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Notch

Notch Products

All (18)
Notch Inhibitors (13)
Notch Antibodies (2)
Notch Activators (2)
New Notch Products

Catalog No.	Product Name	Information	Product Use Citations
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.	Nat Biotechnol, 2024, 10.1038/s41587-024-02386-x Nat Commun, 2024, 15(1):9529 J Clin Invest, 2024, 134(18)e179860
S1575	RO4929097	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.	J Cell Physiol, 2024, 10.1002/jcp.31291 Cell Transplant, 2024, 33:9636897241288932 Res Sq, 2024, rs.3.rs-3843028
S2711	DBZ (Dibenzazepine)	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.	Nat Commun, 2024, 15(1):9771 J Exp Clin Cancer Res, 2024, 43(1):295 Oncogene, 2024,
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, 2024, 15(1):8159 Cell Death Dis, 2024, 15(1):53 Cell Rep, 2024, 43(3):113837
S1168	Valproic Acid sodium	Valproic Acid sodium is a HDAC inhibitor by selectively inducing proteasomal degradation of HDAC2, used in the treatment of epilepsy, bipolar disorder and prevention of migraine headaches. Valproic acid induces Notch1 signaling in small cell lung cancer (SCLC) cells. Valproic acid is under investigation for treatment of HIV and various cancers. Valproic acid (VPA) induces autophagy and mitophagy by upregulation of BNIP3 and mitochondrial biogenesis by upregulating PGC-1α.	J Exp Clin Cancer Res, 2024, 43(1):152 J Immunother Cancer, 2024, 12(11)e009805 Sci Total Environ, 2022, 838(Pt 2):155825
S3944	VPA (Valproic acid)	VPA (Valproic acid) is a fatty acid with anticonvulsant properties used in the treatment of epilepsy. It is also a histone deacetylase (HDAC) inhibitor and is under investigation for treatment of HIV and various cancers. Valproic acid (VPA) induces autophagy and mitophagy by upregulation of BNIP3 and mitochondrial biogenesis by upregulating PGC-1α. Valproic acid activates Notch-1 signaling.	Sci Bull (Beijing), 2024, S2095-9273(24)00799-0 Nat Commun, 2024, 15(1):668 Dev Cell, 2024, S1534-5807(24)00326-5
S1262	Avagacestat (BMS-708163)	Avagacestat (BMS-708163) is a potent, selective, orally bioavailable γ-secretase inhibitor of Aβ40 and Aβ42 with IC50 of 0.3 nM and 0.27 nM, demonstrating a 193-fold selectivity against Notch. Phase 2.	Nat Commun, 2022, 13(1):6345 Sci Rep, 2022, 12(1):7 Cell, 2021, 184(2):521-533.e14
S7169	Crenigacestat (LY3039478)	Crenigacestat (LY3039478) is an oral Notch and gamma-secretase inhibitor with IC50 of 0.41 nM for Notch.	J Exp Clin Cancer Res, 2024, 43(1):286 Cell Death Dis, 2024, 15(1):53 MedComm (2020), 2023, 4(5):e346
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, also inhibits Notch signaling with IC50 of 14.1 nM in H4 human glioma cell. Phase 3.	Cancers (Basel), 2023, 15(6)1883 Sci Rep, 2022, 12(1):7 Calcif Tissue Int, 2022, 111(2):211-223
S7399	FLI-06	FLI-06 is a novel inhibitor of Notch signaling with EC50 of 2.3 μM.	Dev Cell, 2022, 57(2):260-276.e9 Autophagy, 2020, 16:1-24 J Exp Clin Cancer Res, 2020, 39(1):128
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
S9719	Limantrafin (CB-103)	Limantrafin (CB-103) is an orally active inhibitor of the Notch transcription activation complex. 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
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.	Nat Cardiovasc Res, 2024, 3(9):1035-1048 Sci Rep, 2023, 13(1):13700 Dev Cell, 2022, 57(2):260-276.e9
A2389	Tarextumab (Anti-NOTCH3)	Tarextumab (Anti-NOTCH3) is an anti-Notch2/3 fully human IgG2 monoclonal antibody with anti-tumor activity. MW: 145.5 kD.
S0058^New	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.
S6668	NVS-ZP7-4	NVS-ZP7-4,a Zinc transporter SLC39A7 (ZIP7) inhibitor,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.
A2681	Brontictuzumab (Anti-NOTCH1)	Brontictuzumab (Anti-NOTCH1) is a monoclonal antibody that targets Notch1 signal. It inhibits tumor cell proliferation and can be used in the research of leukemia and lymphoma. MW :150 KD.
