cns diseases

δ-secretase inhibitor 11 is an inhibitor of δ-secretase and can be used as a lead compound for translational development of AD treatment.

AGI-43192 is a potent methionine adenosine transferase 2A (MAT2A) inhibitor that penetrates the blood-brain barrier. AGI-43192 inhibits S-adenosine methionine (SAM) production metabolic enzyme and methionine adenosine transferase 2A (MAT2A), which has the potential to study the role of SAM regulation in the central nervous system (CNS) and the treatment of cancer diseases.

GSK-1482160 is a CNS-penetrant negative allosteric modulator of P2X7 receptor with oral activity. The P2X7 receptor is involved in the production of pro-inflammatory cytokines by central and peripheral immune cells, so GSK-1482160 has the potential to study inflammatory diseases. GSK-1482160 shows excellent in vitro potency (in functional and electrophysiological assays at recombinant and naive P2X7 receptors across multiple species including humans) and cross-target selectivity.

AZD6538 is an mGluR5 negative allosteric modulator used in the study of CNS-related diseases such as Alzheimer's disease.

ML365 is a novel selective small molecule inhibitor of TASK1(KCNK3).

KH-259 (compound 1) is a highly potent, selective, and CNS-penetrant HDAC6 inhibitor, with an IC50 of 0.26 μM, exerting antidepressant effects in mice by inhibiting HDAC6 within the brain and holding promise as a valuable tool for neurodegenerative diseases research [1].

S1P receptor agonist 2 (compound 1) is a selective agonist of the S1P5 receptor, exhibiting higher selectivity than for S1P1 and or S1P3 receptors. It is useful in the endogenous SIP signaling system and for mitigating or preventing central nervous system (CNS) diseases, including neurodegenerative diseases.

mTOR inhibitor-12 (Compound 11), a selective, brain-penetrant mTOR inhibitor, exhibits no genotoxicity risk and is utilized in research pertaining to central nervous system (CNS) diseases [1].

BET-IN-24 (example 2) is a bromodomain and extra-terminal (BET) inhibitor used in studies of virology, heart failure, inflammation, central nervous system (CNS) diseases, and various cancers.

NT376 is a potent and selective inhibitor of class IIa Histone deacetylases (HDAC), exhibiting an IC50 value of 32 nM and demonstrating efficacy similar to NT160 (IC50 = 46 nM) in HT-29 cells. This compound is a promising candidate for research into various cancers and central nervous system (CNS) disorders, including Alzheimers and Huntingtons diseases.

NRMA-8 is a small-molecule nuclear receptor modulator capable of penetrating the brain. It holds potential for research into central nervous system (CNS) diseases, including Alzheimer's disease, Parkinson's disease, demyelinating diseases, and glioblastoma.

Lu AF27139 is an effective and selective antagonist of P2X7 receptor (IC50s of 12 and 2.4 nM for human and rat, Kis of 22, 54, and 13 nM for mouse, human, and rat, respectively). Lu AF27139 can be used in CNS diseases studies.