minus-Blebbistatin-S-minus-Blebbistatin-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemE(-)-BlebbistatinCat.No.:HY-13441CASNo.:856925-71-8Synonyms:(S)-(-)-Blebbistatin分⼦式:C₁₈H₁₆N₂O₂分⼦量:292.33作⽤靶点:Myosin作⽤通路:Cytoskeleton储存⽅式:4°C,storedundernitrogen*该产品在溶液状态不稳定，建议您现⽤现配，即刻使⽤。溶解性数据体外实验DMSO:10mg/mL(34.21mM;Needultrasonic)H2O:<0.1mg/mL(insoluble)MassSolvent1mg5mg10mgConcentration制备储备液1mM3.4208mL17.1040mL34.2079mL5mM0.6842mL3.4208mL6.8416mL10mM0.3421mL1.7104mL3.4208mL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；该产品在溶液状态不稳定，建议您现⽤现配，即刻使⽤.体内实验请根据您的实验动物和给药⽅式选择适当的溶解⽅案。以下溶解⽅案都请先按照InVitro⽅式配制澄的储备液，再依次添加助溶剂：(为保证实验结果的可靠性，澄的储备液可以根据储存条件，适当保存；体内实验的⼯作液，建议您现⽤现配，当天使⽤；以下溶剂前显⽰的百分⽐指该溶剂在您配制终溶液中的体积占⽐；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的⽅式助溶)1.请依序添加每种溶剂：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥1mg/mL(3.42mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemESolubility:1mg/mL(3.42mM);Suspendedsolution;Needultrasonic3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥1mg/mL(3.42mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性(-)-Blebbistatin选择性的⾮肌⾁肌球蛋⽩II(myosinII)ATPase活性的抑制剂[1]。IC50&TargetIC50:0.5to5μM(myosinII)[1]体外研究BlebbistatinpotentlyinhibitsseveralstriatedmusclemyosinsaswellasvertebratenonmusclemyosinIIAandIIBwithIC50valuesrangingfrom0.5to5μM.Smoothmusclemyosinisonlypoorlyinhibited(IC50=80μM)[1].Blebbistatindoesnotcompetewithnucleotidebindingtotheskeletalmusclemyosinsubfragment-1.TheinhibitorpreferentiallybindstotheATPaseintermediatewithADPandphosphateboundattheactivesite,anditslowsdownphosphaterelease.Itblocksthemyosinheadsinaproductscomplexwithlowactinaffinity[2].Inculture-activatedhepaticstellatecells,blebbistatinisfoundtochangebothcellmorphologyandfunction.Stellatecellsbecomesmaller,acquireadendriticmorphologyandhavelessmyosinIIA-containingstressfibresandvinculin-containingfocaladhesions.Blebbistatinimpairssiliconewrinkleformation,reducescollagengelcontractionandblocksendothelin-1-inducedintracellularCa2+release.Itpromoteswound-inducedcellmigration[3].体内研究Blebbistatindose-dependentlyandcompletelyrelaxbothKCl-andcarbachol-inducedratdetrusorandendothelin-1-inducedhumanbladdercontraction.Pre-incubationwith10μMblebbistatinattenuatescarbacholresponsivenessby65%whileblockingelectricalfieldstimulation-inducedbladdercontractionreaching50%inhibitionat32Hz[4].PROTOCOLCellAssay[3]FreshlyisolatedHSCsarereplatedon96-wellplate.Atday3,mediumisreplacedbyserum-freemediumandcellsarestarvedovernight,treatedwithorwithoutblebbistatin(25μM)for2hfollowedbystimulationwithplatelet-derivedgrowthfactor-BB(20ng/mL).Afteranovernightincubation,theWST-1cellproliferationassayareperformed[3].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.户使⽤本产品发表的科研⽂献•AdvSci(Weinh).2022Mar3;e2104682.•AdvSci(Weinh).2020Jun17;7(15):1903583.•Theranostics.2019Apr13;9(9):2555-2571.•JCellBiol.2021Oct4;220(10):e202010118.•AnalChem.2017Oct17;89(20):10841-10849.2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemESeemorecustomervalidationsonwww.MedChemEREFERENCES[1].CristinaLucas‐Lopez,etal.AbsoluteStereochemicalAssignmentandFluorescenceTuningoftheSmallMoleculeTool,(–)‐Blebbistatin.[2].PonsaertsR,etal.ThemyosinIIATPaseinhibitorblebbistatinpreventsthrombin-inducedinhibitionofintercellularcalciumwavepropagationincornealendothelialcells.InvestOphthalmolVisSci.2008Nov;49(11):4816-27.McePdfHeightCaution: