BRD9876-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEBRD9876Cat.No.:HY-110208CASNo.:32703-82-5分?式:C??H??N?分?量:234.3作?靶點(diǎn):Kinesin;Microtubule/Tubulin作?通路:CellCycle/DNADamage;Cytoskeleton儲存?式:4°C,sealedstorage,awayfrommoisture*Insolvent:-80°C,6months;-20°C,1month(sealed

storage,awayfrommoisture)溶解性數(shù)據(jù)體外實(shí)驗(yàn)DMSO:50mg/mL(213.40mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM4.2680mL21.3402mL42.6803mL5mM0.8536mL4.2680mL8.5361mL10mM0.4268mL2.1340mL4.2680mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；?旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。儲備液的保存?式和期限：-80°C,6months;-20°C,1month(sealedstorage,awayfrommoisture)。-80°C儲存時，請?jiān)?個?內(nèi)使?，-20°C儲存時，請?jiān)?個?內(nèi)使?。體內(nèi)實(shí)驗(yàn)請根據(jù)您的實(shí)驗(yàn)動物和給藥?式選擇適當(dāng)?shù)娜芙?案。以下溶解?案都請先按照InVitro?式配制澄的儲備液，再依次添加助溶劑：(為保證實(shí)驗(yàn)結(jié)果的可靠性，澄的儲備液可以根據(jù)儲存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)的?作液，建議您現(xiàn)?現(xiàn)配，當(dāng)天使?；以下溶劑前顯?的百分?指該溶劑在您配制終溶液中的體積占?；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的?式助溶)1.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(10.67mM);Clearsolution1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEBIOLOGICALACTIVITY?物活性BRD9876?種“rigor”抑制劑，可將驅(qū)動蛋?5(Eg5)鎖定在增強(qiáng)微管(MTs)結(jié)合的狀態(tài)，從?導(dǎo)致MT的捆綁和穩(wěn)定。BRD9876與酪氨酸104殘相互作?，該殘α4-α6變構(gòu)結(jié)合?袋的?部分。BRD9876特異性靶向微管結(jié)合的Eg5，選擇性抑制CD34細(xì)胞的?髓瘤。BRD9876具有?于多發(fā)性?髓瘤(MM)研究的潛?。體外研究BRD9876(10μM;24hours)revealesrapidarrestofcellsattheG2/Mphasestartingasearlyas2hoftreatmentinMM1Scells[1].BRD9876exhibitsapproximately3-foldselectivityforMM1Smyelomacells(IC50=3.1μM)overCD34+derivedhematopoieticcells(IC50=9.1μM)[1].BRD9876(0.1,1,10,100uM)isabletoovercome,inMM1Scells,stromalresistanceofbonemarrowstromalcells(BMSCs)fromMMbonemarrowaspiratesbutonlyminimaleffectsareobservedwithBRD9876againstprimaryMMcells[1].BRD9876iscompletelyineffectiveatinhibitingthebasalATPaseactivityofEg5,incontrasttoloopL5-bindingmonastrolorα4/α6-bindingBI8whichshowsgreateractivityagainstbasalEg5ATPaseactivity[1].CellCycleAnalysis[1]CellLine:MM1ScellsandCD34hematopoieticcellsConcentration:10μMIncubationTime:24hoursResult:RevealedrapidarrestofcellsattheG2/Mphasestartingasearlyas2hoftreatmentinMM1Scells.ShowedmarkedlylessG2/MarrestinCD34hematopoieticcells.REFERENCES[1].ShrikantaChattopadhyay,etal.Niche-BasedScreeninginMultipleMyelomaIdentifiesaKinesin-5InhibitorwithImprovedSelectivityoverHematopoieticProgenitors.CellRep.2015Feb10;10(5):755-770.[2].Geng-YuanChen,etal.Eg5InhibitorsHaveContrastingEffectsonMicrotubuleStabilityandMetaphaseSpindleIntegrity.ACSChemBiol.2017Apr21;12(4):1038-1046.[3].Chieh-TingFang,etal.HSP70regulatesEg5distributionwithinthemitoticspindleandmodulatesthecytotoxicityofEg5inhibitors.CellDeathDis.2020Sep1;11(8):715.[4].AnkeMaes,etal.Thetherapeuticpotentialofcellcycletargetinginmultiplemyeloma.Oncotarget.2017Jun28;8(52):90501-90520.McePdfHeightCaution:Producthasnotbeenfullyvalidatedfor