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UNC0321 G9a inhibitor

Catalog No.B1126
Size Price Stock
1g Please Inquire Please Inquire

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Sample solution is provided at 25 µL, 10mM.

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Chemical structure

UNC0321

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Chemical Properties

Cas No. 1238673-32-9 SDF Download SDF
Chemical Name 7-[2-[2-(dimethylamino)ethoxy]ethoxy]-6-methoxy-2-(4-methyl-1,4-diazepan-1-yl)-N-(1-methylpiperidin-4-yl)quinazolin-4-amine
Canonical SMILES CN1CCCN(CC1)C2=NC3=CC(=C(C=C3C(=N2)NC4CCN(CC4)C)OC)OCCOCCN(C)C
Formula C27H45N7O3 M.Wt 515.69
Solubility Soluble in DMSO Storage Store at -20°C
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
Shipping Condition Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request

Background

UNC0321 is the most potent small-molecule inhibitor of protein lysine methyltransferase G9a, an enzyme methylating lysine 9 of histone H3 (H3K9) and lysine 373 (K373) of p53, with the inhibition constant Ki value of 63 nM and the half maximal inhibition concentration IC50 values of 9 nM in enzyme-coupled SAH detection assay (ECSD) and 6 nM in chemiluminescence-based oxygen tunneling assay (CLOT) respectively [1].

UNC0321 has also been found to inhibit G9a like protein (GLP), an H3K9 and p53 K373 methyltransferase sharing 80% sequence identity in SET domain with G9a, with IC50 values of 15 nM (ECSD) and 23 nM (CLOT) respectively [1].

Reference

References:
[1] Liu F, Chen X, Allali-Hassani A, Quinn AM, Wigle TJ, Wasney GA, Dong A, Senisterra G, Chau I, Siarheyeva A, Norris JL, Kireev DB, Jadhav A, Herold JM, Janzen WP, Arrowsmith CH, Frye SV, Brown PJ, Simeonov A, Vedadi M, Jin J. Protein lysine methyltransferase G9a inhibitors: design, synthesis, and structure activity relationships of 2,4-diamino-7-aminoalkoxy-quinazolines. J Med Chem. 2010 Aug 12;53(15):5844-57. doi: 10.1021/jm100478y.