Catalog Number: 2392
Chemical Name: 1-[1,3-Dimethyl-4-(2-methylethyl)-1H-pyrazolo[3,4-b]pyridin-6-yl]-4-(3,5-dichloro-4-pyridinyl)-semicarbazide
Biological Activity
Sphingosine-1-phosphate (S1P) receptor antagonist, highly selective for S1P2 (EDG-5). Inhibits S1P binding to human S1P2 receptors with an IC50 value of 17.6 nM. At concentrations up to 10 μM, displays 4.2% inhibition of S1P3 and does not antagonize S1P1. Enhances S1P-induced angiogenesis in vivo.
Technical Data
  • M.Wt:
    408.29
  • Formula:
    C17H19N7OCl2
  • Solubility:
    Soluble to 100 mM in DMSO and to 100 mM in ethanol
  • Purity:
    >98%
  • Storage:
    Store at +4°C
  • CAS No:
    547756-93-4
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis. All Tocris products are intended for laboratory research use only.
Background References
  1. Spingosine 1-phosphate induces contraction of coronary artery smooth muscle cells via S1P2.
    Ohmori et al.
    Cardiovasc.Res., 2003;58:170
  2. Sphingosine 1-phosphate and lysophosphatidic acid receptors: agonist and antagonist binding and progress toward development of receptor-specific ligands.
    Parrill et al.
    Semin.Cell.Dev.Biol., 2004;15:467
  3. Negative regulation of endothelial morphogenesis and angiogenesis by S1P2 receptor.
    Inoki et al.
    Biochem.Biophys.Res.Comm., 2006;346:293
Citations:

The citations listed below are publications that use Tocris products. Selected citations for JTE 013 include:

18 Citations: Showing 1 - 10
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  1. Nogo-A controls structural plasticity at dendritic spines by rapidly modulating actin dynamics.
    Authors: Kellner Et al.
    Hippocampus 2016;6:816
  2. Sphingosylphosphorylcholine inhibits macrophage adhesion to vascular smooth muscle cells
    Authors: Wirrig Et al.
    Biochemical Pharmacology 2016;115:43
  3. Pericyte chemomechanics and the angiogenic switch: insights into the pathogenesis of proliferative diabetic retinopathy?
    Authors: Durham Et al.
    Arthritis Rheum 2015;56:3441
  4. Defective apical extrusion signaling contributes to aggressive tumor hallmarks.
    Authors: Gu Et al.
    Elife 2015;4:e04069
  5. Synergy between sphingosine 1-phosphate and lipopolysaccharide signaling promotes an inflammatory, angiogenic and osteogenic response in human aortic valve interstitial cells.
    Authors: Fernández-Pisonero Et al.
    Am J Physiol Heart Circ Physiol 2014;9:e109081
  6. Sphingosine 1-phosphate (S1P) promotes mitochondrial biogenesis in Hep G2 cells by activating Peroxisome proliferator-activated receptor γ coactivator 1α (PGC-1α).
    Authors: Shen Et al.
    Cell Stress Chaperones 2014;19:541
  7. Acid ceramidase promotes nuclear export of PTEN through sphingosine 1-phosphate mediated Akt signaling.
    Authors: Beckham Et al.
    PLoS One 2013;8:e76593
  8. Sphingosine 1-phosphate counteracts the effects of interleukin-1β in human chondrocytes.
    Authors: Stradner Et al.
    J Urol 2013;65:2113
  9. Acid ceramidase induces sphingosine kinase 1/S1P receptor 2-mediated activation of oncogenic Akt signaling.
    Authors: Beckham Et al.
    Oncogenesis 2013;2:e49
  10. Sphingosine 1-phosphate (S1P) receptors 1 and 2 coordinately induce mesenchymal cell migration through S1P activation of complementary kinase pathways.
    Authors: Quint Et al.
    PLoS One 2013;288:5398
  11. The sphingosine 1-phosphate receptor S1P2 maintains the homeostasis of germinal center B cells and promotes niche confinement.
    Authors: Green Et al.
    Nat Immunol 2011;12:672
  12. Native and reconstituted HDL protect cardiomyocytes from doxorubicin-induced apoptosis.
    Authors: Frias Et al.
    Mol Cancer Res 2010;85:118
  13. S1P2 receptor-dependent Rho-kinase activation mediates vasoconstriction in the murine pulmonary circulation induced by sphingosine 1-phosphate.
    Authors: Szczepaniak Et al.
    Am J Physiol Lung Cell Mol Physiol 2010;299:L137
  14. Sphingosine-1-phosphate prevents permeability increases via activation of endothelial sphingosine-1-phosphate receptor 1 in rat venules.
    Authors: Zhang Et al.
    Cardiovasc Res 2010;299:H1494
  15. Sphingosine 1-phosphate receptor 4 uses HER2 (ERBB2) to regulate extracellular signal regulated kinase-1/2 in MDA-MB-453 breast cancer cells.
    Authors: Long Et al.
    J Biol Chem 2010;285:35957
  16. S1P/S1P2 signaling induces cyclooxygenase-2 expression in Wilms tumor.
    Authors: Li Et al.
    J Biol Chem 2009;181:1347
  17. Induction of antiproliferative connective tissue growth factor expression in Wilms' tumor cells by sphingosine-1-phosphate receptor 2.
    Authors: Li Et al.
    J Clin Endocrinol Metab 2008;6:1649
  18. Sphingosine kinases and sphingosine-1-phosphate are critical for transforming growth factor beta-induced extracellular signal-regulated kinase 1 and 2 activation and promotion of migration and invasion of esophageal cancer cells.
    Authors: Miller Et al.
    Mol Cell Biol 2008;28:4142
Expand to show all 18 Citations

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