AMPK

UCB9386 is a brain-penetrant and selective inhibitor of Nuak1, with a pIC50 of 10.1. It also inhibits Nuak2 and Kak2, showing approximately 50% inhibition at 10 nM.

AMPK-IN-6 (compound 13a) is a potent AMPK inhibitor with an IC50 value of 0.093 µM. It induces apoptosis and suppresses autophagy. Additionally, AMPK-IN-6 exhibits antiproliferative activity and holds potential for research into pulmonary arterial hypertension.

STO-609 acetate is selective, cell-permeable inhibitor of Ca2+-calmodulin-dependent protein kinase kinase (Ki: 80/15 ng/ml, for CaM-KKα/KKβ); competes for the

Resolvin D3 (RvD3) is a dysregulated mediator originating from docosahexaenoic acid (DHA). It plays a crucial role in reducing arthritic inflammation.

IQZ23 inhibits fat cell formation, activates AMPK, cuts triglycerides (EC50=0.033 μM), may aid obesity/metabolic study.

XY221 (Compound 16o) selectively inhibits BRD4 BD2 with an IC50 of 5.8 nM. It demonstrates high selectivity for pan-BD2 and BRD4 BD2 domains, being 667 times more selective than for BRD4 BD1, and 9-32 times more selective than for BRD2/3/T BD2. XY221 can induce apoptosis in MV4-11 cells and exhibits anti-cancer activity.

NUAK1-IN-2 (Compound 24) is an inhibitor of NUAK1 with an IC50 of 3.162 nM, as well as an inhibitor of CDK2/4/6. It is applicable in research related to cancer, neurodevelopmental disorders, and Alzheimer's disease.

Kanglexin is an orally active novel anthraquinone compound. It inhibits NLRP3 inflammasome activation and pyroptosis, offering cardioprotective benefits. By stimulating the FGFR1/ERK signaling pathway, Kanglexin promotes angiogenesis and accelerates wound healing in diabetes. Additionally, it has lipid-lowering effects and inhibits vascular smooth muscle cell dedifferentiation, making it a potential compound for studying hyperlipidemia, fatty liver, and atherosclerosis.

xnum well-chosen unique AMPK-targeted small molecules；

Compound 38-S is an orally active CB1R/AMPK modulator with a K i of 0.81 nM and an IC50 of 3.9 nM for CB1R.

ZLN 024 hydrochloride is an AMPK allosteric activator and stimulates the inactive α1 subunit truncations α1 (1-394) and α1 (1-335) but not α1 (1-312).

Wu-5 is a potent USP10 inhibitor that inhibits FLT3 and AMPK pathways, promoting the breakdown of FLT3-ITD and inducing apoptosis.

ALKBH1-IN-4 prodrug (Compound 29E) is a prodrug of an inhibitor targeting the DNA N6-methyladenine demethylase enzyme ALKBH1. It works by significantly increasing the cellular abundance of 6mA and enhancing the AMPK signaling pathway, which suppresses the vitality of gastric cancer cells. ALKBH1-IN-4 prodrug displays excellent cellular activity and favorable metabolic exposure in vivo, making it a promising candidate for research in gastric cancer-related areas.

SAMS peptide is a specific substrate for the AMP-activated protein kinase (AMPK).

Fluoxetine-Conjugated Platinum(IV) prodrug-1 is an eEF2K inhibitor that can hinder the proliferation of cancer cells, induce DNA damage, and cause cell cycle arrest at the S phase, leading to apoptosis (Apoptosis). It also promotes the accumulation of reactive oxygen species (ROS) and disrupts mitochondrial function. This prodrug inhibits the migration and invasion of TNBC cells by suppressing MMP-2 activity and induces autophagy in TNBC cells through AMPK activation. In the 4T1-Luc mouse model, it exhibits antitumor activity and triggers immune suppression. Fluoxetine-Conjugated Platinum(IV) prodrug-1 is relevant for research in triple-negative breast cancer (TNBC).

Antidiabetic agent 7 (Compound 5m) functions as a potent hyperglycemia inhibitor. It effectively stimulates GLUT4 translocation in skeletal muscle cells by activating the AMPK-dependent pathway. Additionally, this compound is capable of reducing blood glucose levels and exhibits favorable pharmacokinetic properties. Antidiabetic agent 7 is suitable for research related to antihyperglycemic treatments.

Biguanide can reduce oxidative stress in rats with hyperglycemia.

ALKBH1-IN-3 is an effective inhibitor of the DNA N6-methyladenosine (6mA) demethylase ALKBH1. This compound enhances the abundance of 6mA in gastric cancer cell lines HGC27 and AGS, simultaneously inhibiting cell viability and upregulating the AMP-activated protein kinase (AMPK) signaling pathway. ALKBH1-IN-3 holds potential for use in cancer research, including studies on gastric cancer.

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