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A-893

Names

[ CAS No. ]:
1868232-32-9

[ Name ]:
A-893

[Synonym ]:
N-Cyclohexyl-N-[2-(3,4-dichlorophenyl)ethyl]-N-(2-{[(2R)-2-hydroxy-2-(3-oxo-3,4-dihydro-2H-1,4-benzoxazin-8-yl)ethyl]amino}ethyl)-β-alaninamide
Propanamide, N-cyclohexyl-3-[[2-(3,4-dichlorophenyl)ethyl]amino]-N-[2-[[(2R)-2-(3,4-dihydro-3-oxo-2H-1,4-benzoxazin-8-yl)-2-hydroxyethyl]amino]ethyl]-

Biological Activity

[Description]:

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

[Related Catalog]:

Signaling Pathways >> Epigenetics >> Histone Methyltransferase
Research Areas >> Others

[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].

[Cell Assay]

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].

[References]

[1]. Sweis RF, et al. Discovery of A-893, A New Cell-Active Benzoxazinone Inhibitor of Lysine Methyltransferase SMYD2. ACS Med Chem Lett. 2015 Apr 29;6(6):695-700.


[Related Small Molecules]

GSK126 | Tazemetostat (EPZ-6438) | UNC 0642 | GSK343 | Pinometostat (EPZ5676) | 3-Deazaneplanocin A (hydrochloride) | Pemrametostat (GSK3326595) | UNC1999 | BIX-01294 | EPZ031686 | AZ505 (ditrifluoroacetate) | MS023 | EPZ 004777 | EPZ015666 | EPZ015866(GSK591)

Chemical & Physical Properties

[ Density]:
1.3±0.1 g/cm3

[ Boiling Point ]:
790.6±60.0 °C at 760 mmHg

[ Molecular Formula ]:
C29H38Cl2N4O4

[ Molecular Weight ]:
577.542

[ Flash Point ]:
431.9±32.9 °C

[ Exact Mass ]:
576.226990

[ LogP ]:
3.13

[ Vapour Pressure ]:
0.0±2.9 mmHg at 25°C

[ Index of Refraction ]:
1.623

Related Compounds