Bisindolylmaleimide V

Ro 31-6045 (113963-68-1) is a bis indolylmaleimide derivative that is a potent inhibitor of the mitogen-stimulated protein kinase p70 (S6K) acting independently of its upstream activator mTOR.1Does not inhibit PKC (at concentrations <100mM) and therefore may be used as a negative control for bisindolylmaleimide PKC inhibitors2such as GF 109203X3and other structurally related inhibitors4.

Bisindolylmaleimide V is a cell-permeable negative control for protein kinase C inhibition studies with an IC50 value over 100 μM[1]. Bisindolylmaleimide V blocks the activation of mitogen-stimulated protein kinase p70s6k/p85s6k (S6K) in vivo with an IC50 of 8 μM[2].

ChEBI: Ro 31-6045 is a member of indoles.

[1] NELLY MARMY-CONUS  Richard B P  Katherine M Hannan. Ro 31-6045, the inactive analogue of the protein kinase C inhibitor Ro 31-8220, blocks in vivo activation of p70s6k/p85s6k: implications for the analysis of S6K signalling[J]. FEBS Letters, 2002, 519 1-3: 135-140. DOI:10.1016/s0014-5793(02)02738-2
[2] C S HARMON. Bisindolylmaleimide protein-kinase-C inhibitors delay the decline in DNA synthesis in mouse hair follicle organ cultures.[J]. Skin pharmacology : the official journal of the Skin Pharmacology Society, 1997, 10 2: 71-78. DOI:10.1159/000211471
[3] D. TOULLEC. The bisindolylmaleimide GF 109203X is a potent and selective inhibitor of protein kinase C.[J]. The Journal of Biological Chemistry, 1991, 12 1: 15771-15781. DOI:10.1016/s0021-9258(18)98476-0
[4] PETER D. DAVIS. Inhibitors of protein kinase C. 1. 2,3-bisarylmaleimides[J]. Journal of Medicinal Chemistry, 1992, 35 1: 177-184. DOI:10.1021/jm00079a024