MG149

Alias: MG-149; MG 149; MG149; Tip60 HAT inhibitor
Cat No.:V2520 Purity: ≥98%
MG-149 (MG149) is a novel, potent and selectivehistone acetyltransferase (HAT) inhibitor with anticancer activity.
MG149 Chemical Structure CAS No.: 1243583-85-8
Product category: Histone Acetyltransferase
This product is for research use only, not for human use. We do not sell to patients.
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Purity & Quality Control Documentation

Purity: ≥98%

Product Description

MG-149 (MG149) is a novel, potent and selective histone acetyltransferase (HAT) inhibitor with anticancer activity. It inhibits HAT with IC50 of 74 μM and 47 μM for Tip60 and MOF, respectively. It shows little potent for PCAF and p300(IC50 >200 uM). 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.

Biological Activity I Assay Protocols (From Reference)
ln Vitro
MG 149 (Tip60 HAT inhibitor) inhibits roughly 90% of Tip60 activity at 200 μM, but has no inhibitory effect on p300 and PCAF. MG 149 essentially competes with Ac-CoA but not with histone substrates. HAT inhibition experiments with MG 149 indicated that both drugs strongly suppressed HAT activity in nuclear extracts from different locations (p < 0.05) [1].
ln Vivo

Animal Protocol


References
[1]. Ghizzoni M, et al. 6-alkylsalicylates are selective Tip60 inhibitors and target the acetyl-CoA binding site. Eur J Med Chem. 2012 Jan;47(1):337-44.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C22H28O3
Molecular Weight
340.46
CAS #
1243583-85-8
SMILES
O([H])C1=C([H])C([H])=C([H])C(=C1C(=O)O[H])C([H])([H])C([H])([H])C1C([H])=C([H])C(=C([H])C=1[H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])[H]
InChi Key
WBHQYBZRTAEHRR-UHFFFAOYSA-N
InChi Code
InChI=1S/C22H28O3/c1-2-3-4-5-6-8-17-11-13-18(14-12-17)15-16-19-9-7-10-20(23)21(19)22(24)25/h7,9-14,23H,2-6,8,15-16H2,1H3,(H,24,25)
Chemical Name
2-[2-(4-heptylphenyl)ethyl]-6-hydroxybenzoic acid
Synonyms
MG-149; MG 149; MG149; Tip60 HAT inhibitor
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO: 68 mg/mL (199.7 mM)
Water:<1 mg/mL
Ethanol: N/A
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 2.9372 mL 14.6860 mL 29.3720 mL
5 mM 0.5874 mL 2.9372 mL 5.8744 mL
10 mM 0.2937 mL 1.4686 mL 2.9372 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

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Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation:Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

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