A 83-01

Pricing Availability   Qty
说明: Selective inhibitor of TGF-βRI, ALK4 and ALK7
化学名: 3-(6-Methyl-2-pyridinyl)-N-phenyl-4-(4-quinolinyl)-1H-pyrazole-1-carbothioamide
纯度: ≥98% (HPLC)
说明书
引用文献 (84)
评论 (10)
实验方案 (1)
文献 (3)
通路 (1)

生物活性 for A 83-01

A 83-01 is a potent inhibitor of TGF-β type I receptor ALK5 kinase, type I activin/nodal receptor ALK4 and type I nodal receptor ALK7 (IC50 values are 12, 45 and 7.5 nM respectively). A 83-01 blocks phosphorylation of Smad2 and inhibits TGF-β-induced epithelial-to-mesenchymal transition. Only weakly inhibits ALK-1, -2, -3, -6 and MAPK activity. More potent than SB 431542 (Cat. No. 1614). A 83-01 inhibits differentiation of rat induced pluripotent stem cells (riPSCs) and increases clonal expansion efficiency. Helps maintain homogeneity and long-term in vitro self-renewal of human iPSCs. Also promotes neural differentiation of hPSCs as part of a chemical cocktail.

A 83-01 synthesized to Ancillary Material Grade also available.

For more information about how A 83-01 may be used, see our protocol: Converting Fibroblasts into Cardiomyocytes (9C Cocktail)

技术数据 for A 83-01

分子量 421.52
公式 C25H19N5S
储存 Store at -20°C
纯度 ≥98% (HPLC)
CAS Number 909910-43-6
PubChem ID 16218924
InChI Key HIJMSZGHKQPPJS-UHFFFAOYSA-N
Smiles S=C(NC5=CC=CC=C5)N(N=C3C4=NC(C)=CC=C4)C=C3C2=CC=NC1=CC=CC=C12

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 A 83-01

溶剂 最高浓度 mg/mL 最高浓度 mM
溶解性
DMSO 21.08 50

制备储备液 for A 83-01

以下数据基于产品分子量 421.52。 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
0.5 mM 4.74 mL 23.72 mL 47.45 mL
2.5 mM 0.95 mL 4.74 mL 9.49 mL
5 mM 0.47 mL 2.37 mL 4.74 mL
25 mM 0.09 mL 0.47 mL 0.95 mL

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产品说明书 for A 83-01

分析证书/产品说明书
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参考文献 for A 83-01

参考文献是支持产品生物活性的出版物。

Tojo et al (2005) The ALK5 inhibitor A-83-01 inhibits smad signaling and epithelial-to-mesenchymal transition by transforming growth factor-β. Cancer.Sci. 96 791 PMID: 16271073

Hoberg et al (2008) Attachment to laminin-111 facilitates transforming growth factor β-induced expression of matrix metalloproteinase-2 in synovial fibroblasts. Ann.Rheum.Dis. 66 446 PMID: 17124250

Li et al (2009) Generation of rat and human induced pluripotent stem cells by combining genetic reprogramming and chemical inhibitors. Cell Stem Cell 4 16 PMID: 19097958

Sato et al (2015) SnapShot: Growing Organoids from Stem Cells. Cell 161 1700 PMID: 26091044

Mahe et al (2014) Establishment of gastrointestinal epithelial organoids Curr.Protoc.Mouse Biol. 3 217 PMID: 25105065

Bartfeld et al (2015) In vitro expansion of human gastric epithelial stem cells and their responses to bacterial infection. Gastroenterology 148 126 PMID: 25307862

Lancaster et al (2015) Generation of Cerebral Organoids from Human Pluripotent Stem Cells Nat.Protoc. 9 2329 PMID: 25188634

Jung et al (2011) Isolation and in vitro expansion of human colonic stem cells. Nat.Med. 17 1225 PMID: 21892181

Boj et al (2015) Organoid models of human and mouse ductal pancreatic cancer. Cell 160 324 PMID: 25557080

Karthaus et al (2014) Identification of multipotent luminal progenitor cells in human prostate organoid cultures. Cells 159 163 PMID: 25201529

Koehler et al (2014) 3D mouse embryonic stem cell culture for generating inner ear organoids. Nat.Protoc. 9 1229 PMID: 24784820

Chen et al (2019) Chemically defined neural conversion of human pluripotent stem cells. Methods Mol.Biol. 1919 59 PMID: 30656621


If you know of a relevant reference for A 83-01, please let us know.

