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Submit ReviewIN 1130 is a potent and selective inhibitor of TGF-β type I receptor (ALK5). Inhibits Smad-2 phosphorylation (IC50 = 5.3 nM). Exhibits selectivity over a panel of 27 serine/ threonine and tyrosine kinases including P38α. Attenuates TGFβ/Smad signaling, cell migration, invasion, lung metastasis and increases survival of mice in 4TI in vivo models. Suppresses renal fibrosis in obstructive nephropathy in vivo models.
分子量 | 420.47 |
公式 | C25H20N6O |
储存 | Store at +4°C |
纯度 | ≥98% (HPLC) |
CAS Number | 868612-83-3 |
PubChem ID | 11676119 |
InChI Key | RYKSGWSKILPDDY-UHFFFAOYSA-N |
Smiles | CC1=NC(C2=C(C3=CC4=C(N=CC=N4)C=C3)NC(CC5=CC(C(N)=O)=CC=C5)=N2)=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 | 42.05 | 100 | |
1eq. HCl | 42.05 | 100 |
以下数据基于产品分子量 420.47。 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 | 2.38 mL | 11.89 mL | 23.78 mL |
5 mM | 0.48 mL | 2.38 mL | 4.76 mL |
10 mM | 0.24 mL | 1.19 mL | 2.38 mL |
50 mM | 0.05 mL | 0.24 mL | 0.48 mL |
参考文献是支持产品生物活性的出版物。
Moon et al (2006) IN-1130, a novel transforming growth factor-beta type I receptor kinase (ALK5) inhibitor, suppresses renal fibrosis in obstructive nephropathy. Kidney Int. 70 1234 PMID: 16929250
Lee et al (2008) Effect of IN-1130, a small molecule inhibitor of transforming growth factor-beta type I receptor/AVNreceptor-like kinase-5, on prostate cancer cells. J.Urol. 180 2660 PMID: 18951571
Park et al (2014) An novel inhibitor of TGF-beta type I receptor, IN-1130, blocks breast cancer lung metastasis through inhibition of epithelial-mesenchymal transition. Cancer Lett. 351 72 PMID: 24887560
If you know of a relevant reference for IN 1130, please let us know.
关键词: IN 1130, IN 1130 supplier, IN1130, potent, selective, inhibitors, inhibits, TGF-β, type, I, receptor, ALK5, Smad, breast, lung, metastasis, TGF-βRI, TGF-beta, Receptors, 6016, Tocris Bioscience
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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.