Amyloid-β Inhibitor

AChE/BChE-IN-12 (compound 10b), a 3,5-dimethoxy analogue, is a potent AChE, BChE, and β-secretase-1 (BACE-1) inhibitor, with IC₅₀ values of 2.57, 3.26, and 10.65 μM, respectively. AChE/BChE-IN-12 crosses the blood-brain barrier via passive diffusion and inhibits the self-aggregation of amyloid-β monomers. AChE/BChE-IN-12 can be used for Alzheimer’s disease (AD) research.

Dendrobine-N-oxide is a dendrobine-type sesquiterpene alkaloid. It is isolated from Dendrobium nobile. Dendrobine-N-oxide inhibits neuroinflammation, reduces β-Amyloid accumulation, enhances the expression of neurotrophic factors, suppresses the hyperphosphorylation of Tau protein, and exerts anti-neuronal Apoptosis effects. Dendrobine-N-oxide shows no anticancer activity against colon cancer and pancreatic adenocarcinoma. It is used in research on neurodegenerative diseases.

Aβ aggregation-IN-2 (Compound 8i) is an inhibitor of amyloid-β protein (Aβ42) aggregation, showing approximately 91% inhibition of Aβ42 aggregation at 25 μM. It also exhibits Aβ42 disaggregation effects and antioxidant activity. Aβ aggregation-IN-2 can be used for research in the field of Alzheimer's disease.

hAChE/hBACE-1-IN-4 (compound AK-2) is a quinazoline derivative. hAChE/hBACE-1-IN-4 shows significant inhibitory activity against hAChE and hBACE-1 enzymes (hAChE, IC₅₀=0.283 μM; hBACE-1, IC₅₀=0.231 μM). hAChE/hBACE-1-IN-4 has the potential to inhibit Aβ aggregation. hAChE/hBACE-1-IN-4 has non-neurotoxicity , blood-brain barrier permeability and oral activity. hAChE/hBACE-1-IN-4 can be used in Alzheimer's disease research.

RAGE/SERT-IN-1 is a potent and orally active advanced glycation end products (RAGE) and serotonin transporter (SERT) inhibitor with IC₅₀s of 8.26 μM and 31.09 nM, respectively. RAGE/SERT-IN-1 exhibits significant neuroprotective effect against Aβ_25-35-induced neuronal damage and alleviates depressive behavior of mice. RAGE/SERT-IN-1 can be used for researching the comorbidity of Alzheimer's disease and depression.

Protriptyline hydrochloride (Standard) is the analytical standard of Protriptyline hydrochloride (HY-B0949). This product is intended for research and analytical applications. Protriptyline hydrochloride is a potent tricyclic antidepressant (TCA). Protriptyline hydrochloride inhibits AChE activity with an IC₅₀ value of 0.06 mM and inhibits Aβ self-assembly. Protriptyline hydrochloride can be used for the study of depression and Alzheimers disease.

SEN 304 is an Aβ aggregation inhibitor. SEN 304 can bind directly to Aβ(1-42), delay β-sheet formation and promote aggregation of toxic oligomers into a nontoxic form. SEN 304 can be used for research of Alzheimer’s disease.

Glutaminyl Cyclase Inhibitor 2 is a glutaminyl cyclase inhibitor with an IC₅₀ of 1.23 μM.

GSK3β-IN-3 is an ATP-competitive GSK-3β inhibitor (IC₅₀ = 0.90 μM). GSK3β-IN-3 can reduce the phosphorylation level of tau protein in the BR5706 strain and reduce the deposition of Aβ aggregates in the CL2006 strain, and can be used to research Alzheimer's disease (AD).

AChE-IN-19 (compound A15) is a highly potent AChE inhibitor with an IC₅₀ value of 0.56 μM, also inhibits Aβ aggregation. AChE-IN-19 has potent neuroprotective activities and nearly no toxicity on SH-SY5Y cells. AChE-IN-19 can be used for researching Alzheimer's disease.

2,3-Dehydrosilybin A (Standard) is the analytical standard of 2,3-Dehydrosilybin A. This product is intended for research and analytical applications. 2,3-Dehydrosilybin A is a pro-longevity and anti-aggregation compound.

