ampkα

TMPA is a nuclear receptor Nur77 and LKB1 interaction antagonist.

AMPK activator 4 is a potent and selective AMPK activator that does not inhibit mitochondrial complex I. It selectively activates AMPK in muscle tissue, dose-dependently improves glucose tolerance in normal mice, significantly reduces fasting glucose levels, and improves insulin resistance in db/db diabetic mice. [AMPK activator 4 has hypoglycemic effects.]

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

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.

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.

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).

AMPK activator17 (Compound 10g) is an orally bioavailable AMPK activator. It significantly inhibits lipogenesis (IC50: 3.4 μM) and improves dyslipidemia. By activating the AMPK pathway, AMPK activator17 suppresses early adipocyte differentiation (mitotic clonal expansion) and enhances mitochondrial function and fatty acid oxidation in mature adipocytes. It improves dyslipidemia through promoting cholesterol reverse transport. AMPK activator17 is applicable in research on obesity and associated metabolic disorders, such as type 2 diabetes and cardiovascular diseases.

AMPK activator

AMPK activator 2 is a chloroformin derivative with potential anticancer activity, which can up-regulate AMPK signaling pathway and down-regulate mTOR/4EBP1/p70S6K, and inhibit proliferation and migration of human cancer cell lines (UMUC3, T24, A549).

AMPK activator 2 hydrochloride is a fluoroguanidine-containing derivative that up-regulates the AMPK signaling pathway and down-regulates mTOR/4EBP1/p70S6K.AMPK activator 2 hydrochloride inhibits the proliferation and migration of human cancer cell lines (UMUC3, T24, A549).

AMPK activator 6 (Compound GC) activates the AMPK pathway and reduces lipid content in HepG2 and 3T3-L1 cells. It significantly suppresses increases in total cholesterol (TC), low-density lipoprotein-C (LDL-C), triglyceride (TG), and other biochemical indices in blood serum, holding research value in non-alcoholic fatty liver disease (NAFLD) and metabolic syndrome.

AMPK-IN-3 is a novel, selective and potent AMPK inhibitor with inhibitory effects on AMPK (α2), AMPK (α1) and KDR, with IC50 values of 60.7, 107 and 3820 nM, respectively.AMPK-IN-3 showed anticancer activity in K562 cells.

AMPK activator 7 (compound I-3-24) is an AMPK activator with an EC50 of 8.8 nM, useful in studies involving AMPK disorders such as type 2 diabetes, hyperglycaemia, metabolic syndrome, obesity, hypercholesterolaemia, and hypertension.

AMPK activator 8 (Compound 2) is an AMP-activated protein kinase (AMPK) activator that acts on rAMPK α1β1γ1 (EC50: 11 nM), rAMPK α2β1γ1 (EC50: 27 nM), rAMPK α1β2γ1 (EC50: 4 nM), rAMPK α2β2 AMPK activator 8 can be used to study type 2 diabetes.

AMPK Activator 9 (ZM-6), a potent activator of AMPK (α2β1γ1), demonstrates an EC50 of 1.1 µM, indicating its strong efficacy in activating AMPK. This compound holds promise for type 2 diabetes research, highlighting its potential application in understanding and possibly treating this condition.

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.

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].

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. This compound activates AMPK and has been shown to decrease food intake and body weight, in addition to enhancing glucose tolerance and insulin sensitivity [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 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-IN-5 (compound 7m) is a derivative of osthole that inhibits MAPK signaling by blocking the phosphorylation of JNK and p38, thereby suppressing the release of inflammatory cytokines. AMPK-IN-5 can reduce ulcerative colitis induced by dextran sulfate sodium and acute lung injury induced by LPS.

SC4 is a potent, direct AMPK activator. SC4 preferentially activates α2 complexes and stimulates skeletal muscle glucose uptake.