AMPK Activator

CRBNL-Biguanide PROTAC 1 is a Biguanide-PROTAC that recruits Cereblon and an AMPK activator, composed of CRBNL, a hydrophobic linker, and a PEB-Biguanide moiety. The degradation mechanism of CRBNL-Biguanide PROTAC 1 is hypothesized to involve PEB-Biguanide promoting mitochondrial enrichment and activating AMPK, while simultaneously recruiting Cereblon to bring it into proximity with mitochondrial proteins, thereby reducing COXII and NDUFB8 protein levels and perturbing mitochondrial oxidative phosphorylation. CRBNL-Biguanide PROTAC 1 is useful for pancreatic cancer and mitochondrial protein regulation research.

OSU-53 is an orally active AMPK activator and mTOR inhibitor, with an IC₅₀ of 0.3 μM for AMPK, an EC₅₀ of 2-5 μM for AMPK, and an IC₅₀ of 8.23 μM for mTOR. OSU-53 inhibits the Akt signaling pathway, directly activates AMPK by binding to its autoinhibitory domain, reduces IKKβ-mediated phosphorylation of Foxo3a, blocks Akt-mediated phosphorylation of MDM2, and promotes the nuclear localization and stabilization of Foxo3a, while directly inhibiting mTOR. OSU-53 inhibits epithelial-mesenchymal transition (EMT), induces epithelial phenotype, suppresses invasion and metastasis, induces autophagy, inhibits the activation of ERK and Akt, reduces the secretion of nitric oxide and proinflammatory cytokines, and inhibits the migration of MDSC; at high doses, it induces MDSC apoptosis, attenuates the immunosuppressive effect of MDSC, reduces MDSC levels, and blocks incision-induced mechanical hyperalgesia. OSU-53 can be used in studies related to breast cancer, prostate cancer, thyroid cancer, melanoma and postoperative pain.

Xanthosine dihydrate is a nucleoside derived from xanthine and ribose. Xanthosine dihydrate activates the AMPK/FoxO1/AKT/GSK3β signaling cascade. Xanthosine dihydrate promotes cell proliferation and regulates blood glucose metabolism. Xanthosine dihydrate increases milk production in cows and goats. Xanthosine dihydrate is used in mammary stem cell and type 2 diabetes research.

Platycodin D (Standard) is the analytical standard of Platycodin D. This product is intended for research and analytical applications. Platycodin D is a saponin isolated from Platycodon grandiflorus, acts as an activator of AMPKα, with anti-obesity property. WNT/β-catenin pathway mediates the anti-adipogenic effect of platycodin D.

Nandinine is an orally active derivative of Berberine (HY-N0716). Nandinine enhances AMPK activity, inhibits the activation of IKKβ/NF-κB, and regulates the phosphorylation of IRS-1. Nandinine reverses the abnormal production of adipokines, promotes insulin-mediated glucose uptake, and alleviates insulin resistance. Nandinine improves glucose tolerance and increases the insulin sensitivity index in mice. Nandinine can be used in studies related to insulin resistance.

Karanjin (Standard) is the analytical standard of Karanjin. This product is intended for research and analytical applications. Karanjin is an orally active furanoflavonoid which can be isolated from several Leguminosae. Karanjin exhibits evident anti-diabetic, anti-cancer, anti-inflammatory, antioxidant, anticolitis, anti-ulcer, anti-Alzheimer properties and multiple insect repellent/insecticidal, acaricide properties, suggesting the potential of Karanjin to be applied to relevant research.

D-Arabitol-¹³C-2 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.

Candidusin A (CHNQD-0803) (Compound 4) is a AMPK activator with a K_D of 47.28 nM. Candidusin A can be isolated from marine fungus Aspergillus candidus. Candidusin A has cytotoxic activity and induces apoptosis in human prostate cancer cells (22Rv1, PC-3 and LNCaP cells). Candidusin A reduces adipogenesis genes expression and fat deposition, negatively regulates the NF-κB-TNFα inflammatory axis to suppress inflammation, and ameliorates liver injury and fibrosis. Candidusin A can be used for non-alcoholic steatohepatitis (NASH) research.

AMPK activator 10 is an orally active, potent AMPK activator with EC₁₅₀ of 44.3 nM by cell-ELISA. AMPK activator 10 increases the phosphorylation levels of ACC. AMPK activator 10 exhibits a glucose lowering effect.

JJO-1 is an AMPK activator with an EC₅₀ of 1.8 μM. JJO-1 can be used in the study of obesity and type 2 diabetes.

Metformin (1,1-Dimethylbiguanide) glycinate inhibits the mitochondrial respiratory chain in the liver, leading to AMPK activation and enhancing insulin sensitivity, and can be used in the study of type 2 diabetes. Metformin glycinate exerts central glucose-lowering effects by inhibiting Ras-related protein 1 (Rap1) in SF1 hypothalamic neurons. Metformin glycinate also inhibits liver oxidative stress, nitrosative stress, inflammation, and apoptosis caused by liver ischemia/reperfusion injury. In addition, Metformin glycinate regulates the expression of autophagy-related proteins by activating AMPK and inhibiting the mTOR signaling pathway, thereby inducing tumor cell autophagy and inhibiting the growth of renal cell carcinoma in vitro and in vivo.

