| Description | Ethaselen (BBSKE) is an orally active, selective thioredoxin reductase (TrxR) inhibitor with IC 50 s of 0.5 and 0.35 µM for the wild-type human TrxR1 and rat TrxR1, respectively. Ethaselen specifically binds to the unique selenocysteine-cysteine redox pair in the C-terminal active site of Ethaselen (BBSKE) is an orally active, selective thioredoxin reductase (TrxR) inhibitor with IC 50 s of 0.5 and 0.35 µM for the wild-type human TrxR1 and rat TrxR1, respectively. Ethaselen specifically binds to the unique selenocysteine-cysteine redox pair in the C-terminal active site of mammalian TrxR1. Ethaselen, an organoselenium compound, is a potent antitumor candidate that exerts potent inhibition on non-small cell lung cancer (NSCLC) by targeting TrxRIn VitroEthaselen (2.5-10 µM; 12, 24 hours) suppresses A549 cell viability in a both concentration- and time-dependent manner. H1666, which has considerably lower TrxR1 expression level, is less susceptible to 24 h treatment with Ethaselen. Ethaselen inhibits the intracellular TrxR1 activity in a concentration- and time-dependent manner, with IC 50 values of 4.2 and 2 µM for 12- and 24-h treatments, respectively. Ethaselen (2.5-10 µM; 12, 24 hours) has no effect on the protein amounts of TrxR1 and Trx. The mRNA level of TrxR1 does not show significant alteration in Ethaselen-treated A549 cells. Ethaselen (2.5-50 µM; 1-24 hours) causes intracellular Trx oxidation in A549 cells. Ethaselen (5-10 µM; 12, 24 hours) causes a clear concentration-dependent increase in ROS levels in A549 cells. The inhibition constants for Ethaselen binding to free enzyme (K i ) and the enzyme-substrate complex (K is ) were determined to be 0.022 and 0.087 µM, respectively. Ethaselen also inhibits mammalian TrxR1 in a time-dependent manner possibly by forming a covalent Se-S bond with Cys497 of Trx. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Viability AssayCell Line: A549 cell Concentration: 2.5, 5, 7.5, 10 µM Incubation Time: 12, 24 hours Result: Suppressed A549 cell viability in a both concentration- and time-dependent manner.In VivoEthaselen\t(BBSKE; 36-108 mg/kg/day; PO; for 10 days) shows increased inhibition of tumor growth in a dose-independent manner. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Five-week-old female BALB/c nude mice with A549 cellDosage: 36, 72, 108 mg/kg Administration: PO; daily; for 10 days Result: Showed increased inhibition of tumor growth, and the inhibition levels increased with the dose. The TrxR activity levels of the high dose group (108 mg/kg) decreased more than the middle dose group (72 mg/kg) and low dose group (36 mg/kg).IC50& Target:TrxR... Read More | Inquire | Human PTHrP-(1-36) is a secretory form of PTHrP with anticalciuric effects. Human PTHrP-(1-36) enhances beta cell function and proliferation. Human PTHrP-(1-36) can be used in the research of humoral hypercalcemia of malignancy (HHM) and hyperparathyroidism.In VitroHuman PTHrP-(1-36) (EC 50 : 0.05 Human PTHrP-(1-36) is a secretory form of PTHrP with anticalciuric effects. Human PTHrP-(1-36) enhances beta cell function and proliferation. Human PTHrP-(1-36) can be used in the research of humoral hypercalcemia of malignancy (HHM) and hyperparathyroidism.In VitroHuman PTHrP-(1-36) (EC 50 : 0.05 nM) increases intracellular calcium in human epidermal keratinocytes. Human PTHrP-(1-36) (100 nM, 24 h) increases human β-cell proliferation. Human PTHrP-(1-36) (100 nM, 30 min) enhances insulin secretion in human islets. PTHrP-(1-36) (mouse, EC 50 : 1 nM) induces a rapid Ca 2+ response in UMR 106 cells. MCE has not independently confirmed the accuracy of these methods. They are for reference only.In VivoPTHrP-(1-36) (mouse, 160 µg/kg, s.c., for 5 days/week for 7, 30, or 90 days) enhances beta cell regeneration and increases beta cell mass in a mouse model of partial pancreatectomy. PTHrP-(1-36) (mouse, 100 µg/kg, s.c., every other day) reverses the observed decrease of Wisp1 expression in the diabetic mice. MCE has not independently confirmed the accuracy of these methods. They are for reference only.Form:Solid... Read More | Inquire | Inquire |