CGS 15943

Biological Activity

CGS 15943 is a potent adenosine receptor antagonist (K_i values are 3.5, 4.2, 16 and 51 nM for human A₁, A_2A, A_2B 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

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. Leishmania metacyclogenesis is promoted in the absence of purines.
   Serafim T, Figueiredo A, Costa P, Marques-da-Silva E, Goncalves R, de Moura S, Gontijo N, da Silva S, Michalick M, Meyer-Fernandes J, de Carvalho R, Uliana S, Fietto J, Afonso L
   PLoS Negl Trop Dis, 2012;6(9):e1833.
2. Pharmacological characterization of CGS 15943A: a novel nonxanthine adenosine antagonist.
   Ghai et al.
   J.Pharmacol.Exp.Ther., 1987;242:784
3. Adenosine receptors and their ligands.
   Klot
   Naunyn Schmiedebergs Arch.Pharmacol., 2000;362:382
4. Biochemical characterization of the triazoloquinazoline CGS 15943, a novel, non-xanthine adenosine antagonist.
   Williams et al.
   J.Pharmacol.Exp.Ther., 1987;241:415

Product Datasheets