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。 |
-
Genome Biol, 2024, 25(1):58
-
Br J Cancer, 2024, 10.1038/s41416-024-02576-z
-
Biomolecules, 2024, 14(1)95
|
|
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. |
-
Res Sq, 2024, rs.3.rs-3843028
-
Nat Commun, 2023, 14(1):6190
-
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. |
-
Cell Death Dis, 2024, 15(1):53
-
Cell Rep, 2024, 43(3):113837
-
Cell Death Discov, 2024, 10(1):95
|
|
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. |
-
Sci Total Environ, 2022, 838(Pt 2):155825
-
Acta Pharmacol Sin, 2022, 10.1038/s41401-022-00932-4
-
Transl Psychiatry, 2022, 12(1):130
|
|
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
-
Cell Mol Life Sci, 2024, 81(1):92
-
Cell Death Discov, 2024, 10(1):95
|
|
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 6 μmol/L. |
-
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. |
-
Sci Rep, 2023, 13(1):13700
-
Dev Cell, 2022, 57(2):260-276.e9
|
|
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. |
|
|
A2681New |
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. |
|
|
A2681New |
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. |
|
|
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。 |
- Genome Biol, 2024, 25(1):58
- Br J Cancer, 2024, 10.1038/s41416-024-02576-z
- Biomolecules, 2024, 14(1)95
|
|
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. |
- Res Sq, 2024, rs.3.rs-3843028
- Nat Commun, 2023, 14(1):6190
- 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. |
- Cell Death Dis, 2024, 15(1):53
- Cell Rep, 2024, 43(3):113837
- Cell Death Discov, 2024, 10(1):95
|
|
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 6 μmol/L. |
- 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. |
- 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. |
|
|