S2215 |
DAPT
|
DAPT 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. |
-
Nat Biotechnol, 2024, 10.1038/s41587-024-02386-x
-
J Clin Invest, 2024, 134(18)e179860
-
Theranostics, 2024, 14(6):2544-2559
|
|
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
-
Res Sq, 2024, rs.3.rs-3843028
-
Nat Commun, 2023, 14(1):6190
|
|
S5742 |
Deferoxamine mesylate
|
Deferoxamine mesylate 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.Please do not prepare stock solutions with normal saline or PBS, as precipitation may occur. |
-
Cancer Commun (Lond), 2024, 10.1002/cac2.12608
-
Cell Rep Med, 2024, 5(3):101476
-
Emerg Microbes Infect, 2024, 13(1):2382235
|
|
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. |
-
Clin Immunol, 2024, 262:110178
-
Pharmacol Res, 2023, 192:106791
-
Cell Death Dis, 2023, 14(12):825
|
|
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
|
|
S2660 |
MK-0752
|
MK-0752 is a moderately potent γ-secretase inhibitor, which reduces Aβ40 production with IC50 of 5 nM. Phase 1/2. |
-
Nat Cell Biol, 2024, 26(3):353-365
-
Cancers (Basel), 2023, 15(6)1883
-
J Cancer Res Clin Oncol, 2023, 149(16):14691-14699
|
|
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
|
|
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. |
-
Glycobiology, 2023, 33(4):325-341
-
J Agric Food Chem, 2022, 70(5):1536-1546
-
Sci Rep, 2022, 12(1):7
|
|
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. |
-
Front Aging Neurosci, 2022, 14:1013943
-
Chem Biol Interact, 2021, 351:109756
-
Nat Commun, 2020, 23;11(1):433
|
|
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. |
-
Commun Biol, 2024, 7(1):999
-
Heliyon, 2024, 10(9):e30445
-
Research Square, 2024, 10.21203/rs.3.rs-3840462/v1
|
|
S3922 |
(-)-epigallocatechin
|
(-)-Epigallocatechin, widespread in plants, has been shown to exhibit anti-tumor, anti-cancer and anti-inflammatory functions. |
-
J Inflamm Res, 2023, 16:2007-2020
-
Eur J Pharmacol, 2020, 173323
-
Biochim Biophys Acta Biomembr, 2020, 1863(1):183476
|
|
S4760 |
(2-Hydroxypropyl)-β-cyclodextrin (HP-β-CD)
|
(2-Hydroxypropyl)-β-cyclodextrin (HP-β-CD, HP-β-cyclodextrin, Hydroxypropyl betadex, Hydroxypropyl-β-cyclodextrin) is a well-known sugar used in drug delivery, genetic vectors, environmental protection, and the treatment of Niemann-Pick disease type C1 (NPC1). It is an inhibitor of amyloid-β aggregation and widely used drug delivery vehicle to improve stability and bioavailability. |
-
Technol Cancer Res Treat, 2021, 20:15330338211027916
-
Oncotarget, 2015, 6(30):29497-512
|
|
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. |
-
CNS Neurosci Ther, 2022, 10.1111/cns.14000
-
J Ethnopharmacol, 2021, S0378-8741(21)00169-0
|
|
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
|
|
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. |
-
Front Nutr, 2022, 9:961182
|
|
A2813 |
Anti-Amyloid Beta (CSIRO anti-amyloid Beta scFv)
|
Anti-Amyloid Beta (CSIRO anti-amyloid Beta scFv) is a recombinant monoclonal antibody in a single chain fragment variable (scFv) against amyloid beta, has the potential to be used in Alzheimer's disease (AD) research. MW : 145.14 KD. |
|
|
E2948 |
β-Amyloid (25-35)
|
β-Amyloid (25-35) (Amyloid beta-peptide (25-35), Aβ25-35, β-Amyloid peptide (25-35)) , a sequence GSNKGAIIGLM, is a highly toxic synthetic derivative of Amyloid beta-peptide (Aβ-peptides) which forms fibrillary aggregates. β-Amyloid (25-35) is involved in the pathogenesis of Alzheimer's disease. |
|
|
A2833 |
Donanemab (Anti-Amyloid Beta)
|
