| Bioactivity | 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[1]. | ||||||||||||
| Target | KD: 28.77 μM (Skp2) | ||||||||||||
| Invitro | SCFSkp2-IN-2 (Compound AAA-237) (0.3-3 μM; 24-72 h) 可直接与 Skp2 结合，导致 Skp2 被蛋白酶体降解。AAA-237 对 Skp2 mRNA 表达无显著影响，但对 NSCLC 细胞中 Skp2 蛋白表达有时间依赖性的抑制作用[1]。SCFSkp2-IN-2 (0.3-3 μM; 24-72 h) 以剂量和时间依赖的方式抑制 A549 和 H1299 细胞的增殖[1]。SCFSkp2-IN-2 (0.3-3 μM; 24-72 h) 通过调节 Skp2-Cip/Kip 和 PI3K/Akt-FOXO1 信号通路，在 G0/G1 检查点阻止细胞周期[1]。SCFSkp2-IN-2 (0.3-3 μM; 24-72 h) 以剂量和时间依赖的方式诱导 A549 和 H1299 细胞凋亡[1]。SCFSkp2-IN-2 (0.3 μM; 1-7 days) 诱导 NSCLC 细胞衰老[1]。 Western Blot Analysis[1] Cell Line: | ||||||||||||
| In Vivo | SCFSkp2-IN-2 (Compound AAA-237) (15 or 45 mg/kg; i.p.; daily for 14 days) 在肺癌 A549 异种移植小鼠模型中显示出抗肿瘤活性[1]。 Animal Model: | ||||||||||||
| Name | SCFSkp2-IN-2 | ||||||||||||
| CAS | 1375060-02-8 | ||||||||||||
| Formula | C17H20N4O2 | ||||||||||||
| Molar Mass | 312.37 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [1]. Liu J, et al. Anti-tumor effects of Skp2 inhibitor AAA-237 on NSCLC by arresting cell cycle at G0/G1 phase and inducing senescence. Pharmacol Res. 2022 Jul;181:106259. |
SCFSkp2-IN-2
CAS: 1375060-02-8 F: C17H20N4O2 W: 312.37
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
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