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关键词: A 83-01, A 83-01 supplier, A83-01, Selective, inhibitors, inhibits, TGF-βRI, TGF-β, TGF-betaRI, TGFbRI, TGFbR1, tgf-b1ALK4, ALK7, ALK, Receptors, Activin, Receptor-like, Kinase, Serine/Threonine, Kinases, RSTKs, Transforming, Growth, Factor, Beta, A8301, stem, cells, growth, factors, organoids, diffe, TGF-beta, BMP, and, Other, Stem, Cell, Proliferation, Organoids, Neural, Cells, 2939, Tocris Bioscience

84 篇 A 83-01 的引用文献

引用文献是使用了 Tocris 产品的出版物。 A 83-01 的部分引用包括:

Filippini et al (2019) Immunoevolution of mouse pancreatic organoid isografts from preinvasive to metastatic disease. Sci Rep 9 12286 PMID: 31439856

Tanigawa et al (2019) Activin Is Superior to BMP7 for Efficient Maintenance of Human iPSC-Derived Nephron Progenitors. Stem Cell Reports 13 322 PMID: 31378669

Crowell et al (2019) Expansion of Luminal Progenitor Cells in the Aging Mouse and Human Prostate. Cell Rep 28 1499 PMID: 31390564

Jee et al (2019) Development of Collagen-Based 3D Matrix for Gastrointestinal Tract-Derived Organoid Culture. Stem Cells Int 2019 8472712 PMID: 31312220

Genovese (2017) Enhanced Development of Skeletal Myotubes from Porcine Induced Pluripotent Stem Cells. Sci Rep 7 41833 PMID: 28165492

Okiyoneda et al (2013) Mechanism-based corrector combination restores δF508-CFTR folding and function. Nat Chem Biol 9 444 PMID: 23666117

O'Malley et al (2013) High-resolution analysis with novel cell-surface markers identifies routes to iPS cells. Nature 499 88 PMID: 23728301

Yanagida et al (2013) An in vitro expansion system for generation of human iPS cell-derived hepatic progenitor-like cells exhibiting a bipotent differentiation potential. PLoS One 8 e67541 PMID: 23935837

Hirschhorn et al (2012) Differential regulation of Smad3 and of the type II transforming growth factor-β receptor in mitosis: implications for signaling. PLoS One 7 e43459 PMID: 22927969

Rostovskaya et al (2019) Capacitation of human naïve pluripotent stem cells for multi-lineage differentiation. Development 146 PMID: 30944104

Peterson et al (2019) Activating a Reserve Neural Stem Cell Population In Vitro Enables Engraftment and Multipotency after Transplantation. Stem Cell Reports 12 680 PMID: 30930245

Saito et al (2019) Establishment of Patient-Derived Organoids and Drug Screening for Biliary Tract Carcinoma. Cell Rep 27 1265 PMID: 31018139

Mazzucchelli et al (2019) Establishment and Morphological Characterization of Patient-Derived Organoids from Breast Cancer. Biol Proced Online 21 12 PMID: 31223292

Lindesmith et al (2019) Sera Antibody Repertoire Analyses Reveal Mechanisms of Broad and Pandemic Strain Neutralizing Responses after Human Norovirus Vaccination. Immunity 50 1530 PMID: 31216462

Ranganathan et al (2019) Evaluating Shigella flexneri Pathogenesis in the Human Enteroid Model. Infect Immun 87 PMID: 30642900

Wosen et al (2019) Human Intestinal Enteroids Model MHC-II in the Gut Epithelium. Front Immunol 10 1970 PMID: 31481960

Kawamata and Ochiya (2010) Generation of genetically modified rats from embryonic stem cells. Nature 107 14223 PMID: 20660726

Chen et al (2019) Chemically Defined Neural Conversion of Human Pluripotent Stem Cells Methods Mol.Biol. 1919 59 PMID: 30656621

Liu et al (2018) CRISPR-based chromatin remodeling of the endogenous Oct4 or Sox2 locus enables reprogramming to pluripotency. Cell Stem Cell. 22 252 PMID: 29358044

Peng et al (2018) Inflammatory Cytokine TNFα Promotes the Long-Term Expansion of Primary Hepatocytes in 3D Culture. Cell 175 1607 PMID: 30500539

Rajamani et al (2018) Super-Obese Patient-Derived iPSC Hypothalamic Neurons Exhibit Obesogenic Signatures and Hormone Responses. Cell Stem Cell 22 698 PMID: 29681516

Lynch et al (2018) Submucosal Gland Myoepithelial Cells Are Reserve Stem Cells That Can Regenerate Mouse Tracheal Epithelium. Cell Stem Cell 22 653 PMID: 29656941

