1-Oleoyl-2-acetyl-sn-glycerol (1-oleoyl-2-acetyl-glycerol) 是一种细胞渗透性的钙依赖蛋白激酶C (PKC)激活剂，可调节多种可兴奋细胞中的全细胞 Ca2+ 电流，诱导超氧化物的产生。

Prostratin(12-Deoxyphorbol-13-acetate，13-O-乙酰基-12-脱氧佛波醇)是一种具有口服活性的蛋白激酶C（PKC）激活剂，Ki值为12.5 nM。作为一种NF-κB激活剂，Prostratin可激活T细胞中HIV基因的表达。Prostratin能抑制急性髓系白血病（AML）细胞系的生长，并增强阿糖胞苷诱导的AML细胞分化。此外，Prostratin诱导KRAS磷酸化并抑制KRAS突变的肿瘤生长。

UCN-02 (7-epi-Hydroxystaurosporine) 是一种由链霉菌属 N-126 菌株产生，具有选择性和高效性的蛋白激酶 C (PKC) 抑制剂，抑制 PKA。UCN-02 具有抗肿瘤活性。

PKC-IN-1 是 ATP-竞争性可逆 PKC 抑制剂，对人 PKCβ 和 PKCα 的 Ki 值分别为 5.3 和 10.4 nM，对人 PKCα、PKCβI、PKCβII、PKCθ、PKCγ、PKC mu 和 PKCε 的IC50值分别为 2.3、8.1、7.6、25.6、57.5、314 和 808 nM。

Sphingosine (d14:1) is a bioactive sphingolipid that has been found in B. mori (silkworm), P. clarkii (crayfish), and A. aurita (jellyfish) extracts. It increases the germination rate of N. rileyi, an entomopathogenic fungus, with an EC50 value of 10.2 nM. Sphingosine (d14:1) inhibits protein kinase C (PKC) in vitro (IC50 = 7.3 mol%) as well as superoxide generation induced by phorbol 12-myristate 13-acetate in neutrophils and reduces growth of CHO cells (IC50s = 19 and 8 μM, respectively).

Psychosine (Galactosylsphingosine) 是一种 PKC 抑制剂，是半乳糖脑苷脂酶 (GALC) 酶的底物，是 Krabbe 病的潜在生物标志物。Psychosine 具有很强的细胞毒性，可诱导多种细胞死亡。

K-252b is an indolocarbazole isolated from the actinomycete Nocardiopsis and is a PKC inhibitor. K-252b can be used to inhibit extracellular kinases of cells in culture because it can’t pass through the cell membrane freely.

与 H-7 相比，Iso-H7 dihydrochloride 是一种较弱的磷酸激酶 C 抑制剂。

CREBtide is a synthetic substrate for PKA (Km=3.9 µM), which is based on the phosphorylation sequence in d-CREB (cAMP response element binding protein).