Search Site
Related Products
SB525334(TGF-beta1) receptor inhibitor

SB525334

Catalog No. A5602
Size Price Stock Qty
10mM (in 1mL DMSO) $50.00 In stock
Evaluation Sample $28.00 In stock
5mg $50.00 In stock
25mg $150.00 In stock
100mg $480.00 In stock

Tel: +1-832-696-8203

Email: sales@apexbt.com

Worldwide Distributors

Sample solution is provided at 25 µL, 10mM.

Quality Control

Chemical structure

SB525334

Related Biological Data

SB525334

Related Biological Data

SB525334

Biological Activity

Description SB525334 is a potent and selective inhibitor of TGFβ receptor I (ALK5) with IC50 of 14.3 nM, is 4-fold less potent to ALK4 than ALK5 and inactive to ALK2, 3, and 6.
Targets TGF-β1 (ALK5)          
IC50 14.3 nM          

SB525334 Dilution Calculator

Concentration (start)
x
Volume (start)
=
Concentration (final)
x
Volume (final)
 
 
 
C1
V1
C2
V2

calculate

SB525334 Molarity Calculator

Mass
=
Concentration
x
Volume
x
MW*
 
 
 
g/mol

calculate

Chemical Properties

Cas No. 356559-20-1 SDF Download SDF
Chemical Name 6-[2-tert-butyl-5-(6-methylpyridin-2-yl)-1H-imidazol-4-yl]quinoxaline
Canonical SMILES CC1=CC=CC(=N1)C2=C(N=C(N2)C(C)(C)C)C3=CC4=NC=CN=C4C=C3
Formula C21H21N5 M.Wt 343.42
Solubility Soluble in DMSO > 10 mM Storage Store at -20°C
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
Shipping Condition Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request

Background

SB525334 is a potent inhibitor of transforming growth factor-beta1 (TGF-beta1) receptor, activin receptor-like kinase (ALK5). It specifically inhibits ALK5 with IC50 value of 14.3nM, which shows 4-fold higher potency against ALK4 [1].

SB525334 has been demonstrated to reduce smad2/3 nuclear fluorescence induced by TGF-beta1 in human renal proximal tubule epithelial (RPTE) cells. Additionally, SB525334 inhibits TGF-beta1 mediated procollagen and PAI-1 expression in human renal carcinoma cells A498 [1].

SB525334?dose-dependently reduces Urinary protein, procollagen alpha1(I) mRNA and?procollagen alpha1(III) mRNA when administered?orally in acute puromycin aminonucleoside (PAN) rat model of renal disease [1].

References:
[1] Grygielko ET1,?Martin WM,?Tweed C,?Thornton P,?Harling J,?Brooks DP,?Laping NJ. Inhibition of gene markers of fibrosis with a novel inhibitor of transforming growth factor-beta type I receptor kinase in puromycin-induced nephritis. J Pharmacol Exp Ther.?2005 Jun;313(3):943-51.