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SB 431542

Cat. No. 1614 263 篇引用文献 8 条评论 提交评论 说明书 / 分析证书（CoA） / 化学品安全技术说明书（SDS）
GMP Version Available: SB 431542
Pricing Availability   Qty
说明： Potent, selective inhibitor of TGF-βRI, ALK4 and ALK7
化学名： 4-[4-(1,3-benzodioxol-5-yl)-5-(2-pyridinyl)-1H-imidazol-2-yl]benzamide
纯度： ≥99% (HPLC)
说明书
引用文献 (263)
评论 (8)
实验方案 (5)
文献 (3)
通路 (1)
生物活性 Scientific Data 技术数据 溶解性 计算器 说明书 参考文献

生物活性 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.

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.

Scientific Data

dopaminergic neurons derived from hiPSCs using SB 431542 View Larger

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.

化合物库 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. 了解 Tocris 化合物库的更多信息。

技术数据 for SB 431542

分子量 384.39
公式 C22H16N4O3
储存 Store at RT
纯度 ≥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

上方提供的技术数据仅供参考。批次相关数据请参见分析证书。

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

溶解性数据 for SB 431542

溶剂 最高浓度 mg/mL 最高浓度 mM
溶解性
ethanol 3.84 10
DMSO 38.44 100 温和加热

制备储备液 for SB 431542

以下数据基于产品分子量 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.

选择批次从而根据批次分子量重新计算:
浓度/溶剂体积/质量 1 mg 5 mg 10 mg
1 mM 2.6 mL 13.01 mL 26.02 mL
5 mM 0.52 mL 2.6 mL 5.2 mL
10 mM 0.26 mL 1.3 mL 2.6 mL
50 mM 0.05 mL 0.26 mL 0.52 mL

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产品说明书 for SB 431542

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关键词: SB 431542, SB 431542 supplier, Potent, selective, inhibitors, inhibits, 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, epithe, TGF-beta, Stem, Cell, Proliferation, Other, Differentiation, Products, Reprogramming, Organoids, ALK, Hematopoietic, Cells, Neural, 1614, Tocris Bioscience

263 篇 SB 431542 的引用文献

引用文献是使用了 Tocris 产品的出版物。 SB 431542 的部分引用包括：

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Medelnik et al (2018) Signaling-Dependent Control of Apical Membrane Size and Self-Renewal in Rosette-Stage Human Neuroepithelial Stem Cells. Stem Cell Reports 10 1751 PMID: 29779899

Yang et al (2018) Interaction of hepatic stellate cells with neutrophils and macrophages in the liver following oncogenic kras activation in transgenic zebrafish. Sci Rep 8 8495 PMID: 29855567

Albers et al (2018) TGF-β induces Smad2 Phosphorylation, ARE Induction, and Trophoblast Differentiation. Int J Stem Cells 11 111 PMID: 29699384

Molina et al (2018) MAPK and GSK3/ beta -TRCP-mediated degradation of the maternal Ets domain transcriptional repressor Yan/Tel controls the spatial expression of nodal in the sea urchin embryo. PLoS Genet 14 e1007621 PMID: 30222786

Nehme et al (2018) Combining NGN2 Programming with Developmental Patterning Generates Human Excitatory Neurons with NMDAR-Mediated Synaptic Transmission. Cell Rep 23 2509 PMID: 29791859

Li et al (2018) Fast Generation of Functional Subtype Astrocytes from Human Pluripotent Stem Cells. Stem Cell Reports 11 998 PMID: 30269954

Sheng et al (2018) A stably self-renewing adult blood-derived induced neural stem cell exhibiting patternability and epigenetic rejuvenation. Nat Commun 9 4047 PMID: 30279449

Bayo-Puxan et al (2018) Lysosomal and network alterations in human mucopolysaccharidosis type VII iPSC-derived neurons. Sci Rep 8 16644 PMID: 30413728

Molina et al (2017) p38 MAPK as an essential regulator of dorsal-ventral axis specification and skeletogenesis during sea urchin development: a re-evaluation. Development 144 2270 PMID: 28507001

