PI3Kγ is one of four class I PI3Ks, a family of dual lipid and protein kinases involved in the regulation of numerous biological processes, such as cell growth, differentiation, survival, proliferation and migration1. A high-throughput chemoproteomics method has benen optimized to enable multiplexed screening resulting in the finding of CZC24832.
In vitro: Plenty of target- and cell-based studies of CZC24832 revealed regulation of interleukin-17–producing T helper cell (TH17) differentiation by PI3Kg, therefore giving selective inhibition of PI3Kg as a potential treatment for inflammatory and autoimmune diseases [1].
In vivo: CZC24832, the first selective inhibitor of phosphoinositide 3-kinase g (PI3Kg), was found to have efficacy in in vivo models of inflammation [1].
Clinical trial: Currenlty no clinical data are available.
Reference:
[1] 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;8(6):576-82.