1. GPCR/G Protein
    PI3K/Akt/mTOR
  2. Adenosine Receptor
    PI3K
  3. CGS 15943

CGS 15943 

Cat. No.: HY-100678
Handling Instructions

CGS 15943 is an orally bioavailable non-xanthine Adenosine Receptor antagonist. Its Ki for human A1, A2A, A2B, and A3 Adenosine Receptors are 3.5, 4.2, 16, and 50 nM in transfected CHO cells, respectively. .

For research use only. We do not sell to patients.

CGS 15943 Chemical Structure

CGS 15943 Chemical Structure

CAS No. : 104615-18-1

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Description

CGS 15943 is an orally bioavailable non-xanthine Adenosine Receptor antagonist. Its Ki for human A1, A2A, A2B, and A3 Adenosine Receptors are 3.5, 4.2, 16, and 50 nM in transfected CHO cells, respectively. [1][2].

IC50 & Target[1][2]

p110γ

1.1 μM (IC50)

p110δ

8.47 μM (IC50)

adenosine A1 receptor

3.5 nM (Ki)

adenosine A2A receptor

4.2 nM (Ki)

adenosine A2B receptor

16 nM (Ki)

adenosine A3 receptor

51 nM (Ki)

In Vitro

CGS 15943 inhibits the kinase activity of the class IB PI3K isoform p110γ with an IC50 of 1.1 μM and shows slight inhibition on p110δ with an IC50 of 8.47 μM[3].
CGS 15943 (0-20 μM; 72 hours) inhibits growth of HLF and SK-Hep-1 cells, as well as HepG2 and PLC-PRF-5 cells[3].
CGS 15943 (0-20 μM; 24 hours) reduces the phosphorylation of Akt at its residues Ser473 and Thr308 in HLF and Sk-Hep-1 cells[3].

Cell Viability Assay[3]

Cell Line: HLF, SK-Hep-1, HepG2 and PLC-PRF-5 cells
Concentration: 0 μM; 1 μM; 5 μM; 10 μM; 20 μM
Incubation Time: 24 hours
Result: Inhibited growth of four distinct HCC cell lines.

Western Blot Analysis[3]

Cell Line: HLF and Sk-Hep-1 cells
Concentration: 0 μM; 1 μM; 5 μM; 10 μM; 20 μM
Incubation Time: 24 hours
Result: Inhibited the PI3K/Akt pathway in HLF and Sk-Hep-1 cells
Molecular Weight

285.69

Formula

C₁₃H₈ClN₅O

CAS No.

104615-18-1

SMILES

NC1=NC2=C(C=C(Cl)C=C2)C3=NC(C4=CC=CO4)=NN13

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Please store the product under the recommended conditions in the Certificate of Analysis.

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