Notch

Notch Products

  • All (17)
  • Notch Inhibitors (12)
  • Notch Antibodies (2)
  • Notch Activators (2)
  • New Notch Products
Catalog No. Product Name Information Product Use Citations Product Validations
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
J Clin Invest, 2024, 134(18)e179860
Theranostics, 2024, 14(6):2544-2559
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
Res Sq, 2024, rs.3.rs-3843028
Nat Commun, 2023, 14(1):6190
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.
Cell Mol Gastroenterol Hepatol, 2023, 16(3):451-472
Cells, 2023, 12(18)2231
Cells, 2023, 12(18)2231
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
Sci Total Environ, 2022, 838(Pt 2):155825
Acta Pharmacol Sin, 2022, 10.1038/s41401-022-00932-4
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.
Nat Commun, 2024, 15(1):668
Dev Cell, 2024, S1534-5807(24)00326-5
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.
Cell Death Dis, 2024, 15(1):53
MedComm (2020), 2023, 4(5):e346
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.
Cell Death Dis, 2022, 13(11):945
Cell Biosci, 2021, 11(1):87
Naunyn Schmiedebergs Arch Pharmacol, 2020, 10.1007/s00210-020-01988-x
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.

Stem Cell Reports, 2023, 18(7):1516-1533
Sci Rep, 2023, 13(1):13700
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.
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
J Clin Invest, 2024, 134(18)e179860
Theranostics, 2024, 14(6):2544-2559
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
Res Sq, 2024, rs.3.rs-3843028
Nat Commun, 2023, 14(1):6190
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.
Cell Mol Gastroenterol Hepatol, 2023, 16(3):451-472
Cells, 2023, 12(18)2231
Cells, 2023, 12(18)2231
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.
Cell Death Dis, 2024, 15(1):53
MedComm (2020), 2023, 4(5):e346
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.
Cell Death Dis, 2022, 13(11):945
Cell Biosci, 2021, 11(1):87
Naunyn Schmiedebergs Arch Pharmacol, 2020, 10.1007/s00210-020-01988-x
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.

Stem Cell Reports, 2023, 18(7):1516-1533
Sci Rep, 2023, 13(1):13700
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
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
Sci Total Environ, 2022, 838(Pt 2):155825
Acta Pharmacol Sin, 2022, 10.1038/s41401-022-00932-4
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.
Nat Commun, 2024, 15(1):668
Dev Cell, 2024, S1534-5807(24)00326-5
Dev Cell, 2024, S1534-5807(24)00326-5

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Tags: Notch inhibitor|Notch agonist|Notch activator|Notch inducer|Notch antagonist|Notch signaling pathway|Notch assay kit