microglial

Edicotinib (JNJ-527) is a brain penetrant and orally active inhibitor of the colony-stimulating factor-1 receptor (IC50: 3.2 nM). It shows less inhibitory effects on KIT and FLT3 (IC50: 20 nM and 190 nM). It has the potential for Alzheimer's disease and rheumatoid arthritis treatment.

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.

Tuftsin 3TFA is a tetrapeptide. It is a macrophage/microglial activator.

Amyloid β-Protein 10-20 acetate (Amyloid β-Protein 10-20 acetate (152286-31-2 free base)) is a fragment of Amyloid-β peptide, maybe used in the research of neurological disease.Amyloid β protein fragment containing the α-secretase processing site (Lys16-Leu17 bond). It also contains the HHQK domain (residues 13-16) responsible for binding to microglial cells.

PLX5622 is a highly selective, brain-penetrant, and orally active CSF1R inhibitor.

Shanzhiside methylester reduces neuropathic pain by activating spinal GLP-1 receptors and subsequently stimulating microglial β-endorphin expression via the p38 MAPK signaling.

SNU-BP is an agonist of PPAR-gamma, inhibiting lipopolysaccharide (LPS)-induced NO production and pro-inflammatory cytokines. SNU-BP potentiates interleukin-4-induced arginase-1 expression, and promotes microglial polarization toward an M2 anti-inflammatory phenotype.

8-Bromo NAD+ serves as a prodrug for the cyclic ADP-ribose (cADPR) inhibitor, 8-bromo cADPR, undergoing conversion to its active form by the enzyme CD38. At a concentration of 1 mM, it effectively inhibits the rise in intracellular calcium levels and chemotaxis triggered by N-formyl-Met-Leu-Phe (fMLP) in mouse bone marrow-derived neutrophils. Furthermore, when applied at 100 µM, this compound reduces LPS-induced nitrite production and decreases the secretion of TNF-α and IL-2 in mouse primary microglial cells.

Methylene Blue (Basic Blue 9) hydrate functions as an inhibitor of guanylyl cyclase (sGC), monoamine oxidase A (MAO-A), and NO synthase (NOS). This compound, known for its vasopressor activity, is widely utilized as a dye in various medical procedures. It operates via the nitric oxide synthase/guanylate cyclase signaling pathway to diminish prepulse inhibition and possesses the capacity to cross the blood-brain barrier. Methylene Blue hydrate acts as a REDOX cycling compound and inhibits Tau protein aggregation. Moreover, it is effective in reducing cerebral edema, damping microglial activation, and alleviating neuroinflammation, demonstrating its multifaceted therapeutic potential [1] [2] [3].

CHPG is a selective agonist of mGluR5. In BV2 microglial cells, it attenuates SO2-induced oxidative stress and inflammation through the TSG-6 NF-κB pathway.

Tuftsin diacetate, a tetrapeptide (Thr-Lys-Pro-Arg), is a macrophage microglial activator found in the Fc-domain of the heavy chain of immunoglobulin G. It possesses a broad spectrum of activities related to immune system function, exerting effects primarily on phagocytic cells, notably on macrophages.

γ-Fibrinogen377-395 TFA is an inhibitory peptide derived from fibrinogen, which also functions as a fibrinogen epitope. It effectively blocks microglial activation and impedes fibrin-Mac-1 interactions in vitro. Additionally, it exhibits in vivo efficacy by suppressing experimental autoimmune encephalomyelitis (EAE) in mice. This compound has applications in researching multiple sclerosis (MS) and other neuroinflammatory diseases linked to blood-brain barrier disruption and microglial activation [1].

CD33 splicing modulator 1 (Compound 1) is a CD33 splicing modulator that targets the CD33 Siglec 3 myeloid cell surface receptor, known for regulating microglial cell activity, and holds potential for studying neurodegenerative diseases such as Alzheimer's disease.

(4S)-10-Nor-calamenen-10-one (Compound 15), an eudesmane sesquiterpene from Alpinia oxyphylla [1], enhances LPS-induced nitric oxide (NO) production in microglial cells.

15-Methoxypinusolidic acid has anti-inflammatory effects, it inhibits LPS-induced iNOS expression and NO production, independent on MAPK and NF-kappaB. 15-Methoxypinusolidic acid suppresses adipocyte differentiation through the inhibition of PPARgamma-dep

1. beta-Asarone (Cis-Isoelemicin) may be a potential preventive drug for Alzheimer's disease. 2. Beta-Asarone prevents autophagy and synaptic loss by reducing ROCK expression in SAMP8 mice. 3. The co-administration of beta-Asarone(Cis-Isoasarone) and l-dopa may contribute to the treatment of 6-OHDA-induced damage in rats by inhibiting autophagy activity. 4. Beta-Asarone exhibits anti-inflammatory effects by suppressing the production of pro-inflammatory mediators through NF-κB signaling and the JNK pathways in activated microglial cells and might be developed as a promising candidate to treat various neuroinflammatory diseases.

