SB 431542

Name: SB 431542
Brand: Tocris Bioscience
SKU: 1614
Rating: 5 (8 reviews)

Tocris Bioscience, part of Bio-Techne | Catalog # 1614

(8)

Citations (2257)

COA / SDS

Potent, selective inhibitor of TGF-βRI, ALK4 and ALK7

Key Product Details

Description:	Potent, selective inhibitor of TGF-βRI, ALK4 and ALK7
Chemical Name:	4-[4-(1,3-benzodioxol-5-yl)-5-(2-pyridinyl)-1H-imidazol-2-yl]benzamide
Purity:	≥99% (HPLC)
Molecular Weight:	384.39

View Full Technical Details for SB 431542

Technical Data
Citations / Reviews (8)

Biological Activity for SB 431542

SB 431542 is a potent and selective inhibitor of the transforming growth factor-β (TGF-β) type I receptor/ALK5 (IC₅₀ = 94 nM), and its relatives ALK4 and ALK7. Suppresses TGF-β-induced proliferation of human osteosarcoma cells. Replaces SOX2 in reprogramming of fibroblasts into iPSCs. Stimulates proliferation, differentiation and sheet formation of ESC-derived endothelial cells. Inhibits TGF-β-induced EMT, migration, invasion and VEGF secretion in several human cancer cell lines. Also used in a protocol to generate brain organoids from human iPSCs. Can be used in a small molecule cocktail to generate 3D culture of lung alveolar cells, or vascular organoids. Also used in a protocol to generate cortical neurons from hiPSCs or dopaminergic neurons from hPSCs (see our protocol below).

SB 431542 synthesized to cGMP guidelines also available.

For more information about how SB 431542 may be used, see our protocols: 3D Culture of Lung Alveolar Cells, Differentiation of Hematopoietic Progenitors from hPSCs, Generating Midbrain Dopaminergic Neurons from hPSCs, Generating Vascular Organoids, Accelerated Induction of Cortical Neurons from hiPSCs.

Compound Libraries for SB 431542

SB 431542 is also offered as part of the Tocriscreen 2.0 Max, Tocriscreen Kinase Inhibitor Library and Tocriscreen Stem Cell Library. Find out more about compound libraries available from Tocris.

Scientific Data Examples for SB 431542

	Application of SB 431542 in dopaminergic neurons derived from hiPSCs. Dopaminergic neurons derived from human induced pluripotent stem cells (hiPSC) using SB 431542, CHIR 99021 (Catalog # 4423, Tocris), DAPT (Catalog # 2634, Tocris) and Purmorphamine (Catalog # 4551, Tocris). Cells cultured in Neuronal Media supplemented with TGF-3 (Catalog # 8420-B3, R&D Systems), cAMP, GDNF (Catalog # 212-GD, R&D Systems), BDNF (Catalog # 248-BDB, R&D Systems), N21-MAX (Catalog # AR008, R&D Systems). Differentiation shown at days 55 (left) and 62 (right). Images courtesy of Kevin Flynn, Bio-Techne.

Technical Data for SB 431542

M. Wt	384.39
Formula	C₂₂H₁₆N₄O₃
Storage	Store at RT
Purity	≥99% (HPLC)
CAS Number	301836-41-9
PubChem ID	4521392
InChi Key	FHYUGAJXYORMHI-UHFFFAOYSA-N
Smiles	NC(=O)C1=CC=C(C=C1)C1=NC(=C(N1)C1=CC=CC=N1)C1=CC2=C(OCO2)C=C1

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility for SB 431542

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
	ethanol	3.84	10
	DMSO	38.44	100 with gentle warming

Preparing Stock Solutions for SB 431542

The following data is based on the product molecular weight 384.39.

Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	2.60 mL	13.01 mL	26.02 mL
5 mM	0.52 mL	2.60 mL	5.20 mL
10 mM	0.26 mL	1.30 mL	2.60 mL
50 mM	0.05 mL	0.26 mL	0.52 mL

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References for SB 431542

References are publications that support the biological activity of the product.

Schafer An in vivo neuroimmune organoid model to study human microglia phenotypes. Cell 2023 PMID: 37172564
Halder A specific inhibitor of TGF-beta receptor kinase, SB-431542, as a potent antitumor agent for human cancers. Neoplasia 2005 PMID: 15967103
Watabe TGF-beta receptor kinase inhibitor enhances growth and integrity of embryonic stem cell-derived endothelial cells. J.Cell Biol. 2003 PMID: 14676305
Matsuyama SB-431542 and Gle. inhibit transforming growth factor-β-induced proliferation of human osteosarcoma cells. Cancer Res. 2003 PMID: 14633705
Laping 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. 2002 PMID: 12065755
Inman SB-431542 is a potent and specific inhibitor of transforming growth factor-β superfamily type I AVNreceptor-like kinase (ALK) receptors ALK4, ALK5, and ALK7. Mol.Pharmacol. 2002 PMID: 12065756