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Chromatin/Epigenetic

DNA Methyltransferase

(38)

Epigenetic Reader Domain

HIF/HIF Prolyl-Hydroxylase

(76)

Histone Acetyltransferase

(48)

Histone Demethylase

(92)

Histone Methyltransferase

Methionine Adenosyltransferase (MAT)

Cytoskeletal Signaling

Microtubule Associated

PKC

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.

Filter HomeSignaling PathwaysChromatin/Epigenetic-Cytoskeletal SignalingPKC

20-HETE

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.

$498

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Phorbol 12-myristate 13-acetate

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.

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Staurosporine

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.

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Gardenin A

TN411421187-73-5

Gardenin A shows neurotrophic effects via activating MAPK ERK, PKC, and PKA. Gardenin A exhibits antidepressant, anticonvulsant and anxiolytic effects.

$197

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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.

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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.

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PKC β pseudosubstrate acetate

TP1955L

PKC β pseudosubstrate acetate (PKC β pseudosubstrate acetate (172308-76-8 Free base)) is a selective cell-permeable inhibitor of PKC.

$175

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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.

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Phorbol 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.

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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.

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Sangivamycin

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.

$128

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Ro-3306

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.

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Go 6983

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.

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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.

$293

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SU9516

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.

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Sotrastaurin

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.

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TPPB

T17148497259-23-1

TPPB is a kinase C activator of cell-permeable benzolactam-derived protein (Ki: 11.9 nM).

$163

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Hispidin

T7792555-55-5

Hispidin is a polyphenol originally, including antioxidant, anti-inflammatory, and cytoprotective properties

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Mitoxantrone

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.

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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.

$297

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Piceatannol

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.

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Verbascoside

T337561276-17-3

Verbascoside (Kusaginin) is a protein kinase C inhibitor with antimicrobial, anti-inflammatory activities.

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Daphnetin

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.

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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).

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Bisindolylmaleimide I

T6513133052-90-1

Bisindolylmaleimide I (GF109203X) is a potent and highly selective protein kinase C (PKC) inhibitor, exhibiting a Ki of 14 nM.

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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.

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HA-1004

T2752591742-10-8In house

HA-1004 is a inhibitor of PKG, PKA, PKC and MLC.

$195

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Ellagic acid

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.

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Y06137

T133632226534-49-0In house

Y06137 is an effective and selective BET inhibitor with a Kd of 81 nM for BRD4(1) bromodomain. Y06137 can be used for research on the treatment of castration-resistant prostate cancer.

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Plantainoside 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.

$122

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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.

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Fasudil

T1606103745-39-7

Fasudil (HA-1077) is a potent inhibitor of ROCK1, PKA, PKC, and MLCK.

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Fasudil hydrochloride

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.

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Mitoxantrone 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.

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α-Vitamin E

T164859-02-9

α-Vitamin E (Dexrabeprazole Sodium) is a naturally-occurring form of vitamin E, a fat-soluble vitamin with potent antioxidant properties.

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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.

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Valrubicin

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.

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VTX-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).

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Enzastaurin

T6280170364-57-5

Enzastaurin (LY317615) (LY317615) is an effective PKCβ selective inhibitor (IC50: 6 nM), 6- to 20-fold selectivity against PKCα γ ε.

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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.

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Chelerythrine chloride

T34193895-92-9

Chelerythrine Chloride is a cell-permeable inhibitor of protein kinase C, competitive with respect to the phosphate acceptor and non-competitive with respect to ATP.

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ML-7 hydrochloride

T3050110448-33-4

ML-7 hydrochloride (ML-7 HCl) is a cell-permeable, reversible, effective, ATP-competitive, and specific inhibitor of myosin light chain kinase (Ki: 300 nM); also inhibits smooth-muscle myosin light chain kinase, PKA, and PKC.

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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).

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Chelerythrine

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.

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N-Cyclohexyl-4-[1-(1-piperazinyl)-2,6-naphthyridin-3-yl]-2-pyridinamine

T92561071135-06-2

N-Cyclohexyl-4-[1-(1-piperazinyl)-2,6-naphthyridin-3-yl]-2-pyridinamine is a novel 2,6-naphthyridine identified by high throughput screen (HTS) as a dual protein kinase C D (PKC PKD) inhibitor[1].

$148

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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

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Delcasertib

T11740949100-39-4

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

$213

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Miltefosine

T003358066-85-6

Miltefosine (HePC) is the treatment of visceral and cutaneous leishmaniasis drug , and is proceeding clinical trials for this in several countries. Several medical agents produce some potency against visceral or cutaneous leishmaniasis, however a 2005 survey concluded that miltefosine is the only effective oral treatment for both forms of leishmaniasis.

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