notch-1

Notch 1 TFA encodes a member of the NOTCH family of proteins.

Notch inhibitor 1 is an effective Notch inhibitor (IC50s: 7.8 and 8.5 nM for Notch 1 and Notch 3, respectively). Notch inhibitor 1 is also used in the research of cancer.

Tangeretin (NSC-618905), a 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.

Jagged-1 (188-204) TFA(219127-21-6 free base) is a fragment of the JAG-1 protein. JAG-1 is Notch ligand, a peptide that is the most conspicuously expressed ligand in skin. JAG-1 induces epidermal maturation. Exposing submerged keratinocytes monolayers to JAG-1 with elevated calcium concentration produces stratification with loricrin expression and NF-alphaB activation.

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

Crenigacestat (LY3039478) is an orally bioavailable Notch inhibitor with an IC50 of ~1 nM in most of the tumor cell lines tested. Crenigacestat effectively inhibits mutant Notch receptor activity. In a xenograft tumor model, Crenigacestat inhibited expression of Notch-regulated genes and N1ICD cleavage in the tumor microenvironment.

Jagged-1 （188-204）is a fragment of the JAG-1 protein. JAG-1 is Notch ligand, a peptide that is the most conspicuously expressed ligand in skin. JAG-1 induces epidermal maturation. Exposing submerged keratinocytes monolayers to JAG-1 with elevated calcium concentration produces stratification with loricrin expression and NF-αB activation.

IHR-1 is a Potent Smo antagonist (IC50 = 7.6 nM). Selectively inhibits Hedgehog signaling over Wnt and Notch signaling pathways. Blocks Smo accumulation in primary cilium in vitro.

3,5-Bis(4-nitrophenoxy)benzoic acid (Compound W) is an inhibitor of γ-secretase. It also causes a decrease in the released levels of Aβ42 and notch-1 Aβ-like peptide 25 (Nβ25).

Enoticumab (REGN421, SAR153192) is an IgG1κ antibody that specifically targets human Delta-like ligand 4 (Dll4), which serves as a crucial component of the Notch signaling pathway and regulates the uptake of fatty acids through non-transcriptional modulation of macropinocytosis-dependent long-chain fatty acid absorption. Demonstrated efficacy in vivo, Enoticumab was shown to inhibit tumor growth by 86% and 83% in subcutaneous TOV-112D and intraperitoneal A2780 human ovarian tumor xenograft mouse models, respectively, when administered at a dose of 2.5 mg/kg weekly [1].

RBPJ Inhibitor-1 (RIN1), a compound that impedes the functional interaction between RBPJ and SHARP, effectively inhibits NOTCH-dependent tumor cell proliferation[1].

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

Yhhu-3792 hydrochloride is a compound that bolsters the self-renewal capacity of neural stem cells (NSCs), catalyzes the Notch signaling pathway, and upregulates expression of Hes3 and Hes5. It augments the NSC pool, stimulates endogenous neurogenesis in the mouse hippocampal dentate gyrus (DG), and enhances mice's spatial and episodic memory skills. This compound shows promise for researching learning and memory impairments linked to DG dysfunction [1].

1. Bruceine D from Brucea javanica, may have the potential to be used as a natural viricide, or a lead compound for new viricides. 2. Bruceine D inhibits the growth of three pancreatic cancer cell lines, i.e., PANC-1, SW199 and CAPAN-1; induces cytotoxicity in Capan-2 cells via the induction of cellular apoptosis involving the mitochondrial pathway.

Divalproex Sodium (Valproate semisodium) binds to and inhibits gamma-aminobutyric acid (GABA) transaminase and its anticonvulsant activity may be exerted by increasing brain concentration of GABA and by inhibiting enzymes that catabolize GABA or block the reuptake of GABA into glia and nerve endings. It also is an HDAC inhibitor， Comprised of sodium valproate and valproic acid with anticonvulsant and antiepileptic activities. Divalproex may also work by suppressing repetitive neuronal firing through the inhibition of voltage-sensitive sodium channels.

Jagged-1 (188-204) TFA, a fragment of the Jagged-1 (JAG-1) protein, acts as a Notch agonist. This compound is significantly present in both cultured and primary multiple myeloma (MM) cells, where JAG-1 facilitates the maturation of monocyte-derived human dendritic cells [1] [2] [3].

γ-Secretase-IN-1 is a potent γ-secretase inhibitor that displays partial antiproliferative activity on T-47D cells and inhibits β-amyloid(40), β-amyloid(42), and Notch γ-secretase cleavage.