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:
  • Formula:
  • Solubility:
    Soluble to 100 mM in DMSO and to 100 mM in ethanol
  • Purity:
  • Storage:
    Store at +4°C
  • CAS No:
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

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

Showing Results 1 - 10 of 17

  1. Sphingosylphosphorylcholine inhibits macrophage adhesion to vascular smooth muscle cells
    Authors: Wirrig Et al.
    Biochemical Pharmacology
  2. Pericyte chemomechanics and the angiogenic switch: insights into the pathogenesis of proliferative diabetic retinopathy?
    Authors: Durham Et al.
    Arthritis Rheum
  3. Defective apical extrusion signaling contributes to aggressive tumor hallmarks.
    Authors: Gu Et al.
  4. 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
  5. 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
  6. Acid ceramidase promotes nuclear export of PTEN through sphingosine 1-phosphate mediated Akt signaling.
    Authors: Beckham Et al.
    PLoS One
  7. Sphingosine 1-phosphate counteracts the effects of interleukin-1β in human chondrocytes.
    Authors: Stradner Et al.
    J Urol
  8. Acid ceramidase induces sphingosine kinase 1/S1P receptor 2-mediated activation of oncogenic Akt signaling.
    Authors: Beckham Et al.
  9. 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
  10. The sphingosine 1-phosphate receptor S1P2 maintains the homeostasis of germinal center B cells and promotes niche confinement.
    Authors: Green Et al.
    Nat Immunol
  11. Native and reconstituted HDL protect cardiomyocytes from doxorubicin-induced apoptosis.
    Authors: Frias Et al.
    Mol Cancer Res
  12. 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
  13. Sphingosine-1-phosphate prevents permeability increases via activation of endothelial sphingosine-1-phosphate receptor 1 in rat venules.
    Authors: Zhang Et al.
    Cardiovasc Res
  14. 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
  15. S1P/S1P2 signaling induces cyclooxygenase-2 expression in Wilms tumor.
    Authors: Li Et al.
    J Biol Chem
  16. 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
  17. 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
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