Jervine (Standard) (11-Ketocyclopamine (Standard)) is the analytical standard of Jervine (HY-N0836). This product is intended for research and analytical applications. Jervine (11-Ketocyclopamine) is an orally active steroidal alkaloid and Hedgehog signaling pathway inhibitor. Jervine can be isolated from Veratrum californicum. Jervine regulates Wnt, inhibits the AKT/mTOR signaling pathway, and activates the AMPK signaling pathway. Jervine induces DNA damage, Apoptosis, Autophagy, ROS production and Mitochondrial damage. Jervine exhibits anti-cancer and anti-inflammatory activities. Jervine reduces tumor growth rate and weight in xenograft models. Jervine can be used in studies related to triple-negative breast cancer, nasopharyngeal carcinoma and non-small cell lung cancer.

Setmelanotide TFA (RM-493 TFA) is a blood-brain barrier-permeable, selective MC4R agonist with a K_i value of 2.1 nM for hMC4R. Setmelanotide TFA activates the CaMKK2/AMPK signaling pathway. Setmelanotide TFA mediates body weight homeostasis, feeding regulation and energy expenditure modulation; it reduces food intake, induces weight loss, decreases obesity severity, increases daytime activity and energy expenditure, lowers levels of leptin, triglycerides, fasting insulin and diastolic blood pressure, improves insulin sensitivity, glucose tolerance and fatty liver condition, and reverses respiratory depression. Setmelanotide TFA is applicable to research related to obesity, hyperinsulinemia, fatty liver and respiratory depression.

D-Arabinopyranose-¹³C₅ is the ¹³C-labeled D-Arabinopyranose (HY-N7082). D-Arabinpyranose is is an orally active antidepressant and a growth inhibitor of C. elegans (IC₅₀ is 7.5 mM). D-Arabinpyranose can penetrate the blood-brain barrier, selectively interfere with the metabolism of D-ribose and D-fructose, and inhibit the growth of nematodes. D-Arabinpyranose can also inhibit the synthesis of cell biofilm and exert antibacterial activity. D-Arabinpyranose activates the ACSS2-PPARγ/TFEB-CRTC1 axis through the lysosomal AXIN-LKB1-AMPK pathway, inducing CRTC1 transcription, exerts antidepressant-like activity. D-Arabinpyranose is the ring-opened form of the aldopentose D-Arabinpyranose (HY-N7082).

AP39 prodrug 1 (Compound M1) is a mitochondria-targeted H2S prodrug. AP39 prodrug 1 induces ROS-dependent mild mitochondrial uncoupling, activating mitochondria-associated AMPK to suppress Palmitic acid (PA) (HY-N0830)-induced lipid deposition in hepatocytes.

PI3Kα-IN-28 (Compound 23) is an efficient dual targeted PI3K/BRD4 inhibitor. PI3Kα-IN-28 can inhibit the proliferation of various cells, such as KYSE180 and KYSE450 cells. PI3Kα-IN-28 can concentration dependently inhibit migration and colony formation, induce G0/G1 phase arrest, significantly inhibit DNA synthesis, and significantly increase the proportion of senescent cells. PI3Kα-IN-28 can inhibit the expression of p-AKT and c-Myc and activate the AMPK-p27 pathway. PI3Kα-IN-28 can be used for research on cancers such as esophageal cancer.

CB1R/AMPK modulator 1 (Compound 38-S) is an orally active CB1R/AMPK modulator, with an K_i of 0.81 nM and an IC₅₀ of 3.9 nM for CB1R. CB1R/AMPK modulator 1 activates AMPK. CB1R/AMPK modulator 1 reduces food intake and body weight, and improves glucose tolerance and insulin sensitivity.

DBI-2 is an AMPK activator targeting mitochondrial complex I. DBI-2 disrupts the OXPHOS process, and reduces ATP generation in mitochondria. DBI-2 inhibits the proliferation of colorectal cancer (CRC) cells.

PPM-18 (NSC 73233) is a Vitamin K (HY-B2172) analog. PPM-18 prevents LPS-induced IκBα degradation, thereby inhibiting NF-κB activation and nuclear translocation of NF-κB. PPM-18 inhibits LPS-induced nitrite production and iNOS expression. PPM-18 inhibits HDAC6. PPM-18 induces ROS accumulation, activates AMPK, inhibits the mTORC1 and PI3K/AKT pathways, initiates Autophagy, and induces Apoptosis. PPM-18 suppresses seizures in zebrafish and mouse epilepsy models. PPM-18 prevents LPS-induced lethal toxicity and delayed hypotension. PPM-18 exhibits anticancer activity against leukemia and bladder cancer. PPM-18 can be used in research related to septic shock, bladder cancer and atherosclerosis.

BI-9774 is a potent, selective, and orally active AMPK activator, with EC₅₀ values of 20.0 nM and 63.1 nM against human AMPK α1β1γ1 and AMPK α1β2γ1, respectively. BI-9774 binds to the allosteric drug and metabolite (ADaM) site and induces ACC Ser79 phosphorylation in HepG2 cells, with an EC₅₀ of 83.2 nM. BI-9774 can be used in studies related to AMPK signaling, multiple sclerosis, and non-alcoholic fatty liver disease.