EPZ033294 is a SMYD2 inhibitor. EPZ033294 inhibits the enzymatic activity of SMYD2 with a potency of 3.9 nM and is noncompetitive with respect to peptide substrate and either noncompetitive or uncompetitive with respect to SAM. Compared to all other published SMYD2 inhibitors, EPZ033294 binds in a distinct and unique manner, traversing the peptide binding site and inducing a pocket into which the hydrophobic tail of the molecule is inserted. Western blot analysis of intracellular levels of BTF3me1 as a function of EPZ033294 concentration demonstrated a concentration-dependent inhibition of this mark with an IC50 of 2.9 nM.
MedKoo Cat#: 564326
Name: EPZ033294
CAS#: 1887195-17-6
Chemical Formula: C21H23ClN6O
Exact Mass: 410.1622
Molecular Weight: 410.91
Elemental Analysis: C, 61.38; H, 5.64; Cl, 8.63; N, 20.45; O, 3.89
The following data is based on the product molecular weight 410.91 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 |