NCI 126224, a toll-like receptor 4 (TLR4) antagonist, demonstrates selective inhibition of nitric oxide (NO) production in RAW 264.7 macrophages, triggered by the TLR4 agonist LPS (IC50 = 0.31 µM), as opposed to minimal effects on NO production induced by agonists for TLR7/8 (R-848), TLR1/2 (Pam3CSK4), and TLR3 (poly(I:C)). Nevertheless, it also effectively inhibits NO production initiated by the TLR2/6 agonist FSL-1 at an IC50 of 0.6 µM in the same cell line. Moreover, NCI 126224 suppresses LPS-induced NF-κB activity in BV-2 microglial cells and reduces LPS-triggered increases in IL-1β and TNF-α levels in RAW 264.7 macrophages with IC50 values of 5.92, 0.42, and 1.54 µM, respectively.

AZD8797 (KAND567) is an orally available, selective and potent human CX3CR1-converting antagonist with inhibitory effects on CX3CR1 and CXCR2, and potentially protects against SARS-CoV-2-induced neuronal damage, preventing worsening of nociceptive sensitization and microglial activation in a migraine model of rats following seizures.

1. Kamebakaurin (Kamebakaurine) has the ability to protect the liver from APAP-induced hepatotoxicity, presumably by both inhibiting the inflammatory response and oxidative stress. 2. Kamebakaurin inhibits the expression of hypoxia-inducible factor-1α and its target genes to confer antitumor activity. 3. Kamebakaurin has anti-cancer and anti-inflammatory activities through direct inhibition of DNA-binding activity of nuclear factor-kappa B (NF-κB) p50.4. Kamebakaurin has anti-neuroinflammatory activity via inhibition of c-Jun NH -terminal kinase and p38 mitogen-activated protein kinase pathway in activated microglial cells.

HDAC-IN-62 (Compound 5), an HDAC inhibitor, exhibits IC50 values of 0.78, 1.0, and 1.2 μM for HDAC6, HDAC8, and HDAC11, respectively. This compound suppresses microglial activation via autophagy induction and reduces nitric oxide production, demonstrating anti-inflammatory and antidepressant properties. Additionally, HDAC-IN-62 has been shown to inhibit microglial activation in mouse brains [1].

Nargenicin is a macrolide antibiotic that selectively inhibits the growth of S. aureus, methicilin resistant S. aureus (MRSA), and M. luteus (MICs = 0.6, 0.3, and 2.5 μg/ml, respectively) over a panel of 11 Gram-positive and Gram-negative bacteria (MICs = >80 μg/ml). [1] It dose-dependently inhibits S. aureus DnaE in the presence of DNase I-activated DNA and E. coli DnaE when used at concentrations of 0.00001-0.1 and 0.01-100 μg/mL, respectively. [2] In murine BV-2 microglial cells, nargenicin (1 μM) inhibits cytokine expression and nitric oxide production induced by LPS.[3] Nargenicin (200 μM), when used in combination with 1,25-dihydroxyvitamin D3 or all-trans retinoic acid , reduces cell proliferation by 37-47% and increases cell differentiation by 82-85% in HL-60 human myeloid leukemia cells.[4]

(+)-Hannokinol and MESO-hannokinol can significantly inhibit lipopolysaccharide-induced nitric oxide production in BV2 microglial cells at concentrations ranging from 1 microM to 100 microM.

Jaceosidin has anti-oxidative activity. Jaceosidin has anti-inflammatory activity, also a microglial inhibitor with anti-neuroinflammation activity. aceosidin has anticancer activity, modulates the ERK/ATM/Chk1/2 pathway, leading to inactivation of the Cd

Herpotrichone B exhibits significant anti-neuroinflammatory activity by inhibiting lipopolysaccharide (LPS)-induced inflammation in BV-2 microglial cells, demonstrating a half maximal inhibitory concentration (IC50) of 0.11 μM.