Funaki et al (2017) Chemotherapy enhances programmed cell death 1/ligand 1 expression via TGF-β induced epithelial mesenchymal transition in non-small cell lung cancer. Oncol Rep 38 2277 PMID: 28849209

Major et al (2017) Derivation of telencephalic oligodendrocyte progenitors from human pluripotent stem cells. Curr Protoc Stem Cell Biol 39 1H.10.1 PMID: 29081882

Takata et al (2017) Induced-Pluripotent-Stem-Cell-Derived Primitive Macrophages Provide a Platform for Modeling Tissue-Resident Macrophage Differentiation and Function. Immunity 47 183 PMID: 28723550

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Bao et al (2017) Directed differentiation and long-term maintenance of epicardial cells derived from human pluripotent stem cells under fully defined conditions. Nat Protoc 12 1890 PMID: 28817124

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Bershteyn et al (2017) Human iPSC-Derived Cerebral Organoids Model Cellular Features of Lissencephaly and Reveal Prolonged Mitosis of Outer Radial Glia. Cell Stem Cell 20 435 PMID: 28111201

McCauley et al (2017) Efficient Derivation of Functional Human Airway Epithelium from Pluripotent Stem Cells via Temporal Regulation of Wnt Signaling. Cell Stem Cell 20 844 PMID: 28366587

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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

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

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

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

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

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

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Colunga et al (2019) Human Pluripotent Stem Cell-Derived Multipotent Vascular Progenitors of the Mesothelium Lineage Have Utility in Tissue Engineering and Repair. Cell Rep 26 2566 PMID: 30840882

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Charney et al (2017) Foxh1 Occupies cis-Regulatory Modules Prior to Dynamic Transcription Factor Interactions Controlling the Mesendoderm Gene Program. Dev Cell 40 595 PMID: 28325473

Wrighton et al (2014) Signals from the surface modulate differentiation of human pluripotent stem cells through glycosaminoglycans and integrins. J Cell Sci 111 18126 PMID: 25422477

Curado et al (2014) ALK5 and ALK1 play antagonistic roles in transforming growth factor β-induced podosome formation in aortic endothelial cells. Exp Neurol 34 4389 PMID: 25266657

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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

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

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Canfield et al (2019) An isogenic neurovascular unit model comprised of human induced pluripotent stem cell-derived brain microvascular endothelial cells, pericytes, astrocytes, and neurons. Fluids Barriers CNS 16 25 PMID: 31387594

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Caron et al (2019) Low-density lipoprotein receptor-deficient hepatocytes differentiated from induced pluripotent stem cells allow familial hypercholesterolemia modeling, CRISPR/Cas-mediated genetic correction, and productive hepatitis C virus infection. Stem Cell Res Ther 10 221 PMID: 31358055

Garcia et al (2019) Huntington's Disease Patient-Derived Astrocytes Display Electrophysiological Impairments and Reduced Neuronal Support. Front Neurosci 13 669 PMID: 31316341

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de la Mare (2017) Extracellular Hsp90 and TGFβ regulate adhesion, migration and anchorage independent growth in a paired colon cancer cell line model. BMC Cancer 17 202 PMID: 28302086

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Kotton et al (2017) Differentiation of human pluripotent stem cells into functional lung alveolar epithelial cells. Cell Stem Cell. 21 472 PMID: 28965766

Tchieu et al (2017) A modular platform for differentiation of human PSCs into all major ectodermal lineages. Cell Stem Cell 21 399 PMID: 28886367

Ginsberg et al (2015) Direct conversion of human amniotic cells into endothelial cells without transitioning through a pluripotent state. Nat Protoc 10 1975 PMID: 26540589

Rempel et al (2015) A transcriptome-based classifier to identify developmental toxicants by stem cell testing: design, validation and optimization for histone deacetylase inhibitors. Arch Toxicol 89 1599 PMID: 26272509

Zhang et al (2015) Small Molecules Efficiently Reprogram Human Astroglial Cells into Functional Neurons. Cell Stem Cell 17 735 PMID: 26481520

Patsialou et al (2012) Selective gene-expression profiling of migratory tumor cells in vivo predicts clinical outcome in breast cancer patients. Breast Cancer Res 14 R139 PMID: 23113900

