SCFSkp2-IN-2

• CAT Number: I041752
• CAS Number: 1375060-02-8
• Molecular Formula: C17H20N4O2
• Molecular Weight: 312.37
• Purity: ≥95%
• Synonyms: N-[(E)-[4-(diethylamino)-2-hydroxyphenyl]methylideneamino]pyridine-3-carboxamide
• InChI: InChI=1S/C17H20N4O2/c1-3-21(4-2)15-8-7-13(16(22)10-15)12-19-20-17(23)14-6-5-9-18-11-14/h5-12,22H,3-4H2,1-2H3,(H,20,23)/b19-12+
• InChIKey: HEUHCTYMFLTWAX-XDHOZWIPSA-N
• SMILES: CCN(CC)C1=CC(=C(C=C1)C=NNC(=O)C2=CN=CC=C2)O

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].
SCFSkp2-IN-2 (Compound AAA-237) (0.3-3 μM; 24-72 h) can directly bind to Skp2, causing the degradation of Skp2 by proteasome. 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[1].
SCFSkp2-IN-2 (0.3-3 μM; 24-72 h) inhibits the proliferation of A549 and H1299 cells in a dose- and time-dependent manner[1].
SCFSkp2-IN-2 (0.3-3 μM; 24-72 h) arrests the cell cycle at the G0/G1 checkpoint by regulating the Skp2-Cip/Kip and PI3K/Akt-FOXO1 signaling pathways[1].
SCFSkp2-IN-2 (0.3-3 μM; 24-72 h) induces apoptosis of A549 and H1299 cells in a dose- and time-dependent manner[1].
SCFSkp2-IN-2 (0.3 μM; 1-7 days) induces cellular senescence of the NSCLC cells[1].
SCFSkp2-IN-2 (Compound AAA-237) (15 or 45 mg/kg; i.p.; daily for 14 days) shows antitumor activity in lung cancer A549 xenograft mice model[1].

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.
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