pkcγ

PKC-IN-1 is an ATP-competitive and reversible conventional PKC enzymes inhibitor (PKCα, PKCβI, PKCβII, PKCθ, PKCγ, PKC mu and PKCε with IC50s of 2.3, 8.1, 7.6, 25.6, 57.5, 314, 808 nM, respectively).

Staurosporine (AM-2282) is a protein kinase inhibitor with ATP-competitive and non-selective inhibitory activity (IC50=6/15/2/3/3000 nM) against PKC, PKA, c-Fgr, phosphorylase kinase and TAOK2. Staurosporine also induces apoptosis.

Go 6983 is a PKC inhibitor with IC50 values of 7, 7, 6, 10, and 60 nM for PKCα, PKCβ, PKCγ, PKCδ, and PKCζ, respectively. Go 6983 has antitumor activity, cardiovascular protection, and protein kinase C inhibition.

Bisindolylmaleimide I (GF109203X) is a potent and highly selective protein kinase C (PKC) inhibitor, exhibiting a Ki of 14 nM.

HBDDE is a selective model inhibitor of the isoenzymes PKCα and PKCγ with IC 50 s of 43 μM and 50 μM, respectively.HBDDE has a higher affinity for PKCα/PKCγ than the PKCδ, PKCβI, and PKCβII isoenzymes.HBDDE is a derivative of ellagic acid, which induces apoptosis in neuronal cells. HBDDE is a derivative of ellagic acid and induces apoptosis in neuronal cells.

Bisindolylmaleimide VIII acetate (Ro 31-7549 acetate) is a potent and selective PKC inhibitor (IC50: 158 nM for rat brain PKC) with IC50 values of 53, 195, 163, 213, and 175 nM for PKC-α, PKC-βI, PKC-βII, PKC-γ, and PKC-ε, respectively.

A-443654, a pan-Akt inhibitor, exhibits equal potency against Akt1, Akt2, and Akt3 within cells (Ki=160 pM).

Rottlerin (NSC-56346) is a natural product purified from Mallotus Philippinensis and is a specific PKC inhibitor (IC50: PKCδ of 3-6 μM, PKCα,β,γ of 30-42 μM, PKCε,η,ζ of 80-100 μM). Rottlerin causes apoptosis via caspase 3 activation.

Midostaurin (PKC412) is a multi-targeted tyrosine kinase inhibitor with antitumor activity, exhibiting IC50 values ranging from 22 to 500 nM against PKCα/β/γ, Syk, Flk-1, Akt, PKA, c-Kit, c-Fgr, c-Src, FLT3, PDFRβ, and VEGFR1/2. Midostaurin is indicated for the treatment of acute myeloid leukemia (AML) and systemic mastocytosis (SM).

Ruboxistaurin hydrochloride (LY 333531 hydrochloride) is an Isozyme-selective inhibitor of protein kinase C (PKC); competitively and reversibly inhibits PKCβI and PKCβII (IC50 values are 4.7 and 5.9 nM respectively). Selective for PKCβ over other PKC isozymes (IC50values are 0.052, 0.25, 0.30, 0.36, 0.60 and >100 μM for PKCη, -δ, -γ, -α, -ε and -ζ respectively). Exhibits selectivity for PKC over other ATP-dependent kinases, including protein kinase A, casein kinase and src).

Enzastaurin (LY317615) (LY317615) is an effective PKCβ selective inhibitor (IC50: 6 nM), 6- to 20-fold selectivity against PKCα/γ/ε.

Ro 31-8220 Mesylate (Bisindolylmaleimide IX mesylate) is a pan-PKC inhibitor for PKC-α/βI/βII/γ/ε (IC50: 5/24/14/27/24 nM), and also shows potent inhibition against MSK1, MAPKAP-K1b, S6K1, and GSK3β.

PKC β pseudosubstrate acetate (PKC β pseudosubstrate acetate (172308-76-8 Free base)) is a cell-permeable, selective peptide inhibitor of PKC β. PKC β pseudosubstrate acetate can be used for in vivo and in vitro studies of the PKC β signaling pathway.

PKC ζ pseudosubstrate acetate is an inhibitor of protein kinase C (PKC) ζ; attached to cell permeabilisation Antennapedia domain vector peptide. Consists of amino acids 113 - 129 of PKC ζ pseudosubstrate domain linked by a disulphide bridge to the Antenna

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

PKCTheta-IN-2 (compound 14) is a potent and selective PKCθ inhibitor (IC50 = 0.25 nM) that suppresses IL-2 production in mice (IC50 = 682 nM).

PKC-IN-5 (Compound PKCe2054) is a protein kinase C (PKC) inhibitor that disrupts the interaction between PKCe and its anchoring protein RACK2.

PKC-IN-7 is an inhibitor of PKC and can be utilized in research related to diseases such as cancer.

PKC fragment (530-558) is a peptide fragment of protein kinase C (PKC) and is a potent PKC activator. Protein Kinase C (530-558) significantly inhibits osteoclastic bone resorption.

PKCε Inhibitor Peptide acetate is a selective PKCε inhibitor containing the site for its specific receptor for activated C kinase (RACK). PKCε Inhibitor Peptide acetate inhibits the translocation of PKCε, but not α-, β-, and δPKC.

PKC-theta inhibitor is PKC-θinhibitor, with an IC50 of 12 nM.

PKC-theta inhibitor hcl is a selective PKC-θinhibitor(IC50:12 nM).

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

Aurora A/PKC-IN-1 (Compound 2e) is a potent dual inhibitor of Aurora A (AurA) and PKC (α, β1, β2, θ), exhibiting inhibitory activity on AurA (IC50: 6.9 nM) and PKCα (IC50: 16.9 nM), and demonstrating anti-proliferative and anti-metastatic effects on breast cancer cells.