Chemical Information

Biological Activity of CZC24832

CZC24832 is a selective inhibitor of PI 3-kinase γ (IC50 = 1.0 μM in a PI 3-Kγ-dependent fMLP-induced neutrophil migration assay); exhibits limited off-target effects in kinome profiling of 154 identified lipid and protein kinases and 922 other proteins.
IC50 value: 1.0 uM
Target: PI 3Kγ

References on CZC24832

[1]. Bell K, Sunose M, Ellard K, Cansfield A, Taylor J, Miller W, Ramsden N, Bergamini G, Neubauer G. SAR studies around a series of triazolopyridines as potent and selective PI3Kγ inhibitors. oorg Med Chem Lett. 2012 Aug 15;22(16):5257-63.http://www.ncbi.nlm.nih.gov/pubmed/22819766

[2]. Bergamini G, Bell K, Shimamura S, Werner T, Cansfield A, Müller K, Perrin J, Rau C, Ellard K, Hopf C, Doce C, Leggate D, Mangano R, Mathieson T, O'Mahony A, Plavec I, Rharbaoui F, Reinhard F, Savitski MM, Ramsden N, Hirsch E, Drewes G, Rausch O, Bantscheff M, Neubauer G. A selective inhibitor reveals PI3Kγ dependence of T(H)17 cell differentiation. Nat Chem Biol. 2012 Apr 29;8(6):576-82. doi: 10.1038/nchembio.957.