Identification | Back Directory | [Name]
CAY10505 | [CAS]
328960-84-5 | [Synonyms]
5-((5-(4-Fluorophenyl)furan-2-yl)methylene)thiazolidine-2,4-dione (5E)-5-{[5-(4-fluorophenyl)furan-2-yl]methylidene}-1,3-thiazolidine-2,4-dione | [Molecular Formula]
C14H8FNO3S | [MDL Number]
MFCD18382079 | [MOL File]
328960-84-5.mol | [Molecular Weight]
289.28 |
Hazard Information | Back Directory | [Description]
Phosphoinositide 3-kinase γ (PI3Kγ), expressed primarily in hematopoietic cells, plays several important roles in immunity. CAY10505 is a potent inhibitor of PI3K, selectively inhibiting the γ isoform (IC50 = 30 nM) better than the α, β, and δ isoforms (IC50 = 0.94, 20, and 20 μM, respectively).1 Tested against a panel of 80 other kinases, CAY10505 significantly inhibits only the unrelated casein kinase 2 (CK2, IC50 = 20 nM). It also inhibits the phosphorylation of the PI3K substrate PKB/Akt in mouse macrophages (IC50 = 228 nM).1 Oral administration of CAY10505 reduces neutrophil recruitment in mice to an extent that is comparable to that observed in PI3Kγ-deficient mice.1 | [References]
1. Pomel, V., Klicic, J., Covini, D., et al. Furan-2-ylmethylene thiazolidinediones as novel, potent, and selective inhibitors of phosphoinositide 3-kinase γ J. Med. Chem. 49(13),3857-3871(2006). |
|
Company Name: |
Carbosynth
|
Tel: |
+86 512 6260 5585 |
Website: |
www.carbosynth.com |
|