AMPK Activator

Triadimefon (Standard) is the analytical standard of Triadimefon (HY-123037). This product is intended for research and analytical applications. Triadimefon is an orally active fungicide. Triadimefon significantly reduces the phosphorylation of AKT1 and ERK1/2. Triadimefon significantly increases pAMPK levels, but does not affect total AMPK levels. Triadimefon inhibits the growth of Saccharomyces cerevisiae, disrupts hormone homeostasis (affecting the synthesis of testosterone, etc.), inhibits fetal adrenal development in rats, induces metabolic shifts in hepatocytes, and impairs spatial learning and memory.

Buformin (1-Butylbiguanide), a potent AMPK activator, acts as an orally active biguanide antidiabetic agent. Buformin decreases hepatic gluconeogenesis and lowers blood glucose production in vivo. Buformin also has anti-cancer activities and is applied in cancer study (such as, cervical cancer and breast cancer, et al).

IQZ23 inhibits adipocyte differentiation via AMPK pathway activation. IQZ23 exerts a high efficacy in decreasing the triglyceride level (EC₅₀=0.033 μM) in 3T3-L1 adipocytes. IQZ23 could be used for the research of obesity and related metabolic disorders.

PDIC-DPC is a HMGA1 inhibitor and lung-targeting agent. PDIC-DPC upregulates STING expression and enhances STING-mediated immune signaling. PDIC-DPC inhibits the TGFβ-Smad pathway and activates AMPK. PDIC-DPC forms nanocomplexes with fibrinogen β chain and vitronectin, and achieves lung-specific accumulation by binding to pulmonary endothelial receptors. PDIC-DPC reverses established pulmonary fibrosis, reduces collagen deposition, restores alveolar structure, improves pulmonary function, and inhibits in situ ESCC growth. PDIC-DPC can be used for the research of esophageal squamous cell carcinoma and idiopathic pulmonary fibrosis.

Mito-Esculetin (Mito-Esc) is an orally active mitochondria-targeted derivative of Esculetin (HY-N0284). Mito-Esculetin inhibits LPS-induced phosphorylation of STAT3 Tyr-705, partially reverses LPS-mediated depletion of SIRT3, and enhances the AMPK-SIRT1 signaling axis. Mito-Esculetin inhibits PAI-1 activity, regulates miRNA, and induces phosphorylation of IRS and AKT. Mito-Esculetin suppresses oxidant-induced endothelial dysfunction, Ang-II (HY-13948)- and high glucose-induced atherosclerotic plaque formation, Palmitate (HY-N0830)-induced insulin resistance, as well as high glucose-mediated endothelial cell senescence and inflammatory responses. Mito-Esculetin reduces body weight and non-esterified fatty acid (NEFA) levels. Mito-Esculetin can be used in research related to acute coronary syndrome, type 2 diabetes, and hyperglycemia-induced atherosclerosis.

Buformin-d₉ (hydrochloride) is the deuterium labeled Buformin. Buformin (1-Butylbiguanide), a potent AMPK activator, acts as an orally active biguanide antidiabetic agent. Buformin decreases hepatic gluconeogenesis and lowers blood glucose production in vivo. Buformin also has anti-cancer activities and is applied in cancer study (such as, cervical cancer and breast cancer, et al).

AMPK/mTOR modulator-1, Ginsenoside derivative, is an orally active mTOR inhibitor and AMPK activator. AMPK/mTOR modulator-1 activates AMPK signaling with a K_d of 4.759 μM. AMPK/mTOR modulator-1 promotes M1-like tumor-associated macrophage polarization while suppressing M2-like polarization. AMPK/mTOR modulator-1 can enhance glycolysis. AMPK/mTOR modulator-1 significantly inhibits tumor progression and shows anti-inflammation activity. AMPK/mTOR modulator-1 can be used for the research of colorectal cancer.

FuBIG is an iminoguanidine derivative with neuroprotective effects. FuBIGL inhibits L-LDH activation and reduces lactate production. FuBIGL exerts protective effects on inflammatory nerve cells, upregulates the expressions of AMPK, pAMPK and FOXO3, and activates the AMPK pathway in cells. FuBIG exerts anti-inflammatory effects by reducing pro-inflammatory cytokines (IL-6, IL-1β, TNF-α) and increasing the anti-inflammatory cytokine IL-10. FuBIG maintains mitochondrial membrane potential, alleviates mitochondrial dysfunction, reduces ROS production, and relieves oxidative stress. FuBIG upregulates Bcl-2, downregulates Bax and Caspase-3, and inhibits cell apoptosis (apoptosis). FuBIG improves metabolic disorders in diabetic mice, decreases the levels of LDL-C, ALT and AST, and increases HDL-C level simultaneously. FuBIG can be used in the research of diabetic neuroinflammation.

AMPKα1 activator 1 is a selective and orally active AMPKα1 activator with an EC₅₀ of 35.1 nM. AMPKα1 activator 1 shows 176-fold selectivity over AMPKα2. AMPKα1 activator 1 can be used as a cell protectant and a kidney protectant. AMPKα1 activator 1 attenuates elevation of serum creatinine and blood urea nitrogen levels, alleviates kidney damage, and reduces cellular infiltration in renal ischemia-reperfusion injury contexts. AMPKα1 activator 1 can be associated with renal ischemia-reperfusion injury research.

