For research use only. Not for therapeutic Use.
UNC0321 is a potent and selective histone methyltransferase G9a inhibitor with a Ki of 63 pM and with assay-dependent IC50 values of 6-9 nM. UNC0321 also inhibits GLP with assay-dependent IC50 values of 15-23 nM. UNC0321 has anti-apoptotic activity and has potential application in diabetic vascular complications[1][3].
UNC0321 (Compound 29) inhibits the activity of G9a ECSD, G9a CLOT, GLP ECSD and GLP CLOT with IC50 values of 9 nM, 6 nM, 15 nM and 23 nM, respectively[1].
UNC0321 (Compound 3) reduces H3K9me2 levels in MDA-MB-231 cells with an IC50 value of 11 μM[2].
UNC0321 (200 pM; 48 h) significantly inhibits the expression of Rab4 in HUVEC[3].
| Catalog Number | I000950 |
| CAS Number | 1238673-32-9 |
| Synonyms | 7-[2-[2-(dimethylamino)ethoxy]ethoxy]-6-methoxy-2-(4-methyl-1,4-diazepan-1-yl)-N-(1-methylpiperidin-4-yl)quinazolin-4-amine |
| Molecular Formula | C27H45N7O3 |
| Purity | ≥95% |
| InChI | InChI=1S/C27H45N7O3/c1-31(2)15-16-36-17-18-37-25-20-23-22(19-24(25)35-5)26(28-21-7-11-33(4)12-8-21)30-27(29-23)34-10-6-9-32(3)13-14-34/h19-21H,6-18H2,1-5H3,(H,28,29,30) |
| InChIKey | AULLUGALUBVBDD-UHFFFAOYSA-N |
| SMILES | CN1CCCN(CC1)C2=NC3=CC(=C(C=C3C(=N2)NC4CCN(CC4)C)OC)OCCOCCN(C)C |
| Reference | [1]. Liu F, et al. 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. [2]. Liu F, et al. Optimization of cellular activity of G9a inhibitors 7-aminoalkoxy-quinazolines. J Med Chem. 2011 Sep 8;54(17):6139-50. [3]. Nie J. UNC0321 inhibits high glucose induced apoptosis in HUVEC by targeting Rab4. Biomed Pharmacother. 2020 Nov;131:110662. |
