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Xcessbio/MM-102, WDR5-MLL1 Antagonist-Xcessbio Biosciences Inc/2mg solid/M60166-2s

Details
ProductInformation
MolecularWeight:669.80
Formula:C35H49F2N7O4
Purity:≥98%
CAS#:1417329-24-8
Solubility:DMSOupto100mM
ChemicalName:(S)-N-(bis(4-fluorophenyl)methyl)-1-(2-(2-ethyl-2-isobutyramidobutanamido)-5-guanidinopentanamido)cyclopentanecarboxamide
Storage:Powder:4oC1year.DMSO:4oC3month;-20oC1year.

BIOLOGicalActivity:

MM-102isahighlypotentandselectiveinhibitoroftheMLL1/WDR5interactionwithanIC50~2.9nMbindingaffinitytoWDR5.IntheMLL1-AF9transducedmurinecells,MM-102specificallyreducesexpressionoftwocriticalMLL1targetgenes(HoxA9andMeis-1),whicharerequiredforMLL1mediatedleukemogenesis.MM-102alsospecificallyinhibitscellgrowthandinducesapoptosisinleukemiacellsharboringMLL1fusionproteins.MM-102providesthefirstproof-of-conceptsmallmoleculeinhibitortotargettheWDR5/MLL1protein-proteininteractionasanoveltherapeuticapproachforacuteleukemiaharboringMLL1fusionproteins.

HowtoUse:

  • Invitro:MM-102wassuggestedtobeusedat10-100µMfinalconcentrationinvitroandincellularassays.
  • Invivo:n/a

Reference:

  • 1.KaratasH,etal.High-affinity,small-moleculepeptidomimeticinhibitorsofMLL1/WDR5protein-proteininteraction.(2013)JAmChemSoc.135(2):669-82.
  • MM-102_spec.pdf
  • MM-102_MSDS.pdf

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