Protein Kinase C (PKC)

Cat. No.

A46167

CAS No.

145333-02-4

Bisindolylmaleimide XI hydrochloride

Synonyms: Ro 32-0432; Ro 31-8830 hydrochloride

Bisindolylmaleimide XI hydrochloride is a potent and selective inhibitor of protein kinase C (PKC) with IC50 values of 9 nM, 28 nM, 31 nM, 37 nM, and 108 nM for PKCα, PKCβI, PKCβII, PKCγ, and PKCε, respectively. This compound is orally active, making it a valuable tool for exploring the role of PKC in various cell signaling pathways. Its application spans cancer research, neurobiology, and cardiovascular studies, providing insights into PKC-mediated processes and potential therapeutic targets.

Cat. No.

A46169

CAS No.

90921-11-2

(Rac)-Anemonin

Synonyms: (Rac)-Pulsatilla camphor; (Rac)-Anemonine

(Rac)-Anemonin is a dual inhibitor targeting inducible nitric oxide synthase (iNOS) and protein kinase C theta (PKC-θ). It selectively inhibits iNOS while also reducing the stability of the PKC-θ protein, showcasing significant biological activity. Research indicates that (Rac)-Anemonin can alleviate symptoms in dextran sodium sulfate-induced acute ulcerative colitis in murine models, making it valuable for studying inflammation-related diseases.

Cat. No.

A46170

CAS No.

192050-59-2

Ruboxistaurin mesylate

Synonyms: LY333531 mesylate

Ruboxistaurin mesylate is a selective and ATP-competitive inhibitor of protein kinase C-beta (PKCβ) with IC50 values of 4.7 nM and 5.9 nM for the PKCβI and PKCβII isoforms, respectively. This compound shows potential in the study of several pathological conditions, including eye disorders, heart failure, and diabetes. Its specific inhibition of PKCβ can facilitate investigations into the underlying mechanisms of these diseases and the development of targeted therapeutic strategies.

Cat. No.

A46171

CAS No.

31750-48-8

N-Desmethyltamoxifen

N-Desmethyltamoxifen, a potent protein kinase C (PKC) inhibitor, is the primary metabolite of tamoxifen in humans. It demonstrates significantly enhanced PKC inhibitory activity, being ten-fold more potent than its precursor. Additionally, N-Desmethyltamoxifen effectively regulates ceramide metabolism in human acute myeloid leukemia (AML) cells, influencing ceramide glycosylation, hydrolysis, and sphingosine phosphorylation, making it a valuable tool for cancer research and therapeutic studies.

Cat. No.

A46172

CAS No.

2429946-75-6

SAMβA

SAMβA is a selective inhibitor targeting the interaction between mitofusin 1 and βIIPKC. This compound is conjugated to the cell-permeable peptide TAT47-57, facilitating its penetration into cells. SAMβA has demonstrated potential in enhancing heart failure outcomes in rat models, making it a valuable tool for investigating mitochondrial dynamics and associated pathophysiological processes in cardiac research.

Cat. No.

A46174

CAS No.

141774-20-1

NPC-15437 dihydrochloride

NPC-15437 dihydrochloride is a selective and reversible inhibitor of protein kinase C (PKC), demonstrating an IC50 value of 19 μM. This compound has been shown to impact the mechanisms associated with memory consolidation, making it a valuable tool for studying cognitive processes and neurobiology. Its penetrative properties enable effective investigation in various biological systems.

Cat. No.

A46177

CAS No.

1781828-85-0

(S)-Ro 32-0432

(S)-Ro 32-0432 is a selective, orally active inhibitor of protein kinase C (PKC), exhibiting ATP-competitive properties. Its IC50 values demonstrate high potency against various PKC isoforms, including PKCα (9.3 nM) and PKCβI (28 nM). Additionally, (S)-Ro 32-0432 acts as an inhibitor of G protein-coupled receptor kinase 5 (GRK5). This compound is valuable for investigating T-cell activation mechanisms and is relevant for research in chronic inflammatory and autoimmune diseases.

Cat. No.

A46179

CAS No.

152246-40-7

N-myristoyl-RKRTLRRL

N-myristoyl-RKRTLRRL is a potent inhibitor of Protein Kinase C (PKC), specifically targeting the binding of PKC substrates. This compound effectively inhibits calcium- and phosphatidylserine-dependent histone phosphorylation, demonstrating an IC50 of 5 µM. It serves as a valuable tool for research into PKC-related signaling pathways and the mechanisms of histone modification in various biological contexts.

