UNC0379 Chemical Properties

Boiling point:

606.3±65.0 °C(Predicted)

Density 

1.168±0.06 g/cm3(Predicted)

storage temp. 

under inert gas (nitrogen or Argon) at 2–8 °C

solubility 

Soluble in DMSO (up to 30 mg/ml)

pka

10.54±0.20(Predicted)

form 

solid

color 

Tan

Stability:

Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 1 month.

UNC0379 Usage And Synthesis

Description

UNC0379 (CAS 1620401-82-2) is an inhibitor of the lysine methyltransferase SETD8 with selectivity over 15 other methyltransferases.1 IC50’s = 7.3 μM in a radioactive methyl transfer assay and 9.0 μM in an MCE assay. UNC0379 treatment of SY5Y and NGP neuroblastoma cell lines lead to activation of p53 and decreased tumor growth in an ex-vivo tumorigenicity assay.2

References

1) Ma et al. (2014), Discovery of a Selective, Substrate-Competitive Inhibitor of the Lysine Methyltransferase SETD8; J. Med. Chem. 57 6822 2) Veschi et al. (2017), Epigenetic siRNA and Chemical Screens Identify SETD8 Inhibition as a Therapeutic Strategy for p53 Activation in High-Risk Neuroblastoma; Cancer Cell 31 50

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