ampk activator 1

AMPK activator 1 is an AMPK activator (compound No.1-75) with an EC50 of less than 0.1 μM.

AMPK activator 12 is an AMPK activator and GDF15 inducer that elevates the expression level of GDF15 protein in human hepatocytes, which can be used for cancer research.

AMPK Activator 13 is a potent activator of the AMPK pathway, effectively inhibiting mitotic clonal expansion in 3T3-L1 cells and enhancing mitochondrial oxygen consumption rates. This compound is utilized in the study of obesity [1].

AMPK activator 14 (compound 32), an orally active agent, effectively reduces fasted glucose and insulin levels in a db db mouse model of Type II diabetes [1].

AMPK Activator 11 is a nanomolar potent inhibitor of cell proliferation in various colorectal carcinomas (CRCs), acting through the selective activation of AMP-activated protein kinase (AMPK) and enhancement of oxidative phosphorylation (OXPHOS) (mitochondrial metabolism). This compound demonstrates particular efficacy in inhibiting RKO xenograft growth, rendering it useful for anti-tumor and metabolic disease research [1].

AMPK-α1β1γ1 activator 1 (M1), an acyl glucuronide metabolite derived from an Indole-3-carboxylic Acid-based AMPK activator, selectively activates the β1 isoforms of human AMPK with an EC50 of 38.1 nM through direct binding to the human AMPK α1β1γ1 isoform; it is utilized in diabetic nephropathy research [1].

AMPK activator16 (compound 6) functions as an AMP-activated protein kinase (AMPK) inhibitor. It interacts effectively with crucial AMPK residues, significantly activating the enzyme. In N2a cells, AMPK activator16 enhances the expression of phosphorylated AMPK (p-AMPK) and its downstream signaling proteins, such as phosphorylated ACC (Acetyl-CoA Carboxylase) and phosphorylated raptor (p-raptor).

AP39 Prodrug 1 (Compound M1) is a mitochondria-targeted H2S prodrug. In hepatocytes, it induces ROS-dependent mild mitochondrial uncoupling, activates mitochondria-associated AMPK, and inhibits Palmitic acid (PA)-induced lipid accumulation.

IM156 (HL156A; HL271 acetate) is a chemical derivative of Metformin. IM156 is a potent and orally active AMPK activator that increases AMPK phosphorylation. IM156 attenuates aging-associated cognitive impairment in animal model [1] [2]. IM156 is a potent oxidative phosphorylation (OXPHOS) inhibitor which is able to be used for the research of solid tumors [3].

IMM-H007 is a novel lipid-lowering agent, increasing abca1 protein expression

ZLN024 is an activator of AMPK allosteric. ZLN024 allosterically stimulates active AMPK heterotrimers and the inactive α1 subunit truncations α1 (1-394) and α1 (1-335) but not α1 (1-312).

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).

RSVA405 is an AMPK activator (EC50 = 1 μM), and is STAT3 inhibitor

PT-1 is an AMPKα1 activator that dose-dependently activates AMPK α1394, α1335, and α2398 and enhances AMPK phosphorylation.

SIRT1 Activator 1 (Compound 3), a marine-derived xyloallenoide A derivative from the Xylaria sp. mangrove fungus, exhibits angiogenic effects in zebrafish and protects human endothelial progenitor cells (hEPCs) from AngII-induced senescence. It achieves this by elevating SIRT1 expression and modulating the AMPK Akt signaling pathway [1].

AMPK-IN-1 is an activator of the AMP-activated protein kinase (AMPK) enzyme, targeting the α2β2γ1 isoform with an EC50 of 551 nM, and induces phosphorylation of eEF2 independent of the mTORC1 pathway.

KL1333 (NQO1 activator 1) enhances energy metabolism and mitochondrial dysfunction in MELAS fibroblasts. Elevated NAD+ levels trigger the activation of SIRT1 and AMPK, and subsequently activates PGC-1α. NQO1 activator 1 is an orally available NAD+ modulator. It reacts with NAD(P)H: NQO1 as a substrate, resulting in increases in intracellular NAD+ levels via NADH oxidation.

Demethyleneberberine chloride, a natural mitochondria-targeted antioxidant, mitigates colitis in mice and suppresses inflammatory responses by blocking the NF-κB pathway and modulating the equilibrium of Th cells. It is also recognized as an AMPK activator for investigating non-alcoholic fatty liver disease (NAFLD) [1] [2] [3].

Coumermycin A1, a JAK2 signal activator, inhibits DNA Gyrase, consequently impeding bacterial cell division.

HMS607P03 is an activator of SIRT1 which induces autophagic cell death via the AMPK-mTOR-ULK complex and induces mitophagy by the SIRT1-PINK1-Parkin pathway. HMS607P03 downregulates 14-3-3γ, catalase, profilin-1, and HSP90α.