ampk activator 1

AMPK activator 1 is an AMPK activator(compound No.1-75, EC50: <0.1μM).

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].

CCR1/5/8 activator 1 is a cytoplasmic phospholipase A inhibitor with antifungal activity.

Potassium Channel Activator 1 can be used in studies about the treatment of disorders or conditions wherein the dopaminergic system is disrupted such as mood disorders ADHD, schizophrenia, and other psychotic states.

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).

1-ethyl-6-fluoro-4-oxo-7-[4-(3-phenylpropanoyl)piperazin-1-yl]-1,4-dihydroquinoline-3-carboxylic acid is a compound used as a molecular structural unit and is a SMURF1 inhibitor.

NAMPT Activator-1 (compound 1) is an effective and specific activator of niacinamide phosphotransferase (Compound 1) with a wide range of EC50 (3.3-3.7 μM). NAMPT activator-1 effectively protects cultured cells from FK866-mediated toxicity and is a potential neuroprotective compound.

AMPK activator 4 is a potent and selective AMPK activator that does not inhibit mitochondrial complex I. AMPK activator 4 selectively activates AMPK in muscle tissue and 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. 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 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].

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].

Nrf2 activator-1 is a potent activator of NF-E2-related factor 2 (Nrf2).Nrf2 activator-1 can be used to study COPD and other respiratory diseases including asthma, acute lung injury (ALI), acute respiratory distress syndrome (ARDS), and pulmonary fibrosis.

Caspase-3 activator 1 (compound 4b), a Ru(III) metal complex, effectively inhibits gastric tumor growth and metastasis by mediating caspase-3 cleavage. This cleavage enables Caspase-3 to process gasdermin E (GSDME), which results in the production of the GSDME-N terminus, leading to perforation of the gastric tumor cell membrane. Furthermore, compound 4b induces pyroptosis and subsequent immune responses. It can be incorporated with decitabine (DCT) into the 4b-DCT-Lip lipid delivery system [1].

AMPK-IN-1 is an activator of the AMP-activated protein kinase (AMPK) enzyme, specifically targeting the α2β2γ1 isoform with an EC50 of 551 nM. It 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].

KCNQ2/3 activator-1 is a Kv7.2/Kv7.3 (KCNQ2/3) potassium channel activator, details of which are from Compound A of Patent WO2021113757A1.

20S Proteasome activator 1 is a 20S proteasome activator with IC50 of 0.3 μM for trypsin-like sites, 0.7 μM for chymotrypsin-like sites and 1.8 μM for caspase sites. 20S Proteasome activator 1 prevents the accumulation of pathogenic alpha-synuclein A53T mutants through translation in the cellular system, thereby reducing the probability of disease occurrence. The 20S Proteasome activator 1 can be used to study neurodegenerative diseases.

EIF2α Activator 1 (Compound 40) is a chemical compound that activates the phosphorylation of eukaryotic initiation factor 2 alpha (eIF2α), enhancing the expression of downstream proteins ATF and CHOP. It demonstrates antiproliferative effects against K562 and PBMC cells, with IC50 values of 4.00 and 19.3 μM, respectively [1].

NPR-C activator 1 (Compound 1) is a potent activator of natriuretic peptide receptor C (NPR-C), a receptor involved in the regulation of vascular homeostasis. It acts as a potent agonist (EC50 ~ 1 μM) of C-type natriuretic peptide (CNP), showing promising in vivo pharmacokinetic properties [1].

Nav1.1 activator 1 is a highly potent activator of Nav1.1 with BBB penetration.

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].

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

AMPK activator

2-Piperidinecarboxamide, N-[4-(4-methoxyphenyl)-2-thiazolyl]-1-(phenylsulfonyl)- is a potent KCNQ1 channel activator that can be used in long QT syndrome (LQTS) studies.

PKR activator 1 is a potent activator of pyruvate kinase-R (PKR).

RyRs activator 1 is a potent activator of ranibulin receptors (RyRs).RyRs activator 1 has 100% larvicidal activity at 0.5 mg/L and 90% larvicidal activity at 0.01 mg/L.

