| Bioactivity | MS453 is a potent and highly selective SETD8 inhibitor with an IC50 value of 804 nM. MS453 specifically modifies a cysteine residue close to the inhibitor binding site. MS453 is selective for 28 other methyltransferases. The crystal structure of MS453 reveals its binding mode to SETD8, providing an atomic-level view for the development of high-quality chemical probes for SETD8[1]. |
| CAS | 2059892-29-2 |
| Formula | C20H27N5O3 |
| Molar Mass | 385.46 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [1]. Structure-Based Design of a Covalent Inhibitor of the SET Domain-Containing Protein 8 (SETD8) Lysine Methyltransferase |