SB 431542

Cat. No. 1614

SB 431542 C22H16N4O3 [301836-41-9]

Price and Availability

For SB 431542 pricing & availability please select your country from the drop down menu:
Submit
By clicking submit you agree to accept a cookie from Tocris Bioscience. For details, please read our privacy and cookie policy.

Chemical Name: 4-[4-(1,3-benzodioxol-5-yl)-5-(2-pyridinyl)-1H-imidazol-2-yl]benzamide

Biological Activity

Potent and selective inhibitor of the transforming growth factor-β (TGF-β) type I receptor activin receptor-like kinase ALK5 (IC50 = 94 nM), and its relatives ALK4 and ALK7. Suppresses TGF-β-induced proliferation of human osteosarcoma cells. 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.

Licensing Information

Sold for research purposes under agreement from GlaxoSmithKline

Technical Data

M.Wt:
384.39
Formula:
C22H16N4O3
Solubility:
Soluble to 10 mM in ethanol and to 100 mM in DMSO
Purity:
>99 %
Storage:
Store at RT
CAS No:
301836-41-9

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.

Certificate of Analysis / Safety Data Sheet

Certificate of Analysis: View current batch
Select another batch:
Safety Data Sheet: View Safety Data Sheet

Halder et al (2005) A specific inhibitor of TGF-beta receptor kinase, SB-431542, as a potent antitumor agent for human cancers. Neoplasia 7 509. PMID: 15967103.

Matsuyama et al (2003) SB-431542 and Gleevec inhibit transforming growth factor-β-induced proliferation of human osteosarcoma cells. Cancer Res. 63 7791. PMID: 14633705.

Watabe et al (2003) TGF-beta receptor kinase inhibitor enhances growth and integrity of embryonic stem cell-derived endothelial cells. J.Cell Biol. 163 163. PMID: 14676305.

Inman et al (2002) 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. PMID: 12065756.

Laping et al (2002) 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. PMID: 12065755.

If you know of a relevant reference for this product please let us know.

Citations are publications that use Tocris products. Selected citations for SB 431542 include:

Aspalter et al (2015) Alk1 and Alk5 inhibition by Nrp1 controls vascular sprouting downstream of Notch. Nat Commun 6 7264. PMID: 26081042.

Kumar et al (2015) Generation of an expandable intermediate mesoderm restricted progenitor cell line from human pluripotent stem cells. Elife 4. PMID: 26554899.

Oh et al (2015) Human-induced pluripotent stem cells generated from intervertebral disc cells improve neurologic functions in spinal cord injury. Stem Cell Res Ther 6 125. PMID: 26104416.

Pasca et al (2015) Functional cortical neurons and astrocytes from human pluripotent stem cells in 3D culture. Nat Methods 12 671. PMID: 26005811.

Piao et al (2015) Human embryonic stem cell-derived oligodendrocyte progenitors remyelinate the brain and rescue behavioral deficits following radiation. Cell Stem Cell 16 198. PMID: 25658373.

Sanders et al (2015) SMAD-independent down-regulation of caveolin-1 by TGF-β: effects on proliferation and survival of myofibroblasts. PLoS One 10 e0116995. PMID: 25658089.

Woods et al (2015) Increased Expression of TGF-β Signaling Components in a Mouse Model of Fibrosis Induced by Submandibular Gland Duct Ligation. PLoS One 10 e0123641. PMID: 25955532.

Yan et al (2015) Stimulation of hepatocarcinogenesis by neutrophils upon induction of oncogenic kras expression in transgenic zebrafish. J Hepatol 63 420. PMID: 25828472.

Aguila et al (2014) Selection Based on FOXA2 Expression Is Not Sufficient to Enrich for Dopamine Neurons From Human Pluripotent Stem Cells. Stem Cells Transl Med 3 1032. PMID: 25024431.

Babu et al (2014) TGFβ-mediated suppression of CD248 in non-cancer cells via canonical Smad-dependent signaling pathways is uncoupled in cancer cells. BMC Cancer 14 113. PMID: 24555435.

