pkc in 1

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。

PKC-iota inhibitor 1 是一种蛋白激酶 C-iota(PKC-ι ℩)的抑制剂，IC50值为 0.34 μM。

Aurora A PKC-IN-1 (Compound 2e) 是一种有效的 Aurora A (AurA) 和 PKC (α, β1, β2, θ) 双重抑制剂，作用于 AurA (IC50: 6.9 nM) 和 PKCα (IC50: 16.9 nM)。Aurora A PKC-IN-1 对乳腺癌细胞表现出抗增殖和抗转移作用。

PKC-theta inhibitor 1 is an inhibitor of PKCθ (Ki of 6 nM)

PKCβ inhibitor 1 (KUN79359) 是一种 ATP 竞争性和选择性PKCβ抑制剂，对人 PKCβ1 和 PKCβ2 的IC50分别为 21 和 5 nM。

Ebselen (CCG-39161) 是一种谷胱甘肽过氧化物酶模拟物，是电压依赖性钙通道阻断剂。它抑制Mpro 和COVID-19病毒，是HIV-1衣壳 CTD 二聚化的抑制剂，具有抗炎、抗癌和抗氧化活性。

API-1 (NSC-177223) 是Akt PKB 抑制剂，可同 PH 结构域相结合并抑制 Akt 膜易位，有效降低 Akt 的磷酸化水平。它可选择性的抑制PKB，对 PKC 和 PKA 的激活无抑制作用。它可以和 TNF 相关的凋亡诱导配体协同作用从而诱导细胞凋亡。

ZIP acetate(863987-12-6 free base) 是一种新型的细胞渗透性蛋白激酶 Mζ (PKMζ) 抑制剂，它是一种参与 LTP 维持的组成型活性非典型 PKC 同工酶。在体外选择性阻断 PKMζ 诱导的海马切片突触增强。逆转晚期 LTP (IC50 = 1 - 2.5 μM) 并在体内中央给药后导致 1 天前的空间记忆持续丧失。

CaMKII-IN-1是高效的 CaMKII 选择性抑制剂，IC50为63nM，对 CaMKIV, MLCK, p38a, Akt1,和 PKC 这些靶点几乎无作用。

R 59-022 (DKGI-I) 是一种二酰基甘油激酶 （DGK） 抑制剂，也 是一种 5-HT Receptor 拮抗剂，可阻断宿主细胞中的丝状病毒内化。R 59-022 可激活蛋白激酶 C (PKC)，抑制肠平滑肌的收缩力，增强由1-油酰基-2-乙酰甘油诱导的 O2-产生。

ζ-Stat 是非典型的、特异性的PKC-ζ抑制剂，IC50为 5 μM。ζ-Stat 能够减少黑色素瘤细胞系的增殖并诱导细胞凋亡，在体外显示除抗肿瘤活性。

Tpl2 kinase inhibitor is an inhibitor of tumor progression locus 2 (Tpl2; IC50= 0.05 μM).1It is selective for Tpl2 over MEK, p38 MAPK, Src, MK2, and PKC (IC50s = >40, 180, >400, 110, and >400 μM, respectively). Tpl2 kinase inhibitor inhibits LPS-induced TNF-α production in isolated human monocytes and whole blood (IC50s = 0.7 and 8.5 μM, respectively). It enhances differentiation induced by calcitriol in HL-60 and U937 leukemia cells when used at a concentration of 5 μM.2Tpl2 kinase inhibitor (5 μM) inhibits the proliferation of KG-1a leukemia cells.3 1.Garvin, L.K., Green, N., Hu, Y., et al.Inhibition of Tpl2 kinase and TNF-α production with 1,7-naphthyridine-3-carbonitriles: Synthesis and structure-activity relationshipsBioor. Med. Chem. Lett.15(23)5288-5292(2005) 2.Wang, X., and Studzinski, G.P.Expression of MAP3 kinase COT1 is up-regulated by 1,25-dihydroxyvitamin D3 in parallel with activated c-jun during differentiation of human myeloid leukemia cellsJ. Steroid. Biochem. Mol. Biol.121(1-2)395-398(2010) 3.Wang, X., Gocek, E., Novik, V., et al.Inhibition of Cot1/Tlp2 oncogene in AML cells reduces ERK5 activation and up-regulates p27Kip1 concomitant with enhancement of differentiation and cell cycle arrest induced by silibinin and 1,25-dihydroxyvitamin D3Cell Cycle9(22)4542-4551(2010)

