1320288-19-4

1320288-19-4 structure

Name: UNC0631
Chemical Name: N-[1-(Cyclohexylmethyl)-4-piperidinyl]-2-(4-isopropyl-1,4-diazepa n-1-yl)-6-methoxy-7-[3-(1-piperidinyl)propoxy]-4-quinazolinamine
CAS Number: 1320288-19-4
Molecular Formula: C₃₇H₆₁N₇O₂
Molecular Weight: 635.926
Catalog: Biochemical Inhibitor Epigenetics Histone Methyltransferase inhibitor
Create Date: 2019-01-01 20:13:37
Modify Date: 2024-01-02 17:19:11
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.

Name	N-[1-(Cyclohexylmethyl)-4-piperidinyl]-2-(4-isopropyl-1,4-diazepa n-1-yl)-6-methoxy-7-[3-(1-piperidinyl)propoxy]-4-quinazolinamine
Synonyms	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

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.