Domev et al (2014) Immunoevasive pericytes from human pluripotent stem cells preferentially modulate induction of allogeneic regulatory T cells. Stem Cells Transl Med 3 1169. PMID: 25205843.

Fang et al (2014) Ets Related Gene and Smad3 Proteins Collaborate to Activate Transforming Growth Factor-Beta Mediated Signaling Pathway in ETS Related Gene-Positive Prostate Cancer Cells. J Pharm Sci Pharmacol 1 175. PMID: 25745638.

Grunseich et al (2014) Stem cell-derived motor neurons from spinal and bulbar muscular atrophy patients. Neurobiol Dis 70 12. PMID: 24925468.

Huang et al (2014) Efficient generation of lung and airway epithelial cells from human pluripotent stem cells. Nat Biotechnol 32 84. PMID: 24291815.

Nishimura et al (2014) Allele-specific knockdown of ALS-associated mutant TDP-43 in neural stem cells derived from induced pluripotent stem cells. PLoS One 9 e91269. PMID: 24651281.

Rosa et al (2014) miR-373 is regulated by TGFβ signaling and promotes mesendoderm differentiation in human Embryonic Stem Cells. Dev Biol 391 81. PMID: 24709321.

Bialas and (2013) TGF-β signaling regulates neuronal C1q expression and developmental synaptic refinement. Nat Neurosci 16 1773. PMID: 24162655.

Davila et al (2013) Acute reduction in oxygen tension enhances the induction of neurons from human fibroblasts. J Neurosci Methods 216 104. PMID: 23562599.

Jiang et al (2013) Translating dosage compensation to trisomy 21. Nature 500 296. PMID: 23863942.

Kirkeby et al (2013) Generating regionalized neuronal cells from pluripotency, a step-by-step protocol. Front Cell Neurosci 6 64. PMID: 23316134.

Lotz et al (2013) Sustained levels of FGF2 maintain undifferentiated stem cell cultures with biweekly feeding. PLoS One 8 e56289. PMID: 23437109.

Shields et al (2013) Snail cooperates with KrasG12D to promote pancreatic fibrosis. Mol Cancer Res 11 1078. PMID: 23761168.

Spender et al (2013) Transforming growth factor-β directly induces p53-up-regulated modulator of apoptosis (PUMA) during the rapid induction of apoptosis in myc-driven B-cell lymphomas. J Biol Chem 288 5198. PMID: 23243310.

Voon et al (2013) EMT-induced stemness and tumorigenicity are fueled by the EGFR/Ras pathway. PLoS One 8 e70427. PMID: 23950932.

Woodruff et al (2013) The presenilin-1 δE9 mutation results in reduced γ-secretase activity, but not total loss of PS1 function, in isogenic human stem cells. Cell Rep 5 974. PMID: 24239350.

Xia et al (2013) Identification of repurposed small molecule drugs for chordoma therapy. Cancer Biol Ther 14 638. PMID: 23792643.

Boettler et al (2012) TGF-β blockade does not improve control of an established persistent viral infection. Viral Immunol 25 232. PMID: 22620718.

Boeuf et al (2012) BMP and TGFbeta pathways in human central chondrosarcoma: enhanced endoglin and Smad 1 signaling in high grade tumors. BMC Cancer 12 488. PMID: 23088614.

Grönroos et al (2012) Transforming growth factor β inhibits bone morphogenetic protein-induced transcription through novel phosphorylated Smad1/5-Smad3 complexes. Mol Cell Biol 32 2904. PMID: 22615489.

Hoda et al (2012) Suppression of activin A signals inhibits growth of malignant pleural mesothelioma cells. Br J Cancer 107 1978. PMID: 23169291.

Mak et al (2012) Small molecules greatly improve conversion of human-induced pluripotent stem cells to the neuronal lineage. Stem Cells Int 2012 140427. PMID: 22567022.

