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5mg |
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10mg |
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25mg |
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50mg |
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100mg |
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250mg |
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500mg |
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Purity: ≥98%
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.
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].
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ln Vivo |
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Animal Protocol |
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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.
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Molecular Formula |
C22H28O3
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Molecular Weight |
340.46
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CAS # |
1243583-85-8
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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]
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InChi Key |
WBHQYBZRTAEHRR-UHFFFAOYSA-N
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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)
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Chemical Name |
2-[2-(4-heptylphenyl)ethyl]-6-hydroxybenzoic acid
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Synonyms |
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
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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.
Calculation results
Working concentration: mg/mL;
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.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.