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Submit ReviewPF 670462 is a potent and selective casein kinase 1ε (CK1ε) and CK1δ inhibitor (IC50 values are 7.7 and 14 nM respectively) that displays > 30-fold selectivity over 42 other common kinases. Inhibits PER protein nuclear translocation (EC50 = 290 nM) causing phase shifts in circadian rhythms and attenuates methamphetamine-stimulated locomotion in vivo.
PF 670462 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 | 410.32 |
公式 | C19H20FN5.2HCl |
储存 | Desiccate at RT |
纯度 | ≥99% (HPLC) |
CAS Number | 950912-80-8 |
PubChem ID | 51049607 |
InChI Key | PSNKGVAXBSAHCH-UHFFFAOYSA-N |
Smiles | NC1=NC=CC(C2=C(C4=CC=C(F)C=C4)N=CN2C3CCCCC3)=N1.Cl.Cl |
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 | 41.03 | 100 |
以下数据基于产品分子量 410.32。 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 | 2.44 mL | 12.19 mL | 24.37 mL |
5 mM | 0.49 mL | 2.44 mL | 4.87 mL |
10 mM | 0.24 mL | 1.22 mL | 2.44 mL |
50 mM | 0.05 mL | 0.24 mL | 0.49 mL |
参考文献是支持产品生物活性的出版物。
Badura et al (2007) An inhibitor of casein kinase Iε induces phase delays in circadian rhythms under free-running and entrained conditions. J.Pharmacol.Exp.Ther. 322 730 PMID: 17502429
Bryant et al (2009) A role for casein kinase 1 epsilon in the locomotor stimulant response to metha. Psychopharmacology 203 703 PMID: 19050854
Sprose et al (2009) Inhibition of casein kinase I ε/δ produces phase shifts in the circadian rhythms of Cynomolgus monkeys. Psychopharmacology 204 735 PMID: 19277609
If you know of a relevant reference for PF 670462, please let us know.
关键词: PF 670462, PF 670462 supplier, Potent, selective, CK1ε, CK1epsilon, CK1δ, CK1delta, inhibitors, inhibits, Casein, Kinases, 1, PF670462, circadian, rhythms, Kinase, 3316, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 PF 670462 的部分引用包括:
Greer et al (2017) Lack of Casein Kinase 1 Delta Promotes Genomic Instability - The Accumulation of DNA Damage and Down-Regulation of Checkpoint Kinase 1. PLoS One 12 e0170903 PMID: 28125685
Causton et al (2015) Metabolic cycles in yeast share features conserved among circadian rhythms. Curr.Biol. 25 1056 PMID: 25866393
Zhang et al (2013) Dissociation of circadian and circatidal timekeeping in the marine crustacean Eurydice pulchra. Curr Biol 23 1863 PMID: 24076244
Schepetkin et al (2012) Identification and characterization of a novel class of c-Jun N-terminal kinase inhibitors. Mol Pharmacol 81 832 PMID: 22434859
Zhang et al (2018) Oncogenic RAS-induced CK1α drives nuclear FOXO proteolysis. Oncogene 37 363 PMID: 28945225
Krulikas et al (2018) Application of Integrated Drug Screening/Kinome Analysis to Identify Inhibitors of dFdCyd-Resistant Pancreatic Cancer Cell Growth. SLAS Discov 23 850 PMID: 29742358
Kurihara et al (2014) Alleviation of behavioral hypersensitivity in mouse models of inflammatory pain with two structurally different casein kinase 1 (CK1) inhibitors. Mol Pain 10 17 PMID: 24612480
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
Carr et al (2023) The Wnt pathway protein Dvl1 targets Somatostatin receptor 2 for lysosome-dependent degradation. J.Biol.Chem. PMID: 36965619
Cheong et al (2015) Casein kinase 1α-dependent feedback loop controls autophagy in RAS-driven cancers. J Clin Invest 125 1401 PMID: 25798617
Kaucka et al (2015) Asymmetry of VANGL2 in migrating lymphocytes as a tool to monitor activity of the mammalian WNT/planar cell polarity pathway. Cell Commun Signal 13 2 PMID: 25627785
Zantke et al (2013) Circadian and circalunar clock interactions in a marine annelid. PLoS One 5 99 PMID: 24075994
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