1β,6α-Dihydroxyeudesm-4(15)-ene (Voleneol,DE) can attenuate the lipopolysaccharide (LPS)-induced inflammation in BV2 microglial cells, it also can dose-dependently suppress the protein expression of inducible nitric oxide synthase (iNOS) and cyclooxygenas

Potent and selective CB2 receptor agonist (Ki = 12.8 nM; EC50 = 38.67 nM). Exhibits negligible affinity for the CB1 receptor (Ki > 40,000 nM) and no activity at the GPR55. Suppresses neuroinflammation by reducing microglial activation in a multiple sclerosis mouse model. BBB permeable; anti-inflammatory and neuroprotective.

PLX5622 hemifumarate is a highly selective, brain-penetrant, and orally active CSF1R inhibitor with an IC50 of 0.016 μM and Ki of 5.9 nM. It allows for extended and specific microglial elimination preceding and during pathology development and demonstrates desirable PK properties in various animals [1] [2].

T-5342126 is a toll-like receptor 4 (TLR4) antagonist that reduces LPS-induced production of nitric oxide (NO) in RAW 264.7 cells (IC50 = 27.8 μM) and decreases LPS-induced IL-8, TNF-α, and IL-6 production in isolated human whole blood (IC50s = 110.5, 315.6, and 318.4 μM, respectively). T-5342126 (82 mg kg) also reduces ethanol intake and the abundance of ionized calcium-binding adapter molecule 1 (Iba1), a marker of microglial activation, in the central nucleus of the amygdala in ethanol-dependent mice.

γ-Fibrinogen377-395 is a peptide derived from fibrinogen, functioning both as an inhibitory molecule and an epitope. It inhibits microglial activation, disrupts fibrin-Mac-1 interactions in vitro, and mitigates experimental autoimmune encephalomyelitis (EAE) in murine models in vivo. This compound is relevant for research into multiple sclerosis (MS) and other neuroinflammatory disorders characterized by blood-brain barrier compromise and microglial activation [1].

Anti-inflammatory agent 5 effectively inhibits nitric oxide (NO) production in lipopolysaccharide-induced BV-2 microglial cells.

Herpotrichone A exhibits strong anti-neuroinflammatory effects in BV-2 microglial cells induced by lipopolysaccharide (LPS), achieving a half maximal inhibitory concentration (IC50) of 0.41 μM.

LAU-0901, a platelet-activating factor (PAF) receptor antagonist, demonstrates efficacy in reducing infarct volume and enhancing neurological function in rats subjected to middle cerebral artery occlusion (MCAO)-induced cerebral ischemia, at doses of 30, 60, and 90 mg/kg. Furthermore, it diminishes microglial infiltration while promoting astrocytic and neuronal survival in the same model. Additionally, at a dose of 30 mg/kg, LAU-0901, either alone or combined with atorvastatin, shows a capability to inhibit tumor growth in a U87MG glioblastoma mouse orthotopic tumor model.

MAO-B-IN-8 is a highly potent and reversible inhibitor of monoamine oxidase-B (MAO-B), also inhibiting microglial production of neuroinflammatory mediators. This compound is specifically designed for research on neurodegenerative diseases [1].

MMP-9 inhibitor I is an inhibitor of matrix metalloproteinase-9 (MMP-9) that is selective over MMP-1 and MMP-13 (IC50s = 5, 1,050, and 113 nM, respectively). It also decreases the activity of TNF-α converting enzyme (TACE) in a dose-dependent manner (IC50 = 0.54 μM). MMP-9 inhibitor I decreases TNF-α secretion stimulated by LPS in BV-2 microglial cells when used at concentrations of 50 and 100 μM.

NEP(1-40) TFA is a peptide antagonist of the Nogo-66 receptor (NgR), which attenuates myelin-derived inhibition and mitigates injury-induced shifts in microglial morphology distributions [1].

Amyloid β-Protein (10-20) is a fragment of Amyloid-β peptide, maybe used in the research of neurological disease.Amyloid β protein fragment containing the α-secretase processing site (Lys16-Leu17 bond). It also contains the HHQK domain (residues 13-16) re

Nrf2 Activator-8 (Compound 10e), with an EC50 of 37.9 nM, is a potent Nrf2 activator that demonstrates significant antioxidant and anti-inflammatory properties in BV-2 microglial cells. Furthermore, this compound notably ameliorates spatial memory deficits in a mouse model of lipopolysaccharide (LPS)-induced neuroinflammation [1].

Shizukaol B exerts anti-inflammatory effects in LPS-activated microglia partly by modulating JNK-AP-1 signaling pathway; it also shows significant anti-neuroinflammatory effects by inhibiting nitric-oxide (NO) production in lipopolysaccharide (LPS)-stimul