activator

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

Thrombin Receptor Activator for Peptide 5 (TRAP-5), also known as Coagulation Factor II Receptor (1-5) or Proteinase Activated Receptor 1 (1-5), is utilized in coronary heart disease (CHD) research.

CD437 (AHPN) is a specifc Retinoic Acid Receptor γ (RARγ) agonist.

STIMA-1 (2-Vinylquinazolin-4-ol), an active compound, can restore the activity of p63. STIMA-1 can stimulate the proliferation and differentiation of keratinocytes.

Bioymifi (DR5 Activator) is an effective activator of the TRAIL receptor DR5, binding to the extracellular domain (ECD) of DR5 with a Kd of 1.2 μM. Bioymifi can serve as a novel mimetic of TNF-related apoptosis-induced ligand (TRAIL), inducing DR5 aggregation as a sole inducer, and stimulating cell apoptosis.

Apoptozole (Apoptosis Activator VII) inhibits the ATPase domain of Hsc70 and Hsp70, inducing apoptosis.

Wnt pathway activator 2, with an IC50 of 13 nM, is a potent Wnt activator.

ZINC40099027 is a specific adhesion plaque kinase (FAK) activator that promotes gastric mucosal repair in persistent aspirin-associated gastric injury through activation of adhesion plaque kinase, activates human adhesion plaque kinase by accelerating the enzyme activity of the structural domain of FAK kinase, activates cytosolic FAK, and promotes intestinal epithelial wound closure.

p53 Activator 7 is a highly potent and cell-permeable activator of the p53 mutation Y220C (MDM-2/p53), which induces apoptosis.

G6PD activator AG1 is a glucose-6-phosphate dehydrogenase (G6PD) agonist that promotes glucose-6-phosphate dehydrogenase (G6PD) oligomerization to a catalytically competent form. G6PD activator AG1 reduces oxidative stress in cells and zebrafish, reduces chloroquine or diamide-induced oxidative stress in human erythrocytes, and can be used to study glucose-6-phosphate dehydrogenase deficiency.

Nrf2 activator-3 is a potent Nrf2 activator with potential anti-inflammatory, antioxidant, and anti-tumor activities, suitable for studying neurological and immune-related diseases.

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.

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).

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

Thrombin Receptor Activator for Peptide is also called Coagulation Factor II Receptor (1-5) or Proteinase Activated Receptor 1 (1-5), used in the research of coronary heart disease (CHD).

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.

Nampt activator-2 is a NAMPT activator (EC50: 0.023 μM). Nampt activator-2 has an affinity for CYP2C9, 2D6, and 2C19 with affinity values of 0.060 μM, 0.41 μM, and 0.59 μM, respectively.Nampt activator-2 can be used in the study of atherosclerosis, obesity, type II diabetes, insulin resistance, and type I diabetes.

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.]

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.

Adenosine A1 receptor activator T62 is an allosteric enhancer of the adenosine A1 receptor, producing antinociception in animal models of acute pain and reducing hypersensitivity in models of inflammatory and nerve-injury pain[1][2][3].

CASP3 Activator 1541 is an activator of the proenzyme forms of caspase-3, and induces cell death.

NF-κΒ Activator 2 is a potent, orally active compound that efficiently activates NF-κB with an EC50 value of 1.58 μM. By enhancing NF-κB expression and activation, it induces SOD 2 synthesis, rendering it useful for amyotrophic lateral sclerosis (ALS) research [1].

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.

Nrf2 activator-9 (compound D-36) is an agent that mitigates oxidative stress by inhibiting the apoptosis of HUVEC cells induced by oxidized low-density lipoprotein (oxLDL) and high glucose (HG), also protecting vascular endothelial cells (VEC) from oxLDL and HG-induced injury, offering potential therapeutic benefits for atherosclerosis prevention and treatment [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].

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].

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

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

Nrf2-Activator-12G is a potent Nrf-2 activator.

KCa1.1 channel activator-2, a hybrid derivative of Quercetin, selectively stimulates the vascular KCa1.1 channels. This compound demonstrates significant myorelaxant activity.

Nampt activator-4, a positive allosteric modulator (N-PAM) of nicotinamide phosphoribosyltransferase (NAMPT), has an EC50 of 0.058 μM and can enhance nicotinamide adenine dinucleotide (NAD+) levels in cells [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.

NPR-C activator 1 (Compound 1) is a potent agonist (EC50 ~ 1 μM) of natriuretic peptide receptor C (NPR-C), which plays a crucial role in regulating vascular homeostasis, and demonstrates promising in vivo pharmacokinetic properties [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.

AMPK activator C2 is an AMPK allosteric activator.

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).

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.

Nrf2 Activator-7 (Compound 12b) effectively enhances the Nrf2 signaling pathway as a potent Nrf2 activator.

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

Nrf2 activator-5 is a potent activator of Nrf2 that attenuates H2O2-induced oxidative stress and LPS-stimulated inflammation in BV-2 microglia, exhibiting antioxidant and anti-inflammatory activity.

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].

PKM2 activator 3 is a highly potent compound that activates PKM2, with an AC 50 value of 90 nM. It exhibits excellent Caco-2 permeability, a low efflux ratio, and remarkable microsomal stability. PKM2 activator 3 is particularly valuable for anticancer research purposes [1]. (AC 50: the concentration at which 50% enzyme activation occurs.)

Glucokinase activator 1 is a liver-directed glucokinase activator [EC50: 34 nM].

SOS1 activator 1 is an activator of SOS1-mediated nucleotide exchange (Kd: 44 nM).SOS1 is a guanine nucleotide exchange factor that binds to Ras proteins and catalyzes the exchange of GDP for GTP on RAS, resulting in the exchange of GDP originally bound to Ras for GTP.