A-893
A-893 is a cell-active inhibitor of Methyltransferase SMYD2, with an IC50 of 2.8 nM.
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- CAS No.: 1868232-32-9
- Formule: C29H38Cl2N4O4
- Masse moléculaire:577.54
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
Description
IC50 & Target
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SMYD2 |
In Vitro
The ratio of p53K370me1 to overall p53 levels is reduced, as expected, by treatment with either A-893 or AZ505. While this unexpectedly depicts a more robust response with AZ505, further dissection of the data provides clarity into the origin of this. While overall p53 levels are unaffected by A-893, a surprising >3-fold increase is observed with AZ505. Analysis of p53K370me1 levels reveals that inhibitor A-893 exhibited 42% reduction in the methyl mark, while AZ-505 is slightly less effective at 28% reduction[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 1868232-32-9
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Masse moléculaire 577.54
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Formule C29H38Cl2N4O4
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SMILES
O=C(CCNCCC1=CC(Cl)=C(Cl)C=C1)N(C2CCCCC2)CCNC[C@H](O)C3=CC=CC(N4)=C3OCC4=O
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocole
Cell Assay[1]
Human A549 lung carcinoma cells are chosen due to their high SMYD2 expression levels and wild-type p53 status. After 18 h of treatment with 10 μM of compound (e.g. A-893), changes in p53K370me1 are measured along with changes to overall p53 levels[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)