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Biological Activity for CGS 15943
CGS 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.
Technical Data for CGS 15943
|Storage||Store at RT|
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 CGS 15943
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions for CGS 15943
The following data is based on the product molecular weight 285.69. 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|
|0.05 mM||70.01 mL||350.03 mL||700.06 mL|
|0.25 mM||14 mL||70.01 mL||140.01 mL|
|0.5 mM||7 mL||35 mL||70.01 mL|
|2.5 mM||1.4 mL||7 mL||14 mL|
References for CGS 15943
References are publications that support the biological activity of the product.
Ghai et al (1987) Pharmacological characterization of CGS 15943A: a novel nonxanthine adenosine antagonist. J.Pharmacol.Exp.Ther. 242 784 PMID: 3656113
Klotz (2000) Adenosine receptors and their ligands. Naunyn Schmiedebergs Arch.Pharmacol. 362 382 PMID: 11111832
Williams et al (1987) Biochemical characterization of the triazoloquinazoline CGS 15943, a novel, non-xanthine adenosine antagonist. J.Pharmacol.Exp.Ther. 241 415 PMID: 2883298
Wesseler et al (2022) Phenotypic discovery of triazolo[1,5-c]quinazolines as a first-in-class bone morphogenetic protein amplifier chemotype. J.Med.Chem. 65 15263 PMID: 36346705
Shropshire et al (2022) Association of adenosine signaling gene signature with estrogen receptor-positive breast and prostate cancer bone metastasis. Front.Med. (Lausanne) 9 965429 PMID: 36186774
Edling et al (2014) Caffeine and the analog CGS 15943 inhibit cancer cell growth by targeting the phosphoinositide 3-kinase/Akt pathway. Cancer Biol.Ther. 15 524 PMID: 24521981
If you know of a relevant reference for CGS 15943, please let us know.
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Keywords: CGS 15943, CGS 15943 supplier, Potent, adenosines, receptor, antagonists, Non-Selective, Receptors, CGS15943, Non-selective, Adenosine, PI, 3-Kinase, 1699, Tocris Bioscience
7 Citations for CGS 15943
Citations are publications that use Tocris products. Selected citations for CGS 15943 include:
Stoddart et al (2015) Application of BRET to monitor ligand binding to GPCRs. Nat Methods 12 661 PMID: 26030448
Wakisaka et al (2017) An Adenosine Receptor for Olfaction in Fish. Curr Biol 27 1437 PMID: 28502661
Sivaramakrishnan et al (2012) Constitutive lysosome exocytosis releases ATP and engages P2Y receptors in human monocytes. J Cell Sci 125 4567 PMID: 22767503
Peng et al (2016) Purinergic and store-operated Ca(2+) signaling mechanisms in mesenchymal stem cells and their roles in ATP-induced stimulation of cell migration. Stem Cells 34 2102 PMID: 27038239
Diógenes et al (2014) Homeostatic control of synaptic activity by endogenous adenosine is mediated by adenosine kinase. Cereb Cortex 24 67 PMID: 22997174
Ilie et al (2012) Adenosine release during seizures attenuates GABAA receptor-mediated depolarization. J Neurosci 32 5321 PMID: 22496577
Avanzato et al (2016) Activation of P2X7 and P2Y11 purinergic receptors inhibits migration and normalizes tumor-derived endothelial cells via cAMP signaling Scientific Reports 6 32602 PMID: 27586846
Do you know of a great paper that uses CGS 15943 from Tocris? Please let us know.
Reviews for CGS 15943
Average Rating: 5 (Based on 1 Review.)
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This compound was used both in vivo and in vitro. For in vivo experiments we injected the compound systemically into transgenic mice and evaluated the effect of the drug on motor behavior. In vitro we used the drug on slices to evaluate the effect on the physiology of cells.
Drug was dissolved using saline + 0.3% tween 80. (Vortexed for 1 minute and sonicated for 5 min) X3 times.
Literature in this Area
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