UNC0321

Product NameUNC0321
CAS1238673-32-9
MFC27H45N7O3
MW515.69
EINECS604-604-1
MOL File1238673-32-9.mol

Chemical Properties

Boiling point	664.7±65.0 °C(Predicted)
Density	1.150±0.06 g/cm3(Predicted)
storage temp.	Store at -20°C
solubility	DMSO: ≥ 31 mg/mL (60.11 mM)
pka	9.34±0.70(Predicted)
form	Powder

Usage And Synthesis

Definition

ChEBI: 7-[2-[2-(dimethylamino)ethoxy]ethoxy]-6-methoxy-2-(4-methyl-1,4-diazepan-1-yl)-N-(1-methyl-4-piperidinyl)-4-quinazolinamine is a member of quinazolines.

Biological Activity

UNC0321 is a potent and selective histone methyltransferase G9a inhibitor with Ki of 63 pM and IC50 of 6-9 nM.It also inhibits GLP with IC50 values of 15-23 nM.UNC0321 is inactive against SET7/9, SET8/PreSET7, PRMT3 and JMJD2E.

in vitro

In G9a ECSD and CLOT assays, the IC ₅₀ values of 9 nM and 6 nM for UNC0321 (Compound 29), respectively. In GLP ECSD and CLOT assays, the IC ₅₀ values of 15 nM and 23 nM for UNC0321, respectively.
UNC0321 (Compound 3) reduces H3K9me2 levels in MDA-MB-231 cells with an IC50 of 11 μM.

target

G9a

63 pM (Ki)

G9a

6-9 nM (IC ₅₀ )

GLP

15-23 nM (IC ₅₀ )