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Submit ReviewJTE 013
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% (HPLC)
Biological Activity for JTE 013
JTE 013 is a 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.
Compound Libraries for JTE 013
JTE 013 is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.
Technical Data for JTE 013
| M. Wt | 408.29 |
| Formula | C17H19N7OCl2 |
| Storage | Store at +4°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 383150-41-2 |
| PubChem ID | 10223146 |
| InChI Key | RNSLRQNDXRSASX-UHFFFAOYSA-N |
| Smiles | CC(C)C1=C2C(C)=NN(C)C2=NC(NNC(=O)NC2=CC(Cl)=NC(Cl)=C2)=C1 |
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.
Solubility Data for JTE 013
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 40.83 | 100 | |
| ethanol | 40.83 | 100 |
Preparing Stock Solutions for JTE 013
The following data is based on the product molecular weight 408.29. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 2.45 mL | 12.25 mL | 24.49 mL |
| 5 mM | 0.49 mL | 2.45 mL | 4.9 mL |
| 10 mM | 0.24 mL | 1.22 mL | 2.45 mL |
| 50 mM | 0.05 mL | 0.24 mL | 0.49 mL |
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Product Datasheets for JTE 013
References for JTE 013
References are publications that support the biological activity of the product.
Ohmori et al (2003) Spingosine 1-phosphate induces contraction of coronary artery smooth muscle cells via S1P2. Cardiovasc.Res. 58 170 PMID: 12667959
Parrill et al (2004) Sphingosine 1-phosphate and lysophosphatidic acid receptors: agonist and antagonist binding and progress toward development of receptor-specific ligands. Semin.Cell.Dev.Biol. 15 467 PMID: 15271292
Inoki et al (2006) Negative regulation of endothelial morphogenesis and angiogenesis by S1P2 receptor. Biochem.Biophys.Res.Comm. 346 293
If you know of a relevant reference for JTE 013, please let us know.
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Keywords: JTE 013, JTE 013 supplier, S1P2, receptor, antagonists, Receptors, EDG5, Sphingosine-1-Phosphate, JTE013, Sphingosine-1-phosphate, 2392, Tocris Bioscience
20 Citations for JTE 013
Citations are publications that use Tocris products. Selected citations for JTE 013 include:
Chumanevich et al (2016) 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. Mediators Inflamm 2016 1503206 PMID: 26884643
Szczepaniak et al (2010) S1P2 receptor-dependent Rho-kinase activation mediates vasoconstriction in the murine pulmonary circulation induced by sphingosine 1-phosphate. Am J Physiol Lung Cell Mol Physiol 299 L137 PMID: 20435688
Long et al (2010) Sphingosine 1-phosphate receptor 4 uses HER2 (ERBB2) to regulate extracellular signal regulated kinase-1/2 in MDA-MB-453 breast cancer cells. J Biol Chem 285 35957 PMID: 20837468
Kellner et al (2016) Nogo-A controls structural plasticity at dendritic spines by rapidly modulating actin dynamics. Hippocampus 6 816 PMID: 26748478
Durham et al (2015) Pericyte chemomechanics and the angiogenic switch: insights into the pathogenesis of proliferative diabetic retinopathy? Arthritis Rheum 56 3441 PMID: 26030100
Zhang et al (2010) Sphingosine-1-phosphate prevents permeability increases via activation of endothelial sphingosine-1-phosphate receptor 1 in rat venules. Cardiovasc Res 299 H1494 PMID: 20729401
Frias et al (2010) Native and reconstituted HDL protect cardiomyocytes from doxorubicin-induced apoptosis. Mol Cancer Res 85 118 PMID: 19700468
Matsushima-Nishiwaki et al (2018) Sphingosine 1-phosphate (S1P) reduces hepatocyte growth factor-induced migration of hepatocellular carcinoma cells via S1P receptor 2 PLoS One 13 e0209050 PMID: 30543684
Wirrig et al (2016) Sphingosylphosphorylcholine inhibits macrophage adhesion to vascular smooth muscle cells Biochemical Pharmacology 115 43 PMID: 27402344
Shen et al (2014) Sphingosine 1-phosphate (S1P) promotes mitochondrial biogenesis in Hep G2 cells by activating Peroxisome proliferator-activated receptor γ coactivator 1α (PGC-1α). Cell Stress Chaperones 19 541 PMID: 24293320
Gu et al (2015) Defective apical extrusion signaling contributes to aggressive tumor hallmarks. Elife 4 e04069 PMID: 25621765
Fernández-Pisonero et al (2014) Synergy between sphingosine 1-phosphate and lipopolysaccharide signaling promotes an inflammatory, angiogenic and osteogenic response in human aortic valve interstitial cells. Am J Physiol Heart Circ Physiol 9 e109081 PMID: 25275309
Quint et al (2013) Sphingosine 1-phosphate (S1P) receptors 1 and 2 coordinately induce mesenchymal cell migration through S1P activation of complementary kinase pathways. PLoS One 288 5398 PMID: 23300082
Stradner et al (2013) Sphingosine 1-phosphate counteracts the effects of interleukin-1β in human chondrocytes. J Urol 65 2113 PMID: 23666803
Green et al (2011) The sphingosine 1-phosphate receptor S1P2 maintains the homeostasis of germinal center B cells and promotes niche confinement. Nat Immunol 12 672 PMID: 21642988
Li et al (2008) Induction of antiproliferative connective tissue growth factor expression in Wilms' tumor cells by sphingosine-1-phosphate receptor 2. J Clin Endocrinol Metab 6 1649 PMID: 18922980
Li et al (2009) S1P/S1P2 signaling induces cyclooxygenase-2 expression in Wilms tumor. J Biol Chem 181 1347 PMID: 19157443
Beckham et al (2013) Acid ceramidase induces sphingosine kinase 1/S1P receptor 2-mediated activation of oncogenic Akt signaling. Oncogenesis 2 e49 PMID: 23732709
Beckham et al (2013) Acid ceramidase promotes nuclear export of PTEN through sphingosine 1-phosphate mediated Akt signaling. PLoS One 8 e76593 PMID: 24098536
Miller et al (2008) 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. Mol Cell Biol 28 4142 PMID: 18426913
Do you know of a great paper that uses JTE 013 from Tocris? Please let us know.
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