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Chromatin/Epigenetic Filter
Chromatin/EpigeneticPKC
Protein kinase C, commonly abbreviated to PKC, is a family of protein kinase enzymes that are involved in controlling the function of other proteins through the phosphorylation of hydroxyl groups of serine and threonine amino acid residues on these proteins, or a member of this family. PKC enzymes in turn are activated by signals such as increases in the concentration of diacylglycerol (DAG) or calcium ions (Ca2+). Hence PKC enzymes play important roles in several signal transduction cascades.
20-HETE
Cited
T1402179551-86-3In house
20-HETE promotes cell proliferation and migration in cancer and can be used to study prostate tumors and cardiac hypertrophy by activating the protein kinase C pathway to increase FBXO10 expression.20-HETE promotes cell proliferation and migration in cancer and can be used to study prostate tumors and cardiac hypertrophy by activating the protein kinase C pathway.
- 473 €
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CitedPhorbol 12-myristate 13-acetate Cited
TQ019816561-29-8
Phorbol 12-myristate 13-acetate (PMA), a member of the phorbol ester group of natural products, activates PKC, SphK, and NF-κB, and induces THP1 cell differentiation.
- 41 €
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CitedStaurosporine Cited
T668062996-74-1
Staurosporine (AM-2282) is a protein kinase inhibitor with ATP-competitive and non-selective inhibitory activity (IC50=6 15 2 3 3000 nM) against PKC, PKA, c-Fgr, phosphorylase kinase and TAOK2. Staurosporine also induces apoptosis.
- 53 €
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CitedGardenin A
TN411421187-73-5
Gardenin A shows neurotrophic effects via activating MAPK ERK, PKC, and PKA. Gardenin A exhibits antidepressant, anticonvulsant and anxiolytic effects.
- 187 €
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Hypericin
T6S0923548-04-9
Hypericin (Cyclosan) is a natural anthraquinone compound, an extract of Hypericum perforatum, which inhibits PKC, MAO, dopamine-beta-hydroxylase, reverse transcriptase, telomerase, and CYP, etc. Hypericin exhibits antimicrobial, antiviral, antitumor, and antidepressant activities.
- 49 €
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DCPLA-ME
T1098056687-67-3In house
DCPLA-ME (2-[(2-Pentylcyclopropyl)methyl]cyclopropaneoctanoic acid methyl ester) is the methyl ester form of DCPLA and can be used to treat neurodegenerative diseases. It is an effective PKCε activator.
- 75 €
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Midostaurin
T3211120685-11-2
PKC412(Midostaurin (PKC412); CGP41231; CGP41251) is a broad spectrum protein kinase inhibitor. Midostaurin inhibits protein kinase C alpha (PKCalpha), vascular endothelial growth factor receptor 2 (VEGFR2), c-kit, platelet-derived growth factor receptor (PDGFR) and FMS-like tyrosine kinase 3 (FLT3) tyrosine kinases, which may result in disruption of the cell cycle, inhibition of proliferation, apoptosis, and inhibition of angiogenesis in susceptible tumors.
- 44 €
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Hypocrellin A
T577177029-83-5
Hypocrellin A is a natural PKC inhibitor with light-induced antitumor, antifungal and antiviral activities and also exerts immunomodulatory effects on MHC-restricted antigen presentation.
- 44 €
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Ingenol mebutate
TN104775567-37-2
Ingenol mebutate (Ingenol 3-Angelate) is a potent activator of PKC subtypes including PKC-α, PKC-β, PKC-γ, PKC-δ, and PKC-ε with Kis of 0.3, 0.105, 0.162, 0.376, and 0.171 nM. Ingenol mebutate exhibits antiinflammatory and antitumor activity.
- 60 €
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Ro-3306 Cited
T2356872573-93-8
RO-3306 is a selectivity ATP-competitive CDK1 inhibitor (Ki: 20 nM). The selectivity of RO-3306 for CDK1 is >15-fold higher than a diverse panel of human kinases.