Wang et al (2016) Anti-tumor activity of SL4 against breast cancer cells: induction of G2/M arrest through modulation of the MAPK-dependent p21 signaling pathway. Sci Rep 6 36486 PMID: 27819344

Han et al (2022) FOXA2 drives lineage plasticity and KIT pathway activation in neuroendocrine prostate cancer. Cancer Cell 40 1306 PMID: 36332622

He et al (2022) Optimized human intestinal organoid model reveals interleukin-22-dependency of paneth cell formation. Cell Stem Cell 29 1333 PMID: 36002022

Mou et al (2016) Dual SMAD Signaling Inhibition Enables Long-Term Expansion of Diverse Epithelial Basal Cells Cell: Stem Cell 19 217 PMID: 27320041

Foulke-Abel et al (2016) Human Enteroids as a Model of Upper Small Intestinal Ion Transport Physiology and Pathophysiology. Nat Protoc 150 638 PMID: 26677983

Drost et al (2016) Organoid culture systems for prostate epithelial and cancer tissue. Proc Natl Acad Sci U S A 11 347 PMID: 26797458

Zamudio et al (2016) Inhibition of TGFβ cell signaling for limbal explant culture in serumless, defined xeno-free conditions. Exp Eye Res 145 48 PMID: 26554938

Mousavizadeh et al (2016) Angiopoietin-like 4 promotes angiogenesis in the tendon and is increased in cyclically loaded tendon fibroblasts. J Physiol 594 2971 PMID: 26670924

Weeber et al (2015) Preserved genetic diversity in organoids cultured from biopsies of human colorectal cancer metastases. Hum Mol Genet 112 13308 PMID: 26460009

Mattis et al (2015) HD iPSC-derived neural progenitors accumulate in culture and are susceptible to BDNF withdrawal due to glutamate toxicity. Exp Cell Res 24 3257 PMID: 25740845

Bras et al (2015) TGFβ loss activates ADAMTS-1-mediated EGF-dependent invasion in a model of esophageal cell invasion. Nat Genet 330 29 PMID: 25064463

Liao et al (2015) Targeted disruption of DNMT1, DNMT3A and DNMT3B in human embryonic stem cells. Cell 47 469 PMID: 25822089

Boj et al (2015) Organoid models of human and mouse ductal pancreatic cancer. Cell 160 324 PMID: 25557080

Huch et al (2015) Long-term culture of genome-stable bipotent stem cells from adult human liver. Nature 160 299 PMID: 25533785

Tsankov et al (2015) Transcription factor binding dynamics during human ES cell differentiation. Stem Cell Reports 518 344 PMID: 25693565

Kido et al (2015) CPM Is a Useful Cell Surface Marker to Isolate Expandable Bi-Potential Liver Progenitor Cells Derived from Human iPS Cells. Inflamm Bowel Dis 5 508 PMID: 26365514

Sibony et al (2015) Microbial Disruption of Autophagy Alters Expression of the RISC Component AGO2, a Critical Regulator of the miRNA Silencing Pathway. Proc Natl Acad Sci U S A 21 2778 PMID: 26332312

Yang et al (2015) Heightened potency of human pluripotent stem cell lines created by transient BMP4 exposure. Stem Cell Reports 112 E2337 PMID: 25870291

Nantasanti et al (2015) Disease Modeling and Gene Therapy of Copper Storage Disease in Canine Hepatic Organoids. Stem Cell Res 5 895 PMID: 26455412

Li et al (2014) PMA induces SnoN proteolysis and CD61 expression through an autocrine mechanism. Cell Signal 26 1369 PMID: 24637302

Jeong et al (2023) ERdj5 protects goblet cells from endoplasmic reticulum stress-mediated apoptosis under inflammatory conditions Exp Mol Med PMID: 36759578

Tata et al (2018) Myoepithelial Cells of Submucosal Glands Can Function as Reserve Stem Cells to Regenerate Airways after Injury. Cell Stem Cell 22 668 PMID: 29656943

Levardon et al (2018) Expansion of Airway Basal Cells and Generation of Polarized Epithelium. Bio Protoc 8 PMID: 30009215

Yip et al (2018) Colon organoid formation and cryptogenesis are stimulated by growth factors secreted from myofibroblasts. PLoS One 13 e0199412 PMID: 29928021

Yakoub and Sadek (2018) Development and Characterization of Human Cerebral Organoids: An Optimized Protocol. Cell Transplant 27 393 PMID: 29749250

