S0486 |
Hoechst 34580
|
Hoechst 34580 (HOE 34580) is a cell-permeable blue fluorescent dye to stain DNA and nuclei. Hoechst 34580 is also a good candidate for treating the Alzheimer's disease by inhibiting amyloid beta (Aβ) formation with IC50 of 0.86 μM. |
|
|
S0529 |
PBD-150
|
PBD-150 is a potent human glutaminyl cyclase (hQC) Y115E-Y117E variant inhibitor with Ki of 60 nM. |
|
|
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
|
|
S1528 |
LY2811376
|
LY2811376 is the first orally available non-peptidic β-secretase(BACE1) inhibitor with IC50 of 239 nM-249 nM, that act to decrease Aβ secretion with EC50 of 300 nM, demonstrated to have 10-fold selectivity towards BACE1 over BACE2, and more than 50-fold inhibition over other aspartic proteases including cathepsin D, pepsin, or renin. Phase 1. |
-
J Agric Food Chem, 2022, 70(5):1536-1546
-
Analyst, 2022, 10.1039/d2an00031h
-
Sci Rep, 2022, 12(1):7
|
|
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
|
|
S2215 |
DAPT (GSI-IX)
|
DAPT (GSI-IX, LY-374973) 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. |
-
Nature, 2022, 603(7899):159-165
-
Adv Mater, 2022, e2106829
-
Cell Stem Cell, 2022, 29(5):776-794.e13
|
|
S2418 |
Frentizole
|
Frentizole (Frentizol) is a novel inhibitor of amyloid beta peptide (Abeta) binding alcohol dehydrogenase (ABAD) interaction with IC50 of 200 μM. Frentizole is a nontoxic antiviral and immunosuppressive agent used clinically in rheumatoid arthritis and systemic lupus erythematosus. |
|
|
S2660 |
MK-0752
|
MK-0752 is a moderately potent γ-secretase inhibitor, which reduces Aβ40 production with IC50 of 5 nM. Phase 1/2. |
-
EBioMedicine, 2022, 78:103963
-
Sci Rep, 2022, 12(1):7
-
PLoS Genet, 2021, 17(12):e1009969
|
|
S3811 |
Ginsenoside Re
|
Ginsenoside Re (Ginsenoside B2, Panaxoside Re, Sanchinoside Re, Chikusetsusaponin Ivc), an extract from Panax notoginseng, is a major ginsenoside in ginseng and belongs to 20(S)-protopanaxatriol group. It has diverse in vitro and in vivo effects, including vasorelaxant, antioxidant, antihyperlipidemic, and angiogenic actions. Ginsenoside Re decreases the β-amyloid protein (Aβ). Ginsenoside Re plays a role in antiinflammation through inhibition of JNK and NF-κB. |
-
J Ethnopharmacol, 2021, S0378-8741(21)00169-0
|
|
S3923 |
Ginsenoside Rg1
|
Ginsenoside Rg1 (Ginsenoside A2, Panaxoside A, Panaxoside Rg1, Sanchinoside C1, Sanchinoside Rg1), one of the major active components of ginseng, is identified as a protopanaxatriol-type and has pharmacological actions such as neuroprotective and anti-tumor effects on various cancer types. Ginsenoside Rg1 reduces cerebral Aβ levels and NF-κB nuclear translocation. |
-
J Ethnopharmacol, 2021, S0378-8741(21)00169-0
|
|
S4261 |
EUK 134
|
EUK 134, a synthetic superoxide dismutase (SOD)/catalase mimetic, exhibits potent antioxidant activities, and inhibits the formation of β-amyloid and related amyloid fibril. |
-
Chem Biol Interact, 2021, 351:109756
-
Nat Commun, 2020, 23;11(1):433
-
Mol Carcinog, 2020, 10.1002/mc.23240
|
|
S4760 |
(2-Hydroxypropyl)-β-cyclodextrin (HP-β-CD)
|
(2-Hydroxypropyl)-β-cyclodextrin (HP-β-CD, HP-β-cyclodextrin, Hydroxypropyl betadex, Hydroxypropyl-β-cyclodextrin), a well-known sugar used in drug delivery, genetic vector, environmental protection and treatment of Niemann-Pick disease type C1 (NPC1), is an inhibitor of amyloid-β aggregation. |
-
Technol Cancer Res Treat, 2021, 20:15330338211027916
-
Oncotarget, 2015, 6(30):29497-512
|
|
S5101 |
Tabersonine hydrochloride
