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Discovery Antibodies/CyPPA/50 mg/C-110-50 mg

价格
¥5220.00
货号:C-110-50mg
浏览量:59
品牌:Discovery
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商品描述
Cat#:C-110
  • LyophilizedPowder
  • BioassayTested
  • SourceSynthetic
    MW:285.4
    Purity:>98%
    Effectiveconcentration1-100μM.
      • CyPPA
    ChemicalnameN-Cyclohexyl-N-[2-(3,5-dimethyl-pyrazol-1-yl)-6-methyl-4-pyrimidinamine.
    MolecularformulaC16H23N5.
    CASNo.:73029-73-9.
    ActivityCyPPAisanactivatorofsmallconductanceCa2+-activatedK+ channelsKCa2.2(SK2)andKCa2.3(SK3)withEC50 valuesof5.6and14μMforSK3andSK2respectively.ItdisplaysnoactivityatSK1andintermediateconductanceKCa(IK)channels1.CyPPAblocksTRPM7channels2.
      • Hougaard,C. etal. (2007) BrJ.Pharmacol. 151, 655.
      • Chubanov,V. etal. (2012) Br.J.Pharmacol. 166, 1357.
    ShippingandstorageShippedatroomtemperature.Productassuppliedcanbestoredintactatroomtemperatureforseveralweeks.Forlongerperiods,itshouldbestoredat-20°C.
    SolubilityDMSOorethanol.Centrifugeallproductpreparationsbeforeuse(10000xg5min).
    StorageofsolutionsUptofourweeksat4°Corthreemonthsat-20°C.
      • CyPPA
        AlomoneLabsCyPPAenhanceshSK2channelcurrentsintransientlytransfectedHEK293Tcells.
        Cellswerestimulatedwith100μM CyPPA (#C-110)andcurrentsweremeasuredusingwholecellvoltage-clamp.A.Timecourseat-20mVshowingtheeffectof100μMCyPPAanditsinhibitionwith150nM Apamin(#STA-200).B.Representativecurrentsatcontrolconditions(bottom)andfollowingapplicationof100μMCyPPA(top).Currentswereelicitedbya150msvoltagerampfrom-120to60mVevery10secondsfromaholdingpotentialof-80mV(currentresponsesareshownbetween-120and-10mV).Leaksweresubtractedoffline.
    References-Scientificbackground
    • 1.Kohler,M. etal. (1996) Science 273, 1709.
    • 2.Stocker,M. etal. (2000) MolCellNeurosci. 15,476.
    • 3.Hougaard,C. etal. (2007) BrJ.Pharmacol. 151, 655.
    • 4.Seutin,V. etal. (2007) BrJ.Pharmacol. 151, 568.
    • 5.Chubanov,V. etal. (2012) Br.J.Pharmacol. 166, 1357.
      • Ca2+-activatedpotassiumchannels(KCa)areagroupof6/7-TMionchannelsthatselectivelytransportK+ionsacrossbiologicalmembranes.Theyarebroadlyclassifiedintothreesubtypes:SK,IKandBKchannels(small,intermediateandbigconductance).

        Small-conductanceCa2+-activatedK+channels(SKchannels)underliethemediumdurationafterhyperpolarizationthatfollowssingleortrainsofactionpotentialsinmanytypesofneurons.ThisfamilyiscomposedofKCa2.1(SK1),-2.2(SK2),and-2.3(SK3)isoforms,whichareexpresseddifferentiallywithinthecentralnervoussystem(CNS)1,2.

        CyPPAisanactivatorofsmallconductanceKCa channelsthatdisplaysselectivityforSK2andSK3channels(EC50valuesare5.6and14µMforSK3andSK2respectivelyandefficacyis90%and71%forhSK3andhSK2,respectively)3.CyPPAdisplaysnoactivityatSK1andIK(KCa3.1)channels3.

        CyPPAisatoolfordistinguishingSK2andSK3fromSK1andIK;nootheragentsdistinguishthesechannelsfromoneanother.Therefore,itenrichestherepertoireoftoolsavailabletotestthehypothesisthatSKchannelsmaybetargetsforfutureCNSdrugs4.

        CyPPAwasfoundtoblockTRPM7channels,demonstratinganoverlapbetweenpharmacologicalcompoundsactingonTRPandKCachannels5.

    TargetKCa2.2,KCa2.3,TRPM7channels
    receivea5mgfreetrialsample!
    Lastupdate:02/12/2019

    CyPPA(#C-110) isahighlypure,synthetic,andbiologicallyactivecompound.

    Forresearchpurposesonly,notforhumanuse
    Discovery Antibodies的Cyclin dependant kinase 2 (CDK2) is a serine/threonine protein kinase which controls both G1/S and G2/M transitions. CDKs along with cyclins and CDK inhibitors regulate cell cycle progression. Specific cyclins activate different CDKs; in early G1, CDK2 pairs with cyclin E to promote entry into the S phase before switching to partner with cyclin A to drive the cell through S phase. Once activated CDKs phosphorylate downstream proteins to initiate signalling cascades. CDK2 phosphorylates and inactivates the RB1 (pRb) tumour suppressor family of proteins.CDK的活动受到严格控制。CDK2活性可以被包括P21在内的一系列抑制剂抑制。细胞周期失调和增殖控制的丧失与细胞转化和癌症密切相关。CDK2在DNA损伤反应(DDR)中的细胞周期停滞中也似乎起着积极作用,它的抑制作用会阻碍DDR,并使细胞对电离辐射敏感,从而诱导细胞死亡。该抗体与AlexaFluor®488偶联。AlexaFluor®488是一种流行的鲜绿色荧光染料,具有高pH稳定性。
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