Product Size
5 mg
25 mg
Custom Size
Product Overview
Description
A potent, selective and competitive inhibitor of SMYD2 lysine methyltransferase.
Alternative Names
CHEMBL3818617; S,E)-N-(1-(N'-cyano-N-(3-(difluoromethoxy)phenyl)carbamimidoyl)-3-(3,4-dichlorophenyl)-4,5-dihydro-1H-pyrazol-4-yl)-N-ethyl-2-hydroxyacetamide
Target
SMYD2 lysine methyltransferase
Biological Description
A potent and selective competitive inhibitor of SMYD2 lysine methyltransferase (IC50 values are 27 and 58 nM for biochemical and cellular activity assays, respectively). It displays >100-fold selectivity for SMYD2 over a panel of 32 other methyltransferases including SMYD3, SUV420H1, and SUV420H2. Decreases p53K370me levels in HEK293 cells. Reduces methylation in tumor cells in a mouse xenograft model.
Solubility Overview
> 40 mg/mL in DMSO.
Chemical Properties
Chemical Name
N-[(4S)-2-[N-cyano-N'-[3-(difluoromethoxy)phenyl]carbamimidoyl]-5-(3,4-dichlorophenyl)-3,4-dihydropyrazol-4-yl]-N-ethyl-2-hydroxyacetamide
Molecular Weight (Da)
525.34
Molecular Formula
C22H20Cl2F2N6O3
SMILES
CCN([C@H]1CN(N=C1C2=CC(=C(C=C2)Cl)Cl)C(=NC3=CC(=CC=C3)OC(F)F)NC#N)C(=O)CO
Storage & Handling
Storage Instructions
Shipped at 4 °C. Store at -20 °C. Store in the dark.
