生物活性 | |||
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描述 | ZLN024 effectively stimulates both active AMPK heterotrimers and inactive α1 subunit truncations α1 (1-394) and α1 (1-335), although it does not affect α1 (1-312). For ZLN024 to activate AMPK, Thr-172 must be pre-phosphorylated by an upstream kinase, and ZLN024 also shields AMPK Thr-172 from dephosphorylation by PP2Cα. In L6 myotubes, ZLN024 activation of AMPK leads to increased glucose uptake and fatty acid oxidation without altering the ADP/ATP ratio. Identified through random screening using a scintillation proximity assay (SPA) targeting the AMPK α1β1γ1 heterotrimer, ZLN024 has been pinpointed as a novel AMPK activator. It activates AMPK α1β1γ1 and its homologue α2β1γ1 in a dose-dependent manner, enhancing the activity of α1β1γ1 by 1.5-fold with an EC50 of 0.42 µM, and that of α2β1γ1 by 1.7-fold with an EC50 of 0.95 µM. Additionally, ZLN024 boosts the activity of recombinant AMPK α1β2γ1 and α2β2γ1 by 1.7-fold and 1.6-fold, with EC50 values of 1.1 µM and 0.13 µM, respectively[1]. |
实验方案 | |||
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1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
2.76mL 0.55mL 0.28mL |
13.82mL 2.76mL 1.38mL |
27.65mL 5.53mL 2.76mL |
参考文献 |
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