CC-90005 is a potent, selective and orally active inhibitor of protein kinase C-θ (PKC-θ), with an IC50 of 8 nM. CC-90005 shows selectivity for PKC-θ over PKC-δ (IC50=4440 nM). CC-90005 can inhibit T cell activation by IL-2 expression[1]. CC-90005 shows the exquisite selectivity of CC-90005, with IC50s for all other family members of >3 μM[1].CC-90005 is a moderate inhibitor of both CYP2C9 (IC50=8 μM) and CYP2C19 (IC50=5.9 μM) in human liver microsomes[1].CC-90005 inhibits IL-2 expression in LRS_WBC human PBMCs, with an IC50 of 0.15 μM[1].CC-90005 (1-10 μM; 24 h) inhibits T cell proliferation in PBMCs by 51% at 1 μM and 88% at 3 μM[1]. CC-90005 (3-30 mg/kg; p.o. twice daily for 4 days) significantly reduces the popliteal lymph node (PLN) size in a model of chronic T cell activation[1].CC-90005 (100 mg/kg; a single p.o.) significantly inhibits plasma and spleen IL-2 release by 51 and 54%, respectively[1].CC-90005 exhibits reasonable oral bioavailability (66 and 46%) and Cmax (1.18 and 1

Bisindolylmaleimide XI hydrochloride(Ro 32-0432)是一种口服活性的泛PKC抑制剂，对 PKCα、PKCβI、PKCβII、PKCγ 具有抑制作用（IC50=9/28/31/37/108 nM）。

Epsilon-V1-2 是蛋白激酶 C ε（PKCε）的特异性抑制剂。Epsilon-V1-2 被用于卵巢衰老、人颗粒细胞凋亡、脑缺血-再灌注损伤、脑发育、肝细胞胰岛素信号转导以及缺血条件下神经元细胞死亡等相关研究。研究表明，Epsilon-V1-2 能够有效降低 PKCε 的活性，从而促进对线粒体动力学、钙超载、AKT 激活、脑萎缩、胰岛素抵抗及铁死亡等调控通路的深入解析。Epsilon-V1-2 在卒中、SHORT 综合征、肝脂肪变性及脑损伤等疾病模型中显示出显著的治疗相关性。

Protein Kinase C (19-31), a peptide inhibitor of protein kinase C (PKC) derived from the pseudo-substrate regulatory domain of PKCa (residues 19-31) with a serine at position 25 replacing the wild-type alanine, is used as a protein kinase C substrate peptide.

PS432 is an allosteric inhibitor of atypical PKCs. PS432 targets the PIF-pocket resulting in significantly reduce tumor growth without side effects in mouse xenograft model.

Ruboxistaurin (LY333531) 是一种选择性的、口服具有活力的 PKC beta 抑制剂，其 Ki 值为 2 nM。Ruboxistaurin 以 ATP 依赖性的方式竞争性抑制 PKC beta I (IC50: 4.7 nM)。Ruboxistaurin 能够作用于 PKC beta II (IC50: 5.9 nM)。

Phosphate acceptor peptide 是一种 cAMP 依赖性蛋白激酶 (PKA) 的底物。Phosphate acceptor peptide 也是一种弱的PKC 抑制剂。

PKCd (8-17) 是源自蛋白激酶 C (PKC)d V1 结构域的生物活性肽。它能抑制由佛波醇 12-肉豆蔻酸酯 13-乙酸酯 (PMA) 诱导的 PKCd 易位和激活。此外，PKCd (8-17) 在降低心脏和脑细胞缺血损伤、促进成纤维细胞增殖、以及抑制小鼠移植冠状动脉疾病方面具有潜在应用。

Ilmofosine (BM41440) 是一种高效选择性的蛋白激酶C (protein kinase C) 抑制剂，能够诱导细胞周期在G2期停滞。此外，Ilmofosine 还是一种抗利什曼原虫的药物。