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Submit ReviewA 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)
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.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
DMSO | 21.08 | 50 |
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.
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 |
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
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If you know of a relevant reference for A 83-01, please let us know.
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
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:
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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
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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
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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
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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
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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
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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
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To grow primary basal cells
Used in expansion medium for culturing liver organoids
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
Cells are treated with 1 mM A83-01 to inhibit canonical TGFB signaling
2 μM A83–01
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)
add to cell culture to do 3d culture
used it to grow primary basal cells
used it to grow human airway basal 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
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*请注意,Tocris 仅会向正规科研企业/机构地址发送文献。
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.