JTE 013

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JTE 013 | CAS No. 383150-41-2 | Sphingosine-1-phosphate Receptor Antagonists
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Description: S1P2 receptor antagonist

Chemical Name: 1-[1,3-Dimethyl-4-(2-methylethyl)-1H-pyrazolo[3,4-b]pyridin-6-yl]-4-(3,5-dichloro-4-pyridinyl)-semicarbazide

Purity: ≥98%

Product Details
Citations (20)
Supplemental Products
Reviews

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:
383150-41-2

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.

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

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Citations for JTE 013

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

20 Citations: Showing 1 - 10

  1. Sphingosine 1-phosphate (S1P) reduces hepatocyte growth factor-induced migration of hepatocellular carcinoma cells via S1P receptor 2
    Authors: Matsushima-Nishiwaki Et al.
    PLoS One  2018;13:e0209050
  2. Nogo-A controls structural plasticity at dendritic spines by rapidly modulating actin dynamics.
    Authors: Kellner Et al.
    Hippocampus  2016;6:816
  3. Sphingosine-1-Phosphate/Sphingosine-1-Phosphate Receptor 2 Axis Can Promote Mouse and Human Primary Mast Cell Angiogenic Potential through Upregulation of Vascular Endothelial Growth Factor-A and Matrix Metalloproteinase-2.
    Authors: Chumanevich Et al.
    Mediators Inflamm  2016;2016:1503206
  4. Sphingosylphosphorylcholine inhibits macrophage adhesion to vascular smooth muscle cells
    Authors: Wirrig Et al.
    Biochemical Pharmacology  2016;115:43
  5. Pericyte chemomechanics and the angiogenic switch: insights into the pathogenesis of proliferative diabetic retinopathy?
    Authors: Durham Et al.
    Arthritis Rheum  2015;56:3441
  6. Defective apical extrusion signaling contributes to aggressive tumor hallmarks.
    Authors: Gu Et al.
    Elife  2015;4:e04069
  7. 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
  8. 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
  9. Acid ceramidase promotes nuclear export of PTEN through sphingosine 1-phosphate mediated Akt signaling.
    Authors: Beckham Et al.
    PLoS One  2013;8:e76593
  10. Sphingosine 1-phosphate counteracts the effects of interleukin-1β in human chondrocytes.
    Authors: Stradner Et al.
    J Urol  2013;65:2113
  11. Acid ceramidase induces sphingosine kinase 1/S1P receptor 2-mediated activation of oncogenic Akt signaling.
    Authors: Beckham Et al.
    Oncogenesis  2013;2:e49
  12. 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
  13. 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
  14. Native and reconstituted HDL protect cardiomyocytes from doxorubicin-induced apoptosis.
    Authors: Frias Et al.
    Mol Cancer Res  2010;85:118
  15. 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
  16. 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
  17. 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
  18. S1P/S1P2 signaling induces cyclooxygenase-2 expression in Wilms tumor.
    Authors: Li Et al.
    J Biol Chem  2009;181:1347
  19. 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
  20. 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

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