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首页-小分子抑制剂&激动剂-Proteasome/Ubiquitin-E3 Ubiquitin Ligase-AAA237
AAA237

Chemical Structure : AAA237

CAS No.: 1375060-02-8

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AAA237 (AAA-237)

货号: 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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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

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.

物理化学性质&存储条件

分子量 312.37
分子式 C17H20N4O2
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

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

参考文献

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

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