Donanemab (LY3002813) is a humanized IgG1 monoclonal antibody directed at an N‐terminal pyroglutamate amyloid beta (Aβ) epitope. Donanemab has the potential for early Alzheimer's disease research. MW : 145.36 KD. |
|
|
E3560 |
Incised notopterygium rhizome Extract
|
Incised Notopterygium Rhizome Extract is extracted from Notopterygium incisum, which rescues cognitive deficits in APP/PS1 Alzheimer's disease mice by attenuating amyloid-beta, tau, and neuroinflammation pathology. |
|
|
S0529 |
PBD-150
|
PBD-150 is a potent human glutaminyl cyclase (hQC) Y115E-Y117E variant inhibitor with Ki of 60 nM. |
|
|
A2933 |
Anti-Amyloid Beta (Merck anti-Amyloid beta 19.3)
|
Anti-Amyloid Beta (Merck anti-Amyloid beta 19.3) is a human monoclonal antibody targeting beta-amyloid with the potential to treat Alzheimer’s disease. MW: 145.22 KD. |
|
|
S5101 |
Tabersonine hydrochloride
|
Tabersonine, an ingredient extracted from the bean of Voacanga africana, is a potent inhibitor against Aβ(1−42) aggregation and toxicity. |
|
|
E0077 |
Simufilam
|
Simufilam(PTI-125) is a potent, orally active small drug against AD, which interacts to filamin and controls the actin cytoskeleton. Simufilam reduces tau hyperphosphorylation, amyloid and tau formation by preventing and reversing the binding of Aβ42 to α7nAChR. |
|
|
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. |
|
|
S6733 |
Edonerpic maleate
|
Edonerpic maleate (T-817) is a novel neurotrophic agent which can inhibit amyloid-β peptides (Aβ). |
|
|
S9428 |
Brazilin
|
Brazilin (Natural Red 24) is a red pigment obtained from the wood of the brazilwood family. It is used to dye fabric and has diverse biological activities, including neuroprotective, anti-inflammatory, antibacterial, and antioxidant properties. |
|
|
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. |
|
|
S3405 |
CRANAD-2
|
CRANAD-2, a near-infrared (NIR) Amyloid-beta (Aβ) plaque-specific fluorescent probe, penetrates the blood brain barrier and has a high affinity for Aβ aggregates with a Kd of 38 nM. |
|
|
A2764 |
Crenezumab (Anti-Amyloid Beta)
|
Crenezumab (Anti-Amyloid Beta) is a fully humanized immunoglobulin (Ig) G4 monoclonal antibody that targets amyloid beta (Abeta) with potential for use in Alzheimer's disease research. MW: 143.58 kD. |
|
|
A2766 |
Gantenerumab (Anti-Amyloid Beta)
|
Gantenerumab (Anti-Amyloid Beta) is a fully human IgG1 monoclonal antibody against beta-amyloid (Abeta40/42) used in the treatment of Alzheimer's disease. MW: 146.28 kD. |
|
|
A2767 |
GSK 933776 (Anti-Amyloid Beta)
|
GSK 933776 (Anti-Amyloid Beta) is a humanized monoclonal antibody against beta-amyloid used in the treatment of Alzheimer's disease. MW: 145.34 kD. |
|
|
A2588 |
Aducanumab (Anti-Amyloid Beta)
|
Aducanumab (Anti-Amyloid Beta) is a selective human monoclonal antibody targeting aggregated forms of amyloid beta (Aβ). Aducanumab shows brain penetration, and can be used for Alzheimer's disease (AD) research.MW :145.5 KD. |
|
|
A2589 |
Birtamimab (Anti-Amyloid Alpha)
|
Birtamimab(Anti-Amyloid Alpha) is an investigational monoclonal antibody that specifically and selectively targets and clear the amyloid. It can be used for treatment to remove amyloid from the vital organs, and research of light chain amyloidosis.MW :145.5 KD. |
|
|
A2800 |
Anti-Amyloid Beta (CNTO 2125)
|
Anti-Amyloid Beta (CNTO 2125) is a human monoclonal antibody against amyloid beta has the potential to be used in Alzheimer's disease (AD) research. MW : 143.86 KD. |
|
|
S2215 |
DAPT
|
DAPT 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. |
- Nat Biotechnol, 2024, 10.1038/s41587-024-02386-x
