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Cytoskeletal Signaling PKC

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.
Cat No. product name
T6278 SotrastaurinHOT Sotrastaurin is a potent pan-PKC inhibitor (Kis: 0.95/0.64/2.1/3.2/1.8/0.22 nM for PKCα/βI/δ/ε/η/θ).
TP1956L PKC ζ pseudosubstrate acetate PKC ζ pseudosubstrate acetate is an inhibitor of protein kinase C (PKC) ζ; attached to cell permeabilisation Antennapedia domain vector peptide. Consists of am...
T5817 PKC-theta inhibitor hcl PKC-theta inhibitor is a selective PKC-θinhibitor(IC50:12 nM).
T6285 GSK690693 GSK690693 is a pan-Akt inhibitor targeting Akt1/2/3 with IC50 of 2 nM/13 nM/9 nM, also sensitive to the AGC kinase family: PKA, PrkX and PKC isozymes. Phase 1.
T4037 Phorbol Phorbol, a plant-derived diterpene, is a tumor promoter through the activation of protein kinase C.
T4391 Syk Inhibitor II (hydrochloride) Spleen tyrosine kinase (Syk) is a non-receptor tyrosine kinase that, upon phosphorylation, binds to immunoreceptor tyrosine-based activation motifs of FcRγ chai...
T6S0052 Chelerythrine 1. Chelerythrine may have antimanic effect . 2. Chelerythrine can inhibit telomerase activity. 3. Chelerythrine is a well-known protein kinase C inhibitor . 4. C...
T7501 Iso-H7 dihydrochloride Iso-H7 dihydrochloride is a less potent inhibitor of phosphokinase C than H-7.
T5S2017 Ingenol 1. Ingenol mebutate is an effective treatment for actinic keratosis. 2. Formulating novel derivatives from Ingenol esters may be an innovative approach to develo...
T3S1416 Decursin 1. Decursin is able to attenuate kainic acid-induced seizures and could have potential as an antiepileptic drug. 2. Decursin exhibits hepatoprotective effects , ...
T4950 1,2-Dipalmitoyl-sn-glycerol 1,2-Dipalmitoyl-sn-glycerol is an analog of the PKC-activating second messenger diacylglycerol (DAG). It weakly activates PKC.
T5239 Cholesterol 3-Sulfate Sodium Salt Cholesterol sulfate is a sterol sulfate in human plasma. It is a component of cell membrane and has a regulatory function. It also activates multiple protein kin...
T5600 LXS196 LXS196 is a potent, selective and orally active protein kinase C (PKC) inhibitor(IC50 values of 1.9 nM, 0.4 nM and 3.1 μM for PKCα, PKCθ and GSK3β, respectiv...
T6588 Mitoxantrone Mitoxantrone is an anthracenedione antibiotic with antineoplastic activity. Mitoxantrone intercalates into and crosslinks DNA, thereby disrupting DNA and RNA rep...
T5771 Hypocrellin A Hypocrellin A is PKC inhibitor, has light-induced antitumor,antifungal and antiviral activities, it also exerts immunomodulatory effects on MHC-restricted presen...
T5891 D-ERYTHRO-SPHINGOSINE D-erythro-Sphingosine is a protein kinase C (PKC) inhibitor. D-erythro-Sphingosine (Erythrosphingosine) is also a PP2A activator
T5796 Plantainoside D Plantainoside D shows potent antioxidative effects as those of ascorbic acid, it shows angiotensin-converting enzyme (ACE) inhibitory inhibitory activity in vitr...
T7659 Bisindolylmaleimide IV Bisindolylmaleimide IV is a protein kinase C (PKC)  cell permeable inhibitor( IC50 : 0.10 - 0.55 µM)
TQ0198 Phorbol 12-myristate 13-acetate Phorbol 12-myristate 13-acetate (PMA) is a dual SphK and PKC activator.
T7604 Valrubicin Valrubicin (AD 32) inhibits TPA- and PDBu-induced PKC activation (IC50s: 0.85 and 1.25 μM) and has antitumor and anti-inflammatory activity.
T7790 Bisindolylmaleimide V Bisindolylmaleimide V (BIM V) is a weak protein kinase C (PKC)inhibitor( IC50 >100 µM)
T7792 Hispidin Hispidin is a polyphenol originally, including antioxidant, anti-inflammatory, and cytoprotective properties
T8376 PKCβ inhibitor 1 PKCβ inhibitor 1(KUN79359) is a potent, selective and ATP-competitive inhibitor of PKCß isozymes(IC50s of 21 and 5 nM for human PKCβ1 and PKCβ2, respectivel...
TN1047 Ingenol mebutate Ingenol mebutate shows anticancer activity, and P-gp-mediated absorptive transport, dermal penetration, and vascular damage contribute to the anticancer activity...
T2356 Ro 3306 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...
