PKC Inhibitor

CRT0066854 hydrochloride is a potent and selective atypical PKCs inhibitor. CRT0066854 is against full-length (FL) PKCι, PKCζ, and ROCK-II kinases with IC₅₀ values of 132 nM, 639 nM, and 620 nM, respectively.

PKCiota-IN-2 formic is a potent PKCiota (PKC-ι) inhibitor with an IC₅₀ of 2.8 nM. PKCiota-IN-2 formic also inhibits PKC-α and PKC-ε with IC₅₀s of 71 nM and 350 nM, respectively.

PKC/PKD-IN-1 (Compound 13C) is an orally active dual protein kinase C/D (PKC/PKD) inhibitor with an IC₅₀ value of 0.6 nM for PKD1. PKC/PKD-IN-1 can attenuate high-salt diet-induced cardiac hypertrophy and can be used in the study of heart failure.

7-Hydroxystaurosporine (UCN-01), a derivative of Staurosporine (HY-15141), is a selective protein kinase C (PKC) inhibitor with antitumor activity. 7-hydroxystaurosporine induces apoptosis and inhibits cell proliferation in colon carcinoma and leukemia cells, suppresses invasion and migration in glioblastoma cells. 7-Hydroxystaurosporine exhibits efficacy in breast cancer xenograft mouse models. 7-Hydroxystaurosporine can be used for colon carcinoma, breast cancer, glioblastoma and leukemia research.

SAMβA TFA is a rationally designed selective antagonist of Mfn1-βIIPKC association and can bind to TAT (HY-P0281). SAMβA TFA is a selective inhibitor of mitofusin 1-βIIPKC association improves heart failure outcome in rats.

ML192 is a selective ligand antagonist of GPR55. ML192 inhibits the β-arrestin trafficking, ERK1/2 phosphorylation and PKCβII translocation.

PKCTheta-IN-2 (compound 14) is a potent and selective PKCθ inhibitor with an IC₅₀ of 0.25 nM. PKCTheta-IN-2 shows good selectivity over a wide range of kinases, including the PKC subfamily (30 kinases). PKCTheta-IN-2 inhibits the IL-2 production in a mouse (IC₅₀ of 682 nM).

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.

Bisindolylmaleimide III is a protein kinase C (PKC) inhibitor with IC₅₀ values of 0.26, 5.7, and 6 μM against PKCα, PKCδ, and PKCμ, respectively. Bisindolylmaleimide III also exhibits inhibitory activity against other off-targets, with IC₅₀ values of 0.17, 1, and 2 μM against SLK, adenosine kinase (AK), and CDK2, respectively; its K_i for NQO2 is 16.5 μM. Bisindolylmaleimide III selectively binds to activated Rsk1 following EGF stimulation, and serves as a tool for detecting the activation status of intracellular Rsk1 and PKCα, as well as for functional analysis of SLK. Bisindolylmaleimide III can be used in studies of signal transduction and colorectal cancer.

H-8 dihydrochloride is a selective Cyclic nucleotide-dependent protein kinase inhibitor. H-8 dihydrochloride potently inhibits cGMP- and cAMP-dependent protein phosphorylation. H-8 dihydrochloride enhances the vasodilatory effect induced by 8-bromo-cAMP (HY-12306A). H-8 dihydrochloride fails to attenuate the vasodilatory effects induced by 8-bromo-cGMP (HY-101379A), atrial natriuretic peptide II, or Sodium nitroprusside (HY-B0564) in rat aorta.

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.

Cercosporamide is a highly potent, ATP-competitive PKC kinase inhibitor targeting to PKC1, with an IC₅₀ of <50 nM and a K_i of <7 nM. Cercosporamide is a unique Mnk inhibitor.

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.

Phellodendrine is an orally active plant alkaloid. Phellodendrine inhibits the proliferation of KRAS-mutated pancreatic cancer cells by suppressing macropinocytosis and glutamine metabolism, inducing ROS accumulation and mitochondrial apoptosis. Phellodendrine promotes autophagy by activating the AMPK/mTOR pathway, alleviating intestinal damage in ulcerative colitis. Phellodendrine can alleviate gouty arthritis by inhibiting the IL-6/STAT3 signaling pathway. Phellodendrine suppresses allergic reactions by altering the conformation of MRGPRB3/MRGPRX2 protein, thereby inhibiting the activation of PKC and subsequent downstream MAPK and NF-κB signaling. Phellodendrine inhibits the AKT/NF-κB pathway and down-regulates the expression of COX-2, thereby protecting zebrafish embryos from oxidative stress. Phellodendrine has an anti-major depressive disorder (MDD) effect by down-regulating CHRM1, HTR1A, and the PI3K/Akt signaling pathway.

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.

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.

Bisindolylmaleimide XI hydrochloride (Ro 32-0432) is a potent, selective and orally active PKC inhibitor with IC₅₀s of 9 nM, 28 nM, 31 nM, 37 nM, and 108 nM for PKCα, PKCβI, PKCβII, PKCγ, and PKCε, respectively.