

MolecularWeight: | 334.33 |
Formula: | C19H14N2O4 |
Purity: | ≥98% |
CAS#: | 48208-26-0 |
Solubility: | DMSOupto100mM |
ChemicalName: | (S)-2-(1,3-dioxoisoindolin-2-yl)-3-(1H-indol-3-yl)propanoicacid |
Storage: | Powder:4oC1year.DMSO:4oC3month;-20oC1year. |
BIOLOGicalActivity:
RG108isapotent,selectiveandcellpermeableinhibitorofDNAmethyltransferase.Unlike5-azaC,RG108isnotanucleosideandthereforedoesnotmodifyDNA.ItbindstotheenzymeactivesiteandinhibitsDNMTenzymaticactivitywithanIC50~115nM.ItinhibitsDNAmethylationinhumancancercelllinesinvitrowithoutdetectabletoxicity.TreatmentwithRG108resultsinthedemethylationofgenomicDNAandcanreactivateepigeneticallysilencedtumorsuppressorgenes.Ithasbeenshowntoimprovethereprogrammingefficiencyofmouseembryonicfibroblasts(MEFs)intoinducedpluripotentstem(iPS)cells.RG108canpotentiallybeusedtomaintainembryonicstem(ES)cellsinanundifferentiatedstateaswellasreplacetranscriptionfactorsinbothmouseandhumancellreprogramming.
HowtoUse:
- Invitro:RG108wasusedat10-100µMfinalconcentrationinvariousinvitroassays.
- Invivo:n/a
Reference:
- 1.BruecknerB,etal.Epigeneticreactivationoftumorsuppressorgenesbyanovelsmall-moleculeinhibitorofhumanDNAmethyltransferases.(2005)CancerRes.65(14):6305-11.
- 2.StresemannC,etal.FunctionaldiversityofDNAmethyltransferaseinhibitorsinhumancancercelllines.(2006)CancerRes.66(5):2794-800.
- 3.SchirrmacherE,etal.SynthesisandinvitroevaluationofbiotinylatedRG108:ahighaffinitycompoundforstudyingbindinginteractionswithhumanDNAmethyltransferases.(2006)BioconjugChem.17(2):261-6.
- 4.ShiY,etal.InductionofpluripotentstemcellsfrommouseembryonicfibroblastsbyOct4andKlf4withsmall-moleculecompounds.(2008)CellStemCell.3(5):568-74.
- 5.PashaZ,etal.Efficientnon-viralreprogrammingofmyoblaststostemnesswithasinglesmallmoleculetogeneratecardiacProgenitorcells.(2011)PLoSOne.6(8):e23667.
RG108_spec.pdf
RG108_MSDS.pdf
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