YK-3-237-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEYK-3-237Cat.No.:HY-19634CASNo.:1215281-19-8分?式:C??H??BO?分?量:372.18作?靶點(diǎn):Sirtuin作?通路:CellCycle/DNADamage;Epigenetics儲存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實(shí)驗(yàn)DMSO:100mg/mL(268.69mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM2.6869mL13.4344mL26.8687mL5mM0.5374mL2.6869mL5.3737mL10mM0.2687mL1.3434mL2.6869mL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。-80°C儲存時(shí)，請?jiān)?個(gè)?內(nèi)使?，-20°C儲存時(shí)，請?jiān)?個(gè)?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>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.5mg/mL(6.72mM);Clearsolution1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE2.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(6.72mM);ClearsolutionBIOLOGICALACTIVITY?物活性YK-3-237?種SIRT1激活劑，靶向突變體p53。YK-3-237抑制三性乳腺癌細(xì)胞的增殖[1]。IC50&TargetSIRT1體外研究YK-3-237exhibitstheanti-proliferativeactivitiestowardmostofthebreastcancercelllinestestedatsubmicromolarconcentration.YK-3-237preferentiallyinhibitstheproliferationofbreastcancercelllinescarryingmtp53[1].YK-3-237inhibitstheproliferationoftriple-negativebreastcancer(TNBC)HS578T,MDA-MB-453,SUM1315MO2,SUM149PT,BT549,MDA-MB-231,MDA-MB-436,MDA-MB-468,HCC1937withIC50sof0.160±0.043,0.241±0.086,0.253±0.028,0.289±0.066,0.353±0.017,0.431±0.136,0.501±0.062,1.436±0.754,5.031±2.010μM,respectively[1].YK-3-237inhibitstheproliferationofLuminalT47D,MCF7,andZR-75-1withIC50sof1.573±0.370,2.402±0.256,3.822±0.967μM,respectively[1].YK-3-237inhibitstheproliferationofHER2BT474andSK-BR-3withIC50sof1.249±0.372and0.346±0.066μM,respectively[1].YK-3-237(0.01-10μM;24hours)deacetylatesmtp53inTNBCcelllines[1].YK-3-237isapotentactivatorofSirt1,ontheactivationofrenalinterstitialfibroblastsusingNRK-49Fcells[2].ExposureofcellstoYK-3-237alsosignificantlyreducesexpressionofα-SMAandfibronectininadose-dependentmanner,withthemaximuminhibitionoccurringat10μM[2].CellViabilityAssay[1]CellLine:BT549,MDA-MB-468,HS578T,SUM149PTConcentration:0,0.01,0.03,0.1,0.3,1,3,10μMIncubationTime:24hoursResult:ReducedboththeacetylationofK382andthelevelofmtp53inadose-dependentmannerinmtp53TNBCcelllines.REFERENCES[1].YongWeonYi,etal.Targetingmutantp53byaSIRT1activatorYK-3-237inhibitstheproliferationoftriple-negativebreastcancercells.Oncotarget.2013Jul;4(7):984-94.[2].MurugavelPonnusamy,etal.ActivationofSirtuin-1PromotesRenalFibroblastActivationandAggravatesRenalFibrogenesis.JPharmacolExpTher.2015Aug;354(2):142-51.McePdfHeight2/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemECaution:Producthasnotbeenfullyvalidatedf