| 生物活性： |
靶点：PKD
通路：Apoptosis
背景说明：CID755673是一种具有细胞活性的泛PKD1/2/3抑制剂。
生物活性：CID755673 is a potent PKD inhibitor with IC50s of 182 nM， 280 nM and 227 nM for PKD1， PKD2 and PKD3， respectively.[1-2]
In Vitro：CID755673 blocks phorbol ester-induced endogenous PKD1 activation in LNCaP cells in a concentration-dependent manner. CID755673 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 cancer cell proliferation， cell migration， and invasion[1].
In 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 administration 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 weight[2].
细胞实验：The wound-induced migration is triggered by scraping the cells with a plastic pipette tip， and the wound is imaged immediately. The DU145 cells 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 final image[1].
动物实验：Mice: 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/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.) injection[2].
激酶实验：The radiometric kinase assay is carried out by coincubating 0.5 μCi of [γ-32P]ATP， 20 μM ATP， 50 ng of purified recombinant human PKD (PKD1， PKD2， and PKD3) or CAMKIIα proteins， and 2.5 μg of Syntide-2 in 50 μL of kinase buffer that contains 50 mM Tris-HCl， pH 7.5， 4 mM MgCl2， 10 mM β-mercaptoethanol. The reaction is carried out under conditions that the initial rate is within the linear kinetic range[1].
数据来源文献：[1]. 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 K， et al. The PKD inhibitor CID755673 enhances cardiac function in diabetic db/db mice. PLoS One. 2015 Mar 23;10(3):e0120934.
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| 其它标识： |
EC：EINECS 604-604-1
MDL：MFCD03828155
SMILES：O=C1NCCCC2=C1OC3=CC=C(O)C=C32
InChIKey：AACFPJSJOWQNBN-UHFFFAOYSA-N
InChI：InChI=1S/C12H11NO3/c14-7-3-4-10-9(6-7)8-2-1-5-13-12(15)11(8)16-10/h3-4,6,14H,1-2,5H2,(H,13,15)
PubChem CID：755673
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| 基本信息： |
CAS：521937-07-5
英文名称：CID755673
别名：2,3,4,5-四氢-7-羟基-1H-苯并呋喃并[2,3-C]氮杂卓-1-酮
分子式：C12H11NO3
分子量：217.22
规格：10mg ; 25mg ; 50mg ; 5mg
溶解性：Soluble in DMSO
纯度：≥98%
外观(性状)：White to off-white Solid
储存条件：Powder:2-8℃，2 years;Insolvent(母液):-20℃，6 months;-80℃，1 year
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| 靶点： |
PKD |
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