Outten et al (2012) High-throughput screening assay for embryoid body differentiation of human embryonic stem cells. Curr Protoc Stem Cell Biol Chapter 1 Unit 1D.6. PMID: 22415836.

Rostovskaya et al (2012) Transposon-mediated BAC transgenesis in human ES cells. Nucleic Acids Res 40 e150. PMID: 22753106.

Sohni et al (2012) TGFβ1-induced Baf60c regulates both smooth muscle cell commitment and quiescence. PLoS One 7 e47629. PMID: 23110084.

Bedel et al (2011) Novel role for STAT3 in transcriptional regulation of NK immune cell targeting receptor MICA on cancer cells. Cancer Res 71 1615. PMID: 21257710.

Herman-Edelstein et al (2011) Dedifferentiation of immortalized human podocytes in response to transforming growth factor-β: a model for diabetic podocytopathy. Diabetes 60 1779. PMID: 21521871.

Olkhanud et al (2011) Tumor-evoked regulatory B cells promote breast cancer metastasis by converting resting CD4+ T cells to T-regulatory cells. Cancer Res 71 3505. PMID: 21444674.

Paek et al (2011) β-Catenin-dependent FGF signaling sustains cell survival in the anterior embryonic head by countering Smad4. Dev Cell 20 689. PMID: 21571225.

Shields et al (2011) Pancreatic cancer cells respond to type I collagen by inducing snail expression to promote membrane type 1 matrix metalloproteinase-dependent collagen invasion. J Biol Chem 286 10495. PMID: 21288898.

Wilson et al (2011) Human tumour immune evasion via TGF-β blocks NK cell activation but not survival allowing therapeutic restoration of anti-tumour activity. PLoS One 6 e22842. PMID: 21909397.

Fong et al (2010) Tumor-supportive and osteoclastogenic changes induced by breast cancer-derived factors are reversed by inhibition of {gamma}-secretase. J Biol Chem 285 31427. PMID: 20679341.

Ham et al (2010) PPARdelta promotes wound healing by up-regulating TGF-beta1-dependent or -independent expression of extracellular matrix proteins. J Cell Mol Med 14 1747. PMID: 19538467.

Hannigan et al (2010) Epigenetic downregulation of human disabled homolog 2 switches TGF-beta from a tumor suppressor to a tumor promoter. J Clin Invest 120 2842. PMID: 20592473.

Ishida et al (2010) Phosphorylation of Junb family proteins by the Jun N-terminal kinase supports tissue regeneration in zebrafish. Dev Biol 340 468. PMID: 20144602.

Moyano et al (2010) Autocrine transforming growth factor-{beta}1 activation mediated by integrin {alpha}V{beta}3 regulates transcriptional expression of laminin-332 in Madin-Darby canine kidney epithelial cells. Mol Biol Cell 21 3654. PMID: 20844080.

Cacheaux et al (2009) Transcriptome profiling reveals TGF-beta signaling involvement in epileptogenesis. J Neurosci 29 8927. PMID: 19605630.

Clarke et al (2009) Transforming growth factor beta depletion is the primary determinant of Smad signaling kinetics. Mol Cell Biol 29 2443. PMID: 19223462.

Garamszegi et al (2009) Extracellular matrix-induced gene expression in human breast cancer cells. Mol Cancer Res 7 319. PMID: 19276183.

Li et al (2009) Generation of human-induced pluripotent stem cells in the absence of exogenous Sox2. Stem Cells 27 2992. PMID: 19839055.

Patsialou et al (2009) Invasion of human breast cancer cells in vivo requires both paracrine and autocrine loops involving the colony-stimulating factor-1 receptor. Cancer Res 69 9498. PMID: 19934330.

Gressner et al (2008) Activation of TGF-beta within cultured hepatocytes and in liver injury leads to intracrine signaling with expression of connective tissue growth factor. J Cell Mol Med 12 2717. PMID: 18266973.

Stoikos et al (2008) A distinct cohort of the TGFbeta superfamily members expressed in human endometrium regulate decidualization. Hum Reprod 23 1447. PMID: 18434375.

