The PI 3-Kγ Inhibitor II, also referenced under CAS 648449-76-7, controls the biological activity of PI 3-Kγ. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.
Synonym(s):
PI 3-Kγ Inhibitor II, 5-(2,2-Difluoro-benzo[1,3]dioxol-5-ylmethylene)-thiazolidine-2,4-dione, PI 3-K Inhibitor II
A cell-permeable thiazolidinedione compound that acts as a potent and ATP-competitive inhibitor of PI 3-Kγ (Ki = 180 nM; IC50 = 250 nM). Exhibits great selectivity over PI 3-Kα (IC50 = 4.5 µM), PI 3-Kβ and δ (IC50 >20 µM), and shows little effect towards a large panel of receptors, unrelated enzymes, ion channels, and 38 commonly studied kinases. Shown to block MCP-1-mediated monocyte chemotaxis in vitro and exhibit better in vivo efficacy than LY294002 (Cat. No. 440202 and 440204) in blocking RANTES- or thioglycollate-induced peritoneal neutrophil recruitment by oral administration in a murine peritonitis model.
Biochem/physiol Actions
Cell permeable: yes
Primary Target PI 3-Kγ
Product competes with ATP.
Reversible: no
Target IC50: 250 nM against PI 3-Kγ
Packaging
Packaged under inert gas
Warning
Toxicity: Irritant (B)
Reconstitution
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Other Notes
Bilancio, A., et al. 2006. Blood107, 642. Camps, M., et al. 2005. Nat. Med.11, 936.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Storage Class Code
11 - Combustible Solids
WGK
WGK 3
Certificates of Analysis (COA)
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Class I Phosphoinositide 3-kinases (PI3Ks) are master regulators of cellular functions, with the class IB PI3K catalytic subunit (p110γ) playing key roles in immune signalling. p110γ is a key factor in inflammatory diseases and has been identified as a therapeutic
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