aβ42 in 2

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].

42-(2-Tetrazolyl)rapamycin is a prodrug compound derived from a rapamycin analog.

CDK2-IN-42 (Compound H63) is a CDK12 inhibitor with an IC50 of 10 nM. It exhibits activity against ESCC cells by blocking transcription elongation, downregulating core G1 phase genes to induce cell cycle arrest, and altering the CDK12-ATM/ATR-CHEK1/CHEK2 signaling pathway, leading to DNA damage. Additionally, CDK2-IN-42 effectively inhibits tumor growth in human ESCC KYSE150 xenograft mouse models, holding promise for cancer research.

SARS-CoV-2 Mpro-IN-42 (compound C5) is a potent inhibitor of SARS-CoV-2 Mpro, exhibiting an IC50 value of 33.6 nM. It is applicable for research concerning SARS-CoV-2.

Aβ1–42 aggregation inhibitor 2 (compound 7c) is a potent inhibitor of Aβ1-42 aggregation, playing a significant role in Alzheimer's disease research. It exhibits excellent antioxidant properties, metal ion chelation ability, reduces oxidative stress, and demonstrates neuroprotective and anti-neuroinflammatory activities.

VEGFR-2-IN-42 (compound 8c) is a potent inhibitor of VEGFR-2. It inhibits the proliferation of MCF7 cells, with an IC50 value of 25 µM.

COX-2-IN-42 (Compound T1) is a COX-2 inhibitor that protects zebrafish from neuronal damage induced by PTZ.

SHP2-IN-42 is an inhibitor of the phosphatase containing the Src homology 2 domain (SHP2), with an IC50 of 15 nM. It inhibits cell proliferation, induces apoptosis, and causes G1 phase cell cycle arrest. SHP2-IN-42 is applicable in cancer research, including studies on acute myeloid leukemia (AML).

42-O-(2-Aminoethyl)-rapamycin (compound 2.3) is a derivative of the mTOR inhibitor rapamycin. This compound is utilized in pharmaceutical research for the development of conjugates.

PROTAC EZH2 Degrader-42 (compound 57) is a PROTAC degrader and antiproliferative agent that targets EZH2. It induces cIAP-mediated ubiquitination and subsequent proteasomal degradation of EZH2. PROTAC EZH2 Degrader-42 is applicable for research related to lymphoma.

Ab42-IN-C2 is an Aβ1-42 inhibitor.

(Met(O2)35)-Amyloid β-Protein (1-42) is a peptide [1].

SARS-CoV-2-IN-42 (Compound 8q) effectively inhibits SARS-CoV-2 replication with an EC50 of 0.4 μM and demonstrates no significant toxicity to the host cell [1].

42-O-(2-Azidoethyl)-Rapamycin (Compound 4) is an azide compound that serves as a pharmaceutical intermediate for synthesizing Rapamycin derivatives.

Aβ aggregation-IN-2 (Compound 8i) is an inhibitor of amyloid β-protein (Aβ42) aggregation, demonstrating an approximate 91% inhibition rate at 25 μM. It also possesses the ability to induce Aβ42 depolymerization and exhibits antioxidant activity. Aβ aggregation-IN-2 is applicable in Alzheimer's disease research.

Amyloid-β-IN-2 (Compound EX.112) is a selective inhibitor of γ-secretase. In H4 cells, it demonstrates inhibitory activity on Aβ42 secretion, with an EC50 value of 226 nM. Amyloid-β-IN-2 holds potential for research in Alzheimer's disease (AD) and diseases associated with Aβ deposition.

Donecopride is a partial agonist of the serotonin (5-HT) receptor subtype 5-HT4E(Ki= 8.5 nM) and an inhibitor of acetylcholinesterase (AChE; IC50= 16 nM).1It is selective for AChE over butyrylcholinesterase (BChE; IC50= 3,530 nM) but does bind to 5-HT2Band sigma-2 (σ2) receptors (Ki= 1.6 nM for both) in a panel of 42 neurotransmitter receptors and transporters. Donecopride induces release of soluble amyloid precursor protein-α (sAPP-α) in COS-7 cells transiently expressing 5-HT4with an EC50value of 11.3 nM. Oral administration of donecopride (1 mg/kg) reduces brain soluble and insoluble amyloid-β (1-42) levels and increases the time spent exploring the novel object in the novel object recognition (NOR) test in the 5XFAD transgenic mouse model of Alzheimer's disease. Donecopride (3 mg/kg, p.o.) prevents a reduction in spontaneous alternation behavior induced by intracerebroventricular administration of soluble Aβ42 (sAβ42) in the Y-maze in mice.2 1.Lecoutey, C., Hedou, D., Freret, T., et al.Design of donecopride, a dual serotonin subtype 4 receptor agonist/acetylcholinesterase inhibitor with potential interest for Alzheimer's disease treatmentProc. Natl. Acad. Sci. USA111(36)E3825-E3830(2014) 2.Rochais, C., Lecoutey, C., Hamidouche, K., et al.Donecopride, a Swiss army knife with potential against Alzheimer's diseaseBr. J. Pharmacol.177(9)1988-2005(2020)

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)

Amyloid-β (1-8, A2V) is a truncated form of amyloid-β (Aβ) that contains a valine to alanine substitution at position 2 of the Aβ numbering convention (Aβ A2V), which corresponds to position 673 of the amyloid precursor protein (APP) numbering convention (APP A673V). An Aβ (1-40) (Aβ40) A2V peptide increases the production of Aβ and the rate and amount of amyloid fibril formation in vitro, effects that can be reduced by coincubation with wild-type Aβ40. Aβ40 and Aβ42 levels are increased in CHO cells expressing the Aβ A2V mutation and in fibroblasts derived from patients with the Aβ A2V mutation. As a homozygous mutation, Aβ A2V is correlated with Alzheimer's disease with distinctive pathological features, but disease does not develop in patients with a heterozygous Aβ A2V mutation.

1. Licochalcone B (LCB) inhibits the proliferation of human malignant bladder cancer cell lines (T24 and EJ) in vitro and antitumor activity in vivo in MB49 (murine bladder cancer cell line) tumor model. 2. LCB and Licochalcone D(LCD) significantly reduce

5-{8-[(3,4'-Difluoro[1,1'-biphenyl]-4-yl)methoxy]-2-methylimidazo[1,2-a]pyridin-3-yl}-N-methylpyridine-2-carboxamide (1o) exhibited high in vitro potency and brain exposure, significantly reduced brain Aβ42 levels, showed no inhibitory effect on cytochrome p450 enzymes, and demonstrated excellent anti-cognitive deficits in AD model mice.

(Glu20)-Amyloid β-Protein (1-42) represents a variant of amyloid β-protein (Aβ) that fibrillizes more slowly due to the Glu20 mutation, which diminishes Aβ42's tendency to aggregate and inhibits the accumulation of this slowly fibrillizing peptide. Amyloid β-protein is the principal constituent of amyloid deposits in the vascular system and brain parenchyma in Alzheimer's disease [1] [2].

2',3'-Dihydroxy-4',6'-dimethoxychalcone (compound 1) inhibits Amyloid β-protein (Aβ42) fibrillization and aggregation, demonstrating oral activity with detectable presence in the brain [1].

AEP-IN-2 is an inhibitor of asparagine endopeptidase (AEP) that prevents the cleavage of APP and Tau by AEP. It is orally active and reduces levels of Aβ40, Aβ42, and p-Tau [1].