UNC0379

Names

[ CAS No. ]:
1620401-82-2

[ Name ]:
UNC0379

[Synonym ]:
4-Quinazolinamine, 6,7-dimethoxy-2-(1-pyrrolidinyl)-N-[5-(1-pyrrolidinyl)pentyl]-
6,7-Dimethoxy-2-(1-pyrrolidinyl)-N-[5-(1-pyrrolidinyl)pentyl]-4-quinazolinamine
UNC0379

Biological Activity

[Description]:

UNC0379 is a selective, substrate-competitive inhibitor of the lysine methyltransferase SETD8 with IC50 of 7.3±1.0 uM; selective over 15 other methyltransferases.IC50 value: 7.3±1.0 uMTarget: SETD8 inhibitorUNC0379 is a synthetic small-molecule inhibitor that displays inhibitory activity in multiple biochemical assays and is selective for SETD8 over 15 other methyltransferases. The binding affinity of UNC0379 to SETD8 was determined using biophysical assays such as ITC (isothermal titration calorimetry) and SPR (surface plasmon resonance) and is largely consistent with its potency in biochemical assays.

[Related Catalog]:

Signaling Pathways >> Epigenetics >> Histone Methyltransferase

Research Areas >> Cancer

[References]

[1]. Ma A, et al. Discovery of a Selective, Substrate-Competitive Inhibitor of the Lysine Methyltransferase SETD8. J Med Chem. 2014 Aug 14;57(15):6822-33.

[Related Small Molecules]

GSK126 | Tazemetostat (EPZ-6438) | UNC 0642 | GSK343 | Pinometostat (EPZ5676) | 3-Deazaneplanocin A (hydrochloride) | Pemrametostat (GSK3326595) | UNC1999 | BIX-01294 | EPZ031686 | AZ505 (ditrifluoroacetate) | MS023 | EPZ 004777 | EPZ015666 | EPZ015866(GSK591)

Chemical & Physical Properties

[ Density]:
1.2±0.1 g/cm3

[ Boiling Point ]:
606.3±65.0 °C at 760 mmHg

[ Molecular Formula ]:
C₂₃H₃₅N₅O₂

[ Molecular Weight ]:
413.556

[ Flash Point ]:
320.5±34.3 °C

[ Exact Mass ]:
413.279083

[ LogP ]:
2.76

[ Vapour Pressure ]:
0.0±1.7 mmHg at 25°C

[ Index of Refraction ]:
1.606

[ Storage condition ]:
2-8℃

Related Compounds

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