Kashfi et al (2018) Morphological alterations of cultured human colorectal matched tumour and healthy organoids. Oncotarget 9 10572 PMID: 29535828

Roper et al (2018) Colonoscopy-based colorectal cancer modeling in mice with CRISPR-Cas9 genome editing and organoid transplantation. Nat Protoc 13 217 PMID: 29300388

Biffi et al (2018) IL-1-induced JAK/STAT signaling is antagonized by TGF-beta to shape CAF heterogeneity in pancreatic ductal adenocarcinoma. Cancer Discov PMID: 30366930

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

Bayrer et al (2018) LRH-1 mitigates intestinal inflammatory disease by maintaining epithelial homeostasis and cell survival. Nat Commun 9 4055 PMID: 30305617

Li et al (2018) COX-2-PGE2 Signaling Impairs Intestinal Epithelial Regeneration and Associates with TNF Inhibitor Responsiveness in Ulcerative Colitis. EBioMedicine 36 497 PMID: 30190207

Zhang et al (2016) Pharmacological reprogramming of fibroblasts into neural stem cells by signaling-directed transcriptional activation. Cell Stem Cell 18 PMID: 27133794

Chen et al (2021) A versatile polypharmacology platform promotes cytoprotection and viability of human pluripotent and differentiated cells. Nat.Methods 18 528 PMID: 33941937

Stanifer et al (2020) Critical Role of Type III Interferon in Controlling SARS-CoV-2 Infection in Human Intestinal Epithelial Cells Cell Rep 32 107863 PMID: 32610043

Post et al (2020) Snake venom gland organoids. Cell 180 233 PMID: 31978343

Willigen et al (2019) Folding-function relationship of the most common cystic fibrosis-causing CFTR conductance mutants. Life Sci Alliance 2 PMID: 30659068

Barros-Silva et al (2018) Single-Cell Analysis Identifies LY6D as a Marker Linking Castration-Resistant Prostate Luminal Cells to Prostate Progenitors and Cancer. Cell Rep 25 3504 PMID: 30566873

Roe et al (2017) Enhancer Reprogramming Promotes Pancreatic Cancer Metastasis. Cell 170 875 PMID: 28757253

Yang et al (2017) Establishment of mouse expanded potential stem cells. Nature 550 393 PMID: 29019987

Vermilyea et al (2017) Induced Pluripotent Stem Cell-Derived Dopaminergic Neurons from Adult Common Marmoset Fibroblasts. Stem Cells Dev 26 1225 PMID: 28635509

Pietz et al (2017) Immunopathology of childhood celiac disease-Key role of intestinal epithelial cells. PLoS One 12 e0185025 PMID: 28934294

Ma et al (2017) Organoid culture of human prostate cancer cell lines LNCaP and C4-2B. Am J Clin Exp Urol 5 25 PMID: 29181435

Roper et al (2017) In vivo genome editing and organoid transplantation models of colorectal cancer and metastasis. Nat Biotechnol 35 569 PMID: 28459449

Ruetz et al (2017) Constitutively Active SMAD2/3 Are Broad-Scope Potentiators of Transcription-Factor-Mediated Cellular Reprogramming. Cell Stem Cell 21 791 PMID: 29174331

Guo et al (2017) Epigenetic resetting of human pluripotency. Development 144 2748 PMID: 28765214

Dai et al (2015) Maintenance and neuronal differentiation of chicken induced pluripotent stem-like cells. Stem Cells Int 2014 182737 PMID: 25610469

Tan et al (2015) Amnion cell mediated immune modulation following bleo. challenge: controlling the regulatory T cell response. Stem Cell Res Ther 6 8 PMID: 25634246

Zhao et al (2015) High-efficiency reprogramming of fibroblasts into cardiomyocytes requires suppression of pro-fibrotic signalling. Nat Commun 6 8243 PMID: 26354680

Corritore et al (2014) β-Cell differentiation of human pancreatic duct-derived cells after in vitro expansion. Cell Cycle 16 456 PMID: 25437872

Boilàve et al (2013) Immunosurveillance against tetraploidization-induced colon tumorigenesis. Proc Natl Acad Sci U S A 12 473 PMID: 23324343

Kearns et al (2013) Generation of organized anterior foregut epithelia from pluripotent stem cells using small molecules. PLoS One 11 1003 PMID: 23917481

Schwank et al (2013) Generation of BAC transgenic epithelial organoids. Cell Reprogram 8 e76871 PMID: 24204693

Telugu et al (2011) Porcine induced pluripotent stem cells analogous to naïve and primed embryonic stem cells of the mouse. Int J Dev Biol 54 1703 PMID: 21305472

