Amyloid-β Inhibitor

PBD-150 is a human glutaminyl cyclase (hQC) Y115E-Y117E variant inhibitor, with a K_i value of 490 nM.

L803-mts (Myristoylated L 803) is a selective and substrate-competitive GSK-3 peptide inhibitor (IC₅₀: 40 μM). L803-mts also reduces Aβ deposits and ameliorates cognitive deficits in 5XFAD mice. L803-mts shows antidepressive effect in the forced swimming test.

MS1262 is a blood-brain barrier-permeable, selective inhibitor of histone methyltransferases G9a (EHMT2) and GLP (EHMT1), with an IC₅₀ of 19 nM and a K_d of 74 nM against G9a, and an IC₅₀ of 6 nM and a K_d of 19 nM against GLP. MS1262 reduces the dimethylation level of histone H3 lysine 9 and decreases the size of Aβ plaques. MS1262 restores hippocampal long-term potentiation (LTP) and miniature excitatory postsynaptic current (sEPSC) frequency, ameliorates spatial memory deficits, and reverses anxiety-like and depression-like behaviors in AD model mice. MS1262 reverses the expression/phosphorylation levels of early AD biomarkers, providing support for stage-specific diagnosis of AD. MS1262 reduces the risk of thrombus rupture. MS1262 can be used in research related to Alzheimer's disease, colorectal cancer, and triple-negative breast cancer.

3-Hydroxyindole is a hydroxyindole compound. 3-Hydroxyindole can be isolated from the fruits of Aristotelia chilensis. 3-Hydroxyindole inhibits Ferroptosis and scavenges DPPH free radicals. 3-Hydroxyindole protects against β-amyloid-induced toxicity. 3-Hydroxyindole exhibits antioxidant activity. 3-Hydroxyindole can be used in research related to neurodegenerative diseases.

DN5355 is a small molecule compound that targets amyloid β protein (Aβ) and hyperphosphorylated tau protein. DN5355 can inhibit the aggregation of Aβ and tau protein and disaggregate the formed Aβ and tau protein fibers. DN5355 can be used in the study of Alzheimer's disease.

Dehydroevodiamine is a blood-brain barrier-permeable, orally effective AChE and BACE1 inhibitor (IC₅₀ = 40.96 μM). Dehydroevodiamine is isolated and extracted from Evodia rutaecarpa. Dehydroevodiamine attenuates neurotoxicity through multiple targets by inhibiting BACE1 to block Aβ production, inhibiting AChE activity, scavenging ROS, and suppressing calcium influx. Dehydroevodiamine can be used for research on Alzheimer's disease, cerebral ischemia, vascular dementia, and other cognitive disorder-related diseases.

Hoechst 34580 is a marker dye in Hoechst series. Hoechst is A live nuclear marker dye. Hoechst binds to the grooves in the DNA double strand, which tends to be A/ T-rich DNA strand. Although it binds to all nucleic acids, the A/ T-rich double strand DNA significantly enhances fluorescence intensity Therefore,Hoechst dye can be used for living cell labeling. The fluorescence intensity of Hoechst dye increases with the increase of pH of solution.

LX2343 is a BACE1 enzyme inhibitor with an IC₅₀ value of 11.43±0.36 μM. LX2343 acts as a non-ATP competitive PI3K inhibitor with an IC₅₀ of 15.99±3.23 μM. LX2343 stimulates autophagy in its promotion of Aβ clearance.

Lithium orotate is an orally active lithium supplement with reduced binding that can bypass amyloid sequestration in AD mice models. Lithium orotate can prevent Aβ plaque deposition and phospho-tau accumulation and reverse AD pathology, neuroinflammatory changes and memory loss in AD mice models and ageing wild-type mice. Lithium orotate can be used for the research of alcoholism and Alzheimer’s disease.

Theasaponin E1 is an orally effective tea saponin. Theasaponin E1 inhibits the proliferation of cancer cells by activating apoptosis. Theasaponin E1 inhibits angiogenesis in ovarian cancer cells and HUVECs by reducing the expression of VEGF. Theasaponin E1 upregulates the phosphorylation level of ATM protein and the expression level of PTEN protein in cancer cells, decreases the phosphorylation levels of Akt, mTOR, p70S6K and 4E-BP1 proteins, downregulates the expression of HIF-1α and NF-κB, and reduces the protein expression of Notch ligands Dll4 and Jagged1. Theasaponin E1 exerts neuroprotective effects by inhibiting the activity of acetylcholinesterase, activating α-secretase and neprilysin, reducing the concentration of Aβ, and inhibiting the activities of β-secretase and γ-secretase. Theasaponin E1 exhibits toxic effects on cancer cells and quinone reductase-inducing activity, and inhibits tumor growth in vivo. Theasaponin E1 induces ferroptosis in Pomacea canaliculata by synergistically disrupting cholesterol homeostasis and sphingolipid metabolism. Theasaponin E1 possesses anti-biofilm activity against Candida albicans. Theasaponin E1 can be used in the research of ovarian cancer, obesity, Alzheimer's disease and fungal infections.

