ampkα

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

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 activator

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

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 C2 is an AMPK allosteric 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 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-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 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 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 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 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-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 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.

Platycodin D may stimulate TNF-α synthesis or inhibit degradation of TNF-α mRNA. Platycodin D (10 30 μM) suppresses prostaglandin E2 production in rat peritoneal macrophages stimulated by the protein kinase C activator 12-O-tetradecanoyl phorbol 13-acetate (TPA). Platycodin D and D3 are useful as expectorant agents in the treatment of various airway diseases, they can increase mucin release from rat and hamster tracheal surface epithelial cell culture and also from intact rat trachea upon nebulization.

TMPA is a nuclear receptor Nur77 and LKB1 interaction antagonist.

IM-156 acetate, an activator of NADH dehydrogenase (IC50=2.2 μM) and AMP-activated protein kinase alpha (AMPKα), is an orally available and bioavailable inhibitor of mitochondrial oxidative phosphorylation (OxPhos).IM-156 acetate increases AMPKα activity and inhibits chlorhexadiene-induced peritoneal fibrosis and inhibit tumor growth in rats .

1. Epiberberine may be caused drug interactions based on CYP2D6 enzyme. 2. Epiberberine has anti-adipogenic effect is mediated by downregulation of the Raf MEK1 ERK1 2 and AMPKα Akt pathways during 3T3-L1 adipocyte differentiation. 3. Epiberberine, as the brightest FSA emitter among the alkaloids, can also serve as an efficient conformation probe for HTG DNA and discriminate the DNA G-quadruplex from the RNA counterpart.