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Submit ReviewRepSox is a potent and selective inhibitor of the TGF-β type I receptor/ALK5 (IC50 values are 4 and 23 nM for TGF-β type I receptor autophosphorylation and binding respectively). RepSox is selective for TGF-β type I receptor over a range of kinases, including p38 MAPK, JNK1 and GSK3 (IC50 > 16 μM). Enhances the efficiency of cellular reprogramming; replaces Sox2 by inducing Nanog expression.
RepSox synthesized to Ancillary Material Grade also available.
For more information about how RepSox may be used, see our protocols: Highly Efficient Generation of CiPSCs from MEFs, Generation of β cells from hPSCs, Reprogramming MEFs into Skeletal Muscle Progenitors.
RepSox 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。
分子量 | 287.32 |
公式 | C17H13N5 |
储存 | Store at +4°C |
纯度 | ≥99% (HPLC) |
CAS Number | 446859-33-2 |
PubChem ID | 449054 |
InChI Key | LBPKYPYHDKKRFS-UHFFFAOYSA-N |
Smiles | CC1=NC(C2=NNC=C2C4=NC3=CC=CN=C3C=C4)=CC=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.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
DMSO | 28.73 | 100 | |
ethanol | 5.75 | 20 |
以下数据基于产品分子量 287.32。 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 |
---|---|---|---|
1 mM | 3.48 mL | 17.4 mL | 34.8 mL |
5 mM | 0.7 mL | 3.48 mL | 6.96 mL |
10 mM | 0.35 mL | 1.74 mL | 3.48 mL |
50 mM | 0.07 mL | 0.35 mL | 0.7 mL |
参考文献是支持产品生物活性的出版物。
Gellibert et al (2004) Identification of 1,5-naphthyridine derivatives as a novel series of potent and selective TGF-γ type I receptor inhibitors. J.Med.Chem. 47 4494 PMID: 15317461
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
Ichida et al (2009) A small-molecule inhibitor of Tgf-β signaling replaces Sox2 in reprogramming by inducing Nanog. Cell Stem Cell 5 491 PMID: 19818703
If you know of a relevant reference for RepSox, please let us know.
关键词: RepSox, RepSox supplier, potent, inhibitors, inhibits, TGF-βRI, TGF-β, TGF-betaRI, TGFbRI, TGFbR1, tgf-b1ALK5, ALK, Receptors, Receptor-like, Kinase, Serine/Threonine, Kinases, RSTKs, Transforming, Growth, Factors, Beta, stem, cells, SJN2511, 5, inhibitor, II, RepSox, E-616452, SJN251, SJN, 2511, ALK5, Inhibitor, TGF-beta, Stem, Cell, Reprogramming, Organoids, 3742, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 RepSox 的部分引用包括:
Mou et al (2016) Dual SMAD Signaling Inhibition Enables Long-Term Expansion of Diverse Epithelial Basal Cells Cell: Stem Cell 19 217 PMID: 27320041
Zhou et al (2013) GARP-TGF-β complexes negatively regulate regulatory T cell development and maintenance of peripheral CD4+ T cells in vivo. J Immunol 190 5057 PMID: 23576681
Peter D et al (2022) Preventing VEGF-Mediated Vascular Permeability by Experimentally Potentiating BBB Characteristics in Endothelial Cells. Methods Mol Biol 2475 259-274 PMID: 35451764
Li et al (2013) Flow-based pipeline for systematic modulation and analysis of 3D tumor microenvironments. Am J Physiol Renal Physiol 13 1969 PMID: 23563587
Yusuke et al (2023) Generation of induced pluripotent stem cell-derived beta-cells in blood amino acids-like medium. Biol Open 12 PMID: 36811942
Segal et al (2019) Single cell analysis of human foetal liver captures the transcriptional profile of hepatobiliary hybrid progenitors. Nat Commun 10 3350 PMID: 31350390
Lichtenberger et al (2016) Epidermal β-catenin activation remodels the dermis via paracrine signalling to distinct fibroblast lineages. Nat Commun 7 10537 PMID: 26837596
Alon et al (2015) Differential TGF-β Signaling in Glial Subsets Underlies IL-6-Mediated Epileptogenesis in Mice. J Immunol 195 1713-22 PMID: 26136430
Yung et al (2019) Sufu- And Spop-mediated downregulation of Hedgehog signaling promotes beta cell differentiation through organ-specific niche signals. Nat.Commun. 10 4647 PMID: 31604927
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Mice received a dose of 1 μmol RepSox or vehicle only topically onto the back skin.
Mouse primary fibroblasts also treat with RepSox 25 μM.
The following protocols feature additional information for the use of RepSox (Cat. No. 3742).
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.