Identification | Back Directory | [Name]
UNC0379 | [CAS]
1620401-82-2 | [Synonyms]
UNC03 UNC0379 CS-1767 UNC0379, >=98% UNC0379 USP/EP/BP UNC 0379; UNC-0379 UNC0379, UNC-0379, UNC 0379 6,7-Dimethoxy-2-(1-pyrrolidinyl)-N-[5-(1-pyrrolidinyl)pentyl]-4-quinazolinamine 6,7-dimethoxy-2-(pyrrolidin-1-yl)-N-(5-(pyrrolidin-1-yl)pentyl)quinazolin-4-amine 4-Quinazolinamine, 6,7-dimethoxy-2-(1-pyrrolidinyl)-N-[5-(1-pyrrolidinyl)pentyl]- 6,7-dimethoxy-2-(pyrrolidin-1-yl)-N-(5-(pyrrolidin-1-yl)pentyl)quinazolin-4-amine UNC0379 | [Molecular Formula]
C23H35N5O2 | [MDL Number]
MFCD28167817 | [MOL File]
1620401-82-2.mol | [Molecular Weight]
413.57 |
Chemical Properties | Back Directory | [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) | [form ]
solid | [pka]
10.54±0.20(Predicted) | [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. |
Hazard Information | Back Directory | [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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