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Protein kinase C (PKC) inhibitors and activators act on a family of lipid-regulated serine/threonine kinases. Conventional PKC isoforms require calcium and diacylglycerol, novel isoforms need only diacylglycerol, and atypical isoforms respond to neither. Tumor-promoting phorbol esters mimic diacylglycerol and were shown in 1982 to activate PKC directly. 12-O-tetradecanoyl phorbol-13-acetate (TPA) is the standard activator of this kind, and ingenol mebutate also activates several isoforms. Staurosporine was first described as a PKC inhibitor but blocks a wide range of protein kinases. Enzastaurin is selective for PKCβ, while GO6983 and Ro 31-8220 mesylate inhibit multiple conventional and novel isoforms.
Synonyms: 7-epi-Hydroxystaurosporine
UCN-02 (7-epi-Hydroxystaurosporine) is a selective protein kinase C (PKC) inhibitor produced by Streptomyces strain N-12, with IC50s of 62 nM and 250 nM for PKC and protein kinase A (PKA), respectively.
VTX-27 is a selective protein kinase C θ (PKC θ) inhibitor, with Kis of 0.08 nM and 16 nM for PKC θ and PKC δ.
Synonyms: LXS 196
Darovasertib (LXS196) is a potent, selective and orally active protein kinase C (PKC) inhibitor, with IC50 values of 1.9 nM, 0.4 nM and 3.1 μM for PKCα, PKCθ and GSK3β, respectively. It can be used for the treatment of uveal melanoma.
PKC-theta inhibitor is a selective PKC-θinhibitor, with an IC50 of 12 nM.
CMPD101, is a novel membrane-permeable, small-molecule inhibitor of both GRK2 and GRK3 with IC50s of 18 nM and 5.4 nM. CMPD101 also inhibits ROCK-2 and PKCα (IC50s=1.4 μM and 8.1 μM, respectively).
Synonyms: Mallotoxin; NSC 56346; NSC 94525
Rottlerin, a natural product purified from Mallotus Philippinensis, is a specific PKC inhibitor, with IC50 values for PKCδ of 3-6 μM, PKCα,β,γ of 30-42 μM, PKCε,η,ζ of 80-100 μM.
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Synonyms: Bisindolylmaleimide IX
Ro 31-8220 is a potent PKC inhibitor, with IC50s of 5, 24, 14, 27, 24 and 23 nM for PKCα, PKCβI, PKCβII, PKCγ, PKCε and rat brain PKC, respectively.
Synonyms: BIM-X hydrochloride; Ro31-8425 hydrochloride
Bisindolylmaleimide X hydrochloride (BIM-X hydrochloride) is a potent and selective protein kinase C (PKC) inhibitor.
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HA-100 is an isoquinoline compound with an added piperazinylsulfonyl group that acts as an inhibitor of protein kinases (PKs), including PKA, PKC, and PKG (IC50s = 8, 12, and 4 µM, respectively).
Iso-H7 dihydrochloride is an inhibitor of phosphokinase C.
Malantide is a synthetic dodecapeptide derived from the site phosphorylated by cAMP-dependent protein kinase (PKA) on the β-subunit of phosphorylase kinase. Malantide is a highly specific substrate for PKA with a Km of 15 μM and shows protein inhibitor (PKI) inhibition >90% substrate phosphorylation in various rat tissue extracts. Malantide is also an efficient substrate for PKC with a Km of 16 μM.
Hispidin is a phenolic compound and protein kinase C (PKC) inhibitor derived from *Phellinus linteus*. It exhibits strong antioxidant, anticancer, antidiabetic, and anti-dementia activities, making it a promising candidate for research in various disease models.
CRT0066854 is a potent and selective inhibitor of atypical protein kinase C (PKC) isoenzymes. It inhibits full-length PKCι, PKCζ, and ROCK-II with IC₅₀ values of 132 nM, 639 nM, and 620 nM, respectively.
Variegatic acid is a PKCβ1 inhibitor with an IC₅₀ of 36.2 μM, derived from basidiomycete fungi. It effectively inhibits antigen-induced and calcium ionophore-induced β-hexosaminidase release, with IC₅₀ values of 10.4 μM and 22.2 μM, respectively, as well as TNF-α secretion (IC₅₀ values of 16.8 μM and 20.1 μM). By suppressing the enzymatic activity of calcium-activated PKCβ1, variegatic acid also facilitates the generation of hydroxyl radicals through its action on Fe(III), making it valuable for research focused on biological degradation and allergic responses.
