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PKC (Protein kinase C) is a family of protein kinase enzymes that are involved in controlling the function of otherproteins through the phosphorylation of hydroxyl groups of serine and threonine amino acid residues on these proteins. PKC enzymes in turn are activated by signals such as increases in the concentration of diacylglycerol (DAG) or calcium ions (Ca2+). Hence PKC enzymes play important roles in several signal transduction cascades. The PKC family consists of 15 isozymes in humans: PKC-α (PRKCA), PKC-β1 (PRKCB), PKC-β2 (PRKCB), PKC-γ (PRKCG), PKC-δ (PRKCD), PKC-δ1 (PRKD1), PKC-δ2 (PRKD2), PKC-δ3 (PRKD3), PKC-ε (PRKCE), PKC-η (PRKCH), PKC-θ (PRKCQ), PKC-ι (PRKCI), PKC-ζ (PRKCZ), PK-N1 (PKN1), PK-N2 (PKN2), PK-N3 (PKN3). PKC is involved in receptor desensitization, in modulating membrane structure events, in regulating transcription, in mediating immune responses, in regulating cell growth, and in learning and memory. These functions are achieved by PKC-mediated phosphorylation of other proteins.

Cat. No. Product Name CAS No. Information
GY04421

Sotrastaurin

425637-18-9

A potent, selective, orally available pan-PKC inhibitor with Ki of 0.22-3.2 nM for PKC isotypes; displays excellent selectivity against a broad panel of kinases (only GSK-3β IC50<1 uM); inhibits early T-cell activation with no general antiproliferative activity, also inhibits β2-integrin-mediated T-cell adhesiveness; prolongs rat heterotopic heart transplant survival in combination with adjunct immunosuppression agents.

GY02761

CGP60474

164658-13-3

A potent CDK1 inhibitor with IC50 of 17 nM; exhibits lower potency at CDK2 (IC50=50-80nM) and moderate potency at CDK4 (IC50=700 nM).

GY06997

PKC inhibitor 6c

2026603-86-9

PKC inhibitor 6c is a receptor (Ki>10 uM); effectively blocks amphetamine-induced locomotor stimulation, more potently inhibits PKC than tamoxifen and reduces amphetamine-stimulated dopamine efflux.

GY10439

PZ09

1132609-87-0

PZ09 (PKC-zeta inhibitor 9, PKC-ζ inhibitor PZ9) is a potent, isoform selective PKC-zeta (PKC-ζ) inhibitor with IC50 of 5.18 nM, displays excellent selectivity (>200-fold) over other PKC isoforms with exception of PKC-i (10-fold); also shows high selectivity for CDK-2 (>200-fold), as well as a broader range of other kinases (<50% inhibition at 10 uM); PZ09 is a small-molecule inhibitor, the first tool to successfully interrogate aPKC signaling in cells.

GY05372

PKC beta II inhibitor H6

1046787-18-1

PKC-IN-1 is a poent PKC beta II inhibitor with Ki of 14.9 nM, extracted from patent WO 2008096260 A1 as compound example H6.

GY05363

UCN-01

112953-11-4

UCN-01 (7-Hydroxystaurosporine;NSC 638850) is a synthetic derivative of staurosporine that has antiproliferative activity against several in vitro and in vivo cancer models; inhibits a variety of kinases, including Akt, PKC (IC50=30 nM), PDK1 (IC50=6 nM), CDKs (IC50=300-600 nM for Cdk1 and Cdk2); arrests tumor cells in the G1/S phase of the cell cycle and prevents nucleotide excision repair by Chk1 (IC50=7 nM); induces apoptosis.

GY05337

AS2521780

1214726-89-2

AS2521780 is a potent, selective, orally bioavailable PKCθ inhibitor that inhibits combinant human PKCθ enzyme with IC50 of 0.48 nM, >30-fold higher than other PKC isoforms; also displays >100-fold selectivity over a panel of 27 protein kinases (100-fold over CDK2, IC50=84 nM); suppresses CD3/CD28-induced IL-2 gene transcription (IC50=14 nM) in Jurkat T cells and proliferation of human primary T cells (IC50=17 nM), also suppresses concanavalin A-induced cytokine production by rat splenocytes and monkey PBMCs with similar potency; potentially ameliorate T cell-mediated autoimmune diseases in vivo models.

GY05326

Roy-Bz

1246304-91-5

Roy-Bz is the first small-molecule PKCδ-selective activator with EC50 of 58.5 nM, binds to the PKCδ-C1-domain; displays no activity against human cPKCs (a mix of PKCα, β, and γ), nPKCδ, nPKCε and aPKCζ; potently inhibits the proliferation of colon cancer cells (HCT116 IC50=0.58 uM) by inducing a PKCδ-dependent mitochondrial apoptotic pathway involving caspase-3 activation; demonstrates PKCδ-dependent antitumor effect, through anti-proliferative, pro-apoptotic, and anti-angiogenic activities in xenograft mouse models with no apparent toxic side effects.

GY05265

BJE6-106

1564249-38-2

BJE6-106 (B106) is a potent, selective PKCδ inhibitor with IC50 of 50 nM, displays excellent selectivity over classical PKC isozymes (a 1,000-fold PKCδ selectivity over PKCα); induces cell growth inhibition in melanoma cell lines with NRAS mutations at nanomolar concentrations; induces phosphorylation (activation) of JNK1/2 (T183/Y185) most strongly after two hr of exposure in SBcl2 cells, induces phosphorylation of MKK4, JNK and H2AX in NRAS mutant melanoma WM1366 cells.

GY05202

PS-432

2083630-26-4

PS-432 is an allosteric inhibitor of PKCι and PKCζ with IC50 of 16.9 and 18.5 uM, respectively; has no inhibitory activity against PKCα, PKCβ, PKCδ and PKCθ nor the activity of related kinases such as PDK1, PKB/Akt, RSK1, MSK1 and Aurora A; inhibits the proliferation of the lung cancer cell lines A549 (IC50=14.8 ± 4.2 uM) and A427 (IC50=10.4± 0.3 uM) as well as androgen-independent prostate cancer cell line DU145 (IC50 = 20.8 ± 9.0 uM); well tolerated in vivo.

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