Hotline:400-820-3792
Inhibitors?ScreeningLibraries?Proteins
www.MedChemE
RIP1-IN-1
Cat.No.:HY-173185
分?式:C??H??N?O?
分?量:423.46
作?靶点:RIPkinase;Necroptosis
作?通路:Apoptosis
储存?式:Pleasestoretheproductundertherecommendedconditionsin
theCertificateofAnalysis.
BIOLOGICALACTIVITY
?物活性RIP1-IN-1是?种?服有效的RIP1抑制剂,具有很强的RIP1结合亲和?(Kd:110nM)。RIP1-IN-1表现出很
强的抗坏死性凋亡(Necroptosis)活性。RIP1-IN-1通过阻断RIP1、RIP3和MLKL信号通路的磷酸化有效抑制
坏死?体的形成。RIP1-IN-1可抑制坏死性凋亡,可?于急性肝损伤的研究。
IC50TargetRIPK1
110nM(Kd)
体外研究RIP1-IN-1(CompoundN-1)(0-1.6μM,5-24h)caneffectivelyanddose-dependentlyinhibitZ-VAD-FMK(HY-
16658B)inducednecroptosisinHT-29cells,aswellasZ-VAD-FMK(HY-16658B)inducednecroptosisin
U937cells[1].
RIP1-IN-1exhibitsstronganti-necroptosisactivityinHT-29cells(CC50:50μMEC50:8.8nM)[1].
RIP1-IN-1(0.4μM,2-6h)effectivelypreventsthephosphorylationofbothRIP1andRIP3inHT-29cells
treatedwithZ-VAD-FMK(HY-16658B)inatime-dependentmanner,therebyinhibitingthephosphorylationof
thedownstreamtargetMLKL[1].
RIP1-IN-1(0.097-400nM,5h)inhibitsRIP1/3andMLKLphosphorylationinadose-responsivemanner[1].