Protein Kinase C (PKC)

Protein kinase C (PKC) inhibitors and activators act on a family of lipid-regulated serine/threonine kinases. Conventional PKC isoforms require calcium and diacylglycerol, novel isoforms need only diacylglycerol, and atypical isoforms respond to neither. Tumor-promoting phorbol esters mimic diacylglycerol and were shown in 1982 to activate PKC directly. 12-O-tetradecanoyl phorbol-13-acetate (TPA) is the standard activator of this kind, and ingenol mebutate also activates several isoforms. Staurosporine was first described as a PKC inhibitor but blocks a wide range of protein kinases. Enzastaurin is selective for PKCβ, while GO6983 and Ro 31-8220 mesylate inhibit multiple conventional and novel isoforms.

Items 1-25 of 124

  • Staurosporine
    Cat. No.
    A10864

    Staurosporine

    Synonyms: AM-2282; STS

    Staurosporine is a natural product originally isolated in 1977 from the bacterium Streptomyces staurosporeus. The main biological activity of staurosporine is the inhibition of protein kinases through the prevention of ATP binding to the kinase. This is achieved through the stronger affinity of staurosporine to the ATP-binding site on the kinase.

    1 mg
    $50.00
    2 mg
    $70.00
    All 9 sizes
  • Chelerythrine Chloride
    Cat. No.
    A10196

    Chelerythrine Chloride

    Chelerythrine affects translocation of PKC from cytosol to plasma membrane. Shown to prevent neurite growth. Induces apoptosis in a concentration- and schedule-dependent manner.

    5 mg
    $55.00
    10 mg
    $85.00
    All 6 sizes
  • Enzastaurin
    Cat. No.
    A10356

    Enzastaurin (LY317615)

    Synonyms: LY317615

    LY317615 (Enzastaurin) is a potent and selective inhibitor of PKCβ with antiproliferative activity (IC50= ~6 nM).

    5 mg
    $30.00
    10 mg
    $40.00
    All 7 sizes
  • Quercetin
    Cat. No.
    A10766

    Quercetin (Sophoretin)

    Synonyms: Sophoretin; Meletin; Quercetine

    Quercetin inhibits many enzyme systems including tyrosine protein kinase, phospholipase A2, phosphodiesterases, mitochondrial ATPase, PI 3-kinase and protein kinase C.

    500 mg
    $35.00
    1 g
    $45.00
    All 4 sizes
  • Verbascoside
    Cat. No.
    A12014

    Verbascoside

    Synonyms: Acetoside; Kusaginin

    Verbascoside is isolated from Lantana camara, acts as an ATP-competitive inhibitor of PKC, with an IC50 of 25 μM, and has antitumor, anti-inflammatory and antineuropathic pain activity.

    5 mg
    $45.00
    10 mg
    $75.00
    All 6 sizes
  • Ro 31-8220 mesylate
    Cat. No.
    A13514

    Ro 31-8220 mesylate

    Synonyms: BIM IX; Bisindolylmaleimide IX (mesylate)

    Ro 31-8220 mesylate is a PKC-inhibitor, which inhibits stimulated fluid pinocytosis of human PMNs induced by the PKC-activators phorbol myristate acetate (PMA, IC50 = 1.35 x 10(-6) M) or diacylglycerols (OAG, diC8) by 95%.

    1 mg
    $35.00
    2 mg
    $55.00
    All 8 sizes
  • GO6983
    Cat. No.
    A13790

    GO6983

    GO6983 is a potent protein kinase C (PKC) inhibitor. It reduces polymorphonuclear leukocyte adherence and infiltration following myocardial ischemia/reperfusion injury.

    1 mg
    $30.00
    2 mg
    $45.00
    All 8 sizes
  • Bryostatin 1
    Cat. No.
    A10261

    Bryostatin 1

    Synonyms: NSC 339555

    Bryostatin 1 is a macrolactone isolated from the marine bryozoan, Bugula neritina, that modulates protein kinase C (PKC) activity. Bryostain 1 induces an initial rapid activation and autophosphorylation of PKC that results in the translocation of the PKC enzyme to the membrane.

    Out of stock

    All 1 sizes
  • Daphnetin
    Cat. No.
    A10286

    Daphnetin

    Synonyms: 7,8-dihydroxycoumarin

    Daphnetin is a coumarin analog that acts as an inhibitor of several protein kinases. It inhibits EGFR kinase (IC50 = 7.67 μM), PKA (IC50 = 9.33 μM), and PKC (IC50 = 25 μM), in vitro. The inhibition of EGFR kinase by daphnetin was competitive to ATP and non-competitive to the peptide substrate. Also acts as a potent antioxidant and anti-malarial agent.

    5 mg
    $30.00
    10 mg
    $35.00
    All 6 sizes
  • 7-Hydroxystaurosporine
    Cat. No.
    A11275

    7-Hydroxystaurosporine

    Synonyms: UCN-01; KRX-0601

    7-Hydroxystaurosporine is a selective protein kinase C (PKC) inhibitor known for its significant antitumor activity. This compound induces apoptosis and inhibits cell proliferation in colon carcinoma and leukemia cells, while also suppressing invasion and migration in glioblastoma cells. Additionally, 7-hydroxystaurosporine demonstrates efficacy in breast cancer xenograft mouse models, making it a valuable tool for research into colon carcinoma, breast cancer, glioblastoma, and leukemia.