Amilo-5MER (5-MP) is an orally active and selective Serum Amyloid A (SAA) inhibitor. Amilo-5MER specifically inhibits the release of pro-inflammatory cytokines IL-6 and IL-1β from SAA-activated cells. Amilo-5MER reduces chronic inflammation and relieves symptoms of diseases such as rheumatoid arthritis (RA), inflammatory bowel disease (IBD), and multiple sclerosis (MS). Amilo-5MER is promising for research of autoimmune diseases and chronic inflammatory diseases.

EQ-04 is a highly selective positive allosteric modulator (PAM) of α7 nAChR. EQ-04 has no direct inhibitory activity on AChE and BChE. EQ-04 inhibits Aβ aggregation. EQ-04 has safe cytotoxicity and potent neuroprotective activity. EQ-04 can be used for the study of Alzheimer's disease.

Ac-BIM-acid bromide is a derivative of Acridine. Ac-BIM-acid bromide significantly inhibits amyloid fibrillation. Ac-BIM-acid bromide modulates the structure of N-terminal region of Saccharomyces cerevisiae Stm1 protein (Stm1_N^1-113) and the amyloid morphology of human Aβ42 protein, inhibiting theirs growth. Ac-BIM-acid bromide can be used for Alzheimer’s disease research.

Aβ Fibrillization modulator 1 stabilizes Aβ monomers.

7-Deoxy-trans-dihydronarciclasine, an alkaloid, is a tobacco mosaic virus (TMV) inhibitor (IC₅₀: 1.80 μM). 7-Deoxy-trans-dihydronarciclasine is an anti-neuroinflammatory agent. 7-Deoxy-trans-dihydronarciclasine decreases the Aβ and APP levels in the cerebral cortex of Tg2576 mice.

AChE/Aβ-IN-5 (compound AV-2) is a bifunctional inhibitor that targets AChE and auto-induced Aβ (Amyloid-β) aggregation. AChE/Aβ-IN-5 can significantly improve scopolamine- and Aβ-induced cognitive impairment in mice.

COX-2/HDAC6-IN-1 (Compound 11e) is a dual COX-2 and HDAC6 inhibitor, with an IC₅₀ of 0.12 μM against HDAC6 and an IC₅₀ of 0.66 μM against COX-2. COX-2/HDAC6-IN-1 enhances the acetylation level of α-tubulin, regulates epigenetic gene expression, and inhibits the expression of pro-inflammatory mediators (COX-2, IL-1β, IL-6 and TNF-α). COX-2/HDAC6-IN-1 promotes Amyloid-β clearance and reduces excessive phosphorylation of Tau protein. COX-2/HDAC6-IN-1 maintains neuronal morphology by stabilizing MAP2, protects synaptic integrity by regulating synapsin, and restores the expression of memory-related genes. COX-2/HDAC6-IN-1 possesses neuroprotective activity and improves learning and memory abilities in Scopolamine (HY-N0296)-induced Alzheimer's disease mouse models. COX-2/HDAC6-IN-1 is applicable to research related to Alzheimer's disease.

2002-G12 (compound 5a) is an Aβ42 inhibitor that can reduce Aβ42 toxicity by 76%. 2002-G12 can be used in Alzheimer's research.

KMS88009 is a potent small molecule that directly interferes with the formation of amyloid-β oligomers, thereby preserving cognitive behavior when used preventively and reversing cognitive behavior decline when used therapeutically. Oral administration of KMS88009 around the onset of Alzheimer's disease symptoms significantly reduced the assembly of amyloid-β oligomers and improved cognitive behavior in the APP/PS1 double transgenic mouse model. This unique dual mode of action suggests that KMS88009 may be a powerful therapeutic candidate for the treatment of Alzheimer's disease. In an evaluation, the physicochemical properties, pharmacokinetics and toxicity of this anti-amyloidogenic small molecule KMS88009 were studied, as well as post-mortem analysis of APP/PS1 TG mice after behavioral testing.