纯度:98% by TLC;NMR (Conforms)
分子式:C15H15NO5S2
分子量:353.41
溶剂:DMSO (45 mg/ml) Ethanol (9 mg/ml)
性状:Yellow solid
存储:-20°C
Activity (short version):Notch transcriptional activation inhibitor
Function / Pharmacology:Inhibitor of Mastermind Recruitment-1 (IMR-1) disrupts the recruitment of Mastermind-like 1 to the Notch transcriptional activation complex (NTC) on chromatin, which attenuates Notch target gene transcription1. IC50=26 ?M (in vitro assay). IMR-1 inhibits the growth of Notch-dependent cell lines and attenuates the growth of patient-derived tumor xenografts. The ethylester is hydrolyzed by intracellular esterases which produces the free acid compound (IMR-1A), IC50=0.5 ?M (in vitro assay). Binding of IMR-1 to NTC is non-covalent and reversible.1