UNC0321
UNC0321 Basic information
- Product Name:
- UNC0321
- Synonyms:
-
- UNC0321
- 7-(2-(2-(diMethylaMino)ethoxy)ethoxy)-6-Methoxy-2-(4-Methyl-1,4-diazepan-1-yl)-N-(1-Methylpiperidin-4-yl)quinazolin-4-aMine
- 7-[2-[2-(Dimethylamino)ethoxy]ethoxy]-2-(hexahydro-4-methyl-1H-1,4-diazepin-1-yl)-6-methoxy-N-(1-methyl-4-piperidinyl)-4-quinazolinamine
- UNC0321(UNC-0321)
- UNC 0321; UNC-0321; UNC0321; UNC-0321
- 4-Quinazolinamine, 7-[2-[2-(dimethylamino)ethoxy]ethoxy]-2-(hexahydro-4-methyl-1H-1,4-diazepin-1-yl)-6-methoxy-N-(1-methyl-4-piperidinyl)-
- H3K9me2,SAR,PKMT,Histone Methyltransferase,H3K9,quinazoline,inhibit,K373,UNC-0321,p53,UNC0321,UNC 0321,G9a,GLP,Inhibitor
- CAS:
- 1238673-32-9
- MF:
- C27H45N7O3
- MW:
- 515.69
- EINECS:
- 604-604-1
- Mol File:
- 1238673-32-9.mol
UNC0321 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
- color
- White to yellow
UNC0321 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 ) |
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