Bisindolylmaleimide VIII (Ro-31-7549) 是一种具有选择性和高效性的蛋白激酶 C (PKC) 抑制剂,对 PKC-α,PKC-β我,PKC-β第二,PKC-γ,PKC-ε 均具有较好的抑制作用。Bisindolylmaleimide VIII 抑制 T 细胞介导的自身免疫性疾病,可通过蛋白激酶 C 非依赖性机制增强 Fas 介导的细胞凋亡。
TMB 8 is a non-competitive antagonist of nicotinic acetylcholine receptors (nAChRs) with IC50 values of 390 and 350 nM, respectively, for human muscle-type and α3β4 subunit-containing ganglionic nAChRs expressed in TE671 RD or SH-SY5Y cells. It inhibits nicotine-induced dopamine release from ratbrain synaptosomes (IC50 = 480 nM). TMB 8 also reduces calcium availability in smooth and skeletal muscle, blocking the contractile response in isolated rabbit aortic strip when used at a concentration of 50 μM and inhibiting calcium influx and efflux in isolated guinea pig ileum when used at a concentration of 65 μM. It has been used in the study of intracellular calcium dynamics, particularly in smooth muscle. TMB 8 also inhibits protein kinase C (PKC) activity in a dose-dependent manner.
K252d is an indolocarbazole alkaloid found in Nocardiopsis. It is a PKC inhibitor that inhibits PKC isolated from ratbrain, as well as, calcium- and calmodulin-dependent phosphodiesterase isolated from bovine heart.