Notch
Notch signaling is evolutionarily conserved and operates in many cell types and at various stages during development. Notch signaling occurs via cell-cell communication, where transmembrane ligands on one cell activate transmembrane receptors on a juxtaposed cell.
Regulation of Notch signaling is critical to development and maintenance of most eukaryotic organisms. The Notch receptors (NOTCH1, 2, 3, and 4) and ligands (DLL1, 3, and 4, JAG1 and 2) are integral membrane proteins and direct cell-cell interactions are needed to activate signaling. Ligand-expressing cells activate Notch signaling through an unusual mechanism involving Notch proteolysis to release the intracellular domain from the membrane, allowing the Notch receptor to function directly as the downstream signal transducer.
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Notch Verwandte Produkte (123)
Verwandte Produkte (123)
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Recombinant Proteins (52)
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Antibodies (12)
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DAPT
0 ImagesSynonyms: GSI-IXDAPT (GSI-IX) is a potent and orally active γ-secretase inhibitor with IC50s of 115 nM and 200 nM for total amyloid-β (Aβ) and Aβ42, respectively. DAPT inhibits the activation of Notch 1 signaling and induces cell differentiation. DAPT also induces autophagy and apoptosis. DAPT has neuroprotection activity and has the potential for autoimmune and lymphoproliferative diseases, degenerative disease and cancers treatment.
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Valproic acid
0 ImagesSynonyms: VPA; 2-Propylpentanoic acid; Dipropylacetic acidValproic acid (VPA) is an orally active HDAC inhibitor, with IC50 in the range of 0.5 and 2 mM. Valproic acid inhibits HDAC1 (IC50, 400 μM), and induces proteasomal degradation of HDAC2. Valproic acid activates Notch1 signaling and inhibits proliferation in small cell lung cancer (SCLC) cells. Valproic acid is used in the epilepsy, bipolar disorder, metabolic disease, HIV infection and prevention of migraine headaches.
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Tarlatamab
0 ImagesSynonyms: AMG-757Tarlatamab (AMG-757) is a bispecific T-cell engager (BiTE) antibody targeting delta-like ligand 3 (DLL3). DLL3 is a target that is selectively expressed in small-cell lung cancer (SCLC) tumors, but with minimal normal tissue expression. Tarlatamab has the KDs of 0.64 nM and 0.50 nM for human and nonhuman primate (NHP) DLL3, respectively. Tarlatamab has the KDs of 14.9 nM and 12 nM for human and NHP CD3, respectively. Tarlatamab is a first-in-class HLE BiTE immuno-oncology therapy targeting DLL3 and has the potential for SCLC research.
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Valproic acid sodium
0 ImagesSynonyms: Sodium Valproate; VPA sodium; 2-Propylpentanoic acid sodiumValproic acid (Sodium Valproate) sodium is an orally active HDAC inhibitor, with IC50 in the range of 0.5 and 2 mM, also inhibits HDAC1 (IC50, 400 μM), and induces proteasomal degradation of HDAC2. Valproic acid sodium activates Notch1 signaling and inhibits proliferation in small cell lung cancer (SCLC) cells. Valproic acid sodium is used in the treatment of epilepsy, bipolar disorder, metabolic disease, HIV infection and prevention of migraine headaches.
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LY-411575
0 ImagesLY-411575 is a potent γ-secretase inhibitor with IC50 of 0.078 nM/0.082 nM (membrane/cell-based), and also inhibits Notch S3 cleavage with an IC50 of 0.39 nM.
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TAS1440
0 ImagesArt. -Nr.: HY-183067CAS. Nr.: 2098585-77-2TAS1440 is an orally active LSD1/KDM1A inhibitor with a human IC50 of 4.8 nM. TAS1440 non-covalently binds to the histone H3-binding pocket of LSD1, inhibiting demethylase activity and disrupting repressive complexes with INSM1 and SMAD2. TAS1440 activates tumor-suppressive TGF-β and NOTCH signaling pathways via transcriptional reprogramming. TAS1440 can be used for the research of small cell lung cancer, specifically the SCLC-A subtype.
