778649-18-6 Usage
Uses
Butyrolactone 3 is a selective inhibitor of histone acetyltransferase Gcn5 with affinity for the enzyme comparable to its natural substrate. Butyrolactone 3 is very useful tool in understanding and further studying the histone code.
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.
