A potent inhibitor of TGF-β R1/ALK5 kinase
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SB-525334

Item No. 16281

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
6-[2-(1,1-dimethylethyl)-5-(6-methyl-2-pyridinyl)-1H-imidazol-4-yl]-quinoxaline
CAS Number
356559-20-1
Synonyms
  • TGF-β RI Kinase Inhibitor VIII
Molecular Formula
C21H21N5
Formula Weight
343.4
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 30 mg/mlDMSO: 20 mg/mlEthanol: 30 mg/mlEthanol:PBS(pH 7.2) (1:1): 0.5 mg/ml
λmax
235, 365 nm
SMILES
CC(C)(C)C(N1)=NC(C2=CC=CC(C)=N2)=C1C(C=C3)=CC4=C3N=CC=N4
InChi Code
InChI=1S/C21H21N5/c1-13-6-5-7-16(24-13)19-18(25-20(26-19)21(2,3)4)14-8-9-15-17(12-14)23-11-10-22-15/h5-12H,1-4H3,(H,25,26)
InChi Key
DKPQHFZUICCZHF-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $37

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    5 mg

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    10 mg

    $142

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    50 mg

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    Product Description

    SB-525334 is a potent inhibitor of the TGF-β receptor 1 (TGF-β R1, ALK5) kinase (IC50 = 14.36 nM).1 It is ~4-fold less effective against ALK4 and inactive against ALK2, ALK3, and ALK6.1 SB-525334 blocks TGF-β1-induced phosphorylation and nuclear translocation of SMAD2/3 as well as TGF-β1-directed gene expression.1 It is effective in vivo, preventing puromycin aminonucleoside-induced renal fibrosis and bleomycin-induced pulmonary fibrosis.1,2,3 SB-525334 also modulates carcinogenesis and suppresses the development of pulmonary arterial hypertension in animals.3,4,5

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Grygielko, E.T., Martin, W.M., Tweed, C., et al. Inhibition of gene markers of fibrosis with a novel inhibitor of transforming growth factor-β type I receptor kinase in puromycin-induced nephritis. J. Pharmacol. Exp. Ther. 313(3), 943-951 (2005).

    2. Higashiyama, H., Yoshimoto, D., Kaise, T., et al. Inhibition of activin receptor-like kinase 5 attenuates bleomycin-induced pulmonary fibrosis. Exp. Mol. Pathol. 83, 39-46 (2007).

    3. Jarman, E.R., Khambata, V.S., Yun Ye, L., et al. A translational preclinical model of interstitial pulmonary fibrosis and pulmonary hypertension: Mechanistic pathways driving disease pathophysiology. Physiol.Rep. 2(9), 1-19 (2014).

    4. Laping, N.J., Everitt, J.I., Frazier, K.S., et al. Tumor-specific efficacy of transforming growth factor-βRI inhibition in Eker rats. Clin. Cancer Res. 13(10), 3087-3099 (2007).

    5. Thomas, M., Docx, C., Holmes, A.M., et al. 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. Am. J. Pathol. 174(2), 380-389 (2009).