UNC0321

Modify Date: 2024-01-09 20:28:17

UNC0321 Structure
UNC0321 structure
Common Name UNC0321
CAS Number 1238673-32-9 Molecular Weight 515.691
Density 1.2±0.1 g/cm3 Boiling Point 664.7±65.0 °C at 760 mmHg
Molecular Formula C27H45N7O3 Melting Point N/A
MSDS N/A Flash Point 355.8±34.3 °C

 Use of UNC0321


UNC0321 is a potent and selective G9a inhibitor with Ki of 63 pM, UNC0321 is the first G9a inhibitor with picomolar potency and the most potent G9a inhibitor to date.IC50 value: 63 pM(Ki); 9 nM (ECSD assay) [1]Target: G9aIt was found that replacing the 5-carbon chain in compound 13 with an ethoxyethyl chain resulted in compound 29{UNC0321} (IC50 = 6 nM (CLOT) and 9 nM (ECSD)), the most potent G9a inhibitor to date. 29 had a Morrison Ki of 63 pM and was about 40-fold more potent than 10 (Morrison Ki = 2.6 nM) and 250-fold more potent than 3a (Morrison Ki = 16 nM) in this G9a assay. UNC0321 potentially useful small molecule tools for the biomedical research community to investigate the biology of G9a and its role in chromatin remodeling as well as PTMs of other proteins.

 Names

Name 7-{2-[2-(Dimethylamino)ethoxy]ethoxy}-6-methoxy-2-(4-methyl-1,4-d iazepan-1-yl)-N-(1-methyl-4-piperidinyl)-4-quinazolinamine
Synonym More Synonyms

 UNC0321 Biological Activity

Description UNC0321 is a potent and selective G9a inhibitor with Ki of 63 pM, UNC0321 is the first G9a inhibitor with picomolar potency and the most potent G9a inhibitor to date.IC50 value: 63 pM(Ki); 9 nM (ECSD assay) [1]Target: G9aIt was found that replacing the 5-carbon chain in compound 13 with an ethoxyethyl chain resulted in compound 29{UNC0321} (IC50 = 6 nM (CLOT) and 9 nM (ECSD)), the most potent G9a inhibitor to date. 29 had a Morrison Ki of 63 pM and was about 40-fold more potent than 10 (Morrison Ki = 2.6 nM) and 250-fold more potent than 3a (Morrison Ki = 16 nM) in this G9a assay. UNC0321 potentially useful small molecule tools for the biomedical research community to investigate the biology of G9a and its role in chromatin remodeling as well as PTMs of other proteins.
Related Catalog
References

[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.

 Chemical & Physical Properties

Density 1.2±0.1 g/cm3
Boiling Point 664.7±65.0 °C at 760 mmHg
Molecular Formula C27H45N7O3
Molecular Weight 515.691
Flash Point 355.8±34.3 °C
Exact Mass 515.358398
PSA 81.69000
LogP 0.36
Vapour Pressure 0.0±2.0 mmHg at 25°C
Index of Refraction 1.582
Storage condition 2-8℃

 Precursor & DownStream

Precursor  2

DownStream  0

 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
7-{2-[2-(Dimethylamino)ethoxy]ethoxy}-6-methoxy-2-(4-methyl-1,4-diazepan-1-yl)-N-(1-methyl-4-piperidinyl)-4-quinazolinamine
UNC0321
TFA salt