IMR-1 is a novel class of Notch inhibitor targeting the transcriptional activation with an IC50 of 26 μM. IMR-1 prevents the recruitment of Mastermind-like 1 (Maml1) to the Notch Ternary Complex (NTC) on chromatin, inhibits Notch target gene transcription and dramatically inhibits tumor growth.
IC50&Target
IC50: 26 nM (Notch)
体内研究
IMR-1 (i.p.; 15mg/kg; for 28 days) inhibits Notch-dependent tumor growth in patient-derived xenograft models.
Animal Model:
Nude mouses with adenocarcinoma xenograft
Dosage:
15mg/kg
Administration:
I.p.; for 28 days
Result:
Blocks tumor establishment.
分子式
C15H15NO5S2
分子量
353.41
CAS号
310456-65-6
运输条件
Room temperature in continental US; may vary elsewhere.