Cat. No.

A46184

CAS No.

2636771-29-2

PKC-IN-4

PKC-IN-4 is a selective inhibitor of atypical protein kinase C (aPKC) with an IC50 of 0.52 µM. This compound effectively inhibits TNF-α-induced NF-κB signaling in vitro, making it a valuable tool for studies involving inflammatory responses. Additionally, PKC-IN-4 has been shown to block VEGF- and TNF-α-induced permeability across the retinal vasculature, highlighting its potential in retinal disease research and vascular permeability exploration.

Cat. No.

A46185

CAS No.

2230055-52-2

PKCiota-IN-2

PKCiota-IN-2 is a potent inhibitor of Protein Kinase C iota (PKC-ι), exhibiting an IC50 value of 2.8 nM. In addition to its primary target, PKCiota-IN-2 also demonstrates inhibitory activity against PKC-α and PKC-ε with IC50 values of 71 nM and 350 nM, respectively. This compound is valuable for research applications exploring the role of PKC isoforms in signal transduction, cancer, and other diseases.

Cat. No.

A46186

CAS No.

120925-60-2

NA 0345

NA 0345 is a potent protein kinase C (PKC) inhibitor, exhibiting IC50 values of 70 nM in the presence of 12-O-tetradecanoyl-13-acetate and 110 nM in its absence. This compound selectively inhibits PKC activity, effectively reducing the positive inotropic effects associated with α1-adrenergic receptors. NA 0345 is useful in research applications aimed at elucidating the role of PKC in cardiovascular function and signal transduction pathways.

Cat. No.

A46190

CAS No.

508-44-1

Anemonin

Synonyms: Pulsatilla camphor; Anemonine; trans-Anemonin

Anemonin is a dual inhibitor targeting inducible nitric oxide synthase (iNOS) and protein kinase C theta (PKC-θ). This compound significantly reduces the translation and enhances the protein stability of PKC-θ, demonstrating potent anti-inflammatory effects. Anemonin has been shown to alleviate symptoms of dextran sodium sulfate-induced acute ulcerative colitis in murine models, making it a valuable tool for researching inflammation-related diseases.

Cat. No.

A46193

CAS No.

151342-35-7

(S)-Ro 32-0432 free base

(S)-Ro 32-0432 free base is a selective and potent ATP-competitive inhibitor of Protein Kinase C (PKC), with IC50 values of 9.3 nM for PKCα, 28 nM for PKCβI, 30 nM for PKCβII, 36.5 nM for PKCγ, and 108.3 nM for PKCε. Additionally, it acts as a selective inhibitor of G protein-coupled receptor kinase 5 (GRK5). (S)-Ro 32-0432 free base effectively inhibits T-cell activation, making it a valuable tool for research into chronic inflammatory and autoimmune diseases.

Cat. No.

A46197

CAS No.

908012-19-1

PKCη pseudosubstrate inhibitor,myristoylated

PKCη pseudosubstrate inhibitor, myristoylated is a cell-permeable compound designed to inhibit protein kinase C eta (PKCη) activity by mimicking its substrate. This inhibitor allows for the exploration of PKCη’s role in various signaling pathways, facilitating studies on its biological functions in cell proliferation, differentiation, and apoptosis. Researchers can utilize this tool to investigate the therapeutic potential of modulating PKCη activity in various diseases.

Cat. No.

A46200

CAS No.

1221964-50-6

PS315

PS315 is an allosteric inhibitor of protein kinase C (PKC) that targets the PIF-pocket of atypical PKC isoforms. By inducing a displacement of the active site residue Lys111, PS315 effectively inhibits both full-length PKCζ (IC50 = 10 µM) and PKCη (IC50 = 30 µM). This compound has demonstrated anti-cancer properties, making it a valuable tool for research into PKC-related signaling pathways and cancer therapeutics.

Cat. No.

A46201

CAS No.

2948289-20-9

PKCTheta-IN-1

PKCTheta-IN-1 is a selective inhibitor of Protein Kinase C Theta (PKCθ), exhibiting an IC50 value of 0.1 nM. This compound disrupts PKCθ-mediated signaling pathways, contributing to its potential in immunological research and cellular proliferation studies. Its specificity makes it a valuable tool for investigating the role of PKCθ in T-cell activation and other related processes.

Cat. No.

