A fucose analog that inhibits Dll-induced Notch signaling by reducing Notch ligand Dll1-Notch1 binding, but not Jag1.

A novel Notch inhibitor that reduces protein expression of NOTCH1, NICD and HES1 in HEK293 cells and downregulates Notch target genes.

BMS-906024 is a highly potent, selective inhibitor of γ-secretase mediated signaling of Notch1/2/3/4 receptors with IC50 of 1.6/0.7/3.4/2.9 nM, respectively.

IMR-1 Inhibits the Notch Transcriptional Activation Complex to Suppress Tumorigenesis.

IMR-1A is the metabolite of IMR-1. IMR-1 is a novel class of Notch inhibitors targeting the transcriptional activation with IC50 of 6 μmol/L.

LY3039478 a orally bioavailable, novel small molecule Notch inhibitor with an IC50 of ~1nM in most of the tumor cell lines tested.

ZLDI-8 (IAC-8) is a novel Notch signaling pathway inhibitor for Notch activating/cleaving enzyme ADAM-17, significantly decreases the level of NICD and accumulation of NICD in the nucleus; exhibits cytotoxic acitviity against MHCC97-H cells with IC50 of 5.32 uM, reduces the expression of pro-survival/anti-apoptosis regulators, Survivin and cIAP1/2, also increases the expression of epithelial marker E-Cadherin and reduces mesenchymal markers N-Cadherin and Vimentin in HCC cells; significantly disrupted the activity of Notch pathway in HCC cells and inhibits the epithelial-mesenchymal transition (EMT) process of HCC cells; ZLDI-8 treatment enhances the susceptibility of HCC cells to Sorafenib, Etoposide, and Paclitaxel both in vitro and in vivo.

CB-103 is a notch signaling pathway inhibitor extracted from patent US9296682B2. CB-103 is developed for the treatment of cancers.

RBPJ Inhibitor-1 (RIN1), the first RBPJ inhibitor, blocks the functional interaction of RBPJ with SHARP. RBPJ Inhibitor-1 (RIN1) inhibits NOTCH-dependent tumor cell proliferation.