|
Tabersonine, an ingredient extracted from the bean of Voacanga africana, is a potent inhibitor against Aβ(1−42) aggregation and toxicity. |
|
|
S5742 |
Deferoxamine mesylate (Ba 33112)
|
Deferoxamine mesylate (Ba 33112, Desferrioxamine B, DFOM, NSC 644468) is the mesylate salt of Deferoxamine, which forms iron complexes and is used as a chelating agent. Deferoxamine is a ferroptosis inhibitor that stabilizes HIF-1α expression and improves HIF-1α transactivity in hypoxic and hyperglycemic states in vitro. Deferoxamine decreases beta-amyloid (Aβ) deposition and induces autophagy. |
-
Nat Cell Biol, 2022, 24(1):88-98
-
Nat Commun, 2022, 13(1):494
-
Bone Res, 2022, 10(1):26
|
|
S6733 |
Edonerpic maleate
|
Edonerpic maleate (T-817) is a novel neurotrophic agent which can inhibit amyloid-β peptides (Aβ). |
|
|
S8185 |
FPS-ZM1
|
FPS-ZM1 is a blood-brain-barrier permeant, non-toxic, tertiary amide compound which is a high affinity RAGE-specific inhibitor, blocking Aβ binding to the V domain of RAGE. |
-
Nat Med, 2022, 28(4):752-765
-
Nat Commun, 2022, 13(1):1481
-
J Exp Clin Cancer Res, 2022, 41(1):74
|
|
S9087 |
Tenuifolin
|
Tenuifolin, a secondary saponin isolated from hydrolysates of polygalasaponins, inhibits beta-amyloid synthesis in vitro and has nootropic activity in vivo via acetylcholine esterase inhibition and increases norepinephrine and dopamine production. |
|
|
S9664 |
Colivelin
|
Colivelin (CLN) is a brain-penetrant neuroprotective peptide with potent long-term capacity against Aβ deposition, neuronal apoptosis, and synaptic plasticity deficits in neurodegenerative disease. Colivelin is an activator of STAT3. |
-
Thromb J, 2022, 20(1):24
-
J Reprod Immunol, 2022, 151:103623
-
Exp Eye Res, 2021, 213:108823
|
|
S0486 |
Hoechst 34580
|
Hoechst 34580 (HOE 34580) is a cell-permeable blue fluorescent dye to stain DNA and nuclei. Hoechst 34580 is also a good candidate for treating the Alzheimer's disease by inhibiting amyloid beta (Aβ) formation with IC50 of 0.86 μM. |
|
|
S0529 |
PBD-150
|
PBD-150 is a potent human glutaminyl cyclase (hQC) Y115E-Y117E variant inhibitor with Ki of 60 nM. |
|
|
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
|
|
S1528 |
LY2811376
|
LY2811376 is the first orally available non-peptidic β-secretase(BACE1) inhibitor with IC50 of 239 nM-249 nM, that act to decrease Aβ secretion with EC50 of 300 nM, demonstrated to have 10-fold selectivity towards BACE1 over BACE2, and more than 50-fold inhibition over other aspartic proteases including cathepsin D, pepsin, or renin. Phase 1. |
- J Agric Food Chem, 2022, 70(5):1536-1546
- Analyst, 2022, 10.1039/d2an00031h
- Sci Rep, 2022, 12(1):7
|
|
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
|
|
S2215 |
DAPT (GSI-IX)
|
DAPT (GSI-IX, LY-374973) 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. |
- Nature, 2022, 603(7899):159-165
- Adv Mater, 2022, e2106829
- Cell Stem Cell, 2022, 29(5):776-794.e13
|
|
S2418 |
Frentizole
|
Frentizole (Frentizol) is a novel inhibitor of amyloid beta peptide (Abeta) binding alcohol dehydrogenase (ABAD) interaction with IC50 of 200 μM. Frentizole is a nontoxic antiviral and immunosuppressive agent used clinically in rheumatoid arthritis and systemic lupus erythematosus. |
|
|
S2660 |
MK-0752
|
MK-0752 is a moderately potent γ-secretase inhibitor, which reduces Aβ40 production with IC50 of 5 nM. Phase 1/2. |
- EBioMedicine, 2022, 78:103963
- Sci Rep, 2022, 12(1):7
- PLoS Genet, 2021, 17(12):e1009969
|
|
S3811 |
Ginsenoside Re
