Revision 1

#20090Store at -20C

5 mg

Cell Signaling Technology

Orders: 877-616-CELL (2355) [email protected]

Support: 877-678-TECH (8324)

Web: [email protected] cellsignal.com

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For Research Use Only. Not for Use in Diagnostic Procedures.

Background

The small-molecule SB-525334 inhibits transforming growth factor-β1 receptor (TGF-βR1, ALK5) with an IC50 of 14.3 nM. SB-525334 also inhibits the related receptor ALK4 (IC50 = 58.5 nM) but is inactive against ALK2, ALK3, and ALK6. Inhibition of TGF-β downstream signaling by SB-525334 blocks phosphorylation and nuclear translocation of Smad2/3 protein and reduces PAI-1 and procollagen α1(I) mRNA expression in renal epithelial carcinoma cells (1). SB-525334 treatment of a bleomycin-induced pulmonary fibrosis model reduced TGF-β-mediated nuclear translocation of Smad2/3, decreased myofibroblast proliferation, and attenuated pulmonary fibrosis (2). Exposure of mesenchymal and epithelial tumors in Eker rats to SB-525334 reduced the size and number of mesenchymal tumors but had the opposite effect on epithelial cancer cells and lesions (3). Inhibition of ALK5 by SB-525334 in both human pulmonary artery smooth muscle cells and a rat model of pulmonary arterial hypertension resulted in decreased sensitivity to TGF-β, and attenuated pulmonary arterial pressure and right ventricular hypertrophy (4).

  1. Grygielko, E.T. et al. (2005) J Pharmacol Exp Ther 313, 943-51.
  2. Higashiyama, H. et al. (2007) Exp Mol Pathol 83, 39-46.
  3. Laping, N.J. et al. (2007) Clin Cancer Res 13, 3087-99.
  4. Thomas, M. et al. (2009) Am J Pathol 174, 380-9.

Molecular Formula

C21H21N5

Molecular Weight

343.4 g/mol

Purity

>99%

CAS

356559-20-1

Solubility

Soluble in DMSO at 30 mg/mL.

Storage

Store lyophilized at -20ºC, desiccated. In lyophilized form, the chemical is stable for 24 months. Once in solution, store at -20ºC and use within 3 months to prevent loss of potency. Aliquot to avoid multiple freeze/thaw cycles.

Directions for Use

SB-525334 is supplied as a lyophilized powder. For a 15 mM stock, reconstitute 5 mg of powder in 0.97 mL of DMSO. Working concentrations and length of treatment can vary depending on the desired effect.

Background References

    Cross-Reactivity Key

    H: human M: mouse R: rat Hm: hamster Mk: monkey Vir: virus Mi: mink C: chicken Dm: D. melanogaster X: Xenopus Z: zebrafish B: bovine Dg: dog Pg: pig Sc: S. cerevisiae Ce: C. elegans Hr: horse GP: Guinea Pig Rab: rabbit All: all species expected

    Trademarks and Patents

    Cell Signaling Technology is a trademark of Cell Signaling Technology, Inc.
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