pkcθ

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).

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

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

VTX-27 is a selective inhibitor of protein kinase C θ (PKC θ) (Kis: 0.08 nM and 16 nM for PKC θ and PKC δ).

AS2521780 is an inhibitor of PKCθ (IC50: 0.48 nM).

TCS 21311 (NIBR3049) is an effective and highly selective inhibitor of JAK3 (IC50: 8 nM). TCS 21311 inhibits PKCα, PKCθ, and GSK3β (IC50s: 13, 68, and 3 nM, respectively). It displays >100-fold selectivity over JAK1, JAK2, and TYK2.

(-)-Indolactam V, a potent PKC activator, exhibits binding affinities (Kis) of 3.36 nM and 1.03 μM for η-CRD2 and γ-CRD2, respectively, and dissociation constants (Kds) of 5.5 nM (η-C1B), 7.7 nM (ε-C1B), 8.3 nM (δ-C1B), 18.9 nM (β-C1A-long), 20.8 nM (α-C1A-long), 137 nM (β-C1B), 138 nM (γ-C1A), and 213 nM (γ-C1B), also demonstrating antitumor activity.

Sotrastaurin (AEB071) is a potent pan-PKC inhibitor with Kis of 0.95 nM for PKCα, 0.64 nM for PKCβI, 2.1 nM for PKCδ, 3.2 nM for PKCε, 1.8 nM for PKCη, and 0.22 nM for PKCθ.

GSK-690693 is a pan-Akt inhibitor targeting Akt1/2/3 with IC50 of 2 nM/13 nM/9 nM, also sensitive to the AGC kinase family: PKA, PrkX and PKC isozymes. Phase 1.

Myristoylated PKCθ pseudosubstrate peptide inhibitor is a synthetic peptide utilized to investigate the mechanism of action of protein kinase C theta (PKCθ) [1].

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-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-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.

PKC-9 is a PKC-zeta inhibitor 9.

PKC β pseudosubstrate TFA is a selective, cell-permeable inhibitor of PKC [1].

PKCδ Peptide Substrate is a highly specific substrate for the δ-type of Protein kinase C, composed of a sequence that mirrors murine eEF-1α (422-443) and includes Thr-431 [1].

PKCβII Peptide Inhibitor I, a specific PKCβII inhibitor, exhibits cardioprotective properties in a rat cardiac ischemia/reperfusion injury model and mitigates vascular endothelial dysfunction [1].