| MolecularWeight: | 560.30 |
| Formula: | C28H22Cl4N2O2 |
| Purity: | ≥98% |
| CAS#: | n/a |
| Solubility: | DMSOupto50mM |
| ChemicalName: | (3E,5E)-1-((S)-2-amino-3-phenylpropanoyl)-3,5-bis(3,4-dichlorobenzylidene)piperidin-4-one |
| Storage: | Powder:4oC1year.DMSO:4oC3month;-20oC1year. |
BIOLOGicalActivity:
RA190isanovelpotentandselectiveinhibitorofproteasomeUbiquitinreceptorRPN13/ADRM1.Itcovalentlybindstothecysteine88ofubiquitinreceptorRPN13inthe19Sregulatoryparticleandinhibitsproteasomefunction,triggeringrapidaccumulationofpolyubiquitinatedproteins.Multiplemyeloma(MM)lines,eventhoseresistanttobortezomib,weresensitivetoRA190viaendoplasmicreticulumstress-relatedapoptosis.RA190stABIlizedtargetsofhumanpapillomavirus(HPV)E6oncoprotein,andpreferentiallykilledHPV-transformedcells.Afteroralorintraperitonealdosinginmice,RA190distributedtoplasmaandmajororgansexceptthebrain,andinhibitedproteasomefunctioninskinandmuscle.RA190admiNISTrationprofoundlyreducedgrowthofMMandovariancancerxenografts,andoralRA190treatmentretardedHPV16(+)syngeneicmousetumorgrowth,withoutaffectingspontaneousHPV-specificCD8(+)Tcellresponses,suggestingitstherapeuticpotential.
HowtoUse:
Reference:
RA190_spec.pdf
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