AMPK-IN-3

• CAT Number: I042860
• CAS Number: 2417674-27-0
• Molecular Formula: C25H33N5O3
• Molecular Weight: 451.56
• Purity: ≥95%
• Synonyms: 5-[(Z)-[5-(3-amino-3-oxopropyl)-2-oxo-1H-indol-3-ylidene]methyl]-N-[2-(diethylamino)ethyl]-2,4-dimethyl-1H-pyrrole-3-carboxamide
• InChI: InChI=1S/C25H33N5O3/c1-5-30(6-2)12-11-27-25(33)23-15(3)21(28-16(23)4)14-19-18-13-17(8-10-22(26)31)7-9-20(18)29-24(19)32/h7,9,13-14,28H,5-6,8,10-12H2,1-4H3,(H2,26,31)(H,27,33)(H,29,32)/b19-14-
• InChIKey: IQUHNNUWFFXNMM-RGEXLXHISA-N
• SMILES: CCN(CC)CCNC(=O)C1=C(NC(=C1C)C=C2C3=C(C=CC(=C3)CCC(=O)N)NC2=O)C

AMPK-IN-3 (compound 67) is a potent and selective AMPK inhibitor with IC50s of 60.7, 107 and 3820 nM for AMPK (α2), AMPK (α1) and KDR, respectively. AMPK-IN-3 inhibits AMPK does not affect cell viability or cause significant cytotoxicity in K562 cells. AMPK-IN-3 can be used in study of cancer[1].
AMPK-IN-3 (100 nM) shows inhibition values for AMPK(α2), FLT1, JAK1 JH2-pseudokinase and AMPK(α1) for 64%, 43%, 41% and 29%, respectively[1].
AMPK-IN-3 (0.195313, 0.78125, 3.125, 12.5, 50 µM; 2 h) decreases the level of p-ACC in K562 cells[1].
AMPK-IN-3 (1-100 µM; 24, 48, 72 h) shows potent inhibition of cellular AMPK activity but not affect cell viability[1].

Reference

[1]. Matheson CJ, et al. Substituted oxindol-3-ylidenes as AMP-activated protein kinase (AMPK) inhibitors. Eur J Med Chem. 2020 Jul 1;197:112316.
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