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AAA237

Chemical Structure : AAA237

CAS No.: 1375060-02-8

AAA237 (AAA-237)

Catalog No.: PC-21767Not For Human Use, Lab Use Only.

AAA-237 (AAA237) is a small molecule Skp2 E3 ligase inhibitor, binds to Skp2 protein (KD=28.77 uM) and inhibits the degradation of Skp2 substrates, inhibits the proliferation of the NSCLC cells.

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Biological Activity

AAA-237 (AAA237) is a small molecule Skp2 E3 ligase inhibitor, binds to Skp2 protein (KD=28.77 uM) and inhibits the degradation of Skp2 substrates, inhibits the proliferation of the NSCLC cells.
AAA-237 has no significant effect on the mRNA expression of Skp2 but inhibits the protein expression of Skp2 in NSCLC cells in a time-dependent manner.
AAA-237 increases the expression levels of p21Cip1 and p27Kip1 in A549 and H1299 cells.
AAA-237 inhibits the proliferation of A549 and H1299 cells in a dose- and time-dependent manner, inhibits colony formation of A549 and H1299 cells.
AAA-237 arrests the cell cycle at the G0/G1 checkpoint by regulating the Skp2-Cip/Kip and PI3K/Akt-FOXO1 signaling pathways.
AAA-237 (15 or 45 mg/kg) suppresses growth of xenograft tumors by inducing apoptosis and senescence in lung cancer A549 xenograft mice model.

Physicochemical Properties

M.Wt 312.37
Formula C17H20N4O2
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

(E)-N'-(4-(diethylamino)-2-hydroxybenzylidene)nicotinohydrazide

References

1. Liu J, et al. Pharmacol Res. 2022 Jul;181:106259.

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