PKC Inhibitor

Protein Kinase C (19-31), a peptide inhibitor of protein kinase C (PKC), derived from the pseudo-substrate regulatory domain of PKCa (residues 19-31), is used as protein kinase C substrate peptide for testing the protein kinase C activity.

PRKCA Human Pre-designed siRNA Set A contains three designed siRNAs for PRKCA gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.

N-Desmethyltamoxifen 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 is also a potent regulator of ceramide metabolism in human AML cells, limiting ceramide glycosylation, hydrolysis, and sphingosine phosphorylation.

Sphingosine (d14:1) (Tetradecasphing-4-enine), a sphingolipid, is a potent Protein kinase C (PKC) inhibitor. Sphingosine (d14:1) prevents its interaction with sn-1,2-diacylglycerol (DAG)/Phorbol esters.

TAS-301 is an inhibitor of smooth muscle cell migration and proliferation, and inhibits PKC activation induced by PDGF.

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

Vanicoside A is a phenylpropanoid glycoside. Vanicoside A can be isolated from Polygonum pensylvanicum. Vanicoside A inhibits protein kinase C (PKC), induces substantial ROS production. Vanicoside A exhibits anticancer activity against melanoma.

O-Desmethyl Midostaurin (CGP62221; O-Desmethyl PKC412) is the active metabolite of Midostaurin (HY-10230) 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.

Hypericin (Standard) is the analytical standard of Hypericin. This product is intended for research and analytical applications. Hypericin is a naturally occurring substance found in Hyperlcurn perforatum L. Hypericin is an inhibitor of PKC (protein kinase C), MAO (monoaminoxidase), dopamine-beta-hydroxylase, reverse transcriptase, telomerase and CYP (cytochrome P450). Hypericin shows antitumor, antiviral, antidepressive activities, and can induce apoptosis.

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. Kobophenol A inhibits the activity of partially purified rat brain protein kinase C (PKC) with an IC₅₀ of 52 µM.

Verbascoside (Standard) is the analytical standard of Verbascoside. This product is intended for research and analytical applications. Verbascoside is isolated from Acanthus mollis, acts as an ATP-competitive inhibitor of PKC, with an IC₅₀ of 25 μM, and has antitumor, anti-inflammatory and antineuropathic pain activity.

UCN-02 (7-epi-Hydroxystaurosporine) is a selective protein kinase C (PKC) inhibitor with a PKC IC₅₀ value of 62 nM and a PKA IC₅₀ value of 0.25 μM. UCN-02 can be produced by Streptomyces strain N-126. UCN-02 can be used for the research of breast carcinoma.

(Rac)-Anemonin ((Rac)-Pulsatilla camphor; (Rac)-Anemonine) is an isomer of Anemonin. Anemonin is a naturally occurring bislactone small molecule derived from Ranunculaceae with blood-brain barrier permeability, possessing a variety of activities including anti-inflammatory, antioxidant, neuroprotective, melanogenesis-inhibiting, and antiparasitic effects. Anemonin inhibits iNOS to reduce NO release; it inhibits PKC-θ protein expression and downregulates the pro-inflammatory factors TNF-α, IL-1β, and IL-6; it enhances the activities of the antioxidant enzymes SOD, CAT, and GSH-Px, and reduces MDA and ROS levels. Anemonin modulates the Bcl-2 / Bax / caspase-3 pathway to inhibit apoptosis; it downregulates melanogenesis-related molecules including MITF, TYR, TRP1, and TRP2, thereby inhibiting melanin synthesis in human melanocytes. Anemonin inhibits Leishmania and Schistosoma mansoni. Anemonin is used in research related to diseases such as hyperpigmentation, cerebral ischemia/reperfusion injury, inflammation, sepsis-induced acute lung injury, acute ulcerative colitis, leishmaniasis, and schistosomiasis.

PRKCG Human Pre-designed siRNA Set A contains three designed siRNAs for PRKCG gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.

Protein kinase inhibitor 9 (Compound example 175) is an inhibitor of serine/threonine and tyrosine kinase activity. Protein kinase inhibitor 9 can be used for the research of cancer, hyper proliferative disorders, rheumatoid arthritis, disorders of the immune system, transplant rejections and imflammatory disorders.

Midostaurin-d₅ (PKC412-d₅) is a deuterium labeled Midostaurin. Midostaurin is a multi-targeted protein kinase inhibitor which inhibits PKCα/β/γ, Syk, Flk-1, Akt, PKA, c-Kit, c-Fgr, c-Src, FLT3, PDFRβ and VEGFR1/2 with IC₅₀s ranging from 22-500 nM.

D-erythro-Sphingosine (Standard) is the analytical standard of D-erythro-Sphingosine. This product is intended for research and analytical applications. D-erythro-Sphingosine (Erythrosphingosine) is a very potent activator of p32-kinase with an EC50 of 8 μM, and inhibits protein kinase C (PKC). D-erythro-Sphingosine (Erythrosphingosine) is also a PP2A activator[1][2][3][4].

Fasudil (HA-1077; AT877) dihydrochloride is a nonspecific RhoA/ROCK inhibitor and also has inhibitory effect on protein kinases, with an K_i of 0.33 μM for ROCK1, IC₅₀s of 0.158 μM and 4.58 μM, 12.30 μM, 1.650 μM for ROCK2 and PKA, PKC, PKG, respectively. Fasudil dihydrochloride is also a potent Ca²⁺ channel antagonist and vasodilator.

A-3 hydrochloride is a potent, cell-permeable, reversible, ATP-competitive non-selective antagonist of various kinases. It against PKA (K_i=4.3 µM), casein kinase II (K_i=5.1 µM) and myosin light chain kinase (MLCK) (K_i=7.4 µM). A-3 hydrochloride also inhibits PKC and casein kinase I with K_i values of 47 µM and 80 µM, respectively.

PKCθ pseudosubstrate peptide inhibitor, myristoylated TFA is a synthetic peptide that can be used to study the mechanism of action of PKCθ.