A46203

CAS No.

611234-91-4

PKC-IN-7

PKC-IN-7 is a selective inhibitor of protein kinase C (PKC). This compound demonstrates significant anti-proliferative effects in various cancer cell lines and is valuable for investigating the role of PKC in cancer signaling pathways. It is suitable for research applications focused on tumor biology, cell signaling, and therapeutic development for PKC-related diseases.

Cat. No.

A46204

CAS No.

26486-92-0

6-Deoxyisojacareubin

6-Deoxyisojacareubin is a specific inhibitor of Protein Kinase C (PKC) that exhibits concentration-dependent inhibition of QGY-7703 cell proliferation. As a natural product derived from Garcinia nervosa, it serves as a valuable tool in cancer research to explore PKC-related signaling pathways and its effects on tumor cell growth. Its unique properties make it suitable for studies aiming to elucidate the role of PKC in various cancer types.

Cat. No.

A46205

CAS No.

99026-78-5

[Ala113]MBP(104-118)

[Ala113]MBP(104-118) is a noncompetitive inhibitor of protein kinase C (PKC), demonstrating IC50 values between 28-62 μM. This peptide is crucial for studying the regulatory mechanisms of PKC in various biological contexts. Its inhibition of PKC activity makes it a valuable tool for investigating signal transduction pathways and their implications in disease states. Researchers can utilize this reagent to explore PKC's role in cellular processes, contributing to the understanding of therapeutic targets in cancer and other diseases.

Cat. No.

A46207

CAS No.

120685-17-8

Staurosporine-Boc

Staurosporine-Boc is a potent non-selective inhibitor of protein kinases, derived from the actinobacterium Streptomyces staurosporeus. This compound effectively inhibits a wide range of protein kinases, including protein kinase C (PKC), as well as tyrosine and serine/threonine kinases. Due to its broad activity profile, Staurosporine-Boc is extensively utilized in biological research, particularly in studies examining cell signaling pathways and related mechanisms.

Cat. No.

A46210

CAS No.

309247-48-1

Protein Kinase C (19-35) Peptide

Protein Kinase C (19-35) Peptide serves as a pseudosubstrate inhibitor of Protein Kinase C (PKC). By potentially blocking the substrate-binding site within the kinase domain, this peptide renders the cytoplasmic form of PKC inactive. This inhibition is valuable for investigating PKC-related signaling pathways and understanding its role in various cellular processes. Its applications extend to research focused on cell proliferation, differentiation, and apoptosis associated with PKC activity.

Cat. No.

A46212

CAS No.

15854-12-3

aPKC-IN-1

aPKC-IN-1 is a selective inhibitor of atypical protein kinase C zeta (aPKCζ). This compound plays a crucial role in modulating cellular processes related to vascular permeability and inflammation. It is a valuable tool for investigating various disease mechanisms associated with these biological pathways, making it pertinent for research in areas such as cancer and autoimmune disorders.

Cat. No.

A46213

CAS No.

153997-72-9

ICP-103

ICP-103 is a highly selective protein kinase C (PKC) inhibitor with an IC50 of 30 nM. This compound has demonstrated potent inhibitory activity against PKC, making it a valuable tool for cancer research. ICP-103 can be utilized to explore the role of PKC in tumorigenesis and therapeutic resistance, contributing to a deeper understanding of potential cancer treatment strategies.

Cat. No.

A46214

CAS No.

1315378-67-6

pep2-EVKI

Synonyms: YNVYGIEEVKI

pep2-EVKI (YNVYGIEEVKI) is an inhibitor peptide that selectively targets and disrupts the interactions of Protein Interacting with C kinase 1 (PICK1). This compound is known to exert opposing effects on synaptic α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid receptor (AMPAR) function relative to PICK1 expression. It serves as a valuable tool for studying synaptic signaling pathways and understanding the role of PICK1 in synaptic plasticity and related neurobiological processes.

Cat. No.

A46217

CAS No.

125035-83-8

7-Oxostaurosporine

7-Oxostaurosporine is a selective inhibitor of protein kinase C (PKC), demonstrating significant efficacy in inhibiting tumor proliferation. This compound induces apoptosis in cancer cells and effectively disrupts the nuclear factor (NF)-κB/p-p65 signaling pathway, making it valuable for cancer research and therapeutic studies focused on PKC-related pathways. Its potent biological activity highlights its potential utility in understanding tumor biology and developing targeted cancer therapies.