Stemolecule™ SB431542

SB431542 is an inhibitor of the transforming growth factor-β 1 (TGFβ1) activin receptor-like kinases (ALKs). It is a selective and potent inhibitor of ALK-4, -5 and -7. SB431542 inhibits endogenous activin and TGFβ signaling without affecting more divergent BMP signaling utilizing ALK-1, -2, -3, and -6^1,2. SB431542 stimulates proliferation, differentiation, and sheet formation of endothelial cells derived from embryonic stem cells³.

Stemolecule SB431542 is also available as a 10 mM DMSO Stock Solution in DMSO  (5 mg in 1.3 ml) (Cat. No. 04-0010-05).

Stemgent and the Stemolecule brand name are trademarks of REPROCELL Inc., Japan.

Product Name: Stemolecule SB431542

Catalog Number: 04-0010-base

Size:

• 10 mg (Cat. No. 04-0010-10)
• 5 mg (Cat. No. 04-0010)
• 5 mg at 10 mM in DMSO  (5 mg in 1.3 ml) (04-0010-05)

Alternate Name(s): 4-[4-(1,3-benzodioxol-5-yl)-5-pyridin-2-yl-1H-imidazol-2-yl]benzamide

Chemical Formula: C₂₂H₁₆N₄O₃

Molecular Weight: 384.4

CAS Number: 301836-41-9 (anhydrous)

Purity: Greater than 97 % by HPLC analysis

Formulation: White solid

Solubility: Reconstitute in DMSO to the desired concentration. For reconstitution instructions please reference product specifications sheet.

Storage and Stability: Store powder at 4 °C protected from light. Information about the stability of Stemolecules in solution is largely not available. As a general guideline, we recommend that stock solution be freshly made and stored in aliquots at −20 °C, protected from light. The effect of storage of stock solutions should be verified for each application.

Quality Control: The purity of SB431542 was determined by HPLC analysis. The accurate mass was determined by mass spectrometry. Cellular toxicity of SB431542 was tested on mouse embryonic stem cells.

Specification Sheets:

• 04-0010 Specifications Sheet
• 04-0010-10 Specifications Sheet
• 04-0010-05 Specifications Sheet

Safety Data Sheets:

• 04-0010 and 04-0010-10 Safety Data Sheet (SDS)
• 04-0010-05 Safety Data Sheet (SDS)

1. Matsuyama, S., Iwadate, M., Kondo, M., Saitoh, M., Hanyu, A., Shimizu, K., Aburatani, H., Mishima, H.K., Imamura, T., Miyazono, K., Miyazawa, K. SB-431542 and Gleevec inhibit transforming growth factor-β-induced proliferation of human osteosarcoma cells. Cancer Res 63: 7791-7798 (2003).
2. Laping, N.J., Grygielko, E., Mathur, A., Butter, S., Bomberger, J., Tweed, C., Martin, W., Fornwald, J., Lehr, R., Harling, J., Gaster, L., Callahan, J.F., and Olson, B.A. Inhibition of transforming growth factor (TGF)-β1-induced extracellular matrix with a novel inhibitor of the TGF-β type I receptor kinase activity: SB-431542. Mol Pharmacol 62: 58-64 (2002).
3. Inman, G.J., Nicolás, F.J., Callahan, J.F., Harling, J.D., Gaster, L.M., Reith, A.D., Laping, N.J., and Hill, C.S. SB-431542 is a potent and specific inhibitor of transforming growth factor-β superfamily type I activin receptor-like kinase (ALK) receptors ALK4, ALK5, and ALK7. Mol Pharmacol 62: 65-74 (2002).
4. Watabe, T., Nishihara, A., Mishima, K., Yamashita, J., Shimizu, K., Miyazawa, K., Nishikawa, S., and Miyazono, K. TGFβ receptor kinase inhibitor enhances growth and integrity of embryonic stem cell-derived endothelial cells. J Cell Biol 163: 1303-1311 (2003).

Additional Publications

• Mazza NC; Shuck SC; Lin J: Moxley AM; Termini J; Cookson MR; Wilson MA. DJ-1 is not a deglycase and makes a modest contribution to cellular defense against methylglyoxal damage in neurons. J Neurochem 162:245 (2022).
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• Yuva-Aydemir Y; Almeida S; Krishnan G; Gendron TF; Goa F-B. AFF2/FMR2 regulates expression of expanded GGGGCC repeat-containing C9ORF72 allele in ALS/FTD. Nature Commun 10:5466 (2019).
• Leitner D; Ramamoorthy M; Dejosez M; Zwaka TP. Immature mDA Neurons Ameliorate Motor Deficits in a 6-OHDA Parkinson's Disease Mouse Model and are Functional after Cryopreservation. Stem Cell Res in press:doi.org/10.1016/j.scr.2019.101617 (2019).
• Nagaraja S; Quezada MA; Gillespie SM; Arzt M; Lennon JJ; Woo PJ; Hovestadt V; Kambhampati M; Filbin MG; Suva ML; Nazarian J; Monje M. Histone Variant and Cell Context Determine H3K27M Reprogramming of the Enhancer Landscape and Oncogenic State. Molecular Cell 76:1-16 (2019).
• Durens M; Nestor J; Herold K Niescier RF; Lunden FW; Phillips AW; Lin Y-C; Nestor MW. High-content interrogation of human induced pluripotent stem cell-derived cortical organoid platforms. bioRxiv http://dx.doi.org/10.1101/697623. : (2019).
• de Souza JS; Ferreira DR; Herai R; Carromeu C; Torres LB; Araujo BHS; Cugola F; Maciel RMB; Muotri AR; Giannocco G. Altered Gene Expression of Thyroid Hormone Transporters and Deiodinases in iPS MeCP2-Knockout Cells-Derived Neurons. Molecular Neurobiol in press:https://doi.org/10.1007/s12035-019-01645-2 (2019).
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• Zhang Y; Zhang Y; Li M; Mend F; Yu Z; Chen Y; Cui G. Combination of SB431542, CHIR99021 and PD0325901 has a synergic effect on abrogating valproic acid‑induced epithelial‑mesenchymal transition and stemness in HeLa, 5637 and SCC‑15 cells. Oncol Rep In Press:https://doi.org/10.3892/or.2019.7088 (2019).
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