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1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemECasein Kinase II Inhibitor IVCat. No.: HY-111378CAS No.: 863598-09-8分式: CHNO分量: 429.47作靶点: Casein Kinase作通路: Cell Cycle/DNA Damage; Stem Cell/Wnt储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 DMS
2、O : 250 mg/mL (582.11 mM)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 2.3285 mL 11.6423 mL 23.2845 mL5 mM 0.4657 mL 2.3285 mL 4.6569 mL10 mM 0.2328 mL 1.1642 mL 2.3285 mL请根据产品在不同溶剂中的溶解度,选择合适的溶剂配制储备液,并请注意储备液的保存式和期限。BIOLOGICAL ACTIVITY物活性 Casein Kinase II
3、Inhibitor IV表质形成细胞分化的分诱导剂。IC50 & Target Target: Casein Kinase 1体外研究Treatment of human epidermal keratinocytes (NHEKs) with Casein Kinase II Inhibitor IV leads to an increasein the early differentiation markers keratins 1 and 10 at 48 h. Increased levels of IVL and TGM are observed1/2 Master of Small
4、 Molecules 您边的抑制剂师www.MedChemEin cells treated with Casein Kinase II Inhibitor IV at 72 h and persisted at 96 h. In addition, treated withCasein Kinase II Inhibitor IV expressesloricrin, a terminal differentiation marker, at later time points. Similarresults are observed by messenger RNA (mRNA) expr
5、ession analysis of NHEKs treated with Casein KinaseII Inhibitor IV. At early time points (12 and 24 h), treatment with Casein Kinase II Inhibitor IV leads to theupregulation of keratinocyte early differentiation marker genes, including keratin 1 (5.4-fold) and keratin 10(5.4-fold). Terminal differen
6、tiation marker genes, including IVL (1.8-fold), TGM 1 (4.8-fold), loricrin (3.3-fold),and filaggrin (5.6-fold), are upregulated at late time points (36 and 48 h). These results are again consistentwith the ability of Casein Kinase II Inhibitor IV to induce differentiation of epidermal progenitor cel
7、ls intoterminally differentiated keratinocytes 1.PROTOCOLKinase Assay 1 For reporter gene assays with transiently transfected cells, the cells are typically transfected in 150 mm-diamdishes when 30-40% confluent. A reporter plasmid, pGL3/3.7 kbp-IVLLuc plasmid, is transfected into theNHEKs. After 24
8、 h, the transfected cells are plated into 96-well assay plates and treated with compound(Casein Kinase II Inhibitor IV) to a final concentration of 5 M. After incubation for 2 d, reporter gene activityis measured using the Bright-Glo luciferase assay system 1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.REFERENCES1. Hong J, et al. Identification and characterization of small-molecule inducers of epidermal keratinocyte differentiation. ACS Chem Biol.2007 Mar 20;2(3):171-5.McePdfHeightCaution: Product has not been fully validated for medical a
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