- 30 €
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CitedSangivamycin
T960518417-89-5
Sangivamycin (NSC-65346) is an effective inhibitor of protein kinase C (PKC, Ki = 10 μM). Sangivamycin exhibits antiproliferative activity against a variety of human cancers.
- 121 €
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Piceatannol Cited
T061010083-24-6
Piceatannol (Astringenin) is an anti-inflammatory, immunomodulatory and antiproliferative agent. It inhibits p56lck and syk protein tyrosine kinases and inhibits NF-κB activation and gene expression of TNF-induced. It is synthetic from the conversion of resveratrol by cytochrome P450 1B1.
- 37 €
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CitedSotrastaurin
T6278425637-18-9
Sotrastaurin (AEB071) is a potent pan-PKC inhibitor with Kis of 0.95 nM for PKCα, 0.64 nM for PKCβI, 2.1 nM for PKCδ, 3.2 nM for PKCε, 1.8 nM for PKCη, and 0.22 nM for PKCθ.
- 42 €
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Hispidin
T7792555-55-5
Hispidin is a polyphenol originally, including antioxidant, anti-inflammatory, and cytoprotective properties
- 76 €
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TPPB Cited
T17148497259-23-1
TPPB is a kinase C activator of cell-permeable benzolactam-derived protein (Ki: 11.9 nM).
- 154 €
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CitedPhorbol 12,13-dibutyrate
T1652637558-16-0In house
Phorbol 12,13-dibutyrate (Phorbol dibutyrate) is a PKC activator that inhibits α1-adrenoceptor-mediated positive inotropic effects in a concentration-dependent manner, induced by contraction of isolated rabbit vascular smooth muscle.
- 53 €
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HA-1004
T2752591742-10-8In house
HA-1004 is a inhibitor of PKG, PKA, PKC and MLC.
- 185 €
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Go 6983 Cited
T6313133053-19-7
Go 6983, a pan-PKC inhibitor, targets PKCα, PKCβ, PKCγ, PKCδ, and PKCζ, with IC50 values of 7 nM, 7 nM, 6 nM, 10 nM, and 60 nM, respectively.
- 34 €
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CitedDelcasertib
T11740949100-39-4
Delcasertib (KAI-9803) is a potent and selective inhibitor of δ-protein kinase C (δPKC).
- 202 €
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Bisindolylmaleimide VIII
T71125125313-65-7In house
Bisindolylmaleimide VIII (Ro-31-7549) is a selective and potent protein kinase C (PKC) inhibitor with good inhibition of PKC-α, PKC-β I, PKC-β II, PKC-γ, and PKC-ε.Bisindolylmaleimide VIII Bisindolylmaleimide VIII inhibits T cell-mediated autoimmune diseases and enhances Fas-mediated apoptosis through a protein kinase C-independent mechanism.
- 278 €
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HBDDE
T39030154675-18-0In house
HBDDE is a selective model inhibitor of the isoenzymes PKCα and PKCγ with IC 50 s of 43 μM and 50 μM, respectively.HBDDE has a higher affinity for PKCα PKCγ than the PKCδ, PKCβI, and PKCβII isoenzymes.HBDDE is a derivative of ellagic acid, which induces apoptosis in neuronal cells. HBDDE is a derivative of ellagic acid and induces apoptosis in neuronal cells.
- 282 €
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Clitorin
TN151355804-74-5
Clitorin has free radical scavenging property. It shows significant interactions with CD38, it may have anti-hyperglycemic potential.
- 79 €
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Mitoxantrone Cited
T658865271-80-9
Mitoxantrone (mitozantrone) is an anthracenedione antibiotic with antineoplastic activity. Mitoxantrone intercalates into and crosslinks DNA, thereby disrupting DNA and RNA replication. This agent also binds to topoisomerase II, resulting in DNA strand breaks and inhibition of DNA repair. Mitoxantrone is less cardiotoxic compared to doxorubicin.
