Notch

Notch製品

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  • Notch阻害剤 (13)
  • Notch抗体(2)
  • Notch活性剤(2)
  • 新製品
製品コード 製品名称 製品説明 文献中Selleckの製品使用例 お客様のフィードバック
S2215 DAPT DAPT (GSI-IX、LY-374973) は新規の γ-セクレターゼ 阻害剤であり、HEK 293 細胞で 20 nM の IC50 で Aβ 産生を阻害します。 DAPT はヒト舌癌細胞のアポトーシス(apoptosis) を促進し、オートファジー (autophagy) を調節します。
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 6 μmol/L.
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.
S0058New 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 (GSI-IX、LY-374973) は新規の γ-セクレターゼ 阻害剤であり、HEK 293 細胞で 20 nM の IC50 で Aβ 産生を阻害します。 DAPT はヒト舌癌細胞のアポトーシス(apoptosis) を促進し、オートファジー (autophagy) を調節します。
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 6 μmol/L.
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
S0058New 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
S0058New 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.

Notch阻害剤の選択性比較

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