UNC 0224

Potent inhibitor of G9a histone lysine methyltransferase (IC50 = 15 nM).

The associations between environmental quality and preterm birth in the United States, 2000-2005: a cross-sectional analysis.[Pubmed:26051702]

Environ Health. 2015 Jun 9;14:50.

BACKGROUND: Many environmental factors have been independently associated with preterm birth (PTB). However, exposure is not isolated to a single environmental factor, but rather to many positive and negative factors that co-occur. The environmental quality index (EQI), a measure of cumulative environmental exposure across all US counties from 2000-2005, was used to investigate associations between ambient environment and PTB. METHODS: With 2000-2005 birth data from the National Center for Health Statistics for the United States (n = 24,483,348), we estimated the association between increasing quintiles of the EQI and county-level and individual-level PTB; we also considered environmental domain-specific (air, water, land, sociodemographic and built environment) and urban-rural stratifications. RESULTS: Effect estimates for the relationship between environmental quality and PTB varied by domain and by urban-rural strata but were consistent across county- and individual-level analyses. The county-level prevalence difference (PD (95% confidence interval) for the non-stratified EQI comparing the highest quintile (poorest environmental quality) to the lowest quintile (best environmental quality) was -0.0166 (-0.0198, -0.0134). The air and sociodemographic domains had the strongest associations with PTB; PDs were 0.0196 (0.0162, 0.0229) and -0.0262 (-0.0300, -0.0224) for the air and sociodemographic domain indices, respectively. Within the most urban strata, the PD for the sociodemographic domain index was 0.0256 (0.0205, 0.0307). Odds ratios (OR) for the individual-level analysis were congruent with PDs. CONCLUSION: We observed both strong positive and negative associations between measures of broad environmental quality and preterm birth. Associations differed by rural-urban stratum and by the five environmental domains. Our study demonstrates the use of a large scale composite environment exposure metric with preterm birth, an important indicator of population health and shows potential for future research.

Discovery of a 2,4-diamino-7-aminoalkoxyquinazoline as a potent and selective inhibitor of histone lysine methyltransferase G9a.[Pubmed:19891491]

J Med Chem. 2009 Dec 24;52(24):7950-3.

SAR exploration of the 2,4-diamino-6,7-dimethoxyquinazoline template led to the discovery of 8 (UNC0224) as a potent and selective G9a inhibitor. A high resolution X-ray crystal structure of the G9a-8 complex, the first cocrystal structure of G9a with a small molecule inhibitor, was obtained. The cocrystal structure validated our binding hypothesis and will enable structure-based design of novel inhibitors. 8 is a useful tool for investigating the biology of G9a and its roles in chromatin remodeling.

UNC0224 is a potent and selective histone methyltransferase G9a inhibitor with a Ki of 2.6 nM, an IC50 of 15 nM and a Kd of 23 nM. UNC0224 also potently inhibits b>GLP

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