- J Clin Invest, 2024, 134(18)e179860
- Theranostics, 2024, 14(6):2544-2559
|
|
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
- Res Sq, 2024, rs.3.rs-3843028
- Nat Commun, 2023, 14(1):6190
|
|
S5742 |
Deferoxamine mesylate
|
Deferoxamine mesylate 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.Please do not prepare stock solutions with normal saline or PBS, as precipitation may occur. |
- Cancer Commun (Lond), 2024, 10.1002/cac2.12608
- Cell Rep Med, 2024, 5(3):101476
- Emerg Microbes Infect, 2024, 13(1):2382235
|
|
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. |
- Clin Immunol, 2024, 262:110178
- Pharmacol Res, 2023, 192:106791
- Cell Death Dis, 2023, 14(12):825
|
|
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
|
|
S2660 |
MK-0752
|
MK-0752 is a moderately potent γ-secretase inhibitor, which reduces Aβ40 production with IC50 of 5 nM. Phase 1/2. |
- Nat Cell Biol, 2024, 26(3):353-365
- Cancers (Basel), 2023, 15(6)1883
- J Cancer Res Clin Oncol, 2023, 149(16):14691-14699
|
|
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
|
|
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. |
- Glycobiology, 2023, 33(4):325-341
- J Agric Food Chem, 2022, 70(5):1536-1546
- Sci Rep, 2022, 12(1):7
|
|
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. |
- Front Aging Neurosci, 2022, 14:1013943
- Chem Biol Interact, 2021, 351:109756
- Nat Commun, 2020, 23;11(1):433
|
|
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. |
- Commun Biol, 2024, 7(1):999
- Heliyon, 2024, 10(9):e30445
- Research Square, 2024, 10.21203/rs.3.rs-3840462/v1
|
|
S4760 |
(2-Hydroxypropyl)-β-cyclodextrin (HP-β-CD)
|
(2-Hydroxypropyl)-β-cyclodextrin (HP-β-CD, HP-β-cyclodextrin, Hydroxypropyl betadex, Hydroxypropyl-β-cyclodextrin) is a well-known sugar used in drug delivery, genetic vectors, environmental protection, and the treatment of Niemann-Pick disease type C1 (NPC1). It is an inhibitor of amyloid-β aggregation and widely used drug delivery vehicle to improve stability and bioavailability. |
- Technol Cancer Res Treat, 2021, 20:15330338211027916
- Oncotarget, 2015, 6(30):29497-512
|
|
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. |
- CNS Neurosci Ther, 2022, 10.1111/cns.14000
- J Ethnopharmacol, 2021, S0378-8741(21)00169-0
|
|
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
|
|
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. |
- Front Nutr, 2022, 9:961182
|
|
E3560 |
Incised notopterygium rhizome Extract
|
Incised Notopterygium Rhizome Extract is extracted from Notopterygium incisum, which rescues cognitive deficits in APP/PS1 Alzheimer's disease mice by attenuating amyloid-beta, tau, and neuroinflammation pathology. |
|
|
S0529 |
PBD-150
|
PBD-150 is a potent human glutaminyl cyclase (hQC) Y115E-Y117E variant inhibitor with Ki of 60 nM. |
|
|
S5101 |
Tabersonine hydrochloride
|
Tabersonine, an ingredient extracted from the bean of Voacanga africana, is a potent inhibitor against Aβ(1−42) aggregation and toxicity. |
|
|
E0077 |
Simufilam
|
Simufilam(PTI-125) is a potent, orally active small drug against AD, which interacts to filamin and controls the actin cytoskeleton. Simufilam reduces tau hyperphosphorylation, amyloid and tau formation by preventing and reversing the binding of Aβ42 to α7nAChR. |
|
|
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. |
|
|
S6733 |
Edonerpic maleate
|
Edonerpic maleate (T-817) is a novel neurotrophic agent which can inhibit amyloid-β peptides (Aβ). |
|
|
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. |
|
|