A 83-01 sodium (C09-1102-849)

A 83-01 sodium is a potent inhibitor of TGF-β type I receptor ALK5 kinase , ALK4 and ALK7 , with IC 50 s of 12 nM, 45 nM and 7.5 nM against the transcription induced by ALK5 , ALK4 and ALK7 , respectivelyIn VitroA 83-01 sodium is a potent inhibitor of TGF-β type I receptor ALK5 kinase, type I activin/nodal receptor ALK4 and type I nodal receptor ALK7, reduces the level of ALK-5-induced transcription with an IC 50 of 12 nM in Mv1Lu cells, also blocks the ALK4-TD and ALK7-TD induced transcription with IC 50 s of 45 nM and 7.5 nM in R4-2 cells, and weakly suppresses that induced by constitutively active ALK-6, ALK-2, ALK-3, and ALK-1. A 83-01 (0.03-10 μM) potently prevents the growth-inhibitory effects of TGF-β, and completely inhibits the effect at 3 μM. A 83-01 (1-10 μM) inhibits TGF-β-induced Smad activation in HaCaT cells. A 83-01 (1 μM) decreases cell motility, adhesion and invasion increased by TGF-β1 in HM-1 cells, but does not change cell proliferation. MCE has not independently confirmed the accuracy of these methods. They are for reference only.In VivoA 83-01 (50, 150 and 500 μg/mouse, i.p.) sodium significantly improves survival of the mice without body weight or neurobehavioral appearances. A 83-01 (0.5 mg/kg, i.p.) sodium shows a significantly strong antitumor effect in mice bearing M109 cells. MCE has not independently confirmed the accuracy of these methods. They are for reference only.Cell AssayHM-1 cells are seeded into a 96-well plate and are incubated for 18 hr . A 83-01 (1 μM) or vehicle are then added for 12 hr followed by the addition of TGF-β1 (1 ng/mL) or vehicle for 60 hr. The number of viable cells in each well is examined using the WST-1 assay. MCE has not independently confirmed the accuracy of these methods. They are for reference only.Animal administrationMice Female B6C3F1 mice used for the in vivo studies are maintained under specific pathogen-free conditions. To evaluate the effect of A 83-01 on the survival of mice bearing peritoneal dissemination, HM-1 cells (1×10 6 ) are injected into the abdominal cavity via the left flank of the mouse. Starting the next day, A 83-01 (150 μg/body) or vehicles ( PBS with 0.5% DMSO ) are injected into the abdominal cavity three times per week . Mice are euthanized before reaching the moribund state . aladdin has not independently confirmed the accuracy of these methods. They are for reference only.Form:SolidIC50& Target:ALK5 12 nM (IC 50 ) ALK4 45 nM (IC 50 ) ALK7 7.5 nM (IC 50 ). Molecular Formula: C25H19N5NaS Molecular Weight: 444.51