778649-18-6 Usage
Description
Butyrolactone 3 is a chemical compound that acts as a selective inhibitor of histone acetyltransferase Gcn5, an enzyme involved in the regulation of gene expression. It has a high affinity for the enzyme, comparable to its natural substrate, making it a valuable tool for studying the histone code and its role in various biological processes.
Uses
Used in Research Applications:
Butyrolactone 3 is used as a research tool for understanding and further studying the histone code. Its selective inhibition of Gcn5 allows researchers to investigate the specific functions and mechanisms of this enzyme in gene regulation and other cellular processes.
Used in Pharmaceutical Development:
Due to its inhibitory properties, Butyrolactone 3 has potential applications in the development of pharmaceuticals targeting histone acetyltransferase enzymes. This could lead to the discovery of new therapeutic agents for treating diseases associated with abnormal gene expression and chromatin remodeling.
in vitro
the analogs of butyrolactone 3 only showed a weak inhibition of cbp, while butyrolactone 3 led to an inhibition of gcn5. it was important to see that in the presence of acetyl-coa the kd value for binding of histone h3 to gcn5 or pcaf was around 100 mm. moreover, the affinity of butyrolactone 3 to the gcn5 enzyme was found to be comparable to that of the natural substrate h3 and could provide an good starting point for the study of sar. in addition, a nonirreversible inhibition of gcn5 could be determine, and thus a michael addition of nucleophilic groups of the enzymebs active side was unlikely. therefore, the derivatization of gbutyrolactone 3 at position 2 might be a promising starting point for future sar studies [1].
IC 50
100 μm
references
1. m. biel, a. kretsovali, e. karatzali, et al. design, synthesis, and biological evaluation of a small-molecule inhibitor of the histone acetyltransferase gcn5. angewandte chemie international edition 43, 3974-3976 (2004).
Check Digit Verification of cas no
The CAS Registry Mumber 778649-18-6 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 7,7,8,6,4 and 9 respectively; the second part has 2 digits, 1 and 8 respectively.
Calculate Digit Verification of CAS Registry Number 778649-18:
(8*7)+(7*7)+(6*8)+(5*6)+(4*4)+(3*9)+(2*1)+(1*8)=236
236 % 10 = 6
So 778649-18-6 is a valid CAS Registry Number.