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Submit ReviewGW 788388 is a potent inhibitor of transforming growth factor-β type I receptor (ALK5) (IC50 values are 18 and 93 nM for ALK5 binding and for TGF-β cellular assay respectively). Inhibits esophageal squamous cell carcinoma (ESCC)-induced neoangiogenesis. Reduces renal fibrosis in vivo. Orally active.
Sold for research purposes under agreement from GlaxoSmithKline
GW 788388 is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen Stem Cell Library. 了解 Tocris 化合物库的更多信息。
分子量 | 425.48 |
公式 | C25H23N5O2 |
储存 | Store at +4°C |
纯度 | ≥98% (HPLC) |
CAS Number | 452342-67-5 |
PubChem ID | 10202642 |
InChI Key | SAGZIBJAQGBRQA-UHFFFAOYSA-N |
Smiles | O=C(NC5CCOCC5)C(C=C4)=CC=C4C1=CC(C2=CNN=C2C3=CC=CC=N3)=CC=N1 |
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 | 42.55 | 100 |
以下数据基于产品分子量 425.48。 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 | 2.35 mL | 11.75 mL | 23.5 mL |
5 mM | 0.47 mL | 2.35 mL | 4.7 mL |
10 mM | 0.24 mL | 1.18 mL | 2.35 mL |
50 mM | 0.05 mL | 0.24 mL | 0.47 mL |
参考文献是支持产品生物活性的出版物。
Tan et al (2010) Targeted inhibition of AVNreceptor-like kinase 5 signaling attenuates cardiac dysfunction following myocardial infarction. Am.J.Physiol.Heart Circ.Physiol. 298 H1415 PMID: 20154262
Noma et al (2008) The essential role of fibroblasts in esophageal squamous carcinoma-induced angiogenesis. Gastroenterology 134 1981 PMID: 18439605
Gellibert et al (2006) Discovery of 4-{4-[3-(pyridin-2-yl)-1H-pyrazol-4-yl]pyridin-2-yl}-N-(tetrahydro-2H- pyran-4-yl)benzamide (GW788388): a potent, selective, and orally active transforming growth factor-β type I receptor inhibitor. J.Med.Chem. 49 2210 PMID: 16570917
Petersen et al (2008) Oral administration of GW788388, an inhibitor of TGF-beta type I and II receptor kinases, decreases renal fibrosis. Kidney Int. 73 705 PMID: 18075500
If you know of a relevant reference for GW 788388, please let us know.
关键词: GW 788388, GW 788388 supplier, GW788388, transforming, growth, factor, type, I, receptors, tgfbeta, tgfb, tgfβ, inhibitors, inhibits, TGF-βRI, TGF-beta, Receptors, 3264, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 GW 788388 的部分引用包括:
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
Castillero et al (2015) Cardiac myostatin upregulation occurs immediately after myocardial ischemia and is involved in skeletal muscle activation of atrophy. Biochem Biophys Res Commun 457 106 PMID: 25528587
Roux et al (2016) Transforming Growth Factor Beta 1 Modulates the Functional Expression of the Neurokinin-1 Receptor in Human Keratocytes. Curr Eye Res 41 1035 PMID: 26673553
Jajosky et al (2014) RepSox slows decay of CD34+ acute myeloid leukemia cells and decreases T cell immunoglobulin mucin-3 expression. Stem Cells Transl Med 3 836 PMID: 24855276
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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.