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UNC0379 trifluoroacetate salt

Names

[ CAS No. ]:
1620401-83-3

[ Name ]:
UNC0379 trifluoroacetate salt

[Synonym ]:
6,7-Dimethoxy-2-(1-pyrrolidinyl)-N-[5-(1-pyrrolidinyl)pentyl]-4-quinazolinamine trifluoroacetate (1:1)
Acetic acid, 2,2,2-trifluoro-, compd. with 6,7-dimethoxy-2-(1-pyrrolidinyl)-N-[5-(1-pyrrolidinyl)pentyl]-4-quinazolinamine (1:1)
UNC0379 (trifluoroacetate)

Biological Activity

[Description]:

UNC0379 trifluoroacetate 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

[ Molecular Formula ]:
C25H36F3N5O4

[ Molecular Weight ]:
527.580

[ Exact Mass ]:
527.271912

[ Storage condition ]:
2-8℃

Safety Information

[ RIDADR ]:
NONH for all modes of transport

Related Compounds