lps-stimulated

1. 2,5-Dihydroxyacetophenone (Quinacetophenone) possess anti-anxiety, and neuroprotective qualities. 2. 2,5-Dihydroxyacetophenone (Quinacetophenone) reatment can induce a sustained activation of JNK, ERK1/2, and p38 MAPKs, it also can potentiate the pro-apoptotic and anti-proliferative effects of bortezomib in U266 cells. 3. 2,5-Dihydroxyacetophenone (Quinacetophenone) has anti-inflammatory activity in activated macrophages, raising the possibility that this compound has a therapeutic potential for inflammatory conditions. 4. 2,5-Dihydroxyacetophenone (Quinacetophenone) is an uncompetitive inhibitor of murine tyrosinase (K(I) 0.28mm), it strongly inhibits both melanogenesis and cellular tyrosinase activity in vitro in 3-isobutyl-1-methylxanthin-stimulated B16 mouse melanoma cells or in vivo in zebrafish and mouse models.

Tomatidine hydrochloride (Tomatidine HCl) is a steriodal alkaloid structurally similar to Cyclopamine but does not inhibit hedgehog pathway. May be used as a negative control for Cyclopamine and KAAD-Cyclopamine. Tomatidine protects against muscle atrophy and boosting muscle growth.

Laflunimus (HR325) is a DHODH inhibitor that inhibits immunoglobulin IgM and IgG secretion in vitro and in vivo, with an IC50=2.5 μm, and exerts an immunosuppressive effect by interfering with pyrimidine metabolism, and is used in the study of neuralgia.

NLRP3/AIM2-IN-3 is a unique molecule that inhibits NLRP3 and AIM2 inflammasome activation in a species-specific manner. It has an IC50 value for cell lysis of 0.077 ± 0.008 μ M. NLRP3/AIM2-IN-3 is a potent inhibitor of NLRP3 and AIM2 inflammasome-dependent cell lysis with an IC50 value for cell lysis of 0.077 ± 0.008 μ M. NLRP3/AIM2-IN-3 inhibits LPS/nigericin NLRP3/AIM2-IN-3 inhibits LPS/nigericin-stimulated cell lysis in THP-1 macrophages with an IC50 value of 0.077 ± 0.008 μM. NLRP3/AIM2-IN-3 interferes with the interaction of NLRP3 or AIM2 with the bridging protein ASC, inhibiting oligomerization of ASC.

Cot inhibitor-2 is a cot (Tpl2/MAP3K8) inhibitor (IC50: 1.6 nM) with potency, selectivity and oral activity. cot inhibitor-2 inhibits LPS-stimulated TNF-α production in human whole blood with an IC50 of 0.3 μM.

B I09, an IRE-1 RNase inhibitor with an IC50 of 1230 nM, inhibits splicing of XBP1 mRNA in human WaC3 cells and expression of xbp-1 in LPS-stimulated B cells. B I09 can be used to simulate the defects of XBP-1 in CLL cells., an IRE-1 RNase inhibitor with an IC50 of 1230 nM, inhibits splicing of XBP1 mRNA in human WaC3 cells and expression of xbp-1 in LPS-stimulated B cells. B I09 can be used to simulate the defects of XBP-1 in CLL cells., an IRE-1 RNase inhibitor with an IC50 of 1230 nM, inhibits splicing of XBP1 mRNA in human WaC3 cells and expression of xbp-1 in LPS-stimulated B cells. B I09 can be used to simulate the defects of XBP-1 in CLL cells.

Hederagenin (Hederagenol) is a triterpenoid saponin inhibiting LPS-stimulated expression of iNOS, COX-2, and NF-κB.

Anti-inflammatory agent 42 has anti-inflammatory activity and inhibits the expression of TNF-α and IL-6 in LPS-stimulated macrophages.

AMG-548 hydrochloride is an orally active and selective p38α inhibitor (Ki: 0.5 nM) and shows slightly selective over p38β (Ki: 36 nM) and >1000 fold selective against p38γ/p38δ. It is also extremely potent in the inhibition of whole blood LPS stimulated TNFα (IC50: 3 nM).

AMG-548 is a selective and orally active p38α MAPK inhibitor (Ki = 0.5 nM), with higher selectivity than p38β, p38γ, and p38δ, and can also inhibit the TNFα, CK1δ/ε, and Wnt signalling pathways.