PKCβ Inhibitor 1 is a highly selective, ATP-competitive inhibitor targeting protein kinase C beta (PKCβ) with IC50 values of 21 nM for PKCβ1 and 5 nM for PKCβ2. This compound demonstrates over 60-fold selectivity for PKCβ2 compared to other PKC isozymes such as PKCα, PKCγ, and PKCε. It is a valuable tool for investigating the roles of PKCβ in various signaling pathways and its implications in diseases such as cancer and diabetes.
Synonyms: NSC37044
ζ-Stat (NSC37044) is a specific inhibitor of protein kinase C zeta (PKC-ζ), demonstrating an IC50 of 5 μM. This compound has been shown to effectively reduce proliferation in melanoma cell lines while inducing apoptosis. Its antitumor activity in vitro makes ζ-Stat a valuable tool for research into cancer biology and therapeutic development.
Synonyms: Ro 31-7549 acetate; Bis VIII acetate
Bisindolylmaleimide VIII acetate is a potent and selective inhibitor of protein kinase C (PKC), exhibiting an IC50 of 158 nM for rat brain PKC. It demonstrates strong inhibitory activity against various PKC isoforms, with IC50 values of 53 nM for PKC-α, 195 nM for PKC-βI, 163 nM for PKC-βII, 213 nM for PKC-γ, and 175 nM for PKC-ε. This compound is valuable for research applications related to Fas-mediated apoptosis and the modulation of T cell-mediated autoimmune responses.
Synonyms: UCN-1028C
Calphostin C is a selective inhibitor of protein kinase C (PKC), displaying an IC50 of 0.05 μM. This compound disrupts PKC-mediated phosphorylation, promoting tumor apoptosis and exhibiting potential therapeutic benefits. Additionally, Calphostin C has been shown to restore Na+/K+ ATPase activity in diabetic mouse sciatic nerves, offering insights into its role in mitigating diabetic complications. It serves as a valuable tool for research in cancer biology and neuropathy.
Synonyms: NSC37044 trisodium
ζ-Stat trisodium is a selective inhibitor of protein kinase C zeta (PKC-ζ), exhibiting an IC50 of 5 μM. This compound effectively reduces the proliferation of melanoma cell lines and induces apoptotic cell death. Its antitumor activity in vitro supports its potential application in cancer research and therapeutic development.
HBDDE is an isoform-selective inhibitor targeting PKCα and PKCγ, with IC50 values of 43 μM and 50 μM, respectively. This compound exhibits selectivity for PKCα and PKCγ over PKCδ, PKCβI, and PKCβII isozymes. HBDDE has been shown to induce neuronal apoptosis, making it a valuable tool for research involving neuronal cell death and signaling pathways regulated by PKC isoforms.
Synonyms: LY317615 hydrochloride
Enzastaurin hydrochloride is a potent and selective inhibitor of protein kinase C beta (PKCβ), exhibiting an IC50 of 6 nM. This compound demonstrates a 6- to 20-fold preference for PKCβ over other isoforms, including PKCα, PKCγ, and PKCε. Enzastaurin is utilized in research focused on cancer therapeutics and signal transduction pathways, providing insights into the role of PKCβ in cellular processes and disease mechanisms.
Synonyms: LY317615 dihydrochloride
Enzastaurin dihydrochloride is a potent and selective inhibitor of protein kinase C beta (PKCβ), exhibiting an IC50 of 6 nM. This compound demonstrates 6- to 20-fold selectivity over other PKC isoforms, including PKCα, PKCγ, and PKCε. Enzastaurin is utilized in research applications focused on cancer biology and signal transduction pathways, providing insights into therapeutic targets for malignancies and related diseases.
Synonyms: Ro 31-7549; Bis VIII
Bisindolylmaleimide VIII is a highly selective inhibitor of protein kinase C (PKC), exhibiting an IC50 of 158 nM against rat brain PKC. This compound demonstrates significant potency across various PKC isoforms, including IC50 values of 53 nM for PKC-α and 175 nM for PKC-ε. Additionally, Bisindolylmaleimide VIII promotes Fas-mediated apoptosis and serves as a valuable tool in research focused on T cell-mediated autoimmune diseases and efforts to elucidate PKC pathways in cellular signaling.
BHA536 is a selective inhibitor targeting PKCα and PKCβ, effectively modulating the NF-kB signaling pathway. It demonstrates significant antitumor activity by inhibiting the proliferation of CD79-mutated ABC DLBCL cells, inducing cell cycle arrest at the G1 phase, and triggering apoptosis in TMD8 cells. Additionally, BHA536 shows promising antitumor efficacy in in vivo mouse models, making it a valuable tool for cancer research and therapeutic studies.