Yang et al (2008) Rb/E2F4 and Smad2/3 link survivin to TGF-beta-induced apoptosis and tumor progression. Oncogene 27 5326. PMID: 18504435.

Zhang et al (2008) Short-term BMP-4 treatment initiates mesoderm induction in human embryonic stem cells. Blood 111 1933. PMID: 18042803.

Horowitz et al (2007) Combinatorial activation of FAK and AKT by transforming growth factor-beta1 confers an anoikis-resistant phenotype to myofibroblasts. Cell Signal 19 761. PMID: 17113264.

Zhao et al (2006) PPARgamma agonists prevent TGFbeta1/Smad3-signaling in human hepatic stellate cells. Biochem Biophys Res Commun 350 385. PMID: 17010940.

Anumanthan et al (2005) Restoration of TGF-beta signalling reduces tumorigenicity in human lung cancer cells. Br J Cancer 93 1157. PMID: 16251876.

Chen et al (2005) Matrix contraction by dermal fibroblasts requires transforming growth factor-beta/activin-linked kinase 5, heparan sulfate-containing proteoglycans, and MEK/ERK: insights into pathological scarring in chronic fibrotic disease. Am J Pathol 167 1699. PMID: 16314481.

König et al (2005) TGF-{beta}1 activates two distinct type I receptors in neurons: implications for neuronal NF-{kappa}B signaling. J Cell Biol 168 1077. PMID: 15781474.

Mimura et al (2005) Trastuzumab-mediated antibody-dependent cellular cytotoxicity against esophageal squamous cell carcinoma. Clin Cancer Res 11 4898. PMID: 16000588.

Do you know of a great paper that uses SB 431542 from Tocris? If so please let us know.show all ▼show less ▲

View Related Products by Product Action

Keywords: SB 431542, supplier, Potent, selective, inhibitors, TGF-βRI, TGF-β, TGF-betaRI, TGFbRI, TGFbR1, tgf-b1, ALK4, ALK7, Transforming, Growth, Factors, Beta, Receptors, Receptor, Serine/Threonine, Kinases, RSTKs, SB431542, stem, cells, GlaxoSmithKline, GSK, EMT, migration, invasion, epithelial, mesenchymal, transition, organoids, Tocris Bioscience, TGF-β Receptor Inhibitor products

Quick Order

Find multiple products by catalog number

divider line

Cancer Research Product Guide

Cancer Research Product Guide

Highlights over 750 products for cancer research. Request copy or view PDF today.

divider line

Kinase Inhibitor Toolbox

80 Kinase inhibitors
pre-dissolved in DMSO

Kinase Inhibitor Toolbox

Includes many of the latest kinase inhibitors to become commercially available. Covers a wide range of kinase targets including EGFR, MAPK and CDK.

divider line

Kinases Product Listing

Kinases Product Listing

Highlights over 400 products for kinase research. Request copy or view PDF today.

divider line

Immunology Guide

Immunology Product Listing

Highlights over 190 products for immunology research. Request copy or view PDF today.

divider line

Stem Cells Review

Stem Cells Scientific Review

Written by Kirsty E. Clarke, Victoria B. Christie, Andy Whiting and Stefan A. Przyborski. Request copy or view PDF today.

divider line

VEGF Pathway & Anti-Angiogenic Therapy

Written by N. Ferrara & Y. Crawford

Angiogenesis Life Science Poster

A summary of antiangiogenic therapies targeting the VEGF pathway and the mechanisms of therapy resistance. Request copy today.

divider line

TGF-β Pathway

TGF-β  Signaling Pathway

TGF-β signaling is involved in the regulation of growth and proliferation of cells along with migration, differentiation and apoptosis. View pathway or download PDF today.

divider line

Twitter Updates

Follow @Tocris on Twitter

Follow us on Twitter!

Tocris is now actively tweeting. For regular updates on news, events and special offers, follow @Tocris on Twitter.