%

Store at -20 degree C for 3 years powder
-80 degree C for 2 years in solvent

783.83

DMSO: 99mg/mL (126.3mM)
(<1mg/ml refers to the product slightly soluble or insoluble)

C37H50F5N7O6

OC(=O)C(F)(F)F.CCC(CC)(NC(=O)C(C)C)C(=O)N[C@@H](CCCNC(N)=N)C(=O)NC1(CCCC1)C(=O)NC(c1ccc(F)cc1)c1ccc(F)cc1

1883545-52-5

In Vitro Histone Methyltransferase (HMT) Assay: The HMT assay is performed in 50mM HEPES pH 7.8, 100mM NaCl, 1.0mM EDTA, and 5% glycerol at 22 degree C. Each reaction contains 1.5uCi of the co-factor, 3H-S-adenosylmethionine. H3 10-residue peptide is used as the substrate at 50uM. Compounds are added at concentrations ranging from 0.125 to 128 uM and incubated with the pre-assembled WDR5/RbBP5/ASH2L complex at a final concentration of 0.5uM for each protein for 2-5 minutes. Reactions are initiated by addition of the MLL1 protein at a final concentration of 0.5uM and allowed to proceed for 30 min before preparing scintillation counting. To count samples, reactions are spotted on separate squares of P81 filter paper and precipitated by submerging in freshly prepared 50mM sodium bicarbonate buffer with pH 9.0. After washing and drying, samples are vortexed in Ultima Gold scintillation fluid and counted. As a negative control, assays are performed using 0.5uM MLL1/WDR5/RbBP5/ASH2L complex assembled with the non-interacting mutant, WDR5D107A.