Notch

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Notch Products

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  • Notch Inhibitors (11)
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Catalog No. Product Name Information Product Use Citations Product Validations
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.
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.
Sci Rep, 2022, 12(1):7
Cell, 2021, 184(2):521-533.e14
Biochem Biophys Res Commun, 2021, 570:137-142
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.
Nature, 2022, 603(7899):159-165
Clin Cancer Res, 2022, clincanres.2347.2021
Cell Death Dis, 2022, 13(2):173
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.
Sci Rep, 2022, 12(1):7
Life Sci Alliance, 2021, 4(4)e202000844
Cancer Cell, 2020, 13;37(1):104-122e12
S2711 Dibenzazepine (YO-01027) Dibenzazepine (YO-01027, DBZ) 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.
iScience, 2022, 25(2):103813
Sci Rep, 2022, 12(1):7
Nature, 2021, 598(7881):510-514
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.
Dev Cell, 2022, S1534-5807(22)00127-7
Sci Rep, 2022, 12(1):7
Inflammation, 2022, 10.1007/s10753-021-01591-z
S3376 RBPJ Inhibitor-1 (RIN1) RBPJ Inhibitor-1 (RIN1) is a potent inhibitor of the transcription factor RBPJ that disrupts the interaction between NOTCH and RBPJ.
Dev Cell, 2022, 57(2):260-276.e9
S7169 Crenigacestat (LY3039478) Crenigacestat (LY3039478) is an oral Notch and gamma-secretase inhibitor with IC50 of 0.41 nM for Notch.
Hepatology, 2022, 10.1002/hep.32332
Sci Rep, 2022, 12(1):7
Nucleic Acids Res, 2021, gkab800
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 Biosci, 2021, 11(1):87
Naunyn Schmiedebergs Arch Pharmacol, 2020, 10.1007/s00210-020-01988-x
J Infect Dis, 2019, 220(12):1977-1988
S9719 CB-103

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.

Life Sci, 2021, 276:119439
S1168 Valproic Acid (NSC 93819) sodium salt Valproic Acid sodium salt (NSC 93819, Sodium valproate) 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.
Sci Total Environ, 2022, 838(Pt 2):155825
Transl Psychiatry, 2022, 12(1):130
Acta Pharmacol Sin, 2022, 10.1038/s41401-022-00932-4
S3944 Valproic acid (VPA) Valproic acid (VPA, 2-Propylvaleric Acid, Valproate) 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.
Cell Stem Cell, 2022, 29(7):1031-1050.e12
Cell Res, 2022, 10.1038/s41422-022-00668-0
Cell Rep, 2022, 39(12):110994
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.
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.
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.
Sci Rep, 2022, 12(1):7
Cell, 2021, 184(2):521-533.e14
Biochem Biophys Res Commun, 2021, 570:137-142
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.
Nature, 2022, 603(7899):159-165
Clin Cancer Res, 2022, clincanres.2347.2021
Cell Death Dis, 2022, 13(2):173
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.
Sci Rep, 2022, 12(1):7
Life Sci Alliance, 2021, 4(4)e202000844
Cancer Cell, 2020, 13;37(1):104-122e12
S2711 Dibenzazepine (YO-01027) Dibenzazepine (YO-01027, DBZ) 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.
iScience, 2022, 25(2):103813
Sci Rep, 2022, 12(1):7
Nature, 2021, 598(7881):510-514
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.
Dev Cell, 2022, S1534-5807(22)00127-7
Sci Rep, 2022, 12(1):7
Inflammation, 2022, 10.1007/s10753-021-01591-z
S3376 RBPJ Inhibitor-1 (RIN1) RBPJ Inhibitor-1 (RIN1) is a potent inhibitor of the transcription factor RBPJ that disrupts the interaction between NOTCH and RBPJ.
Dev Cell, 2022, 57(2):260-276.e9
S7169 Crenigacestat (LY3039478) Crenigacestat (LY3039478) is an oral Notch and gamma-secretase inhibitor with IC50 of 0.41 nM for Notch.
Hepatology, 2022, 10.1002/hep.32332
Sci Rep, 2022, 12(1):7
Nucleic Acids Res, 2021, gkab800
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 Biosci, 2021, 11(1):87
Naunyn Schmiedebergs Arch Pharmacol, 2020, 10.1007/s00210-020-01988-x
J Infect Dis, 2019, 220(12):1977-1988
S9719 CB-103

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.

Life Sci, 2021, 276:119439
S1168 Valproic Acid (NSC 93819) sodium salt Valproic Acid sodium salt (NSC 93819, Sodium valproate) 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.
Sci Total Environ, 2022, 838(Pt 2):155825
Transl Psychiatry, 2022, 12(1):130
Acta Pharmacol Sin, 2022, 10.1038/s41401-022-00932-4
S3944 Valproic acid (VPA) Valproic acid (VPA, 2-Propylvaleric Acid, Valproate) 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.
Cell Stem Cell, 2022, 29(7):1031-1050.e12
Cell Res, 2022, 10.1038/s41422-022-00668-0
Cell Rep, 2022, 39(12):110994
Tags: Notch inhibitor|Notch agonist|Notch activator|Notch inducer|Notch antagonist|Notch signaling pathway|Notch assay kit