aβ42

Aβ42-IN-2, a γ-secretase modulator with an IC50 of 6.5 nM for Αβ42, can be used for Alzheimer's disease research [1].

Aβ42-IN-1, compound 1v, is a novel, potent and orally active γ-secretase modulator (GSM). Aβ42-IN-1 potently reduced Aβ42 levels with an IC 50 value of 0.091 μM in cultured cells without inhibiting CYP3A4. Aβ42-IN-1 shows a sustained pharmacokinetic profile.

Aβ42-IN-1 free base (compound 1v), an orally active γ-secretase modulator with high brain exposure, effectively lowers Aβ42 levels with an IC50 of 0.091 μM, and significantly diminishes brain Aβ42 levels in mice. Given these properties, Aβ42-IN-1 free base represents a potential disease-modifying agent for Alzheimer's disease [1].

Ro 90-7501 is an amyloid β42 (Aβ42) protofibrillar and TPR-dependent PP5 inhibitor, a novel radiosensitizer for cervical cancer cells, which inhibits ATM phosphorylation, promotes apoptosis, and induces cell-cycle arrest. Ro 90-7501 also exhibits antiviral activity and potential anticancer activity by inhibiting ATM phosphorylation and DNA repair, and by inhibiting HCMV.

γ-Secretase modulator 13 is a γ-secretase modulator (GSMs) that inhibits the production of amyloid β-peptide Aβ42 and can be used to study Alzheimer's disease and tumors.

Hematoxylin (Natural Black 1) is a dye obtained from the heartwood of logwood (Haematoxylon campechianum Linn., Leguminosae) used as a stain in microscopy and in the manufacture of ink.

Aftin-4, an amyloid forty-two inducer, activates γ-secretase, promoting the generation of amyloid-β-1-42 (Aβ1-42) from amyloid-β protein precursor. Aftin-4(Aftin4) increased Aβ-1-42, but not Aβ-1-40 in mouse hipppocampus, accompanied by learning deficits and mitochondrial ultrastructural changes similar to those found in the brains of patients with AD. Aftin-4(Aftin4) can thus be used to induce a rapid, acute Alzheimer's disease-like toxicity in the rodent brain.

Avagacestat (BMS-708163) (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.

γ-Secretase modulator 4 is a potent γ-secretase modulator that reduces Aβ42 levels with IC50s of 0.017 μM in mice and 0.014 μM in humans.

Semagacestat (LY450139) (LY450139) is a γ-secretase blocker for Aβ42/Aβ40/Aβ38 (IC50: 10.9/12.1/12.0 nM) and also inhibits Notch signaling (IC50: 14.1 nM).

Aβ42-IN-7 (Compound CT-01) is a brain-penetrant and selective inhibitor of amyloid-β42 (Aβ42). It acts by inhibiting the aggregation of Aβ42 into neurotoxic soluble oligomers and extracellular fibrillar aggregates. Aβ42-IN-7 provides neuroprotection by reducing amyloid protein-mediated neuronal toxicity. This compound is applicable for Alzheimer's disease (AD) research.

Aβ42 agonist-1 is a small molecule compound with anticancer and NF-κB inhibitory activities. It induces Aβ42 aggregation and can be used to study neurological diseases.

Aβ42 Agonist-2 (compound 7b), a small molecule, facilitates the aggregation of Aβ42 by interacting with Aβ42 oligomers and pentamers, enhancing the self-assembly of nontoxic aggregates and accelerating fibril formation. Additionally, Aβ42 Agonist-2 prevents Aβ42-induced cytotoxicity in HT22 hippocampal neuronal cells [1].

DORA 42 is a dual antagonist of the orexin receptor OX1R and OX2R.

KBH-A42 is an inhibitor of histone deacetylase.

GIP (3-42), human (Gastric Inhibitory Polypeptide (3-42) (human)) is a peptide that acts as a glucose-dependent proinsulinotropic polypeptide (GIP) receptor antagonist and regulates insulin secretion and the metabolic effects of GIP in vivo, which can be used to study type 2 diabetes.

HXJ42 is a PP1 analog that selectively and effectively acts on wild-type ZAP-70 (AS).

CES1-IN-42 (2,2-Dimethoxy-2-phenylacetophenone) is a photoinitiator that can be used to assist in cancer research.

Anti-inflammatory agent 42 has anti-inflammatory activity and inhibits the expression of TNF-α and IL-6 in LPS-stimulated macrophages.

β-Amyloid (1-42), human, Ala(13C3,15N) TFA is a β-Amyloid (1-42), human marked with 13C and 15N. This unprocessed HFIP peptide comprises 42 amino acids and is a brain-permeable amyloid fragment, useful for researching Alzheimer's and Down syndrome. In monomer form, β-Amyloid (1-42), human provides antioxidant and neuroprotective effects. Upon HFIP monomerization and DMSO solvent preparation, it forms soluble oligomers (AβOs) at 4°C, which exhibit synaptotoxicity and neurotoxicity, while at 37°C it forms insoluble fibrils with lower neurotoxicity, involved in oxidative damage. Aβ42 oligomers interact with neuronal surface receptors such as PrPc, mGluR5, and NMDA receptor, activating signaling pathways that induce oxidative stress, calcium imbalance, synaptotoxicity, leading to neuronal dysfunction and death.

Biotin-amyloid-β (1-42) peptide is an affinity probe that allows amyloid-β (1-42) (Aβ42) to be detected or immobilized through interaction with the biotin ligand. It has been used to identify Aβ42 interaction partners in rat hippocampal synaptosomal membranes.

Amyloid-β (1-42) (Aβ42) is a neurotoxic 42-amino acid protein fragment found in amyloid plaques in postmortem cerebral cortex from patients with Alzheimer's disease.1,2,3Aggregation of Aβ42 results in the formation of neurotoxic fibrils or globular oligomers.1Aβ42 accumulates in the brain of many transgenic mouse models of Alzheimer's disease and, in many models, the onset of amyloid deposition positively correlates with deficits in spatial learning and memory.4 1.Wolfe, M.S.Therapeutic strategies for Alzheimer's diseaseNat. Rev. Drug Discov.1(11)859-866(2002) 2.Iwatsubo, T., Odaka, A., Suzuki, N., et al.Visualization of Aβ42(43) and Aβ40 in senile plaques with end-specific Aβ monoclonals: Evidence that an initially deposited species is Aβ42(43)Neuron13(1)45-53(1994) 3.Hardy, J.A., and Higgins, G.A.Alzheimer's disease: The amyloid cascade hypothesisScience256(5054)184-185(1992) 4.Jankowsky, J.L., and Zheng, H.Practical considerations for choosing a mouse model of Alzheimer's diseaseMol. Neurodegener.12(1)89(2017)

TAMRA-Amyloid-β (1-42) peptide is a fluorescently labeled peptide. Amyloid-β (1-42) (Aβ42) is a neurotoxic 42-residue protein fragment found in amyloid plaques in postmortem cerebral cortex from patients with Alzheimer's disease. Aggregation of Aβ42 results in the formation of neurotoxic fibrils or globular oligomers. TAMRA-Amyloid-β (1-42) peptide is a labeled form of Aβ42 containing carboxytetramethyl rhodamine (TAMRA), which displays excitation/emission maxima of 543/572 nm, respectively.

(Met(O)35)-Amyloid β-Protein (1-42) is the oxidized form of Methionine 35 in Aβ42, capable of producing an oligomer size distribution similar to Aβ40. This compound is utilized in Alzheimer's disease (AD) research [1].