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. IMR-1A 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.	Nat Biotechnol, 2024, 10.1038/s41587-024-02386-x Nat Commun, 2024, 15(1):9529 J Clin Invest, 2024, 134(18)e179860
S1575	RO4929097	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.	J Cell Physiol, 2024, 10.1002/jcp.31291 Cell Transplant, 2024, 33:9636897241288932 Res Sq, 2024, rs.3.rs-3843028
S2711	DBZ (Dibenzazepine)	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.	Nat Commun, 2024, 15(1):9771 J Exp Clin Cancer Res, 2024, 43(1):295 Oncogene, 2024,
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, 2024, 15(1):8159 Cell Death Dis, 2024, 15(1):53 Cell Rep, 2024, 43(3):113837
S1262	Avagacestat (BMS-708163)	Avagacestat (BMS-708163) is a potent, selective, orally bioavailable γ-secretase inhibitor of Aβ40 and Aβ42 with IC50 of 0.3 nM and 0.27 nM, demonstrating a 193-fold selectivity against Notch. Phase 2.	Nat Commun, 2022, 13(1):6345 Sci Rep, 2022, 12(1):7 Cell, 2021, 184(2):521-533.e14
S7169	Crenigacestat (LY3039478)	Crenigacestat (LY3039478) is an oral Notch and gamma-secretase inhibitor with IC50 of 0.41 nM for Notch.	J Exp Clin Cancer Res, 2024, 43(1):286 Cell Death Dis, 2024, 15(1):53 MedComm (2020), 2023, 4(5):e346
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, also inhibits Notch signaling with IC50 of 14.1 nM in H4 human glioma cell. Phase 3.	Cancers (Basel), 2023, 15(6)1883 Sci Rep, 2022, 12(1):7 Calcif Tissue Int, 2022, 111(2):211-223
S7399	FLI-06	FLI-06 is a novel inhibitor of Notch signaling with EC50 of 2.3 μM.	Dev Cell, 2022, 57(2):260-276.e9 Autophagy, 2020, 16:1-24 J Exp Clin Cancer Res, 2020, 39(1):128
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
S9719	Limantrafin (CB-103)	Limantrafin (CB-103) is an orally active inhibitor of the Notch transcription activation complex. 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
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.	Nat Cardiovasc Res, 2024, 3(9):1035-1048 Sci Rep, 2023, 13(1):13700 Dev Cell, 2022, 57(2):260-276.e9
S0058^New	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.
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. IMR-1A exhibits anti-tumor activity.
A2389	Tarextumab (Anti-NOTCH3)	Tarextumab (Anti-NOTCH3) is an anti-Notch2/3 fully human IgG2 monoclonal antibody with anti-tumor activity. MW: 145.5 kD.
A2681	Brontictuzumab (Anti-NOTCH1)	Brontictuzumab (Anti-NOTCH1) is a monoclonal antibody that targets Notch1 signal. It inhibits tumor cell proliferation and can be used in the research of leukemia and lymphoma. MW :150 KD.
S1168	Valproic Acid sodium	Valproic Acid sodium is a HDAC inhibitor by selectively inducing proteasomal degradation of HDAC2, used in the treatment of epilepsy, bipolar disorder and prevention of migraine headaches. Valproic acid induces Notch1 signaling in small cell lung cancer (SCLC) cells. Valproic acid is under investigation for treatment of HIV and various cancers. Valproic acid (VPA) induces autophagy and mitophagy by upregulation of BNIP3 and mitochondrial biogenesis by upregulating PGC-1α.	J Exp Clin Cancer Res, 2024, 43(1):152 J Immunother Cancer, 2024, 12(11)e009805 Sci Total Environ, 2022, 838(Pt 2):155825
S3944	VPA (Valproic acid)	VPA (Valproic acid) is a fatty acid with anticonvulsant properties used in the treatment of epilepsy. It is also a histone deacetylase (HDAC) inhibitor and is under investigation for treatment of HIV and various cancers. Valproic acid (VPA) induces autophagy and mitophagy by upregulation of BNIP3 and mitochondrial biogenesis by upregulating PGC-1α. Valproic acid activates Notch-1 signaling.	Sci Bull (Beijing), 2024, S2095-9273(24)00799-0 Nat Commun, 2024, 15(1):668 Dev Cell, 2024, S1534-5807(24)00326-5
S0058^New	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.

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