Amyloid-β Inhibitor

CHI3L1-IN-5 (Compound Z17) is a highly selective CHI3L1 inhibitor with a K_D value of 6 μM. CHI3L1-IN-5 restores the clearance ability of astrocytes by rejuvenating lysosomal function and Aβ uptake. CHI3L1-IN-5 alleviates neuroinflammation by inhibiting the NF-κB pathway. CHI3L1-IN-5 can be used for research on Alzheimer's disease.

NSS-18 is a potent and reversible inhibitor of AChE and MAO-B, with IC₅₀ values of 1.53 and 1.51 μM respectively. NSS-18 can inhibit the self-aggregation of Aβ. NSS-18 inhibits the intracellular generation of ROS induced by Aβ. NSS-18 shows a moderate neuroprotective effect against 6-OHDA (HY-B1081)-induced neurotoxicity. NSS-18 can form chelates with metal ions such as Cu²⁺, Fe³⁺, and Zn²⁺, with the strongest chelation being with Cu²⁺. NSS-18 can be used for the study of Alzheimer's disease.

Anti-Amyloid Beta Antibody (CNTO 2125) is a humanized antibody expressed in CHO cells, targeting Amyloid Beta/Aβ. Anti-Amyloid Beta Antibody (CNTO 2125) features a huIgG1 heavy chain and a huκ light chain, with a predicted molecular weight (MW) of 145 kDa. The isotype control for Anti-Amyloid Beta Antibody (CNTO 2125) can be referenced as Human IgG1 kappa, Isotype Control (HY-P99001).

CM-414 is a brain-penetrant phosphodiesterase 5 (PDE5) and HDAC inhibitor with IC50s of 60 nM, 91 nM, 310 nM, 322 nM and 490 nM for PDE5, HDAC6, HDAC1, HDAC3 and HDAC2, respectively. CM-414 diminishes brain Aβ and tau phosphorylation (pTau) level in Tg2576 mice. CM-414 can be used for the study of Alzheimer's disease (AD).

MEDI-8490 is a fully human monoclonal antibody targeting APP/Aβ. MEDI-8490 can be used in research related to neurodegenerative diseases. Recommended isotype control: Human IgG1 lambda1, Isotype Control (HY-P99992).

AChE/BChE-IN-23 (Compound 6e) is an AChE/BChE inhibitor (IC₅₀: 0.91 μM, 1.19 μM and 1.01 μM for hAChE, eq BChE and hBChE, respectively). AChE/BChE-IN-23 has antioxidant activity and inhibits Aβ1-42 and Tau protein aggregation. AChE/BChE-IN-23 also inhibits microglial activation by reducing ROS release and mitochondrial injury. AChE/BChE-IN-23 suppresses NLRP3 inflammasome and pro-inflammatory cytokines in human microglial cells. AChE/BChE-IN-23 also reverses the Scopolamine (HY-N0296)-induced memory impairment in mice model.

Anti-amyloid agent-2 (compound (R)-38) is an amyloidogenic immunoglobulin light chain stabilizer.

SEN-1269 is a potent Aβ aggregation inhibitor. SEN-1269 blocks Aβ(1-42) aggregation and protects neuronal cell lines exposed to Aβ(1-42). SEN-1269 reduces the deficits in LTP and memory induced by Aβ oligomers. SEN-1269 can be used for the research of Alzheimer's disease.

W2A-28 is a daul modulator of class I HDACs and Wnt/β-catenin. W2A-28 inhibits HDAC1, 2 and 3 activities with IC₅₀ values of 512, 675, and 217 nM, respectively. W2A-28 shows selectivity over other HDACs and Sirtuin family members. W2A-28 activates Wnt/β-catenin signaling via reduced LRP6 degradation, enhances histone acetylation, suppresses tau phosphorylation, and reduces Aβ₄₀ and Aβ₄₂ levels. W2A-28 can be used for the research of Alzheimer's disease.

PTP1B-IN-26 (Compound 7a) is a derivative of phenylthiosemicarbazide‐phenoxy‐1,2,3‐triazole‐N‐phenylacetamide. PTP1B-IN-26 is an inhibitor of protein tyrosine phosphatase 1B (PTP-1B). PTP1B-IN-26 is a competitive inhibitor. PTP1B-IN-26 can be used to research in type 2 diabetes.

