PI 3-Kgamma InhibitorA cell-permeable, potent, selective, and ATP-competitive inhibitor of PI 3-kinase

PI 3-Kγ Inhibitor (CAS 648450-29-7)

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Synonym: 5-Quinoxalin-6-ylmethylene-thiazolidine-2,4-dione, PI 3-K Inhibitor I
Application: A cell-permeable, potent, selective, and ATP-competitive inhibitor of PI 3-kinase
CAS Number: 648450-29-7
Purity: >90%
Molecular Weight: 257.3
Molecular Formula: C12H7N3O2S
* Refer to Certificate of Analysis for lot specific data (including water content).
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PI 3-Kγ Inhibitor is a cell-permeable thiazolidinedione compound that acts as a potent, selective, and ATP-competitive inhibitor of PI 3-kinase γ (PI 3-Kγ) (Ki = 7.8 nM; IC50 = 8 nM, 60 nM, 270 nM, 300 nM for p110-γ, α, β and δ-isoforms, respectively). PI 3-Kγ Inhibitor does not affect the activity of a wide panel of kinases, receptors, enzymes, and ion channels even at concentrations as high as 1 μM. It selectively blocks MCP-1-, but not CSF-1-, dependent Akt phosphorylation and chemotaxis in primary Pik3cg+/+ murine monocytes and in a human monocytic cell line THP-1 (IC50 = 181 nM). PI 3-Kγ Inhibitor has also been shown to exhibit efficacy in reducing neutrophil chemotaxis in murine peritonitis and arthritis models.


References

Barber, D.F., et al. 2005. Nat. Med. 11, 933. Camps, M., et al. 2005. Nat. Med. 11, 936.

Physical State :
Solid
Solubility :
Soluble in DMSO (>5 mg/ml), DMF (~0.2 mg/ml), and ethanol (<1 mg/ml) at 25° C. Insoluble in water.
Storage :
Store at 4° C
Melting Point :
243.03° C (Predicted)
Boiling Point :
565.14° C (Predicted)
Density :
1.55 g/cm3 (Predicted)
Refractive Index :
n20D 1.79 (Predicted)
IC50 :
p110-γ-isoforms: IC50 = 8 nM; p110-α-isoforms: IC50 = 60 nM; p110-β-isoforms: IC50 = 270 nM; p110-δ-isoforms: IC50 = 300 nM; MCP-1-dependent Akt phosphorylation and chemotaxis: IC50 = 181 nM (primary Pik3cg+/+ murine monocytes and in a human monocytic cell line THP-1); C5a-mediated phosphorylation of protein kinase B: IC50 = 90 nM (RAW 264 cells)
Ki Data :
PI 3-Kγ: Ki= 7.8 nM
pK Values :
pKa: 7.04 (Predicted)
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
WGK Germany :
3
PubChem CID :
10377751
MDL Number :
MFCD11100415
SMILES :
C1=CC2=NC=CN=C2C=C1/C=C/3\\C(=O)NC(=O)S3

Download SDS (MSDS)

Certificate of Analysis

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