JTE 013

Cat. No. 2392

JTE 013 C17H19N7OCl2 [547756-93-4]

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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.

Certificate of Analysis / Product Datasheet / Safety Data Sheet

Certificate of Analysis / Product Datasheet
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Inoki et al (2006) Negative regulation of endothelial morphogenesis and angiogenesis by S1P2 receptor. Biochem.Biophys.Res.Comm. 346 293.

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.

Ohmori et al (2003) Spingosine 1-phosphate induces contraction of coronary artery smooth muscle cells via S1P2. Cardiovasc.Res. 58 170. PMID: 12667959.

If you know of a relevant reference for this product please let us know.

Citations are publications that use Tocris products. Selected citations for JTE 013 include:

Wirrig et al (2016) Sphingosylphosphorylcholine inhibits macrophage adhesion to vascular smooth muscle cells Biochemical Pharmacology 115 43. PMID: 27402344.

Durham et al (2015) Pericyte chemomechanics and the angiogenic switch: insights into the pathogenesis of proliferative diabetic retinopathy? Arthritis Rheum 56 3441. PMID: 26030100.

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.

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.

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.

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.

Frias et al (2010) Native and reconstituted HDL protect cardiomyocytes from doxorubicin-induced apoptosis. Mol Cancer Res 85 118. PMID: 19700468.

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.

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.

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.

Li et al (2009) S1P/S1P2 signaling induces cyclooxygenase-2 expression in Wilms tumor. J Biol Chem 181 1347. PMID: 19157443.

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.

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.

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Keywords: JTE 013, supplier, S1P2, receptor, antagonists, Receptors, EDG5, Sphingosine-1-Phosphate, JTE013, Tocris Bioscience, Sphingosine-1-Phosphate Receptor Antagonist products

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