| Identification | Back Directory | [Name]
1H-Indazole-4-carboxamide, N-[(1,2-dihydro-4,6-dimethyl-2-oxo-3-pyridinyl)methyl]-1-(1-methylethyl)-6-[6-[4-(1-methylethyl)-1-piperazinyl]-3-pyridinyl]- | [CAS]
1979157-17-9 | [Synonyms]
EZH2-IN-14
1H-Indazole-4-carboxamide, N-[(1,2-dihydro-4,6-dimethyl-2-oxo-3-pyridinyl)methyl]-1-(1-methylethyl)-6-[6-[4-(1-methylethyl)-1-piperazinyl]-3-pyridinyl]- | [Molecular Formula]
C31H39N7O2 | [MOL File]
1979157-17-9.mol | [Molecular Weight]
541.69 |
| Chemical Properties | Back Directory | [Boiling point ]
793.0±60.0 °C(Predicted) | [density ]
1.26±0.1 g/cm3(Predicted) | [form ]
Solid | [pka]
11.84±0.10(Predicted) | [color ]
Off-white to light yellow |
| Hazard Information | Back Directory | [Uses]
EZH2-IN-14 is a selective EZH2 (Histone Methyltransferase) inhibitor with an IC50 of 12 nM. EZH2-IN-14 inhibits the methyltransferase activity of EZH2/PRC2 (that is, reducing H3K27me3). EZH2-IN-14 shows >200-fold selective for EZH2 over the highly homologous H3K27 methyltransferase EZH1[1]. | [References]
[1] Anqi Ma, et al. Discovery of a first-in-class EZH2 selective degrader. Nat Chem Biol. 2020 Feb;16(2):214-222. DOI:10.1038/s41589-019-0421-4 |
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