NNC 26-9100 is a selective somatostatin sst4 receptor full agonist (K_i: 6 nM, EC₅₀: 2 nM). NNC 26-9100 decreases total soluble Aβ42, increases brain neprilysin activity and improves learning.

Pongamol (Lanceolatin C) is an orally active flavonoid with an IC₅₀ of 75 μM and a K_i of 58 μM against PTPase-1B, and an IC₅₀ of 103.5 μM against intestinal α-Glycosidase. Pongamol reduces the release of IL‑1β, TNF‑α, COX‑2 and iNOS in cells, reverses the nuclear translocation of NF‑κB, and upregulates the levels of Beclin 1 and LC3 Ⅱ/LC3 Ⅰ. Pongamol promotes glucose uptake by increasing the level of GLUT4 on the surface of skeletal muscle cells. Pongamol inhibits epithelial-mesenchymal transition by suppressing the FAK/Akt-mTOR signaling pathway. Pongamol inhibits neuronal cytotoxicity, suppresses cell apoptosis and extends the lifespan of Caenorhabditis elegans by activating the MAPKs/Nrf2 signaling pathway. Pongamol exerts hypoglycemic effects in diabetic mouse models. Pongamol exhibits antibacterial activity. Pongamol alleviates oxidative stress, neuroinflammation, Aβ deposition and excessive phosphorylation of Tau Protein, and restores autophagy function in Alzheimer's disease mouse models by inhibiting the Akt/mTOR signaling pathway. Pongamol is applicable to research related to Alzheimer's disease, type 2 diabetes, non-small cell lung cancer and postprandial hyperglycemia.

D-KLVFFA is the inhibitor of Amyloid-β assembly, with the IC₅₀ of 2.6 μM, that can be used in Alzheimer's disease study.

Oleocanthal is an orally active phenolic seciridoid compound. Oleocanthal can be extracted from olive oil. Oleocanthal inhibits COX-1 and COX-2, reduces ROS and NO, and upregulates Nrf-2 and HO-1. Oleocanthal reduces Aβ deposition. Oleocanthal exhibits anti-Leishmania activity against promastigotes and amastigotes of L. major, with IC₅₀ values of 18.7 and 87 μg/mL, respectively. Oleocanthal exhibits anticancer activity against colon, breast, liver, and melanoma cancers. Oleocanthal also exhibits anti-inflammatory and neuroprotective properties. Oleocanthal can be used in Alzheimer's disease research.

Nivegacetor (RG6289) a potent and selective γ-secretase modulator. Nivegacetor can reduce the production of Aβ42 can be used for the research of Alzheimer's disease.

Donanemab (Mouse IgG2b) is a chimeric antibody composed of humanized variable regions and a mouse IgG2b backbone. Donanemab (Mouse IgG2b) is an anti-amyloid inhibitor used in Alzheimer's disease research.

Biphenyl-3′,3,4,4′-tetrol (BPT) is a potent Aβ40 aggregation inhibitor. Biphenyl-3′,3,4,4′-tetrol (BPT) can be used in the study of neurodegenerative diseases such as Alzheimer's disease.

Anti-Human/Mouse/Rat Amyloid-beta Antibody (MOAB-2) is a mouse-derived IgG2b λ type antibody inhibitor, targeting to Amyloid-beta. Anti-Human/Mouse/Rat Amyloid-beta Antibody (MOAB-2) recognizes unaggregated, oligomeric or fibrillar forms of Aβ42 and unaggregated Aβ40. Anti-Human/Mouse/Rat Amyloid-beta Antibody (MOAB-2) is selective for human Aβ42 over Aβ40, but not amyloid precursor protein (APP). Anti-Human/Mouse/Rat Amyloid-beta Antibody (MOAB-2) can immunostain human or rat and mouse tissue. Anti-Human/Mouse/Rat Amyloid-beta Antibody (MOAB-2) can be used for detections of western blot, immunohistochemistry, immunofluorescence, immunoprecipitation and ELISA.

TML-6, an orally active curcumin derivative, inhibits the synthesis of the β-amyloid precursor protein and β-amyloid (Aβ). TML-6 can upregulate Apo E, suppress NF-κB and mTOR, and increase the activity of the anti-oxidative Nrf2 gene. TML-6 has the potential for Alzheimer’s disease (AD) research.

Mivelsiran (ALN-APP) is an siRNA targeting the β-amyloid precursor protein (APP). Mivelsiran induces sequence-specific degradation of APP mRNA via RNA interference, thereby reducing the levels of APP protein and downstream amyloid cleavage products. Mivelsiran reduces β-amyloid protein levels in the brain, alleviates neuroinflammation, and attenuates microglial proliferation. Mivelsiran can be used for research on early-onset Alzheimer's disease.