Notch

Semagacestat (LY450139) is a γ-secretase blocker for Aβ42, Aβ40 and Aβ38 with IC50 of 10.9 nM, 12.1 nM and 12.0 nM, respectively. Semagacestat also inhibits Notch signaling with IC50 of 14.1 nM.

MK-0752 inhibits the Notch signaling pathway, which may result in induction of growth arrest and apoptosis in tumor cells in which the Notch signaling pathway is overactivated.

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

FLI-06 is a Notch inhibitor and the early secretory pathway inhibitor. FLI-06 disrupts the Golgi apparatus in a manner distinct from that of brefeldin A and golgicide A.

TAPI-2 is an inhibitor of TACE, ADAMs, ACE secretase, and other MMPs (metalloproteinases). TAPI-2 blocks release of DCC7, APP, TNFα, L-selectin, NOTCH, TGFα, IL-6R9, erbB2/HER2, and ACE. This inhibitor has been used in tissue culture.

LY-900009 is a potent inhibitor of Notch with IC50 value of 0.27 nM.

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

Z-Ile-Leu-aldehyde is a potent gamma-Secretase inhibitor; Notch signaling inhibitor.

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 umol/L.

BMS-906024 is an oral and selective gamma secretase inhibitor (GSI) that is a small molecule Notch inhibitor.

BMS-983970 is an oral pan-Notch inhibitor for the treatment of multiplecancers.

Notch inhibitor 1 is a potent Notch inhibitor, with IC50s of 7.8 and 8.5 nM for Notch 1 and Notch 3, respectively. Used in the research of cancer.

CB-103 is a first-in-class, orally active protein-protein interaction (PPI) inhibitor of the NOTCH transcriptional activation complex. CB-103 has anti-tumor activity.

Prednisone acetate is a glucocorticoid that functions as an orally active Notch inhibitor. It exhibits significant anti-inflammatory activity and has the potential to enhance immune responses. This compound is widely used in research to investigate its effects on Notch signaling and its implications in various inflammatory and immune-related conditions.

NADI-351 is a potent orally active inhibitor of Notch1, specifically designed to disrupt Notch1 transcription complexes and decrease its recruitment to target genes. This compound exhibits significant efficacy in inhibiting Notch1 signaling pathways, making it a valuable tool for cancer research. Its selective action provides insights into the role of Notch1 in tumorigenesis and related cellular processes.

ASR-490 is a selective Notch1 inhibitor that effectively reduces the viability of HCT116 and SW620 cancer cell lines by downregulating Notch1 signaling pathways. This compound successfully impedes tumor growth in both control cells and Notch1-overexpressing HCT116 transfectants. In vivo studies demonstrate that ASR-490 significantly inhibits tumor growth in xenograft models, highlighting its potential as a therapeutic agent in cancer research.

Procyanidin B2 3,3'-di-O-gallate is a selective Notch1 inhibitor that demonstrates significant biological activity against cancer stem cells, particularly in prostate cancer. This compound effectively targets both unsorted and sorted cancer stem cells at lower concentrations. By suppressing the activated Notch1 signaling pathway, including responses induced by the Jagged1 ligand, Procyanidin B2 3,3'-di-O-gallate is a valuable tool for research focused on cancer biology and therapeutic development.