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Submit ReviewD 4476 is a selective inhibitor of casein kinase 1 (CK1) and TGF-β type-I receptor (ALK5) that displays > 20-fold selectivity over SAPK2/p38 and a much greater selectivity over all other protein kinases tested. Suppresses site-specific phosphorylation and nuclear exclusion of FOXO1a.
Sold with the permission of GlaxoSmithKline
D 4476 is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen Kinase Inhibitor Library. 了解 Tocris 化合物库的更多信息。
分子量 | 398.41 |
公式 | C23H18N4O3 |
储存 | Store at +4°C |
纯度 | ≥99% (HPLC) |
CAS Number | 301836-43-1 |
PubChem ID | 6419753 |
InChI Key | DPDZHVCKYBCJHW-UHFFFAOYSA-N |
Smiles | O=C(N)C4=CC=C(C=C4)C1=NC(C2=CC(OCCO5)=C5C=C2)=C(C3=NC=CC=C3)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 | 39.84 | 100 | |
ethanol | 19.92 | 50 |
以下数据基于产品分子量 398.41。 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 | 2.51 mL | 12.55 mL | 25.1 mL |
5 mM | 0.5 mL | 2.51 mL | 5.02 mL |
10 mM | 0.25 mL | 1.25 mL | 2.51 mL |
50 mM | 0.05 mL | 0.25 mL | 0.5 mL |
参考文献是支持产品生物活性的出版物。
Callahan et al (2002) Identification of novel inhibitors of the transforming growth factor β1 (TGF-β1) type I receptor (ALK5). J.Med.Chem. 45 999 PMID: 11855979
Rena et al (2004) D4476, a cell-permeant inhibitor of CK1, suppresses the site-specific phosphorylation and nuclear exclusion of FOXO1a. EMBO Rep. 5 60 PMID: 14710188
Bain et al (2007) The selectivity of protein kinase inhibitors: a further update. Biochem.J. 408 297 PMID: 17850214
If you know of a relevant reference for D 4476, please let us know.
关键词: D 4476, D 4476 supplier, Selective, CK1, inhibits, inhibitors, TGF-βRI, TGF-β, TGF-betaRI, TGFbRI, TGFbR1, tgf-b1Casein, Kinase, 1, Kinases, Transforming, Growth, Factors, Beta, Receptors, TGF-beta, RSTK, Receptor, Serine/Threonine, RSTKs, D4476, GlaxoSmithKline, GSK, Casein, 2902, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 D 4476 的部分引用包括:
Zhang et al (2015) GSK3β-Dzip1-Rab8 cascade regulates ciliogenesis after mitosis. PLoS Biol 13 e1002129 PMID: 25860027
Qian et al (2011) Pathogen recognition receptor signaling accelerates phosphorylation-dependent degradation of IFNAR1. PLoS Pathog 7 e1002065 PMID: 21695243
Probst-Kepper et al (2009) Perspectives on Regulatory T Cell Therapies. Toxins (Basel) 36 302 PMID: 21076548
Bartley et al (2016) Mammalian FMRP S499 Is Phosphorylated by CK2 and Promotes Secondary Phosphorylation of FMRP. Eneuro 3 PMID: 27957526
Zemp et al (2014) CK1δ and CK1ε are components of human 40S subunit precursors required for cytoplasmic 40S maturation. J Cell Sci 127 1242 PMID: 24424021
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