Aβ-IN-1

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

Aβ-IN-1 TFA inhibits and reverses different types of protein aggregation.

AChE/Aβ-IN-1 (compound 32) is a potent, orally active acetylcholinesterase (AChE) inhibitor with an IC50 of 86 nM and an NMDA receptor antagonist targeting the GluN1-1b/GluN2B subunit combination with an IC50 of 3.876 μM. It also impedes Aβ aggregation, exhibits favorable blood-brain barrier permeability, offers neuroprotection, and enhances cognitive and spatial memory in rat models [1].

DAGLβ-IN-1 is a universal intermediate for designing DAGL tailored activity-based probes, and is an inhibitor of diacylglycerol lipase-β (DAGLβ).

Casein kinase 1δ-IN-1 (WAY-643895) is an inhibitor of casein kinase 1δ (CK1δ) and can be utilized in the study of neurodegenerative diseases, such as Alzheimer's disease.

PI3Kδ-IN-1 is an efficacious PI3Kδ inhibitor (IC50 of 1.7 nM).

TNF-α-IN-1 is a TNF-α inhibitor.

Cavα2δ-IN-1 demonstrates exceptional specificity for voltage-gated calcium channels Cavα2δ-1 (with a Ki value of 6 nM), in comparison to Cavα2δ-2 (with a Ki value greater than 10,000 nM).

K-Ras-PDEδ-IN-1 is a potent inhibitor of competitive K-Ras-PDEδ that binds to the farnesyl binding pocket of PDEδ (Kd of 8 nM).

Enpp/Carbonic anhydrase-IN-1 (compound 1e) is a potent inhibitor of Enpp and carbonic anhydrase, exhibiting IC50s of 1.36, 1.35, 3.00, 0.88, and 1.02 µM for NPP1, NPP2, NPP3, CA-II, and CA-IX respectively. Enpp/Carbonic anhydrase-IN-1 also demonstrates selective antiproliferative activity for cancer cells.

Amyloid-β-IN-1 (compound 13), a synthetic peptide featuring the hydrophobic C-terminal segment "VVIA-NH2" and its reversed sequence "AIVV-NH2" derived from Aβ 42, acts as an Aβ inhibitor. It effectively inhibits Aβ aggregation and exhibits neuroprotective effects.

hAChE/hBuChE/GSK-3β-IN-1 (Compound 6c) is a multi-target compound designed for Alzheimer's treatment capable of crossing the blood-brain barrier. It inhibits hAChE with an IC50 of 28.88 nM, hBuChE with an IC50 of 131.90 nM, and GSK-3β with an IC50 of 51.42 nM. Additionally, it acts as an inhibitor of tau protein and Aβ protein aggregation.

Bromodomain IN-1 is an inhibitor of Bromodomain.

ERK2 IN-1, a selective ERK2 inhibitor, exhibits an IC50 of 7 nM.

SHP2 IN-1 is an allergic SHP2 (PTPN11) inhibitor(IC50 : 3 nM).

TBK1/IKKε-IN-1 is a dual inhibitor of TBK1 and IKKε with IC50 values of less than 100 nM.

β-Glucuronidase-IN-1 is an E. coli β-glucuronidase (β-glucuronidase) inhibitor with a potent, selective, non-competitive, and orally active IC50 and Ki value of 283 nM and 164 nM, respectively, against E. coli β-glucuronidase.

Lp-PLA2-IN-1 (Lp-PLA2 inhibitor 1) suppresses Lp-PLA2 activity processes for their preparation. Lp-PLA2-IN-1 (Lp-PLA2 inhibitor 1) also inhibits to compositions containing them and to their use in the treatment of diseases associated with the activity of Lp-PLA2, for example, atherosclerosis, Alzheimer's disease.

EGFR/PI3Kα-IN-1 (compound 30k), a dual EGFR/PI3Kα inhibitor, exhibits potent activity with IC 50 values of 3.6 nM (EGFRL858R/T790M) and 30 nM (PI3Kα). It effectively inhibits tumor cell proliferation and demonstrates significant anticancer activity.

TNF-α/IL-1β-IN-1 (compound 11a) is an anti-inflammatory agent that effectively reduces the expression of TNF-α and IL-1β, inhibits oxidative stress and myocardial cell apoptosis, and demonstrates significant activity against septic myocardial injury. Additionally, it improves myocardial blood flow in vivo.

CAⅡ-IN-1 (compound 2i) is an inhibitor of the CA Ⅱ isozyme, exhibiting an IC50 of 0.44 µM. This compound is utilized in metabolic research.

Erα-IN-1 (compound 3c) is an inhibitor of the estrogen receptor α (ERα), effectively blocking ERα activity in MCF7/ERE-LUC cells.

IFNα-IN-1 (AJ2-18) is an inhibitor of IFNα, capable of suppressing the production of IFN-α. It is applicable in inflammation research.

ChAT IN-1 is a selective inhibitor of Choline Acetyltransferase (ChAT) that is utilized in studying mechanisms related to non-neuronal ChAT overexpression in cancers such as colon cancer and lung cancer, as well as in research concerning Alzheimer's disease (AD).