| Identification | Back Directory | [Name]
MG149 | [CAS]
1243583-85-8 | [Synonyms]
MG 149
CS-1878
CHEMBL1215739
MG 149;MG-149
MG149 USP/EP/BP
Tip60 HAT inhibitor
CHEMBL1215739; MG 149; MG-149
2-(4-heptylphenethyl)-6-hydroxybenzoic acid
2-[2-(4-heptylphenyl)ethyl]-6-hydroxy-benzoic acid
Benzoic acid, 2-[2-(4-heptylphenyl)ethyl]-6-hydroxy-
MG149 2-[2-(4-heptylphenyl)ethyl]-6-hydroxy-Benzoic acid
MG 149 Benzoic acid, 2-[2-(4-heptylphenyl)ethyl]-6-hydroxy- | [EINECS(EC#)]
604-604-1 | [Molecular Formula]
C22H28O3 | [MDL Number]
MFCD22123243 | [MOL File]
1243583-85-8.mol | [Molecular Weight]
340.46 |
| Chemical Properties | Back Directory | [Boiling point ]
477.8±33.0 °C(Predicted) | [density ]
1.100±0.06 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
≥114 mg/mL in DMSO; ≥30.5 mg/mL in EtOH; insoluble in H2O | [form ]
Powder | [pka]
3.06±0.30(Predicted) | [color ]
White to off-white | [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) | [InChIKey]
WBHQYBZRTAEHRR-UHFFFAOYSA-N | [SMILES]
OC1=C(C(CCC2=CC=C(C=C2)CCCCCCC)=CC=C1)C(O)=O |
| Hazard Information | Back Directory | [Uses]
MG149 (Tip60 HAT inhibitor) is a selective and potent Tip60 inhibitor with IC50 of 74 uM, similar potentcy for MOF (IC50= 47 uM); little potent for PCAF and p300 (IC50 >200 uM)[1]. | [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]. | [IC 50]
CBP/p300; TIP60 | [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. |
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| Company Name: |
LETOPHARM LIMITED
|
| Telephone: |
+86-21-5821 5861 |
| Website: |
www.letopharm.com |
| Company Name: |
SPIRO PHARMA
|
| Telephone: |
|
| Website: |
www.spiropharma.com.cn |
|