ALK5 Inhibitor IV 是TGF-βI 型受体ALK5，ALK4和ALK7的抑制剂，能够抑制ALK5，ALK4和ALK7诱导的转录，它们的IC50值分别为 12 nM，45 nM 和 7.5 nM。

A 83-01 is a selective inhibitor of TGF-β type I receptor ALK5 kinase, type I activin/nodal receptor ALK4 and type I nodal receptor ALK7 with IC50 values of 12 nM, 45 nM and 7.5 nM, respectively.

A-83-01 (4?μM) treatment increases myotube formation, the expression of MyHC and the expression of Myf5 and MyoD in C2C12 cells[1]. Expression of pSmad3 is increased by the addition of TGF-β1, and the effects of TGF-β1 are inhibited in ovarian cancer cells by A-83-01. TGF-β1 increases cell motility, adhesion and invasion, while A-83-01 decreases these behaviors in HM-1 cells[2]. A-83-01 treatment significantly increases these parameters within 24 h that is positively related to pericyte coverage and tumor cell proliferation. Apparent diffusion coefficient (ADC) determined by diffusion-weighed imaging is decreased by A-83-01 treatment, suggesting the decrease of tumor interstitial fluid pressure[3].

A-83-01 (50, 150 and 500 μg/mouse, i.p.) significantly improves survival of the mice without body weight or neurobehavioral appearances[2]. A-83-01 (0.5 mg/kg, i.p.) shows a significantly stronger antitumor effect in mice bearing M109 cells[4].

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 following the manufacturer's instructions.

909910-43-6

C25H19N5S

421.52

ALK5 Inhibitor IV

DMSO:>10 mM
Powder: -20°C for 3 years
In solvent: -80°C for 2 years