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 selective cell-permeable inhibitor of PKC.

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-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 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].

PKCε (85-92) (ψεRACK) is a peptide and selective PKCε activator that does not affect the activity of other PKC isozymes.PKCε (85-92) induces a pro-angiogenic response in endothelial cells, promotes FGF-2 cytosolization, and regulates VEGF activity.

PKC(85-92),Myristoylated is a myristic acid-conjugated, cell-permeable peptide activator of PKC that has been shown to increase nitric oxide (NO) release in cultured human umbilical vein endothelial cells (HUVECs) [1].

PKCα (C2-4) inhibitor peptide is a specific antagonist to PKCα, preventing the α1A-adrenoreceptor agonist A-61603 [1] from inhibiting I_Kr.

Myristoylated PKCη pseudosubstrate inhibitor is a cell-permeable compound utilized to investigate the mechanism of action of PKCη [1].