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UNC0631

Names

[ CAS No. ]:
1320288-19-4

[ Name ]:
UNC0631

[Synonym ]:
N-(1-(benzo[d][1,3]dioxol-5-yl)propyl)-4-methylbenzenesulfonamide
N-(1-(cyclohexylmethyl)piperidin-4-yl)-2-(4-isopropyl-1,4-diazepan-1-yl)-6-methoxy-7-(3-(piperidin-1-yl)propoxy)quinazolin-4-amine
Benzenesulfonamide,N-[1-(1,3-benzodioxol-5-yl)propyl]-4-methyl
UNC0631
UNC 0631

Biological Activity

[Description]:

UNC 0631 is a potent G9a inhibitor with IC50 value of 4 nM.IC50 value: 4 nM [1]Target: G9aUNC 0631, which had high in vitro potency versus G9a and improved lipophilicity, was highly potent (IC50 < 0.06 μM) in reducing H3K9me2 levels in MDA-MB-231 cells and had low cell toxicity. In particular, compounds 7 was more potent than compound 5 and had a similar tox/function ratio in MDAMB-231 cells. UNC 0631 showed excellent separation of functional potency versus cell toxicity in MDA-MB-231 cells, thecompound was further evaluated in a variety of cell lines to characterize it's cellular potency and cell toxicity. UNC 0631 had excellent tox/functionratios in these cell lines.

[Related Catalog]:

Signaling Pathways >> Epigenetics >> Histone Methyltransferase
Research Areas >> Cancer

[References]

[1]. Liu F, et al. Optimization of cellular activity of G9a inhibitors 7-aminoalkoxy-quinazolines. J Med Chem. 2011 Sep 8;54(17):6139-50.


[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]:
1.1±0.1 g/cm3

[ Boiling Point ]:
763.4±70.0 °C at 760 mmHg

[ Molecular Formula ]:
C37H61N7O2

[ Molecular Weight ]:
635.926

[ Flash Point ]:
415.5±35.7 °C

[ Exact Mass ]:
635.488647

[ PSA ]:
72.46000

[ LogP ]:
6.29

[ Vapour Pressure ]:
0.0±2.6 mmHg at 25°C

[ Index of Refraction ]:
1.579

[ Storage condition ]:
2-8℃

Related Compounds