1868232-32-9

1868232-32-9 structure

Name: A-893
Chemical Name: A-893
CAS Number: 1868232-32-9
Molecular Formula: C₂₉H₃₈Cl₂N₄O₄
Molecular Weight: 577.542
Catalog: Signaling Pathways Epigenetics Histone Methyltransferase
Create Date: 2018-05-05 18:56:56
Modify Date: 2024-01-08 15:45:44
A-893 is a cell-active inhibitor of Methyltransferase SMYD2, with an IC50 of 2.8 nM.

Name	A-893
Synonyms	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]-

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.