A-893

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

A-893 (A893) 是一种有效、选择性和细胞活性的赖氨酸甲基转移酶 SMYD2 抑制剂，IC50 为 2.8 nM。

A-893 (A893) is a potent, selective and cell active lysine methyltransferase SMYD2 inhibitor with IC50 of 2.8 nM; displays high selectivity against a panel of 31 other methyltransferases (<50% inhibition at 1 uM); reduces p53K370me1 without effects on overall p53 levels in A549 p53 cellular assay, has unexpectedly notable improvement in potency (>80-fold) compared with AZ-505 .

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.

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A 893 | A893

Chromatin/Epigenetic

HMTase

HMTase

Cancer

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1868232-32-9

577.547

C29H38Cl2N4O4

>98% (HPLC)

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O=C(N1)COC(C1=CC=C2)=C2[C@@H](O)CNCCN(C3CCCCC3)C(CCNCCC4=CC(Cl)=C(Cl)C=C4)=O

(R)-N-Cyclohexyl-3-[(3,4-dichlorophenethyl)amino]-N-[2-[[2-hydroxy-2-(3-oxo-3,4-dihydro-2H-benzo[b][1,4]oxazin-8-yl)ethyl]amino]ethyl]propanamide

(-20℃)

With Ice Pack

≥ 2 years