BCH

BCH001 is a specific small-molecule inhibitor of PAPD5.

BCH-24426 is a PDE3 inhibitor.

LAT1-IN-1 (BCH) is a selective and competitive inhibitor of L-type amino acid transporter protein 1 (LAT1). LAT1-IN-1 has antitumor activity, inducing apoptosis in tumor cells and inhibiting cell proliferation.

Lamivudine (BCH-189) is a reverse transcriptase inhibitor and ZALCITABINE analog in which a sulfur atom replaces the 3' carbon of the pentose ring. It is used to treat HIV disease.

Troxacitabine, a DNA polymerase inhibitor, is potentially used for the treatment of acute myeloid leukemia (AML). In comparison with gemcitabine, troxacitabine was equally active against MiaPaCa and was more efficacious against Panc-01.

SPD-756, a nucleoside reverse transcriptase inhibitor, is used potentially for the treatment of HIV infection.

BCH-HSP-C01 is a lead compound that restores AP-4 dependent protein transport in neuronal models of adaptor protein complex 4 (AP-4) related hereditary spastic paraplegia. It is applicable in research on autophagy-related diseases.

BCH 2763 is an effective, selective bifunctional thrombin inhibitor that blocks both the anion binding exosite and the active catalytic site.

hBChE-IN-2 is a butyrylcholinesterase (BChE) inhibitor and cannabinoid receptor 2 (CB2R) agonist with neuroprotective activity for the study of Alzheimer's disease-like neurological disorders.

BChE/HDAC6-IN-2 is a selective and potent dual inhibitor of BChE and HDAC6 with neuroprotective and reactive oxygen species (ROS) scavenging activity. BChE/HDAC6-IN-2 is a metal ion co-agonist that inhibits tau phosphorylation and can be used in the study of immune and neurological diseases.

UbcH5c-IN-1 is a selective small-molecule Ubiquitin-conjugating enzyme UbcH5c inhibitor (Kd: 283 nM for E2 UbcH5c-IN-1 by covalent binding with Cys85).

AChE/BChE-IN-21 is an antagonist of the histamine H3 receptor, a calcium channel blocker, and an acetylcholinesterase inhibitor. It exhibits neuroprotective activities against H2O2 and Aβ1-40, and can restore cognitive functions in AD mice.

hBChE-IN-3 (compound 30) serves as both an activator of carbonic anhydrase (CA) and an inhibitor of cholinesterase (ChE), exhibiting IC50 values of 7.4 nM for AchE and 1.9 nM for BchE. This compound is utilized in the research of neurodegenerative and psychiatric disorders.

hBChE-IN-4 (compound 40) serves as an effective activator for hCA and an inhibitor for BChE. It demonstrates affinity for various hCA subtypes with affinity constants (KA) of 266 nM for hCA I, 76.9 nM for hCA II, 918 nM for hCA IV, 893 nM for hCA VB, and 98.0 nM for hCA VII. Inhibition concentrations (IC50) for eeAChE and eqBChE are recorded at 72.1 nM and 4.2 nM, respectively. hBChE-IN-4 is non-cytotoxic and has demonstrated potential cognitive enhancement effects. It holds potential for research in neurodegenerative and other neuropsychiatric disorders.

BChE-IN-35 (Azo-9) is an inhibitor of BChE. This compound exhibits dynamic cis/trans conformational changes, with the cis isomer preferentially binding to BChE. Additionally, BChE-IN-35 can be utilized in research on Alzheimer's disease (AD).

AChE/BChE-IN-22 (compound 7) exhibits competitive inhibition against both AChE and BChE enzymes, with inhibition constants of 28.18 μM and 41.74 μM respectively.

AChE/BChE-IN-23 (Compound 6e) is a dual inhibitor of acetylcholinesterase and butyrylcholinesterase, exhibiting IC50 values of 0.91 μM for AChE, 1.19 μM for eqBChE, and 1.01 μM for hBChE. This compound also demonstrates antioxidant properties and inhibits the aggregation of Aβ1-42 and Tau proteins. Moreover, AChE/BChE-IN-23 prevents the activation of microglial cells by inhibiting the release of reactive oxygen species and mitochondrial damage. Additionally, it reduces the levels of the NLRP3 inflammasome in human microglial cells and reverses memory impairment in mice induced by scopolamine.

AChE/BChE-IN-24 (compound 5k) functions as a neuroprotective agent by inhibiting acetylcholinesterase. It targets both AChE and BChE, demonstrating IC50 values of 16.38 μM and 10.44 μM, respectively.

AChE/BChE-IN-25 (Compound 6e) is an orally active inhibitor of hAChE and eqBChE, with IC50 values of 7.9 nM and 0.79 nM, respectively. This compound exhibits antioxidant activity, effective in scavenging free radicals with an IC50 of 22.91 μM. AChE/BChE-IN-25 demonstrates neuroprotective effects by reducing mitochondrial and cellular oxidative stress in a Drosophila Alzheimer's model and improves spatial and cognitive memory impairments induced by Scopolamine in mouse models.

BChE-IN-39 (Compound 7c) selectively inhibits butyrylcholinesterase (BChE) with an IC50 of 0.08 μM, while showing an IC50 of 3.98 μM for acetylcholinesterase (AChE) inhibition. Additionally, BChE-IN-39 downregulates GSK-3β expression, thereby inhibiting the excessive phosphorylation of tau protein.

BChE-IN-38 (compound 13) is a potent BChE inhibitor, with Ki values of 62.05, 28.78, 14.09, and 1.15 nM for hCAI, hCAII, AChE, and BChE, respectively. BChE-IN-38 also demonstrates cytotoxic activity.

AChE/BChE/MAO-B-IN-5 is a multi-target inhibitor capable of crossing the blood-brain barrier, targeting cholinesterases (AChE and BChE) and monoamine oxidase MAO-B. It exhibits IC50 values of 0.24 µM for AChE, 6.29 µM for BChE, and 0.11 µM for MAO-B. AChE/BChE/MAO-B-IN-5 holds potential for research in neurodegenerative diseases such as Alzheimer's disease.

AChE/BChE-IN-26 (Compound 20aa) is a cholinesterase inhibitor with IC50 values of 0.75 μM for eeAChE and 4.11 μM for eqBChE. This compound possesses antioxidant properties and is applicable in research related to diseases such as Alzheimer's.

BChE-IN-40 (compound D40) is a potent butyrylcholinesterase inhibitor with an IC50 of 0.59 μM. It demonstrates significant anti-inflammatory effects, with an IC50 of 4.55 μM in inhibiting nitric oxide production. Additionally, BChE-IN-40 exhibits excellent permeability across the blood-brain barrier.