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PAI-1-IN-1
0 ImagesPAI-1-IN-1 is an orally active and specific PAI-1 inhibitor with an IC50 of <6.95 μM. PAI-1-IN-1 blocks the interaction between PAI-1 and serine proteases or LRP-1, and enhances plasmin generation. PAI-1-IN-1 restores macrophage efferocytosis and promotes macrophage polarization. PAI-1-IN-1 alleviates PAI-1-mediated inhibition of Furin, promotes MT1-MMP maturation, activates the NOTCH1 signaling pathway, inhibits proliferation and induces apoptosis. PAI-1-IN-1 promotes skeletal muscle regeneration and alleviates inflammation in a mouse model of skeletal muscle injury. PAI-1-IN-1 can be used in research on skeletal muscle injury-induced inflammation and chronic myeloid leukemia.
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TAS1440 benzoate
0 ImagesArt. -Nr.: HY-183067ACAS. Nr.: 2642224-15-3TAS1440 benzoate is an orally active LSD1/KDM1A inhibitor with a human IC50 of 4.8 nM. TAS1440 benzoate non-covalently binds to the histone H3-binding pocket of LSD1, inhibiting demethylase activity and disrupting repressive complexes with INSM1 and SMAD2. TAS1440 benzoate activates tumor-suppressive TGF-β and NOTCH signaling pathways via transcriptional reprogramming. TAS1440 benzoate can be used for the research of small cell lung cancer, specifically the SCLC-A subtype.
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YO-01027
0 ImagesSynonyms: Dibenzazepine; DBZYO-01027 (Dibenzazepine;DBZ) is a potent γ-secretase inhibitor with IC50 values of 2.92 and 2.64 nM for Notch and APPL cleavage, respectively.
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Carvacrol
0 ImagesCarvacrol is an orally active and blood-brain barrier-permeable monoterpenic phenol that can be extract from an abundant number of aromatic plants, including thyme and oregano, possessing antioxidant, antibacterial, antifungal, anticancer, anti-inflammatory, hepatoprotective, spasmolytic, and vasorelaxant properties. Carvacrol also causes cell cycle arrest in G0/G1, downregulates Notch-1, and Jagged-1, and induces apoptosis. Carvacrol is used in low concentrations as a food flavoring ingredient and preservative, as well as a fragrance ingredient in cosmetic formulations.
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Rovalpituzumab
0 ImagesSynonyms: SC-0001Rovalpituzumab is a humanized monoclonal antibody against delta-like protein 3 (DLL3). Rovalpituzumab can be used in the synthesis of antibody-drug conjugate (ADC), Rovalpituzumab Tesirine. Rovalpituzumab has activity against small cell lung cancer (SCLC).
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RBPJ Inhibitor-1
0 ImagesSynonyms: RIN1RBPJ 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.
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Crenigacestat
0 ImagesSynonyms: LY3039478Crenigacestat (LY3039478) is an orally active Notch and γ-secretase inhibitor, with an IC50 of 1 nM in most of the tumor cell lines tested.
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Lumiflavin
0 ImagesLumiflavin (Lumiflavine), a riboflavine analog, causes significant inhibition of riboflavine uptake. Lumiflavin can effectively reduce the riboflavin enrichment in cancer stem-like cells (CSCs) and sensitize the effect of cisplatin Diamminedichloroplatinum (DDP) on CSCs. Lumiflavin is promising for research of ovarian cancer.
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Bruceine D
0 ImagesBruceine D is a Notch inhibitor with anti-cancer activity and induces apoptosis in several human cancer cells. Bruceine D is an effective botanical insect antifeedant with outstanding systemic properties, causing potent pest growth inhibitory activity. Bruceine D has strong anthelmintic activity against D. intermedius with an EC50 value of 0.57 mg/L.
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Yhhu-3792
0 ImagesYhhu-3792 is a Notch activator. Yhhu-3792 enhances the self-renewal capability of neural stem cells (NSCs). Yhhu-3792 promotes the expression of Hes3 and Hes5. Yhhu-3792 increases the spatial and episodic memory abilities of mice. Yhhu-3792 can be used for the study of neurodegenerative diseases (such as Alzheimer's disease) or for neural regeneration after brain injury.