Licochalcone B (Standard) is the analytical standard of Licochalcone B. This product is intended for research and analytical applications. Licochalcone B is an extract from the root of Glycyrrhiza uralensis. Licochalcone B inhibits amyloid β (42) self-aggregation (IC50=2.16 μM) and disaggregate pre-formed Aβ42 fibrils, reduce metal-induced Aβ42 aggregation through chelating metal ionsLicochalcone B inhibits phosphorylation of NF-κB p65 in LPS signaling pathway. Licochalcone B inhibits growth and induces apoptosis of NSCLC cells. Licochalcone B specifically inhibits the NLRP3 inflammasome by disrupting NEK7‐NLRP3 interaction.

AChE/MAO-B-IN-7 (VAV-8) is a blood-brain permeable dual inhibitor of acetylcholinesterase (AchE) and MAO-B agent. AChE/MAO-B-IN-7 can also inhibit Aβ42 aggregation for use in Alzheimer's disease (AD) research.

hAChE-IN-10 (Compound ET11) is the inhibitor for human acetylcholinesterase (AChE) with an IC₅₀ of 6.34 nM. hAChE-IN-10 scavenges free radicals, and exhibits antioxidant activity. hAChE-IN-10 exhibits metal chelating activity, inhibits Cu²⁺-induced Aβ1-42 aggregation, reduces the formation of amyloid plaques, and exhibits neuroprotective activity. hAChE-IN-10 ameliorates the Scopolamine (HY-N0296)-induced cognitive impairment in mouse models.

GL-522 (4-Sulfocalix[8]arene) is a Aβ42 inhibitor. GL-522 bind to Aβ42 through nonspecific and multipoint hydrophobic interactions with a K_d of 276  μM. GL-522 effectively inhibits Aβ42 fibrillation and reduces amyloid cytotoxicity. GL-522 can be used for Alzheimer's disease research.

MNP2 is a NLRP3-ASC interaction inhibitor. MNP2 selectively binds to the PYD domain of ASC (K_a=149 nM) and blocks ASC-PYM binding (K_a=58 nM), thereby inhibiting the interaction between ASC and NLRP3 and suppressing the formation of the NLRP3 inflammasome. MNP2 inhibits IL-1β release and caspase-1 maturation, and reduces the efflux of potassium and chloride ions. MNP2 prevents mitochondrial damage and reactive oxygen species production, and significantly decreases NLRP3 inflammasome formation in neurodegenerative pathologies induced by β-amyloid, Tau protein and α-synuclein. MNP2 is applicable for the research of neurodegenerative diseases.

AChE-IN-62 (Compound 1) is an effective mixed and selective acetylcholinesterase (AChE) inhibitor with an IC₅₀ value of 0.421 μM. AChE-IN-62 exhibits excellent blood-brain barrier permeability and neuroprotective effects. Additionally, AChE-IN-62 can inhibit the aggregation of Aβ_1-42 with an IC₅₀ value of 44.64 μM. AChE-IN-62 is also an effective multi-target-directed ligand (MTDL) that can be utilized in the research of Alzheimer's disease.

AChE-IN-85 (Compound 7k) is an AChE inhibitor with an IC₅₀ of 0.083 μM. AChE-IN-85 can inhibit the release of NO, the production of TNF-α and IL-1β, the levels of LDH and ROS, as well as the aggregation of Aβ42. AChE-IN-85 has anti-inflammatory and neuroprotective effects and can be used in the research of diseases such as Alzheimer's disease.

trans-Sobrerol (NRM-331) is a potent mucofluidifying agent. trans-Sobrerol demonstrates an anti-amnesic effect by enhancing hippocampal cholinergic signaling, alongside exhibiting anti-tau and anti-Aβ synthesis properties. trans-Sobrerol mitigates memory impairment induced by Scopolamine (HY-N0296). trans-Sobrerol can be used in the research of Alzheimer's disease.

AY1511 is an amyloid β (Aβ) aggregation inhibitor with low cytotoxicity.

tau/Aβ40 aggregation-IN-1 (Compound 20) is a tau and Aβ₄₀ aggregation inhibitor with IC₅₀s of 1.8 μM and 1.3 μM, respectively.