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. |
|
|