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PKC Protein Kinase C

Cat.No.  Name Information
M5032 Zoledronic acid monohydrate Zoledronic acid monohydrate(CGP 42446; ZOL 446) is an activator of protein kinase C with apoptotic effects on multiple myeloma cell lines. It inhibited proliferation of human foetal osteoblastic cell line (hFOB) with an IC50 of 40 uM.
M4647 Phorbol 12-myristate 13-acetate Phorbol 12-myristate 13-acetate (PMA) is a dual SphK and protein kinase C (PKC) activator, increases the intracellular Ca2+ concentration ([Ca2+]i) in a dose-dependent manner, with an EC50 of 11.7 nM.
M3629 LY333531 hydrochloride LY333531 hydrochloride competitively and reversibly inhibits PKCβI and PKCβII (IC50 values are 4.7 and 5.9 nM respectively).
M2850 Midostaurin Midostaurin (pkc412) is a multi-targeted kinase inhibitor, including PKCα/β/γ, Syk, Flk-1, Akt, PKA, c-Kit, c-Fgr, c-Src, FLT3, PDFRβ and VEGFR1/2 with IC50 ranging from 80-500 nM.
M2790 K252a K252a is an inhibitor of the BDNF receptor TrkB. K-252a inhibits protein kinase with IC50 values of 470 nM, 140 nM, 270 nM, and 1.7 nM for PKC, PKA, Ca2+/calmodulin-dependent kinase type II, and phosphorylase kinase, respectively. K-252a is a potent inhibitor (IC50 of 3 nM) of the tyrosine protein kinase (TRK) activity of the NGF receptor gp140trk, the product of the trk protooncogene.
M2329 Zoledronic acid Zoledronic Acid (Zoledronate) is a third-generation bisphosphonate (BP), with potent anti-resorptive activity. Zoledronic Acid inhibits the differentiation and apoptosis of osteoclasts. Zoledronic Acid also has anti-cancer effects.
M2066 Staurosporine (AM-2282) Staurosporine (AM-2282) is a potent ATP-competitive kinase inhibitor with IC50 of 0.7, 7, 8.5, 6, 20 nM for PKC, PKA,PKG, p60v-src tyrosine protein kinase, CaM kinase II, respectively.
M31206 Bisindolylmaleimide VIII acetate Bisindolylmaleimide VIII acetate (Ro 31-7549 acetate) is a potent and selective protein kinase C (PKC) inhibitor with an IC50 of 158 nM for rat brain PKC. Bisindolylmaleimide VIII acetate has IC50s of 53, 195, 163, 213, and 175 nM for PKC-α, PKC-βI, PKC-βII, PKC-γ, PKC-ε, respectively.
M13861 Myelin Basic Protein TFA 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).
M13860 Darovasertib Darovasertib (LXS196) is a potent, selective and orally active protein kinase C (PKC) inhibitor, with IC50 values of 1.9 nM, 0.4 nM and 3.1 μM for PKCα, PKCθ and GSK3β, respectively.
M13859 Epsilon-V1-2 Epsilon-V1-2 (ε-V1-2), a PKCε-derived peptide, is a selective PKCε inhibitor. Epsilon-V1-2 inhibits the translocationof PKCε, but not α-, β-, and δPKC.
M10995 Daphnoretin Daphnoretin (Dephnoretin) is extracted from Wikstroemia indica and has antiviral activity. Daphnoretin acts similarly to PMA in that it can directly activate protein kinase C, thereby activating NADPH oxidase.
M10805 Cercosporin Cercosporin is produced by the plant pathogenSporakikuchii and elsinochromes, pigments of the elsinoe family of fungi. Cercosporin is an effective photosensitizer with a short activation wavelength that is primarily suitable for surface PDT photodynamic studies (especially for the avoidance of perforation studies). Cercosporin contains the perylenequinone structural features necessary to PKC activity with an IC50 of 0.6-1.3 μM.
M10770 Ruboxistaurin Ruboxistaurin (LY333531) is an orally active, selective PKC beta inhibitor (Ki=2 nM), ruboxistaurin exhibits ATP-dependent competitive inhibition of PKC beta I, which IC50 4.7 nM. Ruboxistaurin for PKC beta II IC50 5.9 nM.
M10490 Delcasertib Delcasertib (KAI-9803) is a potent and selective δ-protein kinase C (δPKC) inhibitor, it could ameliorate injury associated with ischemia and reperfusion in animal models of acute myocardial infarction (MI).
M9547 VTX-27 VTX-27 is a novel potent and selective PKCθ inhibitor, with Kis of 0.08 nM and 16 nM for PKC θ and PKC δ.
M9484 PKCβ inhibitor PKCβ inhibitor is a potent and selective inhibitor of PKCβ isozymes (IC50 = 5 nM and 21 nM for human PKCβII and βI).
M8141 Rottlerin Recently, Rottlerin (mallotoxin) has been shown to be a potent activator of the large conductance voltage and Ca2 activated K+ channel and to potently leftward shift the conductance-voltage relationship of the channel.
M7837 Hispidin Potent inhibitor of protein kinase Cβ, cytotoxic for cancer cells.
M7647 Bryostatin 1 Bryostatin 1 is a natural macrolide isolated from the moss bug Bugula neritina and a potent PKC modulator of central nervous system (CNS) permeability.Bryostatin 1 binds to the isolated Munc13-1 C1 domain and the full-length Munc13-1 protein with a Ki value of 8.07 and 0.45 nM, respectively, and has anticancer, anti-inflammatory and neuroprotective activities. Bryostatin 1 binds to the isolated C1 domain of Munc13-1 and the full-length Munc13-1 protein with Ki values of 8.07 nM and 0.45 nM, respectively, and exhibits anticancer, anti-inflammatory, and neuroprotective activities.

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