For research use only. Not for therapeutic Use.
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].
EZH2-IN-14 (C24) effectively reduces the H3K27me3 and H3K27me2 marks. EZH2-IN-14 has little effect on the level of EZH2 protein in MDA-MB-468 cells[1].
| Catalog Number | I042467 |
| CAS Number | 1979157-17-9 |
| Synonyms | N-[(4,6-dimethyl-2-oxo-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 | C31H39N7O2 |
| Purity | ≥95% |
| InChI | InChI=1S/C31H39N7O2/c1-19(2)36-9-11-37(12-10-36)29-8-7-23(16-32-29)24-14-25(27-18-34-38(20(3)4)28(27)15-24)30(39)33-17-26-21(5)13-22(6)35-31(26)40/h7-8,13-16,18-20H,9-12,17H2,1-6H3,(H,33,39)(H,35,40) |
| InChIKey | XHJAGCFBPKQPDU-UHFFFAOYSA-N |
| SMILES | CC1=CC(=C(C(=O)N1)CNC(=O)C2=C3C=NN(C3=CC(=C2)C4=CN=C(C=C4)N5CCN(CC5)C(C)C)C(C)C)C |
| Reference | [1]. Anqi Ma, et al. Discovery of a first-in-class EZH2 selective degrader. Nat Chem Biol. 2020 Feb;16(2):214-222. |