AMPK activator 9 (ZM-6) is a potent AMPK (α2β1γ1) activator with an EC₅₀ value of 1.1 µM. AMPK activator 9 has the potential for the research of type 2 diabetes.

Phenformin-d₅ (Phenethylbiguanide-d₅) hydrochloride is the deuterium labeled Phenformin hydrochloride. Phenformin hydrochloride is an orally active biguanide hypoglycemic agent. Phenformin hydrochloride inhibits mitochondrial respiratory chain complex I, leading to an increased AMP/ATP ratio, activation of AMPK, and subsequent inhibition of the mTOR pathway, thereby suppressing cell proliferation, inducing apoptosis and autophagy. Phenformin hydrochloride inhibits cancer stem cells (CSCs) and possesses potent antitumor potential.

Amarogentin (Standard) is the analytical standard of Amarogentin. This product is intended for research and analytical applications. Amarogentin is a secoiridoid glycoside that is mainly extracted from Swertia and Gentiana roots. Amarogentin exhibits many biological effects, including anti-oxidative, anti-tumour, and anti-diabetic activities. Amarogentin exerts hepatoprotective and immunomodulatory effects. Amarogentin promotes apoptosis, arrests G2/M cell cycle and downregulates of PI3K/Akt/mTOR signalling pathways. Amarogentin exerts beneficial vasculo-metabolic effect by activating AMPK.

AMPK activator 8 (compound 2) is an AMP-activated protein kinase (AMPK) activator with EC₅₀s of 11, 27, 4, 2, and 4 nM for rAMPK α1β1γ1, rAMPK α2β1γ1, rAMPK α1β2γ1, rAMPK α2β2γ1, rAMPK α2β2γ3, respectively. AMPK activator 8 can be used for the research of type 2 diabetes.

WMJ-J-09 is an HDAC inhibitor with IC₅₀ values of 7.5 nM (HDAC1), 21.3 nM (HDAC2), 18.4 nM (HDAC3), 90.9 nM (HDAC8), 3.9 nM (HDAC6) and 8715.7 nM (HDAC4). WMJ-J-09 blocks the cell cycle and induces apoptosis in cancer cells. WMJ-J-09 induces cancer cell death through the LKB1-AMPK-p38MAPK-p63-survivin signaling cascade.WMJ-J-09 inhibits HDAC enzyme activity, leading to acetylation of key proteins and thereby regulating cancer cell death. WMJ-J-09 can be used in HCT116 cells and FaDu cells research^[1][2].

AICAR-¹³C₂,¹⁵N (Acadesine-¹³C₂,¹⁵N; AICA Riboside-¹³C₂,¹⁵N) is the ¹³C and ¹⁵N labeled AICAR (HY-13417). AICAR (Acadesine) is an adenosine analog and a AMPK activator. AICAR regulates the glucose and lipid metabolism, and inhibits proinflammatory cytokines and iNOS production. AICAR is also an autophagy, YAP and mitophagy inhibitor.

D-Arabitol-¹³C-1 is the ¹³C labeled D-Arabitol. D-Arabitol is an orally active D-enantiomer of arabitol. D-Arabitol modulates the composition of gut microbiota, increases short-chain fatty acids, and promotes AMPK-PGC-1α-related browning of white adipose tissue. D-Arabitol improves weight gain, fat accumulation, insulin resistance, lipid deposition and inflammatory responses. D-Arabitol serves as the sole carbon/energy source for Bacillus methanolicus MGA3, a strain that can co-utilize it with mannitol. D-Arabitol is applicable to obesity-related research.

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

LW1564 is an inhibitor for HIF-1α with an IC₅₀ of 1.2 µM in HepG2. LW1564 inhibits mitochondrial respiration, reduces ATP production, stimulates HIF-1α degradation, and inhibits proliferation of various cancer cells with GI₅₀ of 0.4-4.6 μM. LW1564 activates AMPK signaling pathway and inhibits lipid synthesis. LW1564 exhibits antitumor in HepG2 xenograft mouse model.

Avicin D is a plant triterpenoid. Avicin D induces Autophagy by activation of AMPK. Avicin D inhibits mTOR and S6 kinase activity. Avicin D selectively induces Apoptosis and downregulates p-STAT-3, bcl-2, and Survivin. Avicin D has properties of being a selective Glucocorticoid receptor modulator. Avicin D inhibits NF-κB activation. Avicin D shows anti-tumor effects against cutaneous T-cell lymphomas.

D-Arabitol-¹³C is the ¹³C labeled D-Arabitol. D-Arabitol is an orally active D-enantiomer of arabitol. D-Arabitol modulates the composition of gut microbiota, increases short-chain fatty acids, and promotes AMPK-PGC-1α-related browning of white adipose tissue. D-Arabitol improves weight gain, fat accumulation, insulin resistance, lipid deposition and inflammatory responses. D-Arabitol serves as the sole carbon/energy source for Bacillus methanolicus MGA3, a strain that can co-utilize it with mannitol. D-Arabitol is applicable to obesity-related research.