MS453 is a potent and selective SETD8 inhibitor. MS453 specifically modifies a cysteine residue near the inhibitor binding site, has an IC50 value of 804 nM, reacts with SETD8 with nearquantitative yield, and is selective for SETD8 against 28 other methyltransferases. SETD8 (also known as SET8, R-SET7, or KMT5A) is the only methyltransferase known to catalyze monomethylation of histone H4 lysine 20 (H4K20). SETD8 inhibitors could be valuable anticancer agents.
MedKoo Cat#: 406847
Name: MS453
CAS#: 2059892-29-2
Chemical Formula: C20H27N5O3
Exact Mass: 385.2114
Molecular Weight: 385.47
Elemental Analysis: C, 62.32; H, 7.06; N, 18.17; O, 12.45
The following data is based on the product molecular weight 385.47 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