|
Ginsenoside Re (Ginsenoside B2, Panaxoside Re, Sanchinoside Re, Chikusetsusaponin Ivc), an extract from Panax notoginseng, is a major ginsenoside in ginseng and belongs to 20(S)-protopanaxatriol group. It has diverse in vitro and in vivo effects, including vasorelaxant, antioxidant, antihyperlipidemic, and angiogenic actions. Ginsenoside Re decreases the β-amyloid protein (Aβ). Ginsenoside Re plays a role in antiinflammation through inhibition of JNK and NF-κB. |
- J Ethnopharmacol, 2021, S0378-8741(21)00169-0
|
|
S3923 |
Ginsenoside Rg1
|
Ginsenoside Rg1 (Ginsenoside A2, Panaxoside A, Panaxoside Rg1, Sanchinoside C1, Sanchinoside Rg1), one of the major active components of ginseng, is identified as a protopanaxatriol-type and has pharmacological actions such as neuroprotective and anti-tumor effects on various cancer types. Ginsenoside Rg1 reduces cerebral Aβ levels and NF-κB nuclear translocation. |
- J Ethnopharmacol, 2021, S0378-8741(21)00169-0
|
|
S4261 |
EUK 134
|
EUK 134, a synthetic superoxide dismutase (SOD)/catalase mimetic, exhibits potent antioxidant activities, and inhibits the formation of β-amyloid and related amyloid fibril. |
- Chem Biol Interact, 2021, 351:109756
- Nat Commun, 2020, 23;11(1):433
- Mol Carcinog, 2020, 10.1002/mc.23240
|
|
S4760 |
(2-Hydroxypropyl)-β-cyclodextrin (HP-β-CD)
|
(2-Hydroxypropyl)-β-cyclodextrin (HP-β-CD, HP-β-cyclodextrin, Hydroxypropyl betadex, Hydroxypropyl-β-cyclodextrin), a well-known sugar used in drug delivery, genetic vector, environmental protection and treatment of Niemann-Pick disease type C1 (NPC1), is an inhibitor of amyloid-β aggregation. |
- Technol Cancer Res Treat, 2021, 20:15330338211027916
- Oncotarget, 2015, 6(30):29497-512
|
|
S5101 |
Tabersonine hydrochloride
|
Tabersonine, an ingredient extracted from the bean of Voacanga africana, is a potent inhibitor against Aβ(1−42) aggregation and toxicity. |
|
|
S5742 |
Deferoxamine mesylate (Ba 33112)
|
Deferoxamine mesylate (Ba 33112, Desferrioxamine B, DFOM, NSC 644468) is the mesylate salt of Deferoxamine, which forms iron complexes and is used as a chelating agent. Deferoxamine is a ferroptosis inhibitor that stabilizes HIF-1α expression and improves HIF-1α transactivity in hypoxic and hyperglycemic states in vitro. Deferoxamine decreases beta-amyloid (Aβ) deposition and induces autophagy. |
- Nat Cell Biol, 2022, 24(1):88-98
- Nat Commun, 2022, 13(1):494
- Bone Res, 2022, 10(1):26
|
|
S6733 |
Edonerpic maleate
|
Edonerpic maleate (T-817) is a novel neurotrophic agent which can inhibit amyloid-β peptides (Aβ). |
|
|
S8185 |
FPS-ZM1
|
FPS-ZM1 is a blood-brain-barrier permeant, non-toxic, tertiary amide compound which is a high affinity RAGE-specific inhibitor, blocking Aβ binding to the V domain of RAGE. |
- Nat Med, 2022, 28(4):752-765
- Nat Commun, 2022, 13(1):1481
- J Exp Clin Cancer Res, 2022, 41(1):74
|
|
S9087 |
Tenuifolin
|
Tenuifolin, a secondary saponin isolated from hydrolysates of polygalasaponins, inhibits beta-amyloid synthesis in vitro and has nootropic activity in vivo via acetylcholine esterase inhibition and increases norepinephrine and dopamine production. |
|
|
S9664 |
Colivelin
|
Colivelin (CLN) is a brain-penetrant neuroprotective peptide with potent long-term capacity against Aβ deposition, neuronal apoptosis, and synaptic plasticity deficits in neurodegenerative disease. Colivelin is an activator of STAT3. |
- Thromb J, 2022, 20(1):24
- J Reprod Immunol, 2022, 151:103623
- Exp Eye Res, 2021, 213:108823
|
|