528108
PI 3-Kγ Inhibitor II
5-(2,2-Difluoro-benzo[1,3]dioxol-5-ylmethylene)-thiazolidine-2,4-dione, PI 3-K Inhibitor II
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Merck KGaA
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25 May 2013
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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.
| Product information | |||
|---|---|---|---|
| Form | Off-white solid | ||
| Primary Target | PI 3-Kg | ||
| Primary Target IC50 | 250 nM | ||
| Primary Target Ki | 180 nM | ||
| Secondary target | PI 3-Kα (IC50 = 4.5 µM), PI 3-Kβ and δ (IC50 > 20 µM) | ||
| Molar mass | 285.2 | ||
| Protect from Light | Yes | ||
| Packaged under inert gas | Yes | ||
| Cell permeable | Yes | ||
| ATP Competitive | Yes | ||
| Purity | ≥98% by HPLC | ||
| Solubility | DMSO or EtOH | ||
| Chemical formula | C11H5F2NO4S | ||
| CAS number | 648449-76-7 | ||
| Store and ship information | |||
|---|---|---|---|
| Storage | +2°C to +8°C | ||
| Ship |
Ambient Temperature Only
Irritant |
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