This Review summarizes the advancements in Pd-catalyzed C(sp(3))-H activation via various redox manifolds, including Pd(0)/Pd(II), Pd(II)/Pd(W), and Pd(II)/Pd(0). While few examples have been reported in the activation of alkane C -H bonds, many C(sp(3))-H activation/C-C and C-heteroatom bond forming reactions have been developed by the use of directing group strategies to control regioselectivity and build structural patterns for synthetic chemistry. A number of mono- and bidentate ligands have also proven to be effective for accelerating C(sp(3))-H activation, directed by weakly coordinating auxiliaries, which provides great opportunities to control reactivity and selectivity (including enantioselectivity) in Pd-catalyzed C-H functionalization reactions.