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经验公式(希尔记法):
C11H5F2NO4S
化学文摘社编号:
分子量:
285.22
UNSPSC Code:
12352200
NACRES:
NA.77
MDL number:
Assay:
≥98% (HPLC)
Form:
solid
Storage condition:
OK to freeze, protect from light
Quality Segment
assay
≥98% (HPLC)
form
solid
potency
180 nM Ki
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
General description
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
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.
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)
存储类别
11 - Combustible Solids
wgk
WGK 3