STAT3-CAIX-IN-1-生命科學(xué)試劑-MCE_第1頁
STAT3-CAIX-IN-1-生命科學(xué)試劑-MCE_第2頁
STAT3-CAIX-IN-1-生命科學(xué)試劑-MCE_第3頁
全文預(yù)覽已結(jié)束

下載本文檔

版權(quán)說明:本文檔由用戶提供并上傳,收益歸屬內(nèi)容提供方,若內(nèi)容存在侵權(quán),請進(jìn)行舉報(bào)或認(rèn)領(lǐng)

文檔簡介

Hotline:400-820-3792Inhibitors ? ScreeningLibraries ? Proteinswww.MedChemESTAT3/CAIX-IN-1Cat.No.:HY-174457CASNo.:3053583-60-8分子式:C??H??F?N?O?S?分子量:687.63作用靶點(diǎn):STAT;CarbonicAnhydrase;Ferroptosis;Apoptosis;ReactiveOxygenSpecies(ROS);Caspase;Bcl-2Family作用通路:JAK/STATSignaling;StemCell/Wnt;MetabolicEnzyme/Protease;Apoptosis;Immunology/Inflammation;NF-κB儲(chǔ)存方式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY生物活性 STAT3/CAIX-IN-1是STAT3(Kd:60.03μM)和CAIX(IC50:80.45nM)的雙靶點(diǎn)抑制劑。STAT3/CAIX-IN-1通過增加活性氧(ROS)和脂質(zhì)過氧化物的水平來誘導(dǎo)鐵死亡(ferroptosis)。STAT3/CAIX-IN-1抑制細(xì)胞遷移,誘導(dǎo)細(xì)胞凋亡(apoptosis),并導(dǎo)致MDA-MB-231細(xì)胞周期停滯。STAT3/CAIX-IN-1可用于三陰性乳腺癌(TNBC)的研究[1]。IC50&TargetCAIXhCAVBhCAIISTAT380.45nM(IC50)25.40nM(IC50)349.30nM(IC50)60.03μM(Kd)體外研究STAT3/CAIX-IN-1(Compound7m)(2-8μM,24h)inhibitsSTAT3phosphorylationinMDA-MB-231cells[1].STAT3/CAIX-IN-1(4μM)bindstoSTAT3toenhanceitsstability[1].STAT3/CAIX-IN-1enhancesproliferationinhibitionoftumorcelllineswithIC50sof2.18μM(hypoxia)and4.21μM(normoxia)intheMDA-MB-231cellline[1].STAT3/CAIX-IN-1(4μM,8μM,24h)inducesferroptosisviatheGPX4pathway,increasesreactiveoxygenspecies(ROS)levels,upregulatesintracellularlipidperoxidationinMDA-MB-231cells[1].STAT3/CAIX-IN-1(2μM,4μM,24-48h)inhibitsthemigrationofMDA-MB-231cells[1].STAT3/CAIX-IN-1(4μM,8μM,24h)inducesapoptosisinMDA-MB-231cells,inducescellcyclearrestinMDA-MB-231cellsattheG1/Sphase[1].STAT3/CAIX-IN-1hasanti-tumoractivitywithIC50sof4.21μM(MDA-MB-231),5.67μM(MCF-7),6.60μM(MDA-MB-231/ADR),14.19μM(MCF-10A)[1].WesternBlotAnalysis[1]1/3 MasterofBioactiveMolecules—您身邊的抑制劑大師www.MedChemECellLine:MDA-MB-231cellsConcentration:2,4,8μMIncubationTime:24hResult:InhibitedthelevelsofpSTAT3-S727andpSTAT3-Y705.Nochangedp-JAK1levels.ReducedGPX4levels.DownregulatedtheexpressionofBcl-2andCyclinD1.CellCycleAnalysis[1]CellLine:MDA-MB-231cellsConcentration:4,8μMIncubationTime:24hResult:AccumulatedinG1phasecells,downregulatedSphasecells.ApoptosisAnalysis[1]CellLine:MDA-MB-231cellsConcentration:4,8μMIncubationTime:24hResult:InducedapoptosisinMDA-MB-231cells.CellMigrationAssay[1]CellLine:MDA-MB-231cellsConcentration:2,4,8μMIncubationTime:24h,48hResult:Reducedmobility.體內(nèi)研究STAT3/CAIX-IN-1(Compound7m)(5mg/kg,10mg/kg,48h)showsanti-tumoractivitywith75%TIR,notchangesweightorbehavior[1].STAT3/CAIX-IN-1(10mg/kg,i.p.,21days,every2days)reducesphosphorylatedSTAT3expressioninBalb/cnudemousexenograftexperiments[1].STAT3/CAIX-IN-1(5mg/kg,10mg/kg,i.p.,21days,every2days)inhibitstumorgrowthonBalb/cnudemicewithMDA-MB-231xenografttumors[1].2/3 MasterofBioactiveMolecules—您身邊的抑制劑大師www.MedChemEAnimalModel:Balb/cnudemicewithMDA-MB-231xenografttumors[1].Dosage:10mg/kgAdministration:i.p.,21days,every2daysResult:ReducedthefluorescenceintensityofpSTAT3-S727(greenfluorescence)andpSTAT3-Y705(redfluorescence).REFERENCESChenL,etal.DiscoveryofDiarylPiperidone-SulfonamideasaNovelDual-TargetInhibitorofSTAT3/CAIXInducingFerroptosisinTriple-NegativeBreastCancerCells.JMedChem.2025Jun26;68(12):12493-12512.McePdfHeightCaution:Producthasnotbeenf

溫馨提示

  • 1. 本站所有資源如無特殊說明,都需要本地電腦安裝OFFICE2007和PDF閱讀器。圖紙軟件為CAD,CAXA,PROE,UG,SolidWorks等.壓縮文件請下載最新的WinRAR軟件解壓。
  • 2. 本站的文檔不包含任何第三方提供的附件圖紙等,如果需要附件,請聯(lián)系上傳者。文件的所有權(quán)益歸上傳用戶所有。
  • 3. 本站RAR壓縮包中若帶圖紙,網(wǎng)頁內(nèi)容里面會(huì)有圖紙預(yù)覽,若沒有圖紙預(yù)覽就沒有圖紙。
  • 4. 未經(jīng)權(quán)益所有人同意不得將文件中的內(nèi)容挪作商業(yè)或盈利用途。
  • 5. 人人文庫網(wǎng)僅提供信息存儲(chǔ)空間,僅對用戶上傳內(nèi)容的表現(xiàn)方式做保護(hù)處理,對用戶上傳分享的文檔內(nèi)容本身不做任何修改或編輯,并不能對任何下載內(nèi)容負(fù)責(zé)。
  • 6. 下載文件中如有侵權(quán)或不適當(dāng)內(nèi)容,請與我們聯(lián)系,我們立即糾正。
  • 7. 本站不保證下載資源的準(zhǔn)確性、安全性和完整性, 同時(shí)也不承擔(dān)用戶因使用這些下載資源對自己和他人造成任何形式的傷害或損失。

最新文檔

評論

0/150

提交評論