microglia

Astramembrangenin (Cycloastragenol (Astramembrangenin)) is a triterpenoid saponin compound and a hydrolysis product of the main active ingredient in Astragalus membranaceus. Cycloastragenol (CAG) may have a novel therapeutic role in depression

7-bromoindirubin-3'-oxime (7BIO) is a caspase independent nonapoptotic cell death inducer. 7BIO is an inhibitor of FLT3, DYRK1A, DYRK2, Aurora B and Aurora C kinases.

PLX5622 is an orally active small-molecule CSF1R inhibitor that selectively depletes microglia in the brains of mice and rats. It is commonly used to establish models related to microglia-associated neuroinflammation, neurodegenerative diseases (such as Alzheimer's disease and Parkinson's disease), brain injury, and neuroimmune regulation.

Geranylgeraniol (FT0626663) is an isoprenoid found in fruits, vegetables, and grains, including rice. Geranylgeraniol (FT0626663) inhibits growth and induces apoptosis of various tumor cells. Geranylgeraniol (FT0626663) protects monocytes against statin-induced cytotoxicity and suppresses the growth of Mycobacterium.

Tolebrutinib (PRN2246) is a potent, selective, orally active and brain-penetrant Bruton tyrosine kinase (BTK) inhibitor(IC50s of 0.4 and 0.7 nM in Ramos B cells and in HMC microglia cells, respectively). It exhibits efficacy in central nervous system immunity. Tolebrutinib can be used for the research of multiple sclerosis (MS).

Edicotinib (JNJ-527) is a blood-brain-penetrating, orally active, selective CSF-1R inhibitor (IC50 value is 3.2 nM), with less inhibitory effects on KIT (IC50 value is 20 nM) and FLT3 (IC50 value is 190 nM). Edicotinib (JNJ-527) can block microglial proliferation and attenuate neurodegeneration, and can be used to study Alzheimer's disease and rheumatoid arthritis.

Mulberrofuran C, a benzofuran present in Morus alba, has inhibitory effects on Aβ₁₋₄₂ auto-aggregation, tau protein aggregation, AChE, antioxidant activity and neuroprotective effects, and has anti-Alzheimer's disease potential.

D-GsMTx4 TFA, a selective spider venom peptide, is a TRPC1/6 and Piezo2 inhibitor that inhibits cation-permeable mechanosensitive channels (MSCs) belonging to the Piezo and TRP channel families, blocks cation-selective stretch-activated channels (SACs), and attenuates lysophosphatidylcholine (LPC)-induced astrocyte toxicity and microglia reactivity. toxicity and microglia reactivity.D-GsMTx4 TFA prevented myocardial infarction in a mouse model of ischemia/reperfusion and can be used to characterize the role of excitatory MSCs in normal physiology and pathology.

Sulfosuccinimidyl oleate (Sulfo-N-succinimidyl oleate) is a long-chain fatty acid that inhibits fatty acid transport into cells. It is a potent and irreversible inhibitor of the mitochondrial respiratory chain and binds the CD36 receptor on the surface of microglia. Sulfosuccinimidyl oleate is neuroprotective and alleviates stroke-induced neuroinflammation [1] [2].

JNJ-54175446 (JNJ-5446) is a CNS-permeable and selective P2X7 receptor antagonist that attenuates the release of IL-1β/IL-18 from microglia, and may be used in the study of depression.

MW01-2-151SRM is a novel small molecule inhibitor of microglia activation that crosses the blood-brain barrier, has anti-neuroinflammatory effects, attenuates the up-regulation of glial cytokines in models of neuroinflammation, and can be used in studies of traumatic brain injury, Alzheimer's disease, and alginate toxicity.

CSF1R-IN-7 is a highly selective CSF-1R inhibitor with good brain penetration for the treatment of a variety of diseases associated with microglia-mediated neuroinflammation, particularly Alzheimer's disease and other neurodegenerative disorders.CSF-1R is a type III receptor tyrosine kinase that is expressed predominantly on microglia (immune cells in the brain) and regulates the development, survival and function of microglia.

PLX5622 hemifumarate is a highly selective, blood-brain barrier-permeable, and orally active CSF1R inhibitor with an IC50 of 0.016 μM and a Ki of 5.9 nM. It can be used to eliminate proliferating and specific microglia before and during disease progression and is applicable for inducing Alzheimer's disease models.

SN50 is a cell permeable NF-κB translocation inhibitor.

HAMI 3379 is a potent and selective antagonist of the Cysteinyl leukotriene (CysLT2) receptor. HAMI 3379 has a protective effect on acute and subacute ischemic brain injury. It also attenuates microglia-related inflammation.

Adenosine-2'-monophosphate (2'-AMP) is a nucleoside derived from the conversion of 2',3'-CAMP. It inhibits inflammatory cytokine production by microglia and suppresses TNF-α and CXCL10 production in activated primary mouse microglia through A2A receptors.

(3R,5R)-Octahydrocurcumin (Compound 7) is a metabolite of Curcumin produced by gut microbiota. It exhibits neuroprotective effects against Aβ25-35-induced cell damage in SH-SY5Y cells and possesses anti-inflammatory properties in LPS-stimulated BV-2 mouse microglia.

AChE-IN-80 (Compound 1) is an inhibitor of acetylcholinesterase (AChE). It suppresses inflammation and reactive oxygen species (ROS) production in cultured neurons and microglia, induces autophagy, and prevents the spread of beta-amyloid (Aβ) fibrils. AChE-IN-80 exhibits antioxidant activity and neuroprotective effects, making it valuable for Alzheimer's disease research.

ADP-β-S trilithium is an ADP analog and P2Y12 receptor activator that upregulates IL-1β and IL-6 in microglia, promoting NLRP3 activation along with NF-κB phosphorylation and nuclear translocation.

hMAO-B-IN-11 (Compound 12) is a selective and reversible inhibitor of human monoamine oxidase B (hMAO-B) with an IC50 value of 0.11 µM. It operates by competitively binding to the active site of hMAO-B, thereby preventing the oxidative deamination of monoamines and reducing hydrogen peroxide production. Additionally, hMAO-B-IN-11 inhibits pro-inflammatory mediators (NO, TNF-α, IL-1β) in activated microglia. This compound holds potential for research in neurodegenerative diseases such as Parkinson's and Alzheimer's.

FGA139 is an inhibitor of cysteine proteases, specifically targeting cathepsin B and L with IC50 values of 4.98 μM and 3.14 μM, respectively. It reduces the production of NO in LPS-induced RAW264.7 cells and lowers TNFα levels in microglia, demonstrating antioxidant and anti-inflammatory properties. Additionally, FGA139 enhances the secretion of neuroprotective metabolites such as purines and linoleic acid in LPS-stimulated microglia. This compound is applicable in the study of neuroinflammatory diseases.

SB1617 is a neuroinflammation modulator with neuroprotective effects, reducing pathogenic tau levels through anti-inflammatory activity mediated by microglia.

STAT3-IN-28 (compound 18) is an inhibitor of STAT3. It can suppress the activation of microglia and exhibits anti-neuroinflammatory effects. Additionally, STAT3-IN-28 is capable of crossing the blood-brain barrier.

TREM2 agonist-4 (Compound 4a) is a TREM2 agonist with a Kd value of 45.9 μM. It activates the TREM2 downstream signaling pathways and enhances the phagocytic function of microglia. TREM2 agonist-4 is applicable for research into neurodegenerative diseases such as Alzheimer's disease.