JI051 is an inhibitor of the cancer-associated transcription factor Hes1 via the PHB2 chaperone.
IMR-1 is a Mastermind Recruitment inhibitor.
IMR-1A is a metabolite of IMR-1, IMR-1A acts as Notch inhibitor and targeting gene transcription by disrupting Mam1 recruitment to chromatin.
BMS-906024 is a novel, oral and potent pan-Notch inhibitor that demonstrated robust anti-tumor activity at tolerated doses in multiple tumor xenograft models.
CB-103 is a novel and potent γ-secretase inhibitor that is currently being investigated in Phase-1 dose escalation in cancer patients.
Crenigacestat (formerly also known as LY3039478) is a novel, potent and orally bioavailable small molecule Notch inhibitor with an IC50 of ~1nM in cell based assays.
Tangeretin (also called Tangeritin; NSC53909; NSC618905), a naturally occuring flavonoid from citrus fruit peels, has been proven to play an important role in anti-inflammatory responses and neuroprotective effects in several disease models, and was also selected as a Notch-1 inhibitor.
NVS-ZP7-4 is a Zinc transporter SLC39A7 (ZIP7) inhibitor that is also the first reported chemical tool to probe the impact of modulating ER zinc levels and investigate ZIP7 as a novel druggable node in the Notch pathway.