product name MG 149
Description: MG149 is a novel, potent and selective histone acetyltransferase inhibitor with IC50 of 74 μM and 47 μM for Tip60 and MOF,respectively. Docking study (molecular modeling) 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.
References: Eur J Med Chem. 2012 Jan;47(1):337-44; Epigenomics. 2013 Aug;5(4):379-96.
340.46
Formula
C22H28O3
CAS No.
1243583-85-8
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 68 mg/mL (199.7 mM)
Water: <1 mg/mL
Ethanol:
Solubility (In vivo)
Synonyms
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19428036
| In Vitro |
In vitro activity: MG149 targets the acetyl-CoA binding site, and inhibits acetyltransferase activity of nuclear extract from tissue samples from different brain regions in mice. MG149 also inhibits the p53 and the NF-κB pathways Kinase Assay: MG 149, at 200 μM, inhibited about 90% of Tip60 activity but had no inhibitory impact on p300 and PCAF. MG 149 was essentially competitive with Ac-CoA and noncompetitive with the histone substrate. HAT inhibition studies with MG 149 demonstrated that both compounds inhibited the HAT activity of the nuclear extracts of different regions significantly (p < 0.05). Cell Assay: 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. |
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| In Vivo | |
| Animal model | |
| Formulation & Dosage | |
| References | Eur J Med Chem. 2012 Jan;47(1):337-44; Epigenomics. 2013 Aug;5(4):379-96. |
