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Notch signaling pathway is a highly conserved cell signaling system present in most multicellular organisms. Notch is present in all metazoans, and mammals possess four different notch receptors, referred to as Notch1, Notch2, Notch3, and Notch4. The notch receptor is a single-pass transmembrane receptor protein. It is a hetero-oligomer composed of a large extracellular portion, which associates in a calcium-dependent, non-covalent interaction with a smaller piece of the notch protein composed of a short extracellular region, a single transmembrane-pass, and a small intracellular region. Notch signaling promotes proliferative signaling during neurogenesis, and its activity is inhibited by Numb to promote neural differentiation. The notch signaling pathway is important for cell-cell communication, which involves gene regulation mechanisms that control multiple cell differentiation processes during embryonic and adult life.

Cat. No.	Product Name	CAS No.	Information
H8280	ZLDI-8	667880-38-8	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.
H8279	Yhhu-3792	2097826-24-7	Yhhu-3792 is a novel small molecule that enhances the self-renewal capability of neural stem cells (NSCs) in vitro and in vivo via activating the Notch signaling pathway; activates Notch signaling pathway and promotes the expression of Notch target genes, Hes3 and Hes5; expands the NSCs pool and promotes endogenous neurogenesis in the hippocampal dentate gyrus (DG) after chronic administration in mice.
H8278	NVS-ZP7-4	2349367-89-9	NVS-ZP7-4 is specific small molecule inhibitor of SLC39A7 (ZIP7), inhibits Notch signaling with IC50 of 0.13 uM in HES-Luc reporter gene assays, selectively induces apoptosis and ER stress; The V430E mutation in ZIP7 can confer transferable resistance to the compound NVS-ZP7-4; NVS-ZP7-4 is 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.
H8277	LY3039478	1421438-81-4	LY3039478 (Crenigacestat) is an exquisitely potent inhibitor of Notch-1 intracellular domain (N1ICD) cleavage with IC50 of 1 nM, also potently inhibits mutant Notch receptor activity; inhibits N1ICD cleavage and expression of Notch-regulated genes in the tumor microenvironment in xenograft tumor models; significantly inhibits the growth of CCRCC cell lines in a concentration-dependent manne, decreases expression of Myc and cyclin A1, causes G0/G1 cell cycle arrest in CCRCC cells, demonstrates in vivo efficacy in CCRCC in mice model.
H8276	IMR-1A	331862-41-0	A small molecule inhibitor of the Notch transcriptional activation complex that prevents the recruitment of Maml1 to the Notch Ternary Complex (NTC) on chromatin (IC50=0.5 uM); non-covalently binds to intracellular domain of Notch (NICD) with Kd of 2.9 uM, inhibits Notch target gene transcription and selectively suppresses colony formation of Notch-dependent cell lines; the acid metabolite of IMR-1.
H8275	IMR-1	310456-65-6	A small molecule inhibitor of the Notch transcriptional activation complex that prevents the recruitment of Maml1 to the Notch Ternary Complex (NTC) on chromatin (IC50=26 uM); non-covalently binds to intracellular domain of Notch (NICD) with Kd of 11 uM, inhibits Notch target gene transcription and selectively suppresses colony formation of Notch-dependent cell lines; dramatically inhibits tumor growth in a patient-derived tumor xenograft model.
H8274	EDD3	25279-15-6	A novel Notch inhibitor that reduces protein expression of NOTCH1, NICD and HES1 in HEK293 cells and downregulates Notch target genes; inhibits proliferation and induces G0/G1 cell cycle arrest of ORL-150 cells through inducing p27KIP1.
H8273	Cowanin	21044-85-9	Cowanin is a novel natural product from Garcinia speciosa that inhibits the Notch signaling pathway with IC50 of 2.4 uM; shows high efficient cytotoxicity against human leukemic cancer cells HPB-ALL (IC50=7.5 uM) than that of DAPT, decreases the protein levels of HES1 and HES5 in assay cells; accelerates nicastrin degradation, which is one of the components of the γ-secretase complex; also inhibits cell proliferation and induces apoptosis of LoVo cells via the MAPK and Akt signaling pathways.
H8272	BMS-983970	1584713-87-0	BMS-983970 (BMS983970) is a potent, orally active, pan-Notch inhibitor, demonstrates robust anti-tumor activity at tolerated doses in multiple tumor xenograft models.
H8271	BMS-906024	1401066-79-2	BMS-906024 (Osugacestat)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; exhibits >200-fold selectivity against a panel of diverse protein targets; inhibits both leukemia (TALL-1) and triple-negative breast cancer (MDA-MB-468) cells with IC50 of 0.4 nM, demonstrates broad-spectrum antineoplastic activity against a wide array of human cancer xenografts

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