GPR40 Activator 1 is a potent GPR40 activator for treatment of type 2 diabetes.

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.

MrgX1-Activator-1 is a MrgX1 receptor activator.

Nln activator 1 is a first-in-class activator of peptidomimetic neurolysin with enhanced brain penetration and stability.

Wnt pathway activator 1 is a potent Wnt activator with an IC50 of 28-29 nM. Wnt pathway activator 1 is a potent Wnt activator for the treatment of androgenetic alopecia (AGA).

EAAT2 activator 1 (3-[(2-Chloro-6-fluorobenzyl)thio]-6-pyridin-2-ylpyridazine) is a thiopyridazine derivative that has been found to increase EAAT2 protein levels in astrocytes.

KCa1.1 Channel Activator-1, a hybrid derivative of Quercetin, selectively stimulates the vascular KCa1.1 channels while also blocking CaV1.2 channels. Additionally, it demonstrates weak myorelaxant activity.

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.

TRPV1 Activator-1 (Compound 8), a capsaicin analog featuring a modified neck structure, specifically interacts with the T551 residue [1].

TFEB activator 1 (Curcumin analog compound C1) is an activator of transcription factor EB (TFEB) with promise for the prevention or treatment of Alzheimer's disease.

Nrf2/HO-1 activator 2 (compound 13m), a difluoro-substituted derivative, is a highly potent activator of Nrf2/HO-1. It exhibits substantial neuroprotective and antioxidant properties by activating the Nrf2/HO-1 pathway through phosphorylation of ERK1/2, JNK, or Akt in PC12 cells. This compound finds utility in the investigation of Parkinson's disease (PD) [1].

GLUT4 activator 1 is a potent glucose transporter type 4 (GLUT4) translocation activator (EC50: 0.14 μM).

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

SIK1 activator 1 can enhances the SIK1 phosphorylation and ameliorated the hyperglyceamia of type 2 diabetic mice. SIK1 activator 1 exhibited remarkable inhibitory activity on hepatic gluconeogenesis.

NR1H4 activator 1 is a potent and selective agonist of Famesoid X Receptor (FXR).

SERCA2a activator 1 is a sarco/endoplasmic reticulum Ca2+-dependent ATPase 2a activator. SERCA2a activator 1 decreases phospholamban inhibition and enhances the systolic and diastolic functions of the heart.

Gcase activator 1 (LTI-291) is a glucocerebrosidase (Gcase) activator.

Bax activator-1 (compound 106) is a Bax activator. It induces Bax-dependent tumor cell apoptosis[1].

Nrf2/HO-1 activator 1 (Compound 24) is a potent neuroprotective agent with significant antioxidant activities, specifically targeting Nrf2/HO-1. It is particularly useful in Parkinson's disease (PD) research, illustrating its potential in therapeutic applications [1].

PI3K/Akt/CREB Activator 1 is a potent, orally active compound that acts as an activator for the PI3K/Akt/CREB pathway. It enhances neuronal proliferation, induces differentiation of Neuro-2a cells into neuron-like morphology, and accelerates axon-dendrite polarization in primary hippocampal neurons by upregulating brain-derived neurotrophic factor. This compound is utilized in vascular dementia (VaD) research.

Glucokinase activator 1 is a liver-directed glucokinase activator (EC50: 34 nM).

AMPK activator 7 (compound I-3-24) is an AMPK activator (EC50: 8.8 nM). AMPK activator 7 can be used in studies involving AMPK disorders, particularly type 2 diabetes, hyperglycaemia, metabolic syndrome, obesity, hypercholesterolaemia and/or hypertension.

NF-κΒ activator 1 can activate the nf-kappa Β gene activator, EC50 of 0.9 microns. NF-κΒ is widely used in eukaryotic cells as a gene regulating cell proliferation and cell survival. NF-κΒ activator 1 induces superoxide dismutase (SOD) 2 1 mRNA expression.

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).