Chemical Name: 9-Chloro-2-(2-furanyl)-[1,2,4]triazolo[1,5-c]quinazolin-5-amine
Biological ActivityCGS 15943 is a potent adenosine receptor antagonist (Ki values are 3.5, 4.2, 16 and 51 nM for human A1, A2A, A2B and A3 receptors respectively). Inhibits the catalytic subunit of the class IB PI3K isoform p110γ (IC50 = 1.1 μM). Blocks HCC and HDAC cell proliferation in vitro via inhibition of the PI3K/Akt pathway; reduces proliferation of ER+ breast cancer cells. Also acts as a BMP-4 mimetic to stimulate osteogenic differentiation. Orally active in vivo.
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Tocris products are intended for laboratory research use only, unless stated otherwise.
Pharmacological characterization of CGS 15943A: a novel nonxanthine adenosine antagonist.
Ghai et al.
Adenosine receptors and their ligands.
Naunyn Schmiedebergs Arch.Pharmacol., 2000;362:382
Biochemical characterization of the triazoloquinazoline CGS 15943, a novel, non-xanthine adenosine antagonist.
Williams et al.
Citations for CGS 15943
The citations listed below are publications that use Tocris products. Selected citations for CGS 15943 include:
7 Citations: Showing 1 - 7
An Adenosine Receptor for Olfaction in Fish.
Authors: Wakisaka Et al.
Curr Biol 2017;27:1437
Activation of P2X7 and P2Y11 purinergic receptors inhibits migration and normalizes tumor-derived endothelial cells via cAMP signaling
Authors: Avanzato Et al.
Scientific Reports 2016;6:32602
Purinergic and store-operated Ca(2+) signaling mechanisms in mesenchymal stem cells and their roles in ATP-induced stimulation of cell migration.
Authors: Peng Et al.
Stem Cells 2016;34:2102
Application of BRET to monitor ligand binding to GPCRs.
Authors: Stoddart Et al.
Nat Methods 2015;12:661
Homeostatic control of synaptic activity by endogenous adenosine is mediated by adenosine kinase.
Authors: Diógenes Et al.
Cereb Cortex 2014;24:67
Adenosine release during seizures attenuates GABAA receptor-mediated depolarization.
Authors: Ilie Et al.
J Neurosci 2012;32:5321
Constitutive lysosome exocytosis releases ATP and engages P2Y receptors in human monocytes.
Authors: Sivaramakrishnan Et al.
J Cell Sci 2012;125:4567
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