| Identification | Back Directory | [Name]
UNC0646 | [CAS]
1320288-17-2 | [Synonyms]
CS-792
UNC0646
UNC0646/UNC-0646
UNC 0646;UNC0646;UNC-0646
N-(1-cyclohexylpiperidin-4-yl)-2-(4-isopropyl-1,4-diazepan-1-yl)-6-Methoxy-7-(3-(piperidin-1-yl)propoxy)quinazolin-4-aMine
N-(1-Cyclohexyl-4-piperidinyl)-2-(4-isopropyl-1,4-diazepan-1-yl)- 6-methoxy-7-[3-(1-piperidinyl)propoxy]-4-quinazolinamine
(1-CYCLOHEXYL-PIPERIDIN-4-YL)-[2-(4-ISOPROPYL-[1,4]DIAZEPAN-1-YL)-6-METHOXY-7-(3-PIPERIDIN-1-YL-PROPOXY)-QUINAZOLIN-4-YL]-AMINE
N-(1-Cyclohexyl-4-piperidinyl)-2-[hexahydro-4-(1-methylethyl)-1H-1,4-diazepin-1-yl]-6-methoxy-7-[3-(1-piperidinyl)propoxy]-4-quinazolinamine
4-Quinazolinamine, N-(1-cyclohexyl-4-piperidinyl)-2-[hexahydro-4-(1-methylethyl)-1H-1,4-diazepin-1-yl]-6-methoxy-7-[3-(1-piperidinyl)propoxy]- | [Molecular Formula]
C36H59N7O2 | [MDL Number]
MFCD22378486 | [MOL File]
1320288-17-2.mol | [Molecular Weight]
621.9 |
| Chemical Properties | Back Directory | [Boiling point ]
754.6±70.0 °C(Predicted) | [density ]
1.128±0.06 g/cm3(Predicted) | [storage temp. ]
Keep in dark place,Sealed in dry,2-8°C | [solubility ]
DMSO: soluble2mg/mL, clear (warmed) | [form ]
powder | [pka]
9.34±0.70(Predicted) | [color ]
white to beige |
| Hazard Information | Back Directory | [Description]
G9a and G9a-like protein (GLP) are euchromatic histone-lysine methyltransferases (EHMT2 and EHMT1, respectively) that can heterodimerize with each other to methylate several proteins in addition to histone H3. UNC0646 is a potent and selective inhibitor of G9a and GLP activities in vitro (IC50s = 6 and 15 nM, respectively) and G9a/GLP-mediated dimethylation of histone 3 on lysine 9 in MDA-MB-231 cells (IC50 = 26 nM). It is highly selective for G9a/GLP over several other protein lysine and arginine methyltransferases. UNC0646 potently inhibits G9a/GLP activity in a variety of cancer cell lines as well as in the human fetal lung IMR-90 line. This compound selectively targets the corepressor function of G9a without affecting its ability to act as a coactivator with glucocorticoid receptor. | [Uses]
UNC0646 is a novel Protein lysine methyltransferase G9a inhibitor. | [Definition]
ChEBI: N-(1-cyclohexyl-4-piperidinyl)-6-methoxy-7-[3-(1-piperidinyl)propoxy]-2-(4-propan-2-yl-1,4-diazepan-1-yl)-4-quinazolinamine is a member of quinazolines. | [IC 50]
G9a: 6 nM (IC50); GLP: <15 nM (IC50) | [storage]
+4°C | [References]
[1] liu f, barsyte-lovejoy d, allali-hassani a, he y, herold jm, chen x, yates cm, frye sv, brown pj, huang j, vedadi m, arrowsmith ch, jin j. optimization of cellular activity of g9a inhibitors 7-aminoalkoxy-quinazolines. j med chem. 2011;54(17):6139-50.
[2] liu f, barsyte-lovejoy d, li f, xiong y, korboukh v, huang xp, allali-hassani a, janzen wp, roth bl, frye sv, arrowsmith ch, brown pj, vedadi m, jin j. discovery of an in vivo chemical probe of the lysine methyltransferases g9a and glp. j med chem. 2013;56(21):8931-42. |
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