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A competitive, selective antagonist of NMB receptors (Kis = 15-45 nM for rat and human receptors expressed in various cell lines); blocks the elevation of intracellular calcium and release of inositol phosphate induced by NMB in cells expressing NMB receptors.
The isoprostanes are a family of eicosanoids of non-enzymatic origin produced by the random oxidation of tissue phospholipids by oxygen radicals. Isoprostanes appear as artifacts in tissue and plasma samples which have undergone oxidative degradation during prolonged or improper storage. They also...
An alkaloid amide from species of the genus Piper, a plant used in traditional medicine that demonstrates antifungal, anticancer, antihyperlipidemic, and anti-inflammatory properties.
A synthetic compound which interacts with BET proteins with high-affinity (Kd = 32.5-42.5 nM); disrupts binding of BET proteins with acetylated histones, suppressing the expression of specific inflammatory genes involved in sepsis and endotoxic shock.
A potent inhibitor of PKA signaling that acts through competitive inhibition of ATP (Ki = 60 nM).
A phytoestrogen that activates ERα and ERβ (EC50s = 320 and 680 nM, respectively); stimulates osteoblast proliferation and differentiation and prevents bone loss following ovariectomy in rats.
A ureido-sulfonamide inhibitor of carbonic anhydrases IX and CAXII (Kis = 45.1 and 4.5 nM, respectively) that binds only under hypoxic conditions, reducing extracellular acidity and resulting in significant inhibition of tumor growth and metastasis in experimental models.
A selective SIP1 agonist (EC50 = 1.35 nM); activates S1P1-mediated p42/p44 MAPK phosphorylation in CHO-K1 cells transfected with S1P1 (EC50 = 46 nM); induces S1P1-dependent lymphopenia in mice, decreasing B and T cells by 65 and 85%, respectively, at 50 nM.
Antigen: peptide from the C-terminal region of human GPR41 Host: rabbit Cross Reactivity: (+) human GPR41 Application(s): FC, IF, and WB
Source: Purified from human plasma, citrullinated with human recombinant PAD2 MW: α chain isoform 1 (95 kDa), α chain isoform 2 (69.8 kDa), β chain (55.9k Da), and,isoform γ-B chain (51.5 kDa)
Source: Recombinant GST-tagged protein expressed in E. coli Mr: 73.4 kDa The isolated individual or tandem bromodomains of BRD4 have been shown to bind acetylated histone tails, serving to couple histone acetylation marks to the transcriptional regulation of target promoters.
A competitive inhibitor of 15-hydroxy PGDH; acts as an agonist on most EP receptor subtypes (Kd d~ 1 nM for isolated EP2 receptors); preserves the self-renewal properties while preventing the differentiation of hematopoietic stem cells during expansion in culture.
An active site-directed agent that inhibits serine proteinases with trypsin-like activity; may also act non-selectively with thiol groups and thereby inhibit cysteine proteinases and other enzymes.
A quinolone antibiotic that inhibits bacterial DNA gyrase, but not eukaryotic topoisomerases, reversibly binding gyrase subunit A in gyrase-DNA complexes, blocking supercoiling activity and inhibiting DNA synthesis at 0.5-5 µg/ml; also blocks neuronal uptake of dopamine in mammals...
The HIF (hypoxia-inducible factor) transcription factor is a member of the basic-helix-loop-helix (bHLH) family of transcription factors and plays an important role in maintaining cellular oxygen homeostasis. HIF-1α has emerged as an important drug target in breast and prostate cancer,...
A nucleoside analog with antiviral activity, inhibiting thymidine kinases from herpes simplex virus types 1 and 2 with Ki values of 0.14 and 0.95 µM, while blocking green monkey Vero cell thymidine kinase less effectively (Ki = 53 µM).
Sodium chloride stock solution contains filtered sodium chloride (5 M). It is ready to use as supplied.
A potent synthetic agonist of GPR55 (EC50 = 0.26 µM); does not act at the related kynurenic acid receptor GPR35 and is a weak antagonist of CB1 and CB2 (IC50s = 21.8 and 15.1 µM, respectively).
A small molecule inducer of adult neural stem cell differentiation; 2.5-20 µM triggers neurogenesis and blocks gliogenesis in HCN cells through a neurotransmitter-mediated calcium signal and myocyte-enhancer factor 2-dependent gene expression pathway.
A DHCR7 inhibitor that prevents cholesterol biosynthesis and Hedgehog signaling; used to recapitulate phenotypes of Smith-Lemli-Opitz syndrome, a disorder brought about by mutations in the DHCR7 gene, in animal models.
Source: Recombinant N-terminal His-tagged protein expressed in E. coli MW: 40.48 kDa Annexin A1 is an endogenous mediator of inflammation, promoting resolution in a number of ways. Normally expressed in intracellular compartments, it is drawn to the cell membrane and both induced and externalized by...
A hybrid molecule of an H2S donor and the NSAID indomethacin that does not cause gastric damage or promote leukocyte adherence to vascular endothelium.
A selective ligand of RORγ (IC50 = 1 μM); does not bind RORα, LXR, or FXR; acts as an inverse agonist of RORγ, inhibiting endogenous IL-17A gene expression and suppressing differentiation of TH17 cells; stimulates T regulatory development.
A reversible, cell-permeable inhibitor of VEGFR2’s kinase activity (IC50 = 70 nM); less potently inhibits PDGFRβ (IC50 = 920 nM); blocks the growth of human umbilical vein endothelial cells stimulated with either VEGF or PDGF (IC50s = 110 nM and 2...