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Product Details

UNC0379 | Selective SETD8 inhibitor

UNC0379 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/Citations

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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Catalog#  10-4870-0005

$65.00
Quantity
Please note that we do not sell to individuals and that all orders placed by non-research organizations will incur a $20 restocking/refund fee.
 
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CAS:
1620401-82-2
Catalog Number:
10-4870
Activity:
Selective SETD8 inhibitor
Chemical Name:
6,7-Dimethoxy-2-(pyrrolidin-1-yl)-N-(5-(pyrrolidin-1-yl)-pentyl)quinazolin-4-amine
Molecular Weight:
413.56
Molecular Formula:
C23H35N5O2
Solubility:
Soluble in DMSO (up to 30 mg/ml)
Physical Properties:
Tan solid
Purity:
98% by TLC
NMR (Conforms)
Storage Temperature:
-20°C
Stability:
Stable for 1 year as supplied. Solutions in DMSO may be stored at -20°C for up to 1 month.
Shipping Code:
RT
Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications.

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