MS2177 is a potent and selective SETD8 inhibitor. MS2177 has an in vitro IC50 of 1.9 μM (σ = 1.05 μM, n = 4) in ascintillation proximity assay. Binding of MS2177 to SETD8 was confirmed by isothermal titration calorimetry (ITC), having a KD of 1.3 μM. SETD8 (also known as SET8, PR-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#: 406846
Name: MS2177
CAS#: Unknown
Chemical Formula: C24H38N6O2
Exact Mass: 442.3056
Molecular Weight: 442.61
Elemental Analysis: C, 65.13; H, 8.65; N, 18.99; O, 7.23
The following data is based on the product molecular weight 442.61 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 |