Raghavan et al (2021) Microenvironment drives cell state, plasticity, and drug response in pancreatic cancer. Cell 184 6119 PMID: 34890551

Tristan et al (2021) Robotic high-throughput biomanufacturing and functional differentiation of human pluripotent stem cells. Stem Cell Rep 16 3076 PMID: 34861164

Duan et al (2021) An airway organoid-based screen identifies a role for the HIF1α-glycolysis axis in SARS-CoV-2 infection. Cell Rep. 37 109920 PMID: 34731648

Kazi et al (2021) Global phosphoproteomics reveal CDK suppression as a vulnerability to KRas addiction in pancreatic cancer. Clin Cancer Res 27 4012 PMID: 33879459

Berkers et al (2019) Rectal Organoids Enable Personalized Treatment of Cystic Fibrosis. Cell Rep 26 1701 PMID: 30759382

Kanitz et al (2019) Conserved regulation of RNA processing in somatic cell reprogramming. BMC Genomics 20 100 PMID: 30704403

Muraoka et al (2019) Role of cyclooxygenase-2-mediated prostaglandin E2-prostaglandin E receptor 4 signaling in cardiac reprogramming. Nat Commun 10 674 PMID: 30787297

Huang et al (2017) Zfp281 is essential for mouse epiblast maturation through transcriptional and epigenetic control of Nodal signaling. Elife 6 PMID: 29168693

Mulas et al (2017) NODAL Secures Pluripotency upon Embryonic Stem Cell Progression from the Ground State. Stem Cell Reports 9 77 PMID: 28669603


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A 83-01 的评论

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Works perfectly.
By Toni Johansson on 04/01/2021
分析类型: In Vitro
种属: Human

To grow primary basal cells

review image

Works well with liver organoids.
By Gautam Kok on 11/19/2020
分析类型: In Vitro
种属: Human
细胞系/组织: Liver organoids

Used in expansion medium for culturing liver organoids

review image

It worked good.
By Anonymous on 07/04/2020
分析类型: In Vitro
种属: Mouse
细胞系/组织: iPSC

Reprogramming media comprises of 3 μM CHIR99021 and 0.5 μM A-83-01.

The cells were then maintained in RM 15 days with fresh media every other day

PMID: 29681516
review image

For TGFB inhibition.
By Anonymous on 06/25/2020
分析类型: In Vitro
种属: Mouse
细胞系/组织: Neural Stem Cells

Cells are treated with 1 mM A83-01 to inhibit canonical TGFB signaling

PMID: 27133794
review image

Neural Induction Conditions.
By Anonymous on 03/22/2020
分析类型: In Vitro
种属: Human
细胞系/组织: H9

2 μM A83–01

PMID: 30656621
review image

To start reprogramming, cultures were switched to reprogramming medium (ES medium supplemented with 1 mM A83-01).
By Anonymous on 12/04/2019
分析类型: In Vitro
种属: Mouse
细胞系/组织: ipsc

To start reprogramming, cultures were switched to reprogramming medium (ES medium supplemented with 10 mM Parnate, 3 mM Chir99021, 1 mM A83-01, and 10 mM Forskolin)

PMID: 29358044
review image

good for cell culture.
By Anonymous on 10/08/2019
分析类型: In Vivo
种属: Mouse
细胞系/组织: ipsc

add to cell culture to do 3d culture

参考文献
review image

works great for TGFB inhibition.
By Anonymous on 08/08/2019
分析类型: In Vitro
种属: Human

used it to grow primary basal cells

PMID: 27320041

for growing cells.
By Anonymous on 02/28/2019
分析类型: In Vitro
种属: Human

used it to grow human airway basal cells


A 83-01 Inhibit TGFb1-activated Cellular Fibrosis in Human Mϋller Cells.
By Ying Yu on 01/08/2018
分析类型: In Vitro
种属: Human
细胞系/组织: Mϋller cells

Human MOI-M1 Mϋller cells seeded in tissue culture (TC)-treated plastic plate (BD). Serum starvation by DMEM medium supplemented with 1% FBS for 24h. Pretreated Human Mϋller cell with A83-01 at 0, 0.25, 0.5, 1 and 2uM for 2h. Then added 0-10 ng/mL TGFb1 for 48h. Picro-Sirius red staining, elution, and OD 540nm measurement for the fibrosis


A 83-01 实验方案

以下实验方案包含使用 A 83-01(目录编号 2939)的更多信息。

该领域的文献

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Pathways for A 83-01

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.