PI 3-Kgamma Inibitore CAS: 648450-29-7
MF: C12H7N3O2S
MW: 257.3
A cell-permeable, potent, selective, and ATP-competitive inhibitor of PI 3-kinase.

PI 3-Kγ Inibitore (CAS 648450-29-7)

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Nomi alternativi: 5-Quinoxalin-6-ylmethylene-thiazolidine-2,4-dione, PI 3-K Inhibitor I
Applicazione: PI 3-Kγ Inhibitor is a cell-permeable, potent, selective, and ATP-competitive inhibitor of PI 3-kinase
Numero CAS: 648450-29-7
Purezza: >90%
Peso molecolare: 257.3
Formula molecolare: C12H7N3O2S
Solo per uso in Ricerca. Non previsto per Uso Diagnostico o Terapeutico.
* Vedere Certificato di Analisi per informazioni sul lotto specifico (incluso il contenuto d'acqua).

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.


Referenze

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

Stato fisico :
Solid
Solubilità :
Soluble in DMSO (>5 mg/ml), DMF (~0.2 mg/ml), and ethanol (<1 mg/ml) at 25° C. Insoluble in water.
CONSERVAZIONE :
Store at 4° C
Punto di scioglimento :
243.03° C (Predicted)
Punto di ebollizione :
565.14° C (Predicted)
Densità :
1.55 g/cm3 (Predicted)
Indice di rifrazione :
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
Valori pK :
pKa: 7.04 (Predicted)
Solo per uso in Ricerca. Non previsto per Uso Diagnostico o Terapeutico.
WGK Germania :
3
PubChem CID :
10377751
Numero MDL :
MFCD11100415
SMILES :
C1=CC2=NC=CN=C2C=C1/C=C/3\\C(=O)NC(=O)S3

Download SDS (MSDS)

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