polarization

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.

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 an irreversible inhibitor of carnitine palmitoyltransferase 1a (CPT-1a) (IC50=5-20 nM). Etomoxir inhibits fatty acid oxidation by inhibiting CPT-1a, inhibits palmitate oxidation, 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.

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.

CSF1R-IN-26 (Compound III-1) is an inhibitor of CSF-1R with an IC50 of 20.07 nM. It promotes the polarization of M2 macrophages to M1 macrophages, inducing apoptosis in MC-38 cancer cells. CSF1R-IN-26 inhibits the activation of the AKT/ERK/STAT3 signaling pathways, remodels the tumor immune microenvironment, and exhibits antitumor activity in mouse models. In SD rats, CSF1R-IN-26 demonstrates favorable pharmacokinetic properties, with a half-life of 1.86 hours and an oral bioavailability of 79.22%.

Antifibrotic agent 1 is an orally active medication designed to treat idiopathic pulmonary fibrosis (IPF). It effectively mitigates IPF-related processes, including TGF-β-induced epithelial-mesenchymal transition (EMT) and fibroblast-to-myofibroblast transition (FMT), as well as profibrotic M2 polarization. Antifibrotic agent 1 selectively inhibits CSF-1R, PDGFR-α, and Src family kinases (SFKs), while sparing VEGFR, FGFR, and Abl to minimize off-target toxicity. In a bleomycin (BLM)-induced pulmonary fibrosis mouse model, it demonstrates strong antifibrotic activity.

SIN 14 is an HO-1 activator that targets and activates HO-1 through an allosteric mechanism. Additionally, SIN 14 can induce the polarization of macrophages from the M1 phenotype to the M2 phenotype.

TE-11 is a MIF tautomerase inhibitor with an IC50 of 5.63 μM. This compound can alleviate Crohn's-like colitis, reduce MIF-induced migration of eosinophils and neutrophils, and prevent M1 polarization and associated metabolic reprogramming.

GPR40 Activator 3 (compound SC) is a potent activator of GPR40. It alleviates pulmonary fibrosis by inhibiting M2 macrophage polarization through the GPR40/PKD1/CD36 axis.

PARP14 inhibitor2 (Compound 3) is an orally active and highly selective PARP14 inhibitor with an IC50 value of less than 30 nM. It effectively inhibits the mono ADP-ribosyltransferase activity of PARP14 and modulates IFN-γ and IL-4 signaling, thereby reversing pro-tumor macrophage polarization and suppressing anti-tumor inflammatory responses. PARP14 inhibitor2 holds potential for research in PARP14-related conditions such as tumors, atopic dermatitis, and autoimmune diseases.

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.