- 31 €
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CitedDaphnetin
T2851486-35-1
Daphnetin (7,8-Dihydroxycoumarin), a natural coumarin derivative, is a protein kinase inhibitor with inhibitory for EGFR (IC50: 7.67 μM), PKA (IC50: 9.33 μM), and PKC (IC50: 25.01 μM), also exhibit anti-oxidant and anti-inflammatory activities.
- 40 €
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Go6976
T6515136194-77-9
Go6976 is a small molecule inhibitor of protein kinase C (PKC). Go6976 has been widely used in biomedical research as a tool to study the role of PKC in various physiological and pathophysiological processes.
- 74 €
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Bisindolylmaleimide I Cited
T6513133052-90-1
Bisindolylmaleimide I (GF109203X) is a potent and highly selective protein kinase C (PKC) inhibitor, exhibiting a Ki of 14 nM.
- 57 €
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CitedVerbascoside Cited
T337561276-17-3
Verbascoside (Kusaginin) is a protein kinase C inhibitor with antimicrobial, anti-inflammatory activities.
- 55 €
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CitedValrubicin
T760456124-62-0
Valrubicin (AD-32) (AD 32) inhibits TPA- and PDBu-induced PKC activation (IC50s: 0.85 and 1.25 μM) and has antitumor and anti-inflammatory activity.
- 37 €
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Ruboxistaurin hydrochloride
T3689169939-93-9
Ruboxistaurin hydrochloride (LY 333531 hydrochloride) is an Isozyme-selective inhibitor of protein kinase C (PKC); competitively and reversibly inhibits PKCβI and PKCβII (IC50 values are 4.7 and 5.9 nM respectively). Selective for PKCβ over other PKC isozymes (IC50values are 0.052, 0.25, 0.30, 0.36, 0.60 and >100 μM for PKCη, -δ, -γ, -α, -ε and -ζ respectively). Exhibits selectivity for PKC over other ATP-dependent kinases, including protein kinase A, casein kinase and src).
- 61 €
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Ellagic acid Cited
T0465476-66-4
Ellagic acid (Gallogen), a thickened tetracyclic natural product, is a potent CK2 inhibitor (IC50=40 nM; Ki=20 nM) with ATP-competitive properties. Ellagic acid is an antioxidant and also possesses antiproliferative activity.
- 41 €
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CitedPlantainoside D
T5796147331-98-4
Plantainoside D (Isoplantamajoside) shows potent antioxidative effects as those of ascorbic acid, it shows angiotensin-converting enzyme (ACE) inhibitory inhibitory activity in vitro with the IC(50) value of 2.17 mM, it also shows inhibitory activity against PKCalpha with the IC50 value14.8microM.
- 115 €
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Enzastaurin Cited
T6280170364-57-5
Enzastaurin (LY317615) (LY317615) is an effective PKCβ selective inhibitor (IC50: 6 nM), 6- to 20-fold selectivity against PKCα γ ε.
- 40 €
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CitedSU9516
T6167377090-84-1
SU9516 is a potent CDK2 inhibitor with an IC50 of 22 nM and also inhibits CDK1 and CDK4, with IC50s of 40 nM and 200 nM, respectively.
- 28 €
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α-Vitamin E Cited
T164859-02-9
α-Vitamin E (Dexrabeprazole Sodium) is a naturally-occurring form of vitamin E, a fat-soluble vitamin with potent antioxidant properties.
- 36 €
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CitedFasudil Cited
T1606103745-39-7
Fasudil (HA-1077) is a potent inhibitor of ROCK1, PKA, PKC, and MLCK.
- 31 €
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CitedFasudil hydrochloride Cited
T3060105628-07-7
Fasudil hydrochloride (HA-1077) is a potent inhibitor of ROCK1, PKA, PKC, and MLCK with Ki of 0.33 μM, 1.0 μM, 9.3 μM and 55 μM, respectively.
