Signaling Pathway

PKC

PKC

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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 severalsignal 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.

PKC Inhibitors & Modulators (24)

Product Name Catalog No. Brief Description
(-)-Indolactam V

HY-12307

(-)-Indolactam V (ILV) is a protein kinase C activator, which strongly directs human ES cell-derived definitive endoderm into pancreatic endoderm.

Bisindolylmaleimide I

HY-13867

Bisindolylmaleimide I (GF109203X) is a highly selective, cell-permeable, and reversible protein kinase C (PKC) inhibitor with a Ki value of 14 nM.

CGP60474

HY-11009

CGP60474 is a promising inhibitor of PKC with a high degree of selectivity versus other serine/threonine and tyrosine kinases and show competitive kinetics relative to ATP.

Chelerythrine Chloride

HY-12048

Chelerythrine is potent, cell-permeable inhibitor of protein kinase C (IC50 = 660 nM); competitive with respect to the phosphate acceptor and non-competitive with respect to ATP.

Enzastaurin

HY-10342

Enzastaurin (LY317615) is a potent PKCβ selective inhibitor with IC50 of 6 nM, 6- to 20-fold selectivity against PKCα, PKCγ and PKCε.

Fasudil Hydrochloride

HY-10341

Fasudil Hcl(HA-1077; AT-877) is a potent inhibitor of ROCK-II, PKA, PKG, PKC, and MLCK with Ki of 0.33 μM, 1.6 μM, 1.6 μM, 3.3 μM and 36 μM, respectively.

Go 6983

HY-13689

Go 6983 is a pan-PKC inhibitor against for PKCα, PKCβ, PKCγ and PKCδ with IC50 of 7 nM, 7 nM, 6 nM and 10 nM, respectively; less potent to PKCζ and inactive to PKCμ.

Ingenol

HY-N0865

Ingenol is an extremely weak PKC (protein kinase C) activator; has been found to induce apoptosis and act as an anticancer agent.

Ingenol Mebutate

HY-B0719

Ingenol Mebutate (PEP 005) is a substance found in the sap of the plant Euphorbia peplus and an inducer of cell death.

NSC305787

HY-18931

NSC305787 is a small molecule inhibitor of PKC, with IC50 of 8.3 μM, 9.4 μM, 55 μM for PKCΙ phosphorylation of recombinant ezrin, of moesin, and of radixin.

NSC305787 hydrochloride

HY-18931A

NSC305787 hydrochloride is a small molecule inhibitor of PKC, with IC50 of 8.3 μM, 9.4 μM, 55 μM for PKCΙ phosphorylation of recombinant ezrin, of moesin, and of radixin.

Phorbol 12-myristate 13-acetate

HY-18739

Phorbol 12-myristate 13-acetate (PMA) is a PKC-activating phorbol ester, increases the intracellular Ca2+ concentration ([Ca2+]i) in a dose-dependent manner, with an EC50 of 11.7 nM.

PKC-IN-1

HY-16903

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

PKC412

HY-10230

PKC412(Midostaurin; CGP41231; CGP41251) is a broad spectrum protein kinase inhibitor; inhibits conventional PKC isoforms (α, β, γ), PDFRβ, VEGFR2, Syk, PKCη, Flk-1, Flt3, Cdk1/B, PKA, c-Kit, c-Fgr, c-Src, VEGFR1 and EGFR.

Quercetin

HY-18085

Quercetin is a flavonoid with anticancer activity; mitochondrial ATPase and phosphodiesterase inhibitor and Inhibits PI3-kinase activity and slightly inhibits PIP kinase activity.

Ro 31-8220

HY-13866A

Ro 31-8220(Bisindolylmaleimide IX) is a pan-PKC inhibitor with IC50 of 5 nM, 24 nM, 14 nM, 27 nM, and 24 nM for PKC-α, PKC-βI, PKC-βII, PKC-γ, and PKC-ε, respectively.

Ro 31-8220 mesylate

HY-13866

Ro 31-8220 mesylate (Bisindolylmaleimide IX) is a pan-PKC inhibitor with IC50 of 5 nM, 24 nM, 14 nM, 27 nM, and 24 nM for PKC-α, PKC-βI, PKC-βII, PKC-γ, and PKC-ε, respectively.

Ruboxistaurin hydrochloride

HY-10195B

Ruboxistaurin hydrochloride is a isozyme-selective inhibitor of protein kinase C (PKC), a competitive reversible inhibitors of PKCβI  and PKCβII with IC50 value of 4.7 nM and 5.9 nM respectivily.

Sotrastaurin

HY-10343

Sotrastaurin, a first-in-class protein kinase C (PKC) inhibitor, is aiming to become the first oral treatment that inhibits T-cell activation since the introduction of calcineurin inhibitors.

Staurosporine

HY-15141

Staurosporine is a prototypical potent ATP-competitive kinase inhibitor with IC50 of 0.7, 7, 8.5, 6, 20 nM for PKC, PKA,PKG, p60v-src tyrosine protein kinase, CaM kinase II, respectively.