Luo and Su (2012) Opposing nodal and BMP signals regulate left-right asymmetry in the sea urchin larva. PLoS Biol 10 e1001402 PMID: 23055827

Xiao et al (2009) SB-431542 inhibition of scar formation after filtration surgery and its potential mechanism. Invest Ophthalmol Vis Sci 50 1698 PMID: 19098325

Walshe et al (2009) TGF-beta is required for vascular barrier function, endothelial survival and homeostasis of the adult microvasculature. PLoS One 4 e5149 PMID: 19340291

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

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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

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

Easterbrook et al (2019) Analysis of the Spatiotemporal Development of Hematopoietic Stem and Progenitor Cells in the Early Human Embryo. Stem Cell Reports 12 1056 PMID: 30956115

Haidar et al (2019) Neuropathy-causing mutations in HSPB1 impair autophagy by disturbing the formation of SQSTM1/p62 bodies. Autophagy 15 1051 PMID: 30669930

Nguyen et al (2019) Constructing an Isogenic 3D Human Nephrogenic Progenitor Cell Model Composed of Endothelial, Mesenchymal, and SIX2-Positive Renal Progenitor Cells. Stem Cells Int 2019 3298432 PMID: 31191670

Gentsch et al (2019) The Spatiotemporal Control of Zygotic Genome Activation. iScience 16 485 PMID: 31229896

Gentsch et al (2019) Maternal pluripotency factors initiate extensive chromatin remodelling to predefine first response to inductive signals. Nat Commun 10 4269 PMID: 31537794

Offermann et al (2017) MED15 overexpression in prostate cancer arises during androgen deprivation therapy via PI3K/mTOR signaling. Oncotarget 8 7964 PMID: 27974704

Saini et al (2017) Nicotinamide Ameliorates Disease Phenotypes in a Human iPSC Model of Age-Related Macular Degeneration. Cell Stem Cell 20 635 PMID: 28132833

Subramanian et al (2017) Dynamic behaviour of human neuroepithelial cells in the developing forebrain. Nat Commun 8 14167 PMID: 28139695

Kunnen et al (2017) Fluid shear stress-induced TGF-β/ALK5 signaling in renal epithelial cells is modulated by MEK1/2. Cell Mol Life Sci 74 2283 PMID: 28168444

Yang et al (2017) Serotonin Activated Hepatic Stellate Cells Contribute to Sex Disparity in Hepatocellular Carcinoma. Cell Mol Gastroenterol Hepatol 3 484 PMID: 28462385

Christoforou et al (2017) Core Transcription Factors, MicroRNAs, and Small Molecules Drive Transdifferentiation of Human Fibroblasts Towards The Cardiac Cell Lineage. Sci Rep 7 40285 PMID: 28071742

Maturana et al (2016) Mutations in LRRK2 impair NF-κB pathway in iPSC-derived neurons. J Neuroinflammation 13 295 PMID: 27863501

Nott et al (2016) Histone deacetylase 3 associates with MeCP2 to regulate FOXO and social behavior. Nat Neurosci 19 1497 PMID: 27428650

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Topalovski et al (2016) Hypoxia and Transforming Growth Factor β Cooperate to Induce Fibulin-5 Expression in Pancreatic Cancer. J Biol Chem 291 22244 PMID: 27531748

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

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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

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Sommer et al (2018) Th17 lymphocytes induce neuronal cell death in a human iPSC-based model of Parkinson's disease. Cell Stem Cell. 23 123 PMID: 29979986

Tebbenkamp et al (2018) The 7q11.23 Protein DNAJC30 Interacts with ATP Synthase and Links Mitochondria to Brain Development. Cell 175 1088 PMID: 30318146

Mehta et al (2018) Human Huntington's Disease iPSC-Derived Cortical Neurons Display Altered Transcriptomics, Morphology, and Maturation. Cell Rep 25 1081 PMID: 30355486

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McCauley et al (2018) Derivation of Epithelial-Only Airway Organoids from Human Pluripotent Stem Cells. Curr Protoc Stem Cell Biol 45 e51 PMID: 30040246

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Surendran et al (2022) An improved protocol for generation and characterization of human-induced pluripotent stem cell-derived retinal pigment epithelium cells STAR Protoc 3 101803 PMID: 36386870

