GBR-12935-dihydrochloride-SDS-MedChemExpress.pdf
《GBR-12935-dihydrochloride-SDS-MedChemExpress.pdf》由会员分享,可在线阅读,更多相关《GBR-12935-dihydrochloride-SDS-MedChemExpress.pdf(5页珍藏版)》请在文库网上搜索。
1、CID755673Cat. No.: HY-12239CAS No.: 521937-07-5Molecular Formula: CHNOMolecular Weight: 217.22Target: PKDPathway: ApoptosisStorage: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 monthSolvent PKD3, IC50: 227 nM; PKD2, IC50: 280 nMIn Vitro CID755673 exhibits selective PKD1 inhibition whe
2、n compared with AKT, polo-like kinase 1 (PLK1), CDK activating kinase (CAK), CAMKII, and three different PKC isoforms. It is not competitive with ATP for enzyme inhibition. CID755673 blocks phorbol ester-induced endogenous PKD1 activation in LNCaP cells in a concentration-dependent manner. CID755673
3、 inhibitS the known biological actions of PKD1 including phorbol ester-induced class IIa histone deacetylase 5 nuclear exclusion, vesicular stomatitis virus glycoprotein transport from the Golgi to the plasma membrane, and the ilimaquinone-induced Golgi fragmentation. CID755673 inhibits prostate can
4、cer cell proliferation, cell migration, and invasion1.Product Data Sheet InhibitorsAgonistsScreening Librarieswww.MedChemE1In Vivo Acute administration of the PKD inhibitor CID755673 to normal mice reduces both PKD1 and 2 phosphorylation in a time and dose-dependent manner. Chronic CID755673 adminis
5、tration to T2D db/db mice for two weeks reduces expression of the gene expression signature of PKD activation, enhances indices of both diastolic and systolic left ventricular function and is associated with reduced heart weight2.PROTOCOLKinase Assay 1 The radiometric kinase assay is carried out by
6、coincubating 0.5 Ci of -32PATP, 20 M ATP, 50 ng of purified recombinant human PKD (PKD1, PKD2, and PKD3) or CAMKII proteins, and 2.5 g of Syntide-2 in 50 L of kinase buffer that contains 50 mM Tris-HCl, pH 7.5, 4 mM MgCl2, 10 mM -mercaptoethanol. The reaction is carried out under conditions that the
7、 initial rate is within the linear kinetic range1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Cell Assay 1 The wound-induced migration is triggered by scraping the cells with a plastic pipette tip, and the wound is imaged immediately. The DU145 cell
8、s are then are treated with or without CID755673 at different concentrations. The wound is imaged immediately (0 h) and at different intervals with an inverted phase-contrast microscope with a 10 objective. At the end of the assay, cells are fixed with methanol and stained with crystal violet for a
9、final image1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Animal Administration 2Mice: For acute inhibitor studies, C57BL6 mice are administered a single dose of vehicle (5% DMSO in PBS, pH 7.4), or the selective PKD inhibitor CID755673 at 1 or 10mg/
10、kg body weight. Mice are killed one or four hr later and heart collected for later analysis. For chronic inhibitor experiments, 8-week old db/db mice receives vehicle or CID755673 at 1 or 10mg/kg bodyweight for 16 days, by daily intraperitoneal (i.p.) injection2.MCE has not independently confirmed t
11、he accuracy of these methods. They are for reference only.CUSTOMER VALIDATIONSee more customer validations on www.MedChemEREFERENCES1. Sharlow ER, et al. Potent and selective disruption of protein kinase D functionality by a benzoxoloazepinolone. J Biol Chem. 2008 Nov 28;283(48):33516-26.2. Venardos
12、 K, et al. The PKD inhibitor CID755673 enhances cardiac function in diabetic db/db mice. PLoS One. 2015 Mar 23;10(3):e0120934.3. YangLei, et al. Regulation of protein kinase D1 on the expression of eNOS and Ang1 in myocardium of rats with myocardial infartion. Journal of Jinan University (Natural Sc
13、ience 10(7):10528-10534 Chinese Journal of Pathophysiology. 2016null32(1):146-150null155. Journal of Jinan University (Natural Science & Medicine Edition). 2015 Dec 36 (6). Harvard Medical School LINCS LIBRARYwww.MedChemE2Caution: Product has not been fully validated for medical applications. For re
14、search Inhibitors, Agonists, Screening Librarieswww.MedChemESafety Data SheetRevision Date:Oct.-10-2018Print Date: Oct.-10-20181. PRODUCT AND COMPANY IDENTIFICATION1.1 Product identifierProduct name : CID755673Catalog No. : HY-12239CAS No. : 521937-07-51.2 Relevant identified uses of the substance o
15、r mixture and uses advised againstIdentified uses : Laboratory chemicals, manufacture of substances.1.3 Details of the supplier of the safety data sheetCompany: MedChemExpress USATel: 609-228-6898Fax: 609-228-5909E-mail: 1.4 Emergency telephone numberEmergency Phone #: 609-228-68982. HAZARDS IDENTIF
- 配套讲稿:
如PPT文件的首页显示word图标,表示该PPT已包含配套word讲稿。双击word图标可打开word文档。
- 特殊限制:
部分文档作品中含有的国旗、国徽等图片,仅作为作品整体效果示例展示,禁止商用。设计者仅对作品中独创性部分享有著作权。
- 关 键 词:
- GBR 12935 dihydrochloride SDS MedChemExpress