A 83-01 sodium

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 , respectively

In Vitro

A 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 Vivo

A 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 Assay

HM-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 administration

Mice 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:Solid

IC50& Target:ALK5 12 nM (IC 50 ) ALK4 45 nM (IC 50 ) ALK7 7.5 nM (IC 50 )