AnovelspecificinhibitoroftheJumonjifamilyofhistonedemethylasesinvitro,incancercellsandintumorsinvivo.IC50=230,340,435,445,855and1100nMforJARID1A,JMJD2E,JMJD2B,JMJD2A,JMJD3andJMJD2Crespectively. Reducestumorburdenandprolongslifeinamousemodel.SuppressestranslationinitiationandenhancesmTORinhibitorsensitivity.Inhibitsthegrowthoftemozolomide-resistantglioblastomacellsandcrossesthebloodbrainbarrier.
ArecentstudyhasshownthatJIB-04increasestheexpressionofPD-L1in SUM149-MAbreastcancercelllines.IncreasedPD-L1expressioninbreastcancercelllinesrendersthemresponsivetovarioustherapiesnotjustimmunecheckpointblockadeofPD-L1.HencetheseresultssuggestthatJIB-04isapotentialanti-canceragentthatcanhaltcancerprogressionandpreventresistancetotherapies.
AdditionalInformation
Product# | J-2519 |
---|---|
CAS# | 199596-05-9 |
ChemicalName | (E)-5-chloro-2-(2-(phenyl(pyridin-2-yl)methylene)hydrazinyl)pyridine |
Formula | C170H13CIN4 |
MW | 308.8 |
Appearance | yellowpowder |
Purity | >98%(TLC);NMR(Conforms) |
Solubility | MaybedissolvedinDMSO(30mg/ml) |
StorageTemp | Storedesiccatedassuppliedat-20°Cforupto2years.Storesolutionsat-20°Cforupto2months. |