PKCα Activator

(-)-Indolactam V is a PKC activator, with K_is of 3.36 nM, 1.03 μM for η-CRD2 (PKCη surrogate peptide), γ-CRD2 (PKCγ surrogate peptide), and K_ds of 5.5 nM (η-C1B), 7.7 nM (ε-C1B), 8.3 nM (δ-C1B), 18.9 nM (β-C1A-long), 20.8 nM (α-C1A-long), 137 nM (β-C1B), 138 nM (γ-C1A), 213 nM (γ-C1B), and has antitumor activity.

18:0-22:6 DG (1-Stearoyl-2-docosahexaenoyl-sn-glycerol) is a diacylglycerol (DG) that can interact with RasGRP (Ras guanine nucleotide-releasing protein) (K_i = 8.37 μM) and modulate the activation of MAP kinases (such as ERK1/ERK2), which play a crucial role in cellular signaling processes. 18:0-22:6 DG can also activate protein kinase C (PKC) isozyme. 18:0-22:6 DG can be used for research of cancer, immunology and metabolic disease.

βGlcCer is a glycosphingolipid. βGlcCer directly increases the development and PKCα and PKCδ activation in mouse bone marrow-derived DCs (BMDCs). β-GlcCer accumulating in Gaucher disease activates microglia through macrophage-inducible C-type lectin (Mincle) to induce phagocytosis of living neurons, which exacerbates Gaucher symptoms.