Home TGF-beta/Smad TGF-beta/Smad inhibitor A-83-01 For research use only.

A-83-01

A-83-01 is a potent inhibitor of TGF-β type I receptor (ALK5-TD) with IC50 of 12 nM. A-83-01 also inhibits the transcription induced by activin/nodal type I receptor (ALK4-TD) and nodal type I receptor (ALK7-TD) with IC50 of 45 nM and 7.5 nM, respectively.Solutions are unstable and should be fresh-prepared.

A-83-01 Chemical Structure

A-83-01 Chemical Structure

CAS: 909910-43-6

Selleck's A-83-01 has been cited by 28 publications

Purity & Quality Control

Batch: Purity: >97%
97

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Biological Activity

Description A-83-01 is a potent inhibitor of TGF-β type I receptor (ALK5-TD) with IC50 of 12 nM. A-83-01 also inhibits the transcription induced by activin/nodal type I receptor (ALK4-TD) and nodal type I receptor (ALK7-TD) with IC50 of 45 nM and 7.5 nM, respectively.Solutions are unstable and should be fresh-prepared.
Targets
ALK7 [1]
(Cell-free assay)		 ALK5 [1]
(Cell-free assay)		 ALK4 [1]
(Cell-free assay)
7.5 nM 12 nM 45 nM
In vitro
In vitro

A-83-01 inhibits the transcriptional activity induced by TGF-β type I receptor ALK-5 and that by activin type IB receptor ALK-4 and nodal type I receptor ALK-7, the kinase domains of which are structurally highly related to those of ALK-5. A-83-01 is potent in the inhibition of ALK5 and also prevents phosphorylation of Smad2/3 and the growth inhibition induced by TGF-β.[1]
Cell Research Cell lines Wild-type mink lung epithelial (Mv1Lu) cells, R mutant of Mv1Lu (R4-2) cells, HaCaT cells, C2C12 cells, NMuMG cells
Concentrations 1 μM
Incubation Time 1 h
Method

Cell proliferation assay: Mv1Lu cells are seeded in duplicate at a density of 2.5 × 104 cells/well in 24-well plates. The following day, cells are pretreated for 1 h with 1 μM A-83-01 and then cultured with TGF-β (1 ng/mL) for 24 h, 48 h, or 72 h. Cells are trypsinized and counted with a Coulter counter. To explore whether A-83-01 reduces the growth-inhibitory effects of TGF-β in concentration-dependent fashion, Mv1Lu cells are seeded as above and pretreated for 1 h with various concentrations of A-83-01. After pretreatment, cells are cultured with TGF-β (1 ng/mL) for 48 h and counted.
In Vivo
In vivo

A83-01 treatment significantly increases the number of Nkx2.5+ cardiomyoblasts at baseline and after myocardial injury, resulting in an increase in newly formed cardiomyocytes. A83-01 treatment significantly improves ventricular elastance and stroke work, leading to improved contractility after injury.[2]
Animal Research Animal Models 8–10 week old Nkx2.5 enhancer-eGFP transgenic mice
Dosages 10 mg/kg
Administration IP

Chemical lnformation & Solubility

Molecular Weight 421.52 Formula

C25H19N5S
CAS No. 909910-43-6 SDF --
Smiles CC1=NC(=CC=C1)C2=NN(C=C2C3=CC=NC4=CC=CC=C34)C(=S)NC5=CC=CC=C5
Storage (From the date of receipt) 3 years -20°C powder Solutions are unstable. Prepare fresh or purchase small, pre-packaged sizes. Repackage upon receipt.

In vitro
Batch:

DMSO : 21 mg/mL ( (49.81 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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