Protein kinase C (PKC ) is a calcium-independent, phospholipid- and diacylglycerol-dependent serine threonine kinase involved in diverse signaling pathways, including those involved in neuronal signaling, cytoskeletal function, and inflammation.[1] PKC inhibitor peptide is a synthetic peptide corresponding to an amino acid sequence found in the amino terminal C2 domain of most mammalian forms of PKC .[2] It selectively and reversibly inhibits the translocation of PKC to intracellular membranes, blocking activation.[2] PKC inhibitor peptide is commonly used in cells to evaluate the role of PKC in various cellular responses.[3],[4],[5]

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 1.2 μM) following oral administration (10 and 3 mg kg) in rat and dog, respectively[1].CC-90005 exhibits the mean residence time (0.52 and 2.0 h), CL (69.1 and 20.5 mL min kg) and Vss (2.11 and 2.44 L kg) following intravenous administration (2 and 1 mg kg) in rat and dog, respectively[1]. [1]. Papa P, et, al. Discovery of the Selective Protein Kinase C-θ Kinase Inhibitor, CC-90005. J Med Chem. 2021 Aug 26;64(16):11886-11903.

Ingenol 3,20-dibenzoate is a powerful activator of protein kinase C (PKC) isoforms. It effectively induces the translocation of nPKC-delta, -epsilon, and -theta as well as PKC-mu from the cytosolic fraction to the particulate fraction. Through de novo synthesis of macromolecules, it triggers apoptosis with characteristic morphology. Moreover, Ingenol 3,20-dibenzoate enhances IFN-γ production and degranulation in NK cells, particularly when stimulated by NSCLC cells[1][2].

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).

Phellopterin 是一种分离自P. trifoliata 中的天然产物。它能够调节 Akt 和 PKC 通路，抑制 TNF-alpha 诱导的 VCAM-1 表达，进而减少单核细胞与内皮细胞的粘附。

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。

PKC-IN-4 (compound 7l) is a highly potent and orally active inhibitor of atypical protein kinase C (aPKC), exhibiting an IC 50 value of 0.52 μM. In vitro studies have demonstrated that PKC-IN-4 effectively suppresses NF-κB activity induced by TNF-α. Moreover, this compound effectively impedes the permeability of the retinal vasculature, induced by both VEGF and TNFα. [1]

Nardosinone 是一个 dbcAMP 和 staurosporine 的神经生成作用增强剂，分离自Nardostachys chinensis 中。Nardosinone 可能成为一种有用的药理学工具，不仅可用于研究神经生长因子 (NGF) 的作用机理，而且可用于研究神经毒性物质的作用机理。

PKCiota-IN-1 是一种有效的 PKCiota (PKC-ι)抑制剂，IC50为 2.7 nM。PKCiota-IN-1 还抑制PKC-α和PKC-ε，IC50分别为 45 nM 和 450 nM。

[Ala113]MBP(104-118) TFA 是 protein kinase C (PKC)的非竞争性的肽抑制剂，IC50值范围为 28-62 μM。

Pep2m, myristoylated TFA (Myr-Pep2m TFA)为具备细胞渗透性的肽。该化合物通过破坏PKMζ与其下游靶点NSF GluR2的相互作用而发挥作用，其中PKMζ为具有自主活性的PKC同工酶。

Malantide TFA 是一种合成的十二肽，由被磷酸化酶激酶β亚基上的PKA 磷酸化的位点衍生而来。Malantide TFA 是PKA 的高度特异性底物，Km 为 15 μM，并且在各种大鼠组织提取物中显示出 PKI 抑制 > 90％底物磷酸化。Malantide TFA 也是PKC 的有效底物，Km 为 16 μM。