Description: MBP146-78 is a potent and selective inhibitor of cGMP-dependent protein kinases (cGMP-dependent protein kinases). Target: Parasite. Smiles: CN1CCC(CC1)c1cc(c([nH]1)-c1ccc(F)cc1)-c1ccncc1. References: Nare B , Allocco J J , Liberator P A , et al. Evaluation of a Cyclic GMP-Dependent Protein Kinase...

MBP146-78 is an inhibitor of parasitic cGMP-dependent protein kinases (PKGs, IC50s = 1.9 and 1 nM for the E. tenella and T. gondii enzymes, respectively). It inhibits P. berghei sporozoite development into liver-stage parasites in HepG2 cells in a concentration-dependent manner. MBP146-78 (50 mg/kg) prevents P....

MBP146-78 inhibits the growth of Eimeria spp. both in vitro and in vivo. The molecular target of MBP146-78 was identified as cGMP-dependent protein kinase (PKG) using a tritiated analogue to purify a approximately 120-kDa protein from lysates of Eimeria tenella. This represents the first example of a protozoal PKG....

BGG463 (NVP-BGG463) was generated by a rational 'hybrid design' approach. Like Imatinib, BGG463 disrupts the assembly of the hydrophobic spine, a characteristic feature of the active state of several kinases, thereby locking the kinase in an inactive 'DFG-out' conformation. BGG463 can inhibit c-ABL-T334I, BCR-ABL...