Estradiol 17-(β-D-Glucuronide) sodium, a metabolite of estrogen, is well known to cause intrahepatic cholestasis in humans[1].
CC260 is a selective PI5P4Kα and PI5P4Kβ inhibitor with Kis of 40 nM and 30 nM, respectively. CC260 does not inhibit or weakly inhibits other protein kinases, such as Plk1 and RSK2. CC260 can be used for cell energy metabolism, diabetes and cancer research[1].
Propionylglycine is a peptide[1].
Trigonelline chloride, an alkaloid with potential antidiabetic activity, is present in considerable amounts in coffee.
Deoxynivalenol, a mycotoxin of the trichothecenes family, crosses the intestinal mucosa by a paracellular pathway through the tight junctions. The Deoxynivalenol transport is not affected by P-glycoprotein (PgP) or multidrug resistance-associated proteins (MRPs) inhibitors[1].
Picilorex is an active compound. Picilorex can be used for the research of anorectic[1].
Brassinazole (0.5, 1, 5 μM) causes markedly deformed seedlings, whose morphology is similar to that of BR-deficient mutants. Brassinazole causes cress dwarfism, altering leaf morphology such as the typical downward curl and dark green appearance of Arabidopsis BR-deficient mutants. However, administration of 10 nM BR reversed dwarfism[1].
UU-T02 is a novel potent, selective small-molecule inhibitor of β-catenin/Tcf4 interaction with Ki of 1.36 uM; displays 63-fold and 175-fold selectivity over β-catenin/E-cadherin and β-catenin/APC interactions, respectively.
Pumosetrag Hydrochloride (MKC-733; DDP-733) is an orally available 5-HT3 partial agonist developed for the treatment of irritable bowel syndrome and gastroesophageal reflux disease.
TIM-063 (TIM063) is a potent, selective, ATP-competitive CaMKK inhibitor with Ki of 0.35/0.2 uM for CaMKKα and CaMKKβ, respectively.TIM-063 directly targets the catalytic domain of CaMKK, similar to STO-609.TIM-063 suppressed the ionomycin-induced phosphorylation of exogenously expressed CaMKI, CaMKIV, and endogenous AMPKα in HeLa cells with an IC50 of 0.3 uM.TIM-063 suppressed CaMKK isoform-mediated CaMKIV phosphorylation in transfected COS-7 cells.TIM-063 displayed cell permeability and the ability to inhibit CaMKK activity in cells. TIM-063 is a useful chemical probe for the precise analysis of CaMKK-mediated signaling pathways.
Deoxycalyciphylline B is a hepatotoxic alkaloid that can be isolated from Daphniphyllum calycinum[1].
3-Phosphoglyceric acid barium is a metabolic intermediate in both glycolysis and the Calvin cycle. 3-Phosphoglyceric acid barium is involved in alveolar macrophage epigenetic regulation[1].
Adenosylhomocysteinase (SAHH; AHCY) is a highly conserved enzyme. Adenosylhomocysteinase reversible catalyzes S-adenosylhomocysteine (SAH) to adenosine and L-homocysteine. The serum exosomal Adenosylhomocysteinase level can be used as a prognostic biomarker in HBV-LC patients[1][2].
PF-04991532 is a potent, hepatoselective glucokinase activator with EC50s of 80 and 100 nM in human and rat, respectively.
Gastrin I (1-14), human is 1-14 fragment of human gastrin I peptide. Gastrin I is an endogenous, gastrointestinal peptide hormone. Gastrin is the major hormonal regulator of gastric acid secretion[1].
GSK0660 is a potent antagonist of PPARβ and PPARδ, with IC50s of 155 nM for both isoforms.
(rel)-Atorvastatin, a relative configuration of Atorvastatin. Atorvastatin is an orally active HMG-CoA reductase inhibitor, has the ability to effectively decrease blood lipids. Atorvastatin inhibits human SV-SMC proliferation and invasion with IC50s of 0.39 μM and 2.39 μM, respectively[1][2][3].
