Home TGF-beta/Smad TGF-beta/Smad inhibitor TP0427736 HCl For research use only.

TP0427736 HCl

TP0427736 is a potent inhibitor of ALK5 kinase activity with an IC50 of 2.72 nM and this effect is 300-fold higher than the inhibitory effect on ALK3 (IC50 = 836 nM for ALK3). It also inhibits Smad2/3 phosphorylation in A549 cells induced by TGF-β1 with an IC50 value of 8.68 nM.

TP0427736 HCl Chemical Structure

TP0427736 HCl Chemical Structure

CAS No. 864374-00-5

Purity & Quality Control

Batch: S870001 DMSO]67 mg/mL]false]Water]Insoluble]false]Ethanol]Insoluble]false Purity: 99.04%
99.04

TP0427736 HCl Related Products

Signaling Pathway

TGF-beta/Smad Signaling Pathways

TGF-beta/Smad Signaling Pathway

Biological Activity

Description TP0427736 is a potent inhibitor of ALK5 kinase activity with an IC50 of 2.72 nM and this effect is 300-fold higher than the inhibitory effect on ALK3 (IC50 = 836 nM for ALK3). It also inhibits Smad2/3 phosphorylation in A549 cells induced by TGF-β1 with an IC50 value of 8.68 nM.
Targets
ALK5 [1]
(Cell-free assay)
2.72 nM
In vitro
In vitro

TP0427736 inhibits Smad2/3 phosphorylation in a concentration-dependent manner, with an IC50 value of 8.68 nM. In a cell-based assay of outer root sheath cells, TP0427736 rescued the inhibited proliferation by TGF-β1 and TGF-β2 in a concentration-dependent manner[1].
Cell Research Cell lines A549 cells
Concentrations --
Incubation Time 2 h
Method

A549 cells are cultured in plates overnight at 37℃ in a 5% CO2, 95% air atmosphere. Cells are pretreated with various concentrations of TP0427736 or DMSO as a control for 2 h, followed by the addition of 1 ng/mL TGF-β1. After 1 h of incubation, the cells are washed with PBS and lysed with RIPA solution, then mixed with biotinylated anti-Smad2/3 antibody. The mixture is transferred to a streptavidin-coated 96 well plate and incubated for 2 h. The mixture is then discarded, and each well is treated with rabbit anti-phosphoserine antibody, followed by Eu-labeled anti-rabbit IgG antibody and DELFIA Enhancement solution. The developed fluorescence is measured using an ARVO multi-label counter. The IC50 values are determined by analyzing the concentration-response curves.
In Vivo
In vivo

TP0427736 decreases shortening of hair follicle length during the transition from the late anagen phase to the catagen phase[1].

Chemical Information & Solubility

Molecular Weight 334.85 Formula

C14H11ClN4S2
CAS No. 864374-00-5 SDF --
Smiles CC1=CSC(=N1)C2=C(N=CN2)C3=CC4=C(C=C3)N=CS4
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 67 mg/mL ( (200.08 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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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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