MG149

製品コードS7476 バッチS747602

印刷

化学情報

Chemical Structure Synonyms Tip60 HAT inhibitor Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C22H28O3
分子量 340.46 CAS No. 1243583-85-8
Solubility (25°C)* 体外 DMSO 68 mg/mL (199.72 mM)
Ethanol 68 mg/mL (199.72 mM)
Water Insoluble
体内 （毎回新しく調製した物を用意してください）
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O
3.4mg/ml Taking the 1 mL working solution as an example, add 50 μL of 68 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
Clear solution
5% DMSO 95% Corn oil
0.56mg/ml Taking the 1 mL working solution as an example, add 50 μL of 11.2 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results. 
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 MG149 (Tip60 HAT inhibitor) is a potent histone acetyltransferase inhibitor with IC50 of 74 μM and 47 μM for Tip60 and MOF,respectively.
in vitro MG149 targets the acetyl-CoA binding site, and inhibits acetyltransferase activity of nuclear extract from tissue samples from different brain regions in mice. [1] MG149 also inhibits the p53 and the NF-κB pathways. [2]

プロトコル(参考用のみ)

キナーゼアッセイ Biochemical inhibition assays
Radioisotope-labeled acetyltransferase assays are carried out at 30°C in a reaction volume of 30 µL. The reaction buffer contained 50 mM HEPES at pH 8.0, 0.1 mM EDTA, 50 µg/mL BSA, 1 mM dithiothreitol, 0.1% Triton-X100, and 2% DMSO. 14C-labeled Ac-CoA is used as the acetyl donor. The peptide containing the N-terminal 20-amino acid sequence of histone H4 is used as substrate for p300 and Tip60, and the peptide containing the N-terminal 20-amino acid sequence of histone H3 is employed as substrate for PCAF. The HAT reaction is initiated with the HAT enzyme after the other components (Ac-CoA, peptide substrate, and the inhibitor) are equilibrated at 30°C for 5 min. Rate measurements were based on initial conditions (generally less than 15% consumption of the limiting substrate). After the reaction, the mixture is loaded onto a Waterman P81 filter paper and then washed with 50 mM sodium bicarbonate (pH 9.0) for three times. The paper is air dried and the amount of radioactivity incorporated into the peptide substrate is quantified by liquid scintillation counting. In all the cases, background acetylation (in the absence of enzyme) is subtracted from the total signals. The IC50 is determined as the concentration of an inhibitor at which half of the enzyme activity is inhibited. For IC50 determination, a range of at least seven inhibitor concentrations varied at least 20-fold around the IC50 are tested. All the assays were performed at least twice, and duplicates generally agreed within 20%. The conditions for the IC50 measurement are ; for the Tip60 assay, the reaction contained 10 nM Tip60, 1 µM Ac-CoA, 100 µM H4-20 and the reaction time is 7 min, for the PCAF assay, the reaction contained 1 nM PCAF, 1 µM Ac-CoA, 100 µM H3-20 and the reaction time is 3.5 min, for the p300 assay, the reaction contains 5 nM p300, 1 µM Ac-CoA, 100 µM H4-20 and the reaction time is 5 min, for the MOF assay, the reaction contains 1 nM MOF, 1 µM Ac-CoA, 100 µM H4-20 and the reaction time is 5 min.

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

TIP60 mediates stress-induced hypertension via promoting glutamatedmPFC-to-vCA1 release [ Clin Exp Hypertens, 2023, 45(1):2259130] PubMed: 37817460
Mof plays distinct roles in hepatic lipid metabolism under healthy or non-alcoholic fatty liver conditions [ iScience, 2023, 26(12):108446] PubMed: 38034359
The Males Absent on the First (MOF) Mediated Acetylation Alters the Protein Stability and Transcriptional Activity of YY1 in HCT116 Cells [ Int J Mol Sci, 2023, 24(10)8719] PubMed: 37240065
TIP60 buffers acute stress response and depressive behaviour by controlling PPARγ-mediated transcription [ Brain Behav Immun, 2022, S0889-1591(22)00025-3] PubMed: 35114329
FACT subunit SUPT16H associates with BRD4 and contributes to silencing of interferon signaling [ Nucleic Acids Res, 2022, 50(15):8700-8718] PubMed: 35904816
Attenuation of histone H4 lysine 16 acetylation (H4K16ac) elicits a neuroprotection against ischemic stroke by alleviating the autophagic/lysosomal dysfunction in neurons at the penumbra [ Brain Res Bull, 2022, 184:24-33] PubMed: 35351588
Inhibition of Rice SerotoninN-Acetyltransferases by MG149 Decreased Melatonin Synthesis in Rice Seedlings [ Biomolecules-, 2021, 11(5), 658] PubMed: None
Inhibition of Rice Serotonin N-Acetyltransferases by MG149 Decreased Melatonin Synthesis in Rice Seedlings [ Biomolecules, 2021, 11(5)658] PubMed: 33946959
Mof acetyltransferase inhibition ameliorates glucose intolerance and islet dysfunction of type 2 diabetes via targeting pancreatic α-cells [ Mol Cell Endocrinol, 2021, 537:111425] PubMed: 34391847
FACT subunit SUPT16H associates with BRD4 and contributes to silencing of antiviral interferon signaling [ bioRxiv, 2021, 2021.04.21.440833] PubMed: 33907746

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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