N-Desmethyltamoxifen hydrochloride is the major metabolite of tamoxifen in humans. N-Desmethyltamoxifen, a poor antiestrogen, is a ten-fold more potent protein kinase C (PKC) inhibitor than Tamoxifen. N-Desmethyltamoxifen hydrochloride is also a potent re

PKCiota-IN-51 is a potent and selective inhibitor of Protein Kinase C iota (PKC-ι) with IC50 of 2.7 nM, >15-fold selectivity over PKC-α and PKC-β.

Delcasertib (KAI-9803) hydrochloride is a potent and selective δ-protein kinase C (δPKC) inhibitor. Delcasertib (KAI-9803) hydrochloride could ameliorate injury associated with ischemia and reperfusion in animal models of acute myocardial infarction (MI).

Ro 32-0432 hydrochloride is a potent, selective, ATP-competitive and orally active PKC inhibitor. The IC50 values of Ro 32-0432 hydrochloride for PKCα, PKCβI, PKCβII, PKCγ and PKCε are 9.3 nM, 28 nM, 30 nM, 36.5 nM and 108.3 nM, respectively. Ro 32-0432 hydrochloride is also a selective G protein-coupled receptor kinase 5 (GRK5) inhibitor. Ro 32-0432 hydrochloride prevents T-cell activation and has the potential for chronic inflammatory and autoimmune diseases research.

ζ-Stat trisodium (NSC37044 trisodium) is a specific and atypical PKC-ζ inhibitor, with an IC50 of 5 μM. ζ-Stat trisodium can reduce melanoma cell lines proliferation and induce apoptosis, and has antitumor activity in vitro.

PKC-iota inhibitor 1 (compound 19) is a protein kinase C-iota (PKC-ι ?) inhibitor with an IC50 value of 0.34 μM.

Ingenol 3,20-dibenzoate is a potent protein kinase C (PKC) isoform-selective agonist. Ingenol 3,20-dibenzoate induces selective translocation of nPKC-delta, -epsilon, and -theta and PKC-mu from the cytosolic fraction to the particulate fraction and induces morphologically typical apoptosis through de novo synthesis of macromolecules. Ingenol 3,20-dibenzoate increases the IFN-γ production and degranulation by NK cells, especially when NK cells are stimulated by NSCLC cells.

ZIP is a selective peptide inhibitor of PKMζ. ZIP injections can block the impairment in morphine conditioned place preference induced.

ZIP TFA is a selective peptide inhibitor of PKMζ. ZIP TFA injections can block the impairment in morphine conditioned place preference induced.

PKC β pseudosubstrate is a selective cell-permeable inhibitor of PKC.

PKC β pseudosubstrate TFA is a selective cell-permeable inhibitor of PKC.

[Ala113]MBP(104-118) is an noncompetitive peptide inhibitors of protein kinase C (PKC), with IC50s ranging from 28-62 μM.

[Ala107]MBP(104-118) is an noncompetitive peptide inhibitors of protein kinase C (PKC), with IC50s ranging from 46-145 μM.

[Ala107]MBP(104-118) TFA is an noncompetitive peptide inhibitors of protein kinase C (PKC), with IC50s ranging from 46-145 μM.

[Ala113]MBP(104-118) TFA is an noncompetitive peptide inhibitors of protein kinase C (PKC), with IC50s ranging from 28-62 μM.

Pep2m, myristoylated (Myr-Pep2m) is a cell-permeable peptide. Pep2m, myristoylated can disrupt the protein kinase ζ (PKMζ) downstream targets, N-ethylmaleimide-sensitive factor/glutamate receptor subunit 2 (NSF/GluR2) interactions.

Epsilon-V1-2 (ε-V1-2), a PKCε-derived peptide, is a selective PKCε inhibitor. Epsilon-V1-2 inhibits the translocationof PKCε, but not α-, β-, and δPKC.

HBDDE, a derivative of Ellagic acid, is an isoform-selective PKCα and PKCγ inhibitor with IC50s of 43 μM and 50 μM, respectively. HBDDE shows selective for PKCα/PKCγ over PKCδ, PKCβI and PKCβII isozymes. HBDDE induces neuronal apoptosis.

Ruboxistaurin (LY333531) is an orally active, selective PKCβ inhibitor (Ki=2 nM). Ruboxistaurin exhibits ATP dependent competitive inhibition of PKCβI with an IC50 of 4.7 nM. Ruboxistaurin inhibits PKCβII with an IC50 of 5.9 nM.

1-Stearoyl-2-arachidonoyl-sn-glycerol is a diacylglycerol (DAG) containing polyunsaturated fatty acids. 1-Stearoyl-2-arachidonoyl-sn-glycerol can activate PKC. 1-Stearoyl-2-arachidonoyl-sn-glycerol also can augment nonselective cation channel (NSCC) activity.

Leucosceptoside A is a phenylethanoid glycoside with anti-hyperglycemic and anti-hypertensive activities. Leucosceptoside A shows inhibitory activity against α-glucosidase and PKCα (IC50 of 19.0 μM).

CC-90005 is a potent, selective and orally active inhibitor of protein kinase C-θ (PKC-θ), with an IC50 of 8 nM. CC-90005 shows selectivity for PKC-θ over PKC-δ (IC50=4440 nM). CC-90005 can inhibit T cell activation by IL-2 expression.