SCFSkp2-IN-2

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

SCFSkp2-IN-2 (Compound AAA-237) 是一种 Skp2 抑制剂，其 KD 为 28.77 μM。AAA-237 诱导 NSCLC 细胞凋亡 (apoptosis)，显示出抗肿瘤活性。

SCFSkp2-IN-2 (Compound AAA-237) is a Skp2 inhibitor with a KD of 28.77 μM. AAA-237 induces apoptosis of NSCLC cells and shows antitumor activities.

Western Blot AnalysisCell Line:A549 and H1299 cellsConcentration:0.3, 1 and 3 μMIncubation Time:24, 48 and 72 hResult: Increased the expression levels of p21Cip1 and p27Kip1. Decreased the level of Skp2. Reduced the expression levels of CDK2, p-CDK2, cyclin E1, CDK4, p-CDK4 and cyclin D. Increased the levels of cleaved PARP, cleaved caspase 3, cleaved caspase 9 and Bax. Decreased the expression of PARP and Bcl-2.Cell Proliferation Assay Cell Line:A549 and H1299 cells Concentration:0.3, 1 and 3 μM Incubation Time:24, 48 and 72 h Result:Inhibited the proliferation of A549 and H1299 cells in a dose- and time-dependent manner. The IC50 for A549 was 3?μM at 24?h, 2.5?μM at 48?h and 0.7?μM at 72?h. The IC50 for H1299 was 3.9?μM at 24?h, 1.8?μM at 48?h and 1.1?μM at 72?h.Cell Cycle Analysis Cell Line:A549 and H1299 cells Concentration:0.3, 1 and 3 μM Incubation Time:24, 48 and 72 h Result: Arrested the cell cycle at G0/G1 in a dose- and time-dependent manner. Apoptosis Analysis Cell Line:A549 and H1299 cells Concentration:0.3, 1 and 3 μM Incubation Time:24, 48 and 72 h Result:The ratio of JC-1 monomer/JC-1 polymer was increased in A549 and H1299 cells as the concentration was increased.

Animal Model:A549 xenograft model Dosage:15 or 45?mg/kg Administration:Intraperitoneal administration, daily for 14 days Result:Significantly reduced tumor volume and weight. The tumor growth inhibition of the low dose and high dose was 55% and 64%, respectively. No obvious weight loss or abnormal behavior was observed. Reduced the expression of Ki67 in tumor tissue. Reduced the expression of Skp2 and Bcl-2 and increased the expression of p27, the cleaving of caspase 3, caspase 9, PARP and Bax.

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Apoptosis

Apoptosis

Apoptosis | E1/E2/E3 Enzyme

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1375060-02-8

312.37

C17H20N4O2

>98% (HPLC)

In Vitro:?DMSO 中的溶解度 : 125 mg/mL (400.17 mM; 超声助溶 (<60°C)

N(CC)(CC)C1=CC(O)=C(/C=N/NC(=O)C=2C=CC=NC2)C=C1

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(-20℃)

With Ice Pack

≥ 2 years