1243583-85-8 Usage
Biological Activity
mg 149 is an inhibitor of histone acetyltransferases (hat) with ic50 values of 74μm and 47μm for tip60 and mof, respectively [1].mg 149 is an anacardic acid derivative. it shows selective inhibition towards the myst type of hats: tip60 and mof with ic50 values of 74μm and 47μm, respectively. the docking study shows that the inhibition of tip60 by mg 149 is competitive with respect to ac-coa in the ac-coa binding pocket of tip60. mg 149 also inhibits the activity of hat in nuclear extracts from hela cells using biotinylated histone h3 or histone h4 peptides as substrates. it is found to be more potent for histone h3 compared to histone h4. additionally, dna microarrays demonstrate that mg149 inhibits p53 and nf-kb pathways as well as a very limited number of other pathways [1, 2].
references
[1] ghizzoni m, wu j, gao t, haisma hj, dekker fj, george zheng y. 6-alkylsalicylates are selective tip60 inhibitors and target the acetyl-coa binding site. eur j med chem. 2012 jan;47(1):337-44. [2] dekker fj, van den bosch t, martin ni. small molecule inhibitors of histone acetyltransferases and deacetylases are potential drugs for inflammatory diseases. drug discov today. 2014 may;19(5):654-60.
Check Digit Verification of cas no
The CAS Registry Mumber 1243583-85-8 includes 10 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 7 digits, 1,2,4,3,5,8 and 3 respectively; the second part has 2 digits, 8 and 5 respectively.
Calculate Digit Verification of CAS Registry Number 1243583-85:
(9*1)+(8*2)+(7*4)+(6*3)+(5*5)+(4*8)+(3*3)+(2*8)+(1*5)=158
158 % 10 = 8
So 1243583-85-8 is a valid CAS Registry Number.
1243583-85-8Relevant articles and documents
Improved inhibition of the histone acetyltransferase PCAF by an anacardic acid derivative
Ghizzoni, Massimo,Boltjes, André,Graaf, Chris De,Haisma, Hidde J.,Dekker, Frank J.
experimental part, p. 5826 - 5834 (2010/10/01)
Several lines of evidence indicate that histone acetyltransferases (HATs) are novel drug targets for treatment of diseases like, for example, cancer and inflammation. The natural product anacardic acid is a starting point for development of small molecule inhibitors of the histone acetyltransferase (HAT) p300/CBP associated factor (PCAF). In order to optimize the inhibitory potency, a binding model for PCAF inhibition by anacardic acid was proposed and new anacardic acid derivatives were designed. Ten new derivatives were synthesized using a novel synthetic route. One compound showed a twofold improved inhibitory potency for the PCAF HAT activity and a twofold improved inhibition of histone acetylation in HEP G2 cells.
