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.

CNS-5161 hydrochloride (CNS 5161A) is a small molecule antagonist and an NMDA receptor antagonist that selectively and non-competitively blocks the action of glutamate, and can be used for research on neurological diseases.

LY3372689 (Formulaic Ia) is an oral, highly selective, CNS-permeable O-GlcNAcase (OGA) inhibitor. LY3372689 exerts a neuroprotective effect by inhibiting OGA enzymatic activity, increasing the O-GlcNAc glycosylation level of tau protein, and thereby reducing abnormal tau phosphorylation and the formation of neurofibrillary tangles. LY3372689 can be used in research on tau-related diseases, including Alzheimer’s disease.

LRRK2-IN-7 (Compound 25) is a potent, highly selective, CNS-permeable LRRK2 kinase inhibitor with an IC₅₀ of 0.9 nM. LRRK2-IN-7 exhibits more than 1,000-fold selectivity over other kinases, ion channels, and CYP enzymes. LRRK2-IN-7 can be used in research on neurodegenerative diseases.

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.

H3R antagonist 6 (Compounds 3) (H3-2406) is a histamine receptor 3 (H3R) antagonist with an IC50 of 5.6 nM. The 18F-labeled version exhibits high radiochemical yield, molar activity, and moderate brain uptake, although it shows off-target binding with the Sigma-1 receptor. It serves as a radioligand for positron emission tomography (PET) imaging in the study of central nervous system (CNS) diseases.

H3R antagonist 7 (compounds 4) is a histamine subtype 3 receptor (H3R) antagonist with a Ki value of 3.15 nM. It can potentially be used as a PET radioligand in the study of central nervous system (CNS) diseases.

CDK9-IN-44 (Compound 7) is a selective inhibitor of CDK9 with an IC50 of 7.6 μM. It effectively inhibits CDK9/cyclin T1 kinase activity, impedes transcription elongation, reduces the expression of oncogenic proteins such as MCL1 and c-MYC, and induces apoptosis in tumor cells. CDK9-IN-44 shows potential for research in glioblastoma (GBM) and central nervous system (CNS) diseases.

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

GSK-345931A (compound 3) is a potent and orally active RIP2 (receptor interacting protein 2) inhibitor that suppresses production of multiple pro-inflammatory cytokines, suitable for studying autoimmune diseases.

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

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.

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].

TG8-260 is a selective second-generation EP2 antagonist (oral bioavailability 77.3%). It inhibits microglial inflammatory gene expression, used for CNS and peripheral inflammatory disease research.

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.