product name UNC0379
Description: UNC0379 is a highly selective, substrate competitive inhibitor of N-lysine methyltransferase SETD8 with IC50 of 7.9 μM. UNC0379 is active in multiple biochemical assays. Its affinity to SETD8 was confirmed by ITC (isothermal titration calorimetry) and SPR (surface plasmon resonance) studies. Importantly, UNC0379 is selective for SETD8 over 15 other methyltransferases.
References: J Med Chem. 2014 Aug 14;57(15):6822-33.
413.56
Formula
C23H35N5O2
CAS No.
1620401-82-2
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: Soluble in DMSO
Water:
Ethanol:
Solubility (In vivo)
Synonyms
other peoduct :
| In Vitro |
In vitro activity: UNC0379 is competitive with the peptide substrate and noncompetitive with the cofactor SAM Kinase Assay: Enzyme assay The interaction between UNC0379 and protein SETD8 was further explored using a ProteOn XPR36 biosensor (Bio-Rad Laboratories, Inc.) at 25 °C. PBS buffer (phosphate buffered saline, pH 7.4) supplemented with 0.005% Tween-20 was used as the running buffer. A GLH (catalog no. 176-5013, Bio-Rad Laboratories, Inc.) sensor chip was first activated by flowing a mixture of 20 mM sulfo-NHS and 20 mM EDC over the chip surface for 5 min at a flow rate of 30 μL/min. SETD8 was then diluted to 20 and 10 μg/mL in 5 mM NaOAc, pH 5.0, and immobilized onto two ligand channels (30 μL/min for 2 min). The surface was then deactivated by flowing 1 M ethanolamine for 5 min at a flow rate 60 μL/min. A blank injection of the running buffer was made, after which four concentrations of the compound in the running buffer (100, 33.3, 11.1, and 3.7 μM) and a running buffer were injected simultaneously at a flow rate of 50 μL/min for 60 s. The sensorgrams obtained at the four concentrations of the compound were fit simultaneously after subtracting a ligand reference (inner spot) and a double compound reference (buffer) using a Langmuir model to obtain on (ka) and off (kd) rates. The kinetic KD was calculated based on the on and off rates for three replicates. An equilibrium analysis of the data was also performed to calculate the KD. Cell Assay: |
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| Formulation & Dosage | |
| References | J Med Chem. 2014 Aug 14;57(15):6822-33. |
