MAK-683

MAK-683 is an inhibitor of trimethylation of histone 3 lysine 27 (H3K27) by polycomb repressive complex 2 (PRC2), a complex that includes embryonic ectoderm development protein (EED). MAK-683 has an IC50 value of 5.9 nM in an EED-H3K27me3 peptide competition binding assay and inhibits H3K27 trimethylation in G401 cells (IC50 = 2.6 nM). It inhibits proliferation of KARPAS422 B cell lymphoma cells with an IC50 value of 3 nM.Formal Name: N-[(5-fluoro-2,3-dihydro-4-benzofuranyl)methyl]-8-(2-methyl-3-pyridinyl)-1,2,4-triazolo[4,3-c]pyrimidin-5-amine. CAS Number: 1951408-58-4. Molecular Formula: C20H17FN6O. Formula Weight: 376.4. Purity: >98%. Formulation: (Request formulation change), A solid. Solubility: DMSO: 15 mg/ml. lambdamax: 298 nm. SMILES: FC1=CC=C(OCC2)C2=C1CNC3=NC=C(C4=C(C)N=CC=C4)C5=NN=CN35. InChi Code: InChI=1S/C20H17FN6O/c1-12-13(3-2-7-22-12)16-10-24-20(27-11-25-26-19(16)27)23-9-15-14-6-8-28-18(14)5-4-17(15)21/h2-5,7,10-11H,6,8-9H2,1H3,(H,23,24). InChi Key: XLIBABIFOBYHSV-UHFFFAOYSA-N.