528108

PI 3-Kγ Inhibitor II

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
• Empirical Formula (Hill Notation): C₁₁H₅F₂NO₄S
• CAS Number: 648449-76-7
• Molecular Weight: 285.22
• UNSPSC Code: 12352200
• NACRES: NA.77
• MDL number: MFCD19705528
• Assay: ≥98% (HPLC)
• Form: solid
• Storage condition: OK to freeze, protect from light

Properties

• Quality Segment: 100
• assay: ≥98% (HPLC)
• form: solid
• potency: 180 nM K_i
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze, protect from light
• color: off-white
• solubility: DMSO: 10 mg/mL, ethanol: 5 mg/mL
• shipped in: ambient
• storage temp.: 2-8°C
• SMILES string: FC1(Oc2c(ccc(c2)\C=C3\SC(=O)NC\3=O)O1)F
• InChI: 1S/C11H5F2NO4S/c12-11(13)17-6-2-1-5(3-7(6)18-11)4-8-9(15)14-10(16)19-8/h1-4H,(H,14,15,16)/b8-4+
• InChI key: SRLVNYDXMUGOFI-XBXARRHUSA-N

Description

General description

A cell-permeable thiazolidinedione compound that acts as a potent and ATP-competitive inhibitor of PI 3-Kγ (K_i = 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

Preparation Note

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

Disclaimer

Toxicity: Irritant (B)

Safety Information

• Storage Class: 11 - Combustible Solids
• wgk: WGK 3