For research use only. Not for therapeutic Use.
EM127 (compound 11c) is a SMYD3 covalent inhibitor with high selectivity, high affinity (KD=13 μM) and site-specificity. EM127 effectively inhibits ERK1/2 phosphorylation and reduces transcriptional regulation of SMYD3 target genes. EM127 effectively and prolongedly impairs methyltransferase activity. EM127 can be used in cancer research, particularly in SMYD3 positive tumours[1].
EM127 (5 μM; 24, 48, 72 h) shows good anti-proliferative activity in MDA-MB-231and HCT116 cells[1].
EM127 (5 μM; 24, 48, 72 h) attenuates the expression of SMYD3 target genes while does not affect expression when SMYD3 is knocked out or expressed at low levels in MDA-MB-231 cells[1].
EM127 (1, 3.5, 5 μM; 48, 72 h) decreases ERK1/2 phosphorylation in a dose- and time-dependent manner in HCT116 and MDA-MB-231cells[1].
| Catalog Number | I042857 |
| CAS Number | 1886879-71-5 |
| Synonyms | N-[1-(2-chloroacetyl)piperidin-4-yl]-5-cyclopropyl-1,2-oxazole-3-carboxamide |
| Molecular Formula | C14H18ClN3O3 |
| Purity | ≥95% |
| InChI | InChI=1S/C14H18ClN3O3/c15-8-13(19)18-5-3-10(4-6-18)16-14(20)11-7-12(21-17-11)9-1-2-9/h7,9-10H,1-6,8H2,(H,16,20) |
| InChIKey | OENTXAYVUCLRJQ-UHFFFAOYSA-N |
| SMILES | C1CC1C2=CC(=NO2)C(=O)NC3CCN(CC3)C(=O)CCl |
| Reference | [1]. Parenti M D, et al. Discovery of the 4-aminopiperidine-based compound EM127 for the site-specific covalent inhibition of SMYD3. European Journal of Medicinal Chemistry, 2022: 114683. |