    1 mg
    $560.00
    5 mg
    $1,780.00
    All 2 sizes
  • Sotrastaurin
    Cat. No.
    A11554

    Sotrastaurin (AEB071)

    Synonyms: AEB 071

    Sotrastaurin is a protein kinase C inhibitor for the prevention of transplant rejection and treatment of psoriasis.

    1 mg
    $40.00
    5 mg
    $90.00
    All 8 sizes
  • Ruboxistaurin
    Cat. No.
    A12399

    Ruboxistaurin (LY333531)

    Synonyms: LY 333531

    Ruboxistaurin (LY333531) is a potent, selective inhibitor of Protein Kinase C isozymes, PKC β I(IC50=4.7 nM) and PKC β II (IC50=5.9 nM).

    5 mg
    $95.00
    10 mg
    $170.00
    All 5 sizes
  • Go 6976
    Cat. No.
    A12419

    Go 6976

    Go6976 is a potent PKC inhibitor with IC50 of 7.9 nM, 2.3 nM, and 6.2 nM for PKC (Rat brain), PKCα, and PKCβ1, respectively. Also a potent inhibitor of JAK2 and Flt3.

    1 mg
    $70.00
    5 mg
    $175.00
    All 7 sizes
  • Midostaurin
    Cat. No.
    A12650

    Midostaurin (PKC 412)

    Synonyms: CGP 41251; PKC412

    PKC 412 is a broad spectrum protein kinase inhibitor. Inhibits conventional PKC isoforms α/β/γ, PDFRβ, VEGFR2, Syk, Flk-1, Flt3, Cdk1/B, PKA, c-Kit, c-Fgr, c-Src, VEGFR1 and EGFR. Displays potent antitumor activity.

    1 mg
    $40.00
    5 mg
    $75.00
    All 8 sizes
  • Delcasertib
    Cat. No.
    A12829

    Delcasertib

    Synonyms: KAI-9803; BMS-875944

    Delcasertib (KAI-9803) is a potent and selective δ-protein kinase C (δPKC) inhibitor.

    1 mg
    $205.00
    5 mg
    $490.00
    All 7 sizes
  • GF 109203X
    Cat. No.
    A13197

    GF 109203X

    Synonyms: GO6850; Bisindolylmaleimide I

    GF 109203X is a potent and selective inhibitor of protein kinase C, selective for the α and β1 isoforms (IC50 values are 0.0084, 0.0180, 0.210, 0.132, and 5.8 μM for α, β1, δ, ε and ζ isoforms respectively). Selective over MLCK, PKG and PKA (IC50 values are 0.6, 4.6, and 33 μM respectively). Potent antagonist at the 5-HT3 receptor (Ki = 29.5 nM).

    5 mg
    $55.00
    10 mg
    $95.00
    All 6 sizes
  • PKC (19-36)
    Cat. No.
    A14871

    PKC (19-36)

    PKC (19-36), pseudosubstrate peptide inhibitor of protein kinase C (IC50 = 0.18 uM).

    1 mg
    $75.00
    5 mg
    $215.00
    All 5 sizes
  • TAS 301
    Cat. No.
    A15557

    TAS 301

    TAS 301 is an inhibitor of smooth muscle cell migration and proliferation.

    5 mg
    $35.00
    10 mg
    $60.00
    All 6 sizes
  • PKC-IN-1
    Cat. No.
    A16212

    PKC-IN-1

    PKC-IN-1 is a poent PKC beta II inhibitor with Ki of 14.9 nM; compound example H6 from patent WO 2008096260 A1.

    2 mg
    $190.00
    5 mg
    $315.00
    All 7 sizes
  • NSC305787
    Cat. No.
    A16213

    NSC305787

    NSC305787 is a small molecule inhibitor of PKC, with IC50 of 8.3 uM, 9.4 uM, 55 uM for PKC phosphorylation of recombinant ezrin, of moesin, and of radixin.

    5 mg
    $315.00
    10 mg
    $475.00
    All 5 sizes
  • Ruboxistaurin (LY333531 HCl)
    Cat. No.
    A16604

    Ruboxistaurin (LY333531 HCl)

    Synonyms: LY-333531

    LY333531 is a β-specific protein kinase C inhibitor. It competitively and reversibly inhibits PKCβ1 and PKCβ2 with IC50 values of 4.7 and 5.9 nM respectively.

    1 mg
    $60.00
    2 mg
    $85.00
    All 9 sizes
  • HA-100 (C1)
    Cat. No.
    A17019

    HA-100 (C1)

    Synonyms: HA100

    HA-100 is an isoquinoline compound with an added piperazinylsulfonyl group that acts as an inhibitor of protein kinases (PKs), including PKA, PKC, and PKG (IC50 = 8, 12, and 4 μM, respectively).

    5 mg
    $50.00
    10 mg
    $90.00
    All 6 sizes
  • BJE6-106
    Cat. No.
    A18627

    BJE6-106

    Synonyms: B-106

    BJE6-106 (B106) is a potent, selective 3rd generation PKCδ inhibitor with an IC50 of 0.05 μM and targets selectivity over classical PKC isozyme PKCα (IC50=50 μM).

    5 mg
    $310.00
    10 mg
    $495.00
    All 6 sizes
  • PKC-theta inhibitor 1
    Cat. No.
    A18966

    PKC-theta inhibitor 1

    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.

    1 mg
    $310.00
    5 mg
    $945.00
    All 6 sizes

Items 1-25 of 124

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