For research use only. Not for therapeutic Use.
UNC1999 (Cat No.:I001657) is a potent inhibitor of the lysine methyltransferases EZH2 (Enhancer of Zeste Homolog 2) and EZH1 (Enhancer of Zeste Homolog 1). It competitively binds to the SAM (S-adenosyl methionine) binding site of EZH2 and EZH1, inhibiting their enzymatic activity. UNC1999 exhibits high selectivity for EZH2 and EZH1 over other methyltransferases and non-epigenetic targets. It reduces the levels of the histone mark H3K27me3, which is associated with gene repression. In preclinical studies, UNC1999 has shown promise in prolonging the survival of mice with MLL-AF9 fusion-positive leukemia.
| Catalog Number | I001657 |
| CAS Number | 1431612-23-5 |
| Synonyms | N-[(6-methyl-2-oxo-4-propyl-1H-pyridin-3-yl)methyl]-1-propan-2-yl-6-[6-(4-propan-2-ylpiperazin-1-yl)pyridin-3-yl]indazole-4-carboxamide |
| Molecular Formula | C₃₃H₄₃N₇O₂ |
| Purity | ≥95% |
| Target | Histone Methyltransferase |
| Solubility | 10 mM in DMSO |
| Storage | Store at -20° C |
| IC50 | 2 nM(EZH2); 45 nM(EZH1) |
| IUPAC Name | N-[(6-methyl-2-oxo-4-propyl-1H-pyridin-3-yl)methyl]-1-propan-2-yl-6-[6-(4-propan-2-ylpiperazin-1-yl)pyridin-3-yl]indazole-4-carboxamide |
| InChI | InChI=1S/C33H43N7O2/c1-7-8-24-15-23(6)37-33(42)28(24)19-35-32(41)27-16-26(17-30-29(27)20-36-40(30)22(4)5)25-9-10-31(34-18-25)39-13-11-38(12-14-39)21(2)3/h9-10,15-18,20-22H,7-8,11-14,19H2,1-6H3,(H,35,41)(H,37,42) |
| InChIKey | DPJNKUOXBZSZAI-UHFFFAOYSA-N |
| SMILES | CCCC1=C(C(=O)NC(=C1)C)CNC(=O)C2=C3C=NN(C3=CC(=C2)C4=CN=C(C=C4)N5CCN(CC5)C(C)C)C(C)C |
| Reference | 1: Katona BW, Liu Y, Ma A, Jin J, Hua X. EZH2 inhibition enhances the efficacy of 2: Konze KD, Ma A, Li F, Barsyte-Lovejoy D, Parton T, Macnevin CJ, Liu F, Gao C, |
