Home Neuronal Signaling Notch

Notch Inhibitors

Cat.No. Product Name Information Product Use Citations Product Validations
S7169 Crenigacestat (LY3039478) Crenigacestat (LY3039478) is an oral Notch and gamma-secretase inhibitor with IC50 of 0.41 nM for Notch.
Cancer Commun (Lond), 2025, 10.1002/cac2.70021
J Exp Clin Cancer Res, 2024, 43(1):286
Cell Death Dis, 2024, 15(1):53
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S7399 FLI-06 FLI-06 is a novel inhibitor of Notch signaling with EC50 of 2.3 μM.
Cell Rep Med, 2025, S2666-3791(25)00231-9
Dev Cell, 2022, 57(2):260-276.e9
Autophagy, 2020, 16:1-24
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S8280 IMR-1 IMR-1 is a novel class of Notch inhibitors targeting the transcriptional activation with IC50 of 26 μM.
Oncogene, 2024,
Cell Death Dis, 2022, 13(11):945
Cell Biosci, 2021, 11(1):87
S3376 RIN1 (RBPJ Inhibitor-1) RIN1 (RBPJ Inhibitor-1) is a potent inhibitor of the transcription factor RBPJ that disrupts the interaction between NOTCH and RBPJ.
Cell Commun Signal, 2024, 22(1):608
bioRxiv, 2024, 2024.12.02.626505
Nat Cardiovasc Res, 2024, 3(9):1035-1048
S9719 Limantrafin (CB-103)

An orally active inhibitor of the Notch transcription activation complex, Limantrafin (CB-103) produces Notch loss-of-function phenotypes in flies and mice and inhibits the growth of human breast cancer and leukemia xenografts.
Sci Rep, 2024, 14(1):21912
Stem Cell Reports, 2023, 18(7):1516-1533
Sci Rep, 2023, 13(1):13700
S0225 IMR-1A IMR-1A, an acid metabolite of IMR-1, is a potent inhibitor of Notch with IC50 of 0.5 μM and Kd of 2.9 μM. This compound exhibits anti-tumor activity.
S2215 DAPT DAPT is a novel γ-secretase inhibitor, which inhibits Aβ production with IC50 of 20 nM in HEK 293 cells. DAPT enhances the apoptosis of human tongue carcinoma cells and regulates autophagy.
Signal Transduct Target Ther, 2025, 10(1):334
Cell Host Microbe, 2025, 33(3):408-419.e8
Nat Commun, 2025, 16(1):8693
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S1575 RO4929097 (RG-4733) RO4929097 (RG-4733) is a γ secretase inhibitor with IC50 of 4 nM in a cell-free assay, inhibiting cellular processing of Aβ40 and Notch with EC50 of 14 nM and 5 nM, respectively. Phase 2.
Nat Commun, 2025, 16(1):10435
Cell Rep Med, 2025, S2666-3791(25)00102-8
Cell Death Dis, 2025, 16(1):150
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S2714 LY411575 LY411575 is a potent γ-secretase inhibitor with IC50 of 0.078 nM/0.082 nM (membrane/cell-based), also inhibits Notch cleavage with IC50 of 0.39 nM in APP or NΔE expressing HEK293 cells. LY411575 induces apoptosis.
Nat Commun, 2025, 16(1):5913
Dev Cell, 2025, S1534-5807(25)00468-X
Cell Rep, 2025, 44(4):115508
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S2711 Dibenzazepine (YO-01027) DBZ (Dibenzazepine) is a dipeptidic γ-secretase inhibitor with IC50 of 2.6 nM and 2.9 nM in cell-free assays for APPL and Notch cleavage, respectively.
Acta Neuropathol Commun, 2025, 13(1):87
Sci Rep, 2025, 15(1):12154
Nat Commun, 2024, 15(1):9771
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S1594 Semagacestat (LY450139) 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. It also inhibits Notch signaling with IC50 of 14.1 nM in H4 human glioma cell. This compound has reached Phase 3 clinical trials.
Cell Rep Med, 2025, S2666-3791(25)00102-8
Biochim Biophys Acta Mol Basis Dis, 2025, 1871(8):167992
Cancers (Basel), 2023, 15(6)1883
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S1262 Avagacestat (BMS-708163) Avagacestat (BMS-708163) is a potent, selective, and orally bioavailable γ-secretase inhibitor of Aβ40 and Aβ42 with IC50 values of 0.3 nM and 0.27 nM, respectively. This compound demonstrates a 193-fold selectivity against Notch and has reached Phase 2 clinical trials.
Nat Commun, 2022, 13(1):6345
Sci Rep, 2022, 12(1):7
Cell, 2021, 184(2):521-533.e14
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S0058 Compound E Compound E (γ-Secretase-IN-1) is a potent inhibitor of γ-secretase, which blocks γ-secretase-mediated cleavage of Notch with an IC50 of 0.32 nM. It also suppresses the production of β-amyloid(40) and β-amyloid(42) with IC50 values of 0.24 nM and 0.37 nM, respectively. It also inhibits Notch signalling, significantly disrupting gonadotropin-dependent follicle growth and halting progression to the preovulatory stage of development.
E6426New Sulindac sulfide Sulindac sulfide is a potent, reversible and noncompetitive inhibitor of γ42-secretase with an IC50 of 20.2 μM. It preferentially reduces Aβ42 generation, inhibits Aβ40 and Notch intracellular domain production, and can be used in Alzheimer's disease research.