PKC

A PKMζ inhibitor

CRT 0066854 hydrochloride is a potent and selective atypical PKCs inhibitor.

A-3 hydrochloride is a potent, cell-permeable, reversible, ATP-competitive non-selective antagonist of various kinases.

O-Desmethyl Midostaurin (CGP62221; O-Desmethyl PKC412) is the active metabolite of Midostaurin via cytochrome P450 liver enzyme metabolism. O-Desmethyl Midostaurin can be used as an indicator for Midostaurin metabolism in vivo. Midostaurin is a multi-targeted protein kinase inhibitor?with?IC50?ranging from 22-500 nM.

Pep2m, myristoylated TFA (Myr-Pep2m TFA) is a cell-permeable peptide.

Ingenol 3,20-dibenzoate is a potent protein kinase C (PKC) isoform-selective agonist.

PKCβ inhibitor 1 is a potent, ATP-competitive, and selective PKCβ inhibitor with IC50s of 21 and 5 nM for human PKCβ1 and PKCβ2, respectively. PKCβ inhibitor 1 exhibits selectivity of more than 60-fold in favor of PKCβ2 relative to other PKC isozymes (PKCα, PKCγ, and PKCε).

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

CC-90005 is a potent, selective and orally active inhibitor of protein kinase C-θ (PKC-θ), with an IC50 of 8 nM.

Ruboxistaurin is an orally available inhibitor of protein kinase C (PKC), with IC 50 values of 0.36μM, 0.0047μM, and 0.0059μM for PKCα, βI, and βII, respectively.

Sangivamycin (NSC 65346), a nucleoside analog, is a potent inhibitor of protein kinase C (PKC) with an Ki of 10 μM. Sangivamycin has potent antiproliferative activity against a variety of human cancers.

Myelin Basic Protein (MHP4-14) TFA, a synthetic peptide comprising residues 4-14 of myelin basic protein, is a very selective PKC substrate (Km=7 μM).

Kobophenol A, an oligomeric stilbene, blocks the interaction between the ACE2 receptor and S1-RBD with an IC50 of 1.81 μM and inhibits SARS-CoV-2 viral infection in cells with an EC50 of 71.6 μM.

Aurothiomalate sodium is a potent and selective oncogenic PKCι signaling inhibitor.

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

Protein kinase inhibitor H-7 is a potent inhibitor of protein kinase C (PKC) and cyclic nucleotide dependent protein kinase, with a Ki of 6 μM for PKC.

Aprinocarsen (ISIS 3521) sodium is a specific antisense oligonucleotide inhibitor of protein kinase C-alpha (PKC-alpha). Aprinocarsen sodium is a 20-mer oligonucleotide that can regulate cell differentiation and proliferation. It can inhibit the growth of human tumor cell lines in nude mice. Aprinocarsen sodium has value as a chemotherapy compound for human cancer.

R 59-022 (DKGI-I) hydrochloride is a DGK inhibitor (IC50: 2.8 μM). R 59-022 hydrochloride inhibits OAG phosphorylation to OAPA. It is also a 5-HT receptor antagonist that can activate protein kinase C (PKC). R 59-022 enhances the production of thromboxane in platelets induced by thrombin and inhibits phosphatidic acid production in neutrophils.

Z-Arg-SBzl is a substrate for activating protein C in both cows and humans.

(S)-Ro 32-0432 is a potent, selective, ATP-competitive and orally active PKC inhibitor.

PKC-theta inhibitor 1 is the PKCθ inhibitor with an Ki value of 6 nM, inhibits IL-2 production in vivo with an IC50 of 0.19 μM.

Vanicoside A is a protein kinase C(PKC) inhibitor from Polygonum pensylvanicum.