1. Epigenetics
  2. Histone Methyltransferase

A-893 

Cat. No.: HY-19563
Handling Instructions

A-893 is a cell-active inhibitor of Methyltransferase SMYD2, with an IC50 of 2.8 nM.

For research use only. We do not sell to patients.

A-893 Chemical Structure

A-893 Chemical Structure

CAS No. : 1868232-32-9

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Description

A-893 is a cell-active inhibitor of Methyltransferase SMYD2, with an IC50 of 2.8 nM.

IC50 & Target

IC50: 2.8 nM (SMYD2)[1].

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].

References
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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

577.54

Formula

C₂₉H₃₈Cl₂N₄O₄

CAS No.

1868232-32-9

SMILES

O=C(CCNCCC1=CC(Cl)=C(Cl)C=C1)N(C2CCCCC2)CCNC[[email protected]](O)C3=CC=CC(N4)=C3OCC4=O

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Shipping

Room temperature in continental US; may vary elsewhere

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A-893
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A-893

Cat. No.: HY-19563