(Glu17,21,24)-Osteocalcin (1-49) (human) is a bone-specific protein involved in bone formation and glucose metabolism[1].
D-Mannoheptulose is a major non-structural carbohydrate in avocado. D-mannoheptulose is a specific inhibitor of D-glucose phosphorylation. D-Mannoheptulose can block insulin release and utilization of carbohydrate in rat[1][2][3].
Picroside IV is an iridoid glycoside found in the underground parts of Picrorhiza scrophulariiflora. Picroside IV is a derivative of Catalpol (HY-N0820)[1]. Catalpol has neuroprotective, hypoglycemic, anti-inflammatory, anti-cancer, anti-spasmodic, anti-oxidant effects and anti-HBV effects[2].
S6K-18 is a potent and selective p70S6K1 inhibitor with an IC50 of 52 nM[1].
PF-04620110 is an orally active, selective and potent diglyceride acyltransferase-1 (DGAT1) inhibitor with IC50 of 19 nM.IC50 value: 19 nM [1]Target: DGAT1PF-04620110 and imipramine (internal standard) were separated using a Hypersil Gold C18 column, with a mixture of acetonitrile and 10 mm ammonium formate (90:10, v/v) as the mobile phase. The ion transitions monitored in positive-ion mode [M + H](+) of multiple-reaction monitoring were m/z 397.0 -260.2 for PF-04620110 and m/z 280.8 - 86.0 for imipramine. The detector response was specific and linear for PF-04620110 at concentrations within the range 0.05-50 μg/mL and the signal-to-noise ratios for the samples were ≥10 [2].
Solnatide (AP 301) is an inhaled synthetic peptide agent composed of 17 natural amino acids. Solnatide can directly activate the epithelial sodium channel. Solnatide can be used for the research of lung function[1][2].
Tauro-β-muricholic acid (TβMCA) is a trihydroxylated bile acid. Tauro-β-muricholic acid is a competitive and reversible FXR antagonist (IC50 = 40 μM). Tauro-β-muricholic acid has antiapoptotic effect. Tauro-β-muricholic acid inhibits bile acid-induced hepatocellular apoptosis by maintaining the mitochondrial membrane potential[1][2].
Cholesterol glucuronide is an endogenous metabolite of lipid generated in the liver by UDP glucuonyltransferase[1][2].
Sergliflozin etabonate (GW-869682X) is a potent and orally active sodium glucose cotransporter (SGLT2) inhibitor. Sergliflozin etabonate shows antidiabetic and antihyperglycemic effects. Sergliflozin etabonate significantly reduces non-fasting blood glucose levels in diabetic mice. Sergliflozin etabonate has the potential for the research of diabetes[1].
HIF-2α-IN-7 is a hypoxia inducible factor 2α (HIF-2α) inhibitor. HIF-2α-IN-7 can inhibit HIF-2α with an EC50 value of 6nM. HIF-2α-IN-7 can be used for the research of various types of diseases including cancer, liver disease, inflammatory disease, pulmonary diseases and iron load disorders[1].
SPT-IN-1 (compound 1) is an orally active and potent SPT (serine palmitoyl transferase) inhibitor, with an IC50 of 5.19 nM for hSPT1. SPT-IN-1 can be used for type 2 diabetes and dyslipidemia research[1].
Thyminose-d2 is the deuterium labeled Thyminose. Thyminose is an endogenous metabolite[1].
Isoacteoside is a natural compound which exhibit significant inhibition of advanced glycation end product formation with IC50 values of 4.6-25.7 μM, compared with those of aminoguanidine (IC50=1,056 μM) and quercetin (IC50=28.4 μM) as positive controls.IC50 value:Target:In the rat lens aldose reductase assay, acteoside, isoacteoside, and poliumoside exhibited greater inhibitory effects on rat lens aldose reductase with IC50 values of 0.83, 0.83, and 0.85 μM, respectively, than those of the positive controls, 3,3-tetramethyleneglutaric acid (IC50=4.03 μM) and quercetin (IC50=7.2 μM).