ce1

BACE1-IN-1 is a high brain penetrant BACE1 inhibitor (IC50s: 32 and 47 nM for human BACE1 and BACE2).

BACE1-IN-2 is a BACE1 inhibitor (IC50: 22 nM).

BACE1-IN-4 is a potent and highly selective BACE1 inhibitor (IC50: 3.8 nM; Ki: 1.9 nM), exhibiting greater selectivity for BACE1 over BACE2.

BACE1-IN-5 (Compound 15), a potent β-site amyloid precursor protein cleaving enzyme 1 (BACE1) inhibitor, demonstrates significant efficacy with an IC50 of 9.1 nM for BACE1 inhibition and an impressive IC50 of 0.82 nM against cellular amyloid-β (Aβ) production. Additionally, it is engineered to enhance hERG inhibition and P-gp efflux, indicating its optimized medicinal chemistry profile [1].

BACE1-IN-6 is a BACE1 inhibitor with an IC50 value of 1.5 nM.

BACE1 2-IN-1 (compound 34) is an effective BACE1 and BACE2 inhibitor with IC50 values of 0.01 and 0.0053 μM, respectively. It exhibits a lower Pgp efflux ratio, improved passive permeability, and decreased metabolic stability in liver microsomes.

AChE BACE1 GSK3β-IN-1 is an orally active, blood-brain barrier-permeable, moderately bioavailable triple inhibitor of AChE, BACE1, and GSK3β, utilized for Alzheimer's disease (AD) research.

BACE1-IN-12 is a potent BACE1 inhibitor (IC50: 8.9 μM) that can cross the blood-brain barrier. BACE1-IN-12 selectively inhibits BuChE (butylcholinesterase) activity (IC50: 3.2 μM). BACE1-IN-12 has potential for anti-Alzheimer's disease studies.

BACE1-IN-8 is a potent inhibitor of BACE1 (β-site APP lyase 1) (IC50: 3.9 μM).

BACE1-IN-10 is a potent inhibitor of BACE1, demonstrating sub-micromolar activity against recombinant BACE1 (rBACE1) [1].

BACE1-IN-13 (Compound 36), an orally active inhibitor of BACE1, exhibits high potency with an IC50 of 2.9 nM and demonstrates greater efficacy in hAβ42 cells (IC50 = 1.3 nM). It is considered safe for the cardiovascular system and induces a sustained reduction of Aβ42 in both mouse and dog animal models [1].

Nevadensin is an important herb-based constituent inhibiting estragole bioactivation. Nevadensin protects against a methyleugenol-induced marker of hepatocarcinogenicity in male F344 rat. It also exhibits inhibition activity against Mycobacterium tuberculosis, with equal MIC value of 200 microg mL.

Tanshinone IIA anhydride is a potent, irreversible inhibitor of human carboxylesterase (CE), exhibiting inhibitory constants (K i values) of 1.9 nM for human CE1 and 1.4 nM for human intestinal CE (hiCE), respectively [1].