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Huang et al (2016) Generating trunk neural crest from human pluripotent stem cells. Sci Rep 6 19727 PMID: 26812940

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Growing organoids.
By Anonymous on 08/14/2023
分析类型： In Vitro
种属： Human
细胞系/组织： colorectal cancer organoids

I used the inhibitor for growing colorectal cancer organoids. Concentration is at 10 uM.

review image
Effective inhibition of TGFb family receptors.
By Paul Humphreys on 12/11/2020
分析类型： In Vitro
种属： Human
细胞系/组织： hESCs/Tc28a2s

I have used SB431542 for both selective inhibition of TGFb family receptors in TGFb activity assays and to drive differentiation of pluripotent stem cells towards mesodermal tissues.Concentration: 1nM working

If possible perform titration of SB431542 with TGFb signalling output depending upon cell type or application.

review image
Differentiation to cortical neurons.
By Julieta O'Flaherty on 12/11/2020
分析类型： In Vitro
种属： Human
细胞系/组织： Induced pluripotent stem cells

I routinely use this product to differentiate human induced pluripotent stem cells into cortical neurons. I use it at 10uM. Once reconstituted, I would only store it for a maximum of one month in -80C

Keep at -80C for a maximum of 1 month

review image
iPSC differentiation.
By Stephanie Hsiao on 10/13/2020
分析类型： In Vitro
种属： Human
细胞系/组织： iPSC

Differentiation of human iPSCs into hematopoietic progenitor cells

iPSC culture medium with 4 uM SB431542

review image
For hPSC culture.
By Anonymous on 06/30/2020
分析类型： In Vitro
种属： Human
细胞系/组织： Human PSC

For hPSC culture, final concentration 10 μM.

Make 100µl aliquots and keep them at −20 °C for up to 6 months.

review image
Dífferentiation of iPSC into neural progentor cells.
By Vladimir Milenkovic on 01/15/2020
分析类型： In Vitro
种属： Human
细胞系/组织： iPSC

Human induced pluripotent stem cells (iPSCs) were differentiated into neural progenitor cells (NPCs) as described in Chambers et al. 2009 (PMID: 19252484.) SB431542 was used at 20uM. Differentiated NPCs were then immunostained using PAX6 monoclonal Ab, and we had over 80% of PAX6 positive cells.

review image
endothelial differentiation.
By Anonymous on 05/01/2018
分析类型： In Vitro
种属： Human
细胞系/组织： stem cells differentiated endothelial cells

Stems cells undergoing differentiation to endothelial cells utilize addition of SB 431542. FLK+ve cells cultured with SB 431542 revealed colonies of endothelial cells (arrows)

review image
Works great..
By Anonymous on 01/04/2018
分析类型： In Vitro
种属： Human
细胞系/组织： Induced pluripotent stem cells

I used this product for differentiation of iPSCs into dopaminergic neurons according to the protocol published in Kriks et al, 2011.I used the concentration 10uM and it works really well.

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Stem Cell Research Product Guide

Stem Cell Research Product Guide

This product guide provides a background to the use of small molecules in stem cell research and lists over 200 products for use in:

  • Self-renewal and Maintenance
  • Differentiation
  • Reprogramming
  • Organoid Generation
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Stem Cells Scientific Review

Stem Cells Scientific Review

Written by Kirsty E. Clarke, Victoria B. Christie, Andy Whiting and Stefan A. Przyborski, this review provides an overview of the use of small molecules in the control of stem cell growth and differentiation. Key signaling pathways are highlighted, and the regulation of ES cell self-renewal and somatic cell reprogramming is discussed. Compounds available from Tocris are listed.

Stem Cells Poster

Stem Cells Poster

Written by Rebecca Quelch and Stefan Przyborski from Durham University (UK), this poster describes the isolation of pluripotent stem cells, their maintenance in culture, differentiation, and the generation and potential uses of organoids.

Pathways for SB 431542

TGF-β Signaling Pathway

TGF-β Signaling Pathway

The TGF-β signaling pathway is involved in the regulation of growth and proliferation of cells along with migration, differentiation and apoptosis.