- 33 €
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CitedVTX-27
T133141321924-70-2
VTX-27 is a selective inhibitor of protein kinase C θ (PKC θ) (Kis: 0.08 nM and 16 nM for PKC θ and PKC δ).
- 80 €
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CMPD101
T14989865608-11-3
CMPD101 is a membrane-permeable small-molecule inhibitor of GRK2 3 (IC50: 18 nM and 5.4 nM). Which can be used for the study of heart failure. CMPD101 exhibits less selectively against GRK1, GRK5, ROCK-2 and PKCα with IC50s of 3.1 μM , 2.3 μM, 1.4 μM and 8.1 μM, respectively.
- 57 €
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D-ERYTHRO-SPHINGOSINE
T5891123-78-4
D-erythro-Sphingosine (trans-4-Sphingenine) is a protein kinase C (PKC) inhibitor. D-erythro-Sphingosine (Erythrosphingosine) is also a PP2A activator
- 37 €
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Pinoresinol dimethyl ether
T2S053129106-36-3
Pinoresinol dimethyl ether is a nonphenolic furan lignan isolated from the stem bark of Magnolia kobus with neurological activity. It stimulates upstream MAPK, PKC and PKA pathways and induces neural protrusion growth in PC12 cells.
- 95 €
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CGP60474
T14943164658-13-3
CGP60474 is an inhibitor of VEGFR-2 (IC50 = 84 nM) and an inhibitor of ATP-competitive PKC. CGP60474 is also a highly potent anti-endotoxemic agent and inhibits cyclin-dependent kinase (CDK) potently.
- 28 €
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Chelerythrine Cited
T6S005234316-15-9
1. Chelerythrine (Broussonpapyrine) may have antimanic effect . 2. Chelerythrine can inhibit telomerase activity. 3. Chelerythrine is a well-known protein kinase C inhibitor . 4. Chelerythrine has potential antiproliferative and antitumor effects.
- 47 €
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CitedMitoxantrone dihydrochloride
T015870476-82-3
Mitoxantrone dihydrochloride (NSC-301739) is the hydrochloride salt of an anthracenedione antibiotic with antineoplastic activity. It is a type II topoisomerase inhibitor.
- 47 €
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Darovasertib
T56001874276-76-2
Darovasertib (LXS196) is a potent, selective, and orally active protein kinase C (PKC) inhibitor with IC50 values of 1.9 nM for PKCα, 0.4 nM for PKCθ, and 3.1 μM for GSK3β.
- 45 €
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Ζ-Stat
T354073316-02-7
ζ-Stat (NSC37044), a specific and atypical inhibitor of PKC-ζ with an IC50 of 5 μM, demonstrates the ability to inhibit proliferation and induce apoptosis in melanoma cell lines, exhibiting antitumor activity in vitro[1][2].
- 113 €
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Syk Inhibitor II dihydrochloride
T4391227449-73-2
Spleen tyrosine kinase (Syk) is a non-receptor tyrosine kinase that, upon phosphorylation, binds to immunoreceptor tyrosine-based activation motifs of FcRγ chains and mediates downstream signaling related to platelet function and inflammation. Syk inhibit
- 125 €
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A-443654
T14072552325-16-3
A-443654, a pan-Akt inhibitor, exhibits equal potency against Akt1, Akt2, and Akt3 within cells (Ki=160 pM).
- 79 €
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Rottlerin Cited
T1679182-08-6
Rottlerin (NSC-56346) is a natural product purified from Mallotus Philippinensis and is a specific PKC inhibitor (IC50: PKCδ of 3-6 μM, PKCα,β,γ of 30-42 μM, PKCε,η,ζ of 80-100 μM). Rottlerin causes apoptosis via caspase 3 activation.
- 33 €
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