AMG-548 dihydrochloride is an orally active and selective p38α inhibitor (Ki: 0.5 nM) and shows slightly selective over p38β (Ki: 36 nM) and >1000 fold selective against p38γ/p38δ. It is also extremely potent in the inhibition of whole blood LPS stimulate

Murrayafoline A is a natural carbazole alkaloid found primarily in plants of the genera Murraya and Glycosmis. Murrayafoline A directly targets Specific Protein 1 (Sp1), thereby inhibiting the NF-κB and MAPK signaling pathways. Murrayafoline A attenuates the Wnt/β-catenin pathway by promoting the degradation of intracellular β-catenin. Murrayafoline A induces G0/G1 phase arrest in platelet-derived growth factor (PDGF)-stimulated vascular smooth muscle cells. Murrayafoline A enhances contractility and L-type calcium currents in rat ventricular myocytes by activating protein kinase C. Murrayafoline A inhibits LPS-induced neuroinflammation in vivo. Murrayafoline A can be used in research on inflammation, vascular complications, and colorectal cancer.

BI1543673 is an inhibitor of interleukin-1 receptor-associated kinase 4 (IRAK4). It can diminish inflammatory responses in human lung tissue stimulated by TLR4 and TLR7/8. Additionally, BI1543673 reduces inflammatory signaling in a mouse lung inflammation model induced by LPS.

Compound 11, a selective PPARδ agonist, demonstrates an EC50 of 20 nM, indicating its high affinity for PPARδ receptors. This compound efficiently reduces levels of nitric oxide (NO), as well as the pro-inflammatory cytokines TNFα and IL-6 in LPS-stimulated RAW264.7 cells via the NF-κB pathway, showcasing its anti-inflammatory properties. Additionally, Compound 11 exhibits remarkable stability in human liver microsomes and plasma. It significantly ameliorates foot edema induced by Carrageenan, displaying favorable pharmacokinetic properties with a bioavailability of approximately 100%.

iNOs-IN-5 (Compound BN-4) is an inhibitor of iNOS with an IC50 value of 0.1707 μM, effectively reducing NO expression in RAW264.7 cells stimulated by LPS (HT-D1056). It further diminishes the expression of ROS and lactate dehydrogenase induced by hypoxic injury, displaying anti-necrotic and anti-apoptotic properties. In an SD rat model, iNOs-IN-5 exhibits neuroprotective effects against cerebral ischemia and is capable of crossing the blood-brain barrier.

Lambertellin, an effective antibiotic, acts as both a bactericide and fungicide. It exerts anti-inflammatory effects in LPS-stimulated RAW 264.7 macrophages by modulating the activation of MAPK and NF-κB signaling pathways.

KR-31080, an imidazo[4,5-b]pyridine derivative, functions as an inhibitor of the angiotensin II receptor. At a concentration of 2 μm, KR-31080 reduces the production of NO in LPS-stimulated BV-2 cells by 8.3%.

(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.

SARS-CoV-2-IN-107 (Compound A7) is an inhibitor of SARS-CoV-2 3CLpro, with an IC50 of 261.3 nM. It inhibits the replication of SARS-CoV-2, exhibiting an EC50 of 11.7 μM. Additionally, SARS-CoV-2-IN-107 demonstrates anti-inflammatory activity in LPS-stimulated RAW264.7 macrophages, with a NO inhibition rate of 68.6%.

Nitric oxide production-IN-11k is a compound that inhibits TLR4, JNK, and NF-κB signaling pathways. It suppresses nitric oxide (NO) production in LPS-stimulated RAW264.7 cells, with an IC₅₀ of 23.2 µM. By downregulating TLR4 expression and reducing the phosphorylation level of JNK, Nitric oxide production-IN-11k inhibits the activation of NF-κB, thereby blocking the transcription of inflammation-related genes. This leads to decreased expression of iNOS and COX-2, and consequently reduces the production of inflammatory mediators such as NO, PGE₂, and TNF-α, exerting anti-inflammatory effects. Nitric oxide production-IN-11k shows potential application value in the study of rheumatoid arthritis and other inflammatory diseases.

BS-153 is a novel synthetic oxazolidinone drug that exhibits anti-inflammatory effects by blocking the activation of the NF-κB/PKCθ pathway. It can suppress the expression levels of iNOS, COX-2, and pro-inflammatory cytokines (TNF-α, IL-1β, and IL-6) in LPS-stimulated RAW264.7 cells.

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.

NF-κB-IN-15 (compound 14r) is a potent NF-κB inhibitor. It reduces NO levels in LPS-stimulated cells and suppresses the release of IL-6, TNF-α, and IL-1β. Additionally, it hinders LPS-induced p65 phosphorylation and IκBα degradation. NF-κB-IN-15 exhibits anti-inflammatory properties and holds potential for research in acute lung injury (ALI).

Anti-inflammatory agent 78 (compound L-37) is a potent anti-inflammatory agent. It effectively inhibits PGE2, PGE1, COX-2, and COX-1. Additionally, Anti-inflammatory agent 78 suppresses the release of NO in LPS-stimulated RAW 264.7 cell lines.