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Cat. No. M2108
SB-525334 Structure
Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
5mg USD 61  USD61 In stock
10mg USD 97  USD97 In stock
50mg USD 366  USD366 In stock
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Quality Control & Documentation
Biological Activity

SB-525334 is a potent and selective inhibitor of the transforming growth factor-beta1 (TGF-beta1) receptor, activin receptor-like kinase (ALK5). In cell-based assays, SB-525334 (1 microM) blocked TGF-beta1-induced phosphorylation and nuclear translocation of Smad2/3 in renal proximal tubule cells and inhibited TGF-beta1-induced increases in plasminogen activator inhibitor-1 (PAI-1) and procollagen alpha1(I) mRNA expression in A498 renal epithelial carcinoma cells. SB-525334 inhibited ALK5 kinase activity with an IC50 of 14.3 nM and was approximately 4-fold less potent as an inhibitor of ALK4 with IC50 of 58.5 nM. SB-525334 significantly increased apoptotic cell death in gemcitabine-resistant cells. SB-525334 reverses pulmonary arterial pressure and inhibits right ventricular hypertrophy in a rat model of PAH effectively. SB-525334 treatment showed significant attenuation in Smad2/3 nuclear translocation, decrease in CTGF-expressing cells, myofibroblast proliferation and type I collagen deposition.

Product Citations
Customer Product Validations & Biological Datas
Source Am J Physiol Renal Physiol (2015). Figure 4. SB-525334
Method Endothelial function
Cell Lines rats
Concentrations -
Incubation Time 24-h
Results Aortic endothelial cell lysates obtained from the four groups of rats on day 7 of the experiment demonstrated activation of ALK5 by HS intake as well as the anticipated inhibition of ALK5 by SB-525334
Chemical Information
Molecular Weight 343.42
Formula C21H21N5
CAS Number 356559-20-1
Solubility (25°C) DMSO 60 mg/mL
Ethanol 40 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.


[1] Thomas M, et al. Am J Pathol. Activin-like kinase 5 (ALK5) mediates abnormal proliferation of vascular smooth muscle cells from patients with familial pulmonary arterial hypertension and is involved in the progression of experimental pulmonary arterial hypertension induced by monocrotaline.

[2] Laping NJ, et al. Clin Cancer Res. Tumor-specific efficacy of transforming growth factor-beta RI inhibition in Eker rats.

[3] Higashiyama H, et al. Exp Mol Pathol. Inhibition of activin receptor-like kinase 5 attenuates bleomycin-induced pulmonary fibrosis.

[4] Grygielko ET, et al. J Pharmacol Exp Ther. Inhibition of gene markers of fibrosis with a novel inhibitor of transforming growth factor-beta type I receptor kinase in puromycin-induced nephritis.

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Keywords: SB-525334 supplier, TGF-beta/Smad, inhibitors, activators

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