polarization

IMP-1710 is a selective UCH-L1 inhibitor with an IC50 value of 38 nM in a fluorescence polarization assay.IMP-1710 has antifibrotic activity. [1]

Etomoxir is a carnitine palmitoyltransferase 1a (CPT-1a) inhibitor that inhibits fatty acid oxidation by inhibiting CPT-1a and inhibits palmitate oxidation in humans, rats, and guinea pigs. Etomoxir has an inhibitory effect on adenine nucleotide translocase and can inhibit macrophage polarization by disrupting CoA homeostasis.

PF-04447943 (Edelinontrine) is a potent and selective phosphodiesterase 9A inhibitor with an IC50 of 12 nM, which is 78-fold more selective than that used for other PDE family members (IC50>1000 nM).PF-04447943 exhibits anti-inflammatory activity, attenuates inflammatory responses by inhibiting oxidative stress, inflammation, and modulating T-cell polarization, and may be useful for research on sickle cell anemia.

L-Methionine sulfoxide (H-Met(O)-OH) is a metabolite of Methionine that modulates oxidative stress and purinergic signaling parameters, while inducing M1 classical macrophage polarization.

Betamethasone disodium phosphate (Betamethasone 21-phosphate disodium salt) is a corticosteroid with anti-inflammatory properties that promotes the polarization of M1 to M2 macrophages by reducing the secretion of pro-inflammatory cytokines, and is utilized in research on keloids and rheumatoid arthritis.

The quinuclidine PHA 568487 free base is an agonist of the alpha 7 nicotinic acetylcholine receptor that was designed to mitigate the bioactivation associated with the core scaffold and subsequently remove associated liabilities with in vivo tolerability.

KPLH1130, a specific pyruvate dehydrogenase kinase (PDK) inhibitor, enhances glucose tolerance in mice fed a high-fat diet (HFD). It effectively hinders macrophage polarization and mitigates proinflammatory reactions.

Anti-MRSA agent 18 (E17) is an inhibitor of MRSA, exhibiting MIC values of 2 μg mL for S. aureus and 4 μg mL for MRSA. This compound accelerates bacterial death by interacting with the bacterial cell membrane constituents, phosphatidylglycerol and cardiolipin, leading to changes in membrane permeability and polarization. Additionally, it increases intracellular ROS, along with leakage of DNA and proteins.

Neuroprotective agent 5 (compound 28) acts as a brain-penetrating agent with anti-neuroinflammatory, antioxidant, and neuroprotective properties. It exhibits potent inhibition of nitric oxide (NO) with an EC50 of 0.49 μM and suppresses the release of pro-inflammatory mediators PGE2 and TNF-α. Additionally, it downregulates the expression of iNOS and COX-2 proteins, facilitating the polarization of BV-2 cells from a pro-inflammatory M1 phenotype to an anti-inflammatory M2 phenotype. Neuroprotective agent 5 also dose-dependently inhibits acetylcholinesterase (AChE) activity and the aggregation of Aβ42. This compound is useful for research into Alzheimer's disease.

DBL-6-13 is an inhibitor of WDR5, displaying moderate binding affinity with dissociation constants (Kd) of 6.8 μM and 9.1 μM as determined by microscale thermophoresis analysis and fluorescence polarization analysis, respectively.

9-tert-Butyldoxycycline exhibits immunomodulatory activity by altering the polarization state of polymorphonuclear neutrophils and ameliorating inflammatory responses in ischemia-reperfusion injury models. Additionally, 9-tert-Butyldoxycycline serves as a ligand for the Tet-On inducible gene expression system.

Myelin Basic Protein (87-99) Acetate (Myelin Basic Protein (87-99) Acetate (118506-26-6 Free base)) is an encephalitogenic peptide that induces basic protein-specific T cell proliferation. Myelin Basic Protein (87-99) Acetate causes a Th1 polarization in peripheral blood mononuclear cells, which is implicated in multiple sclerosis (MS).

Astragalus polysaccharide, a natural product derived from Astragalus propinquus, exhibits anticancer activity and has been shown to be effective in hepatocellular carcinoma (HCC) by inhibiting the M2 polarization of tumor-associated macrophages (TAM).

Lipoxin A4 (LXA4) is a lipoxygenase-derived arachidonate-like mediator with anti-inflammatory properties.Lipoxin A4 attenuates MSU crystal-induced NLRP3 inflammasome activation through inhibition of Nrf2, and regulates M1 M2 macrophage polarization through the FPR2-IRF pathway.Lipoxin inhibits oxidative stress and inflammation.

1-Oleoyl Lysophosphatidic Acid (1-Oleoyl LPA) is a biologically active phospholipid that can exert multiple biological effects in various disease states of the kidney by activating a complex network of at least six homologous G protein-coupled receptors and their heterotrimeric G proteins. 1-Oleoyl Lysophosphatidic Acid promotes polarization of BV-2 and primary murine microglia toward an M1-like phenotype and can be used to study cancer and atherosclerosis.

Prostaglandin E3 (PGE3) is an eicosapentaenoic acid (EPA) derivative with anti-inflammatory and anti-tumor activity, inhibits polarization to M1 macrophages, and shows anti-proliferative effects in human lung cancer cells.

FAM-DEALA-Hyp-YIPD is a fluorescent HIF-1α peptide (Kd= 180-560 nM) used to assess VHL binding in Fluorescence Polarization (FP) displacement assays and evaluate the effect of VHL binding on degradation activity. It has an excitation maximum of 485 nm and an emission maximum of 535 nm. A longer peptide version, FAM-DEALAHypYIPMDDDFQLRSF, is also available.

FAM-DEALAHypYIPMDDDFQLRSF is a 5,6-carboxyfluorescein (FAM) labeled HIF-1α peptide. It binds with high affinity to von Hippel-Lindau (VHL) protein (KD= 3 nM). Can be used to assess ligand binding to VHL in a direct fluorescence polarization (FP) displacement assay. Excitation/emission maxima (λ) = 485/520 nm. This product is a longer peptide version of FAM-DEALA-Hyp-YIPD.

Neotuberostemonine (NTS) is one of the main antitussive alkaloids in the root of Stemona tuberosa Lour, it has a significant protective effect on bleomycin (BLM)-induced pulmonary fibrosis through suppressing the recruitment and M2 polarization of macroph

PCAF-IN-1 is a highly selective PCAF (p300 CBP-associated factor) inhibitor with potential anti-tumor, anti-inflammatory, and anti-heart disease effects. Inhibition of PCAF attenuates cardiac remodeling after myocardial infarction, reduces polarization of M1-type macrophages, and attenuates autoimmune arthritis.

TDRL-X80 is a potent inhibitor of the pigmented dry skin protein (XPA), inhibiting the DNA binding activity of XPA. It acts on single, double, and cisplatin-damaged DNA with IC50 values of 18, 20, and 29 μM in fluorescence polarization (FP) assays and 21, 39, and 28 μM in ELISA assays.

DHU-Se1 is a potent anti-inflammatory agent that stimulates the release of reactive selenium compounds from macrophages and reduces the expression of cellular inflammatory factors such as iNOS and TNF-α. Additionally, DHU-Se1 blocks the polarization of macrophages from M0 to M1, thereby alleviating the inflammatory process.

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.

L-Kynurenine sulfate, an aryl hydrocarbon receptor (AHR) agonist, activates AHR-driven polarization of naive T cells towards the anti-inflammatory [Treg] phenotype.