T3375 Verbascoside Verbascoside is a protein kinase C inhibitor with antimicrobial, anti-inflammatory activities.
T6680 Staurosporine Staurosporine is a potent PKC inhibitor for PKCα/γ/η (IC50: 2/5/4 nM), less potent to PKCε (73 nM), PKCδ (20 nM) and little action to PKCζ (1086 nM).
T6280 Enzastaurin Enzastaurin (LY317615) is an effective PKCβ selective inhibitor (IC50: 6 nM), 6- to 20-fold selectivity against PKCα/γ/ε.
T1606 Fasudil Fasudil is a potent inhibitor of ROCK1, PKA, PKC, and MLCK.
T3060 Fasudil hydrochloride Fasudil Hydrochloride 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.
T0228 Methyl hesperidin Methyl Hesperidin, a flavanone glycoside (flavonoid) (C28H34O15), is abundant in citrus fruits. Its aglycone form is called hesperetin.
T3050 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-musc...
T3211 Midostaurin PKC412(Midostaurin; CGP41231; CGP41251) is a broad spectrum protein kinase inhibitor. Midostaurin inhibits protein kinase C alpha (PKCalpha), vascular endothelia...
T3684 CP21R7 CP21R7 is an effective and specific GSK3β inhibitor. It is used as an activator of stem cells prior to the induction of differentiation of stem cells to smooth...
T6513 Bisindolylmaleimide I GF109203X is a potent and highly selective protein kinase C (PKC) inhibitor with a Ki of 14 nM.
T6313 Go 6983 Go 6983 is a pan-PKC inhibitor against for PKCα, PKCβ, PKCγ, PKCδ and PKCζ with IC50 of 7 nM, 7 nM, 6 nM, 10 nM and 60 nM, respectively.
T6643 Ro 31-8220 Mesylate Ro 31-8220 is a pan-PKC inhibitor for PKC-α/βI/βII/γ/ε (IC50: 5/24/14/27/24 nM), and also shows potent inhibition against MSK1, MAPKAP-K1b, S6K1, and GSK3β...
T3689 Ruboxistaurin hydrochloride 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). S...
T2757 Myricetrin Myricitrin, a flavonoid compound isolated from the root bark of Myrica cerifera, exerts antinociceptive effects.
TN1299 6,7,4'-Trihydroxyisoflavone 6,7,4'-Trihydroxyisoflavone, is a novel inhibitor of PKCα in suppressing solar UV-induced matrix metalloproteinase 1, which has antioxidant, and anti-cancer act...
T2441 TAS301 TAS-301, an inhibitor of smooth muscle cell migration and proliferation, inhibits intimal thickening after balloon injury to rat carotid arteries.
T6932 PD168393 PD168393 is an irreversible EGFR inhibitor (IC50: 0.70 nM), irreversibly alkylate Cys-773; inactive against PKC, FGFR, PDGFR, and insulin.
T6605 NH125 NH125 is a selective eEF-2 kinase inhibitor with IC50 of 60 nM, >125-fold selectivity over PKC, PKA, and CaMKII, and also a potent histidine kinase inhibitor.
T6167 SU9516 SU9516 is a potent CDK2 inhibitor, with an IC50 of 22 nM, and also has inhibitory effects on CDK1 and CDK4, with IC50s of 40 nM and 200 nM, respectively.
T3419 Chelerythrine chloride Chelerythrine Chloride is a cell-permeable inhibitor of protein kinase C, competitive with respect to the phosphate acceptor and non-competitive with respect to ...
T0465 Ellagic acid Ellagic acid is a fused four ring compound isolated from the kino of Eucalyptus maculata Hook and E. Hemipholia F. Muell. Activates Factor XII of the blood clott...
T2851 Daphnetin Daphnetin, 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...
T0979 Dequalinium chloride Dequalinium Chloride, a topical bacteriostat, is a selective blocker of apamin-sensitive K+ channels. It is used in wound dressings and mouth infections and may ...
T0033 Miltefosine Miltefosine is the treatment of visceral and cutaneous leishmaniasis drug , and is proceeding clinical trials for this in several countries. Several medical agen...
T1648 Vitamin E (+)-α-Tocopherol is a naturally-occurring form of vitamin E, a fat-soluble vitamin with potent antioxidant properties.
TN1136 Procyanidin A1 Procyanidin A1 has antiallergic effects, it inhibits degranulation downstream of protein kinase C activation or Ca2+; influx from an internal store in RBL-2H3 ce...
TN1513 Clitorin Clitorin has free radical scavenging property. It shows significant interactions with CD38, it may have anti-hyperglycemic potential.
TP1887L1 [Ala107]-MBP (104-118) acetate(99026-77-4 free base) [Ala107]-MBP (104-118) acetate is synthetic peptide analog of bovine myelin basic protein (MBP). Non-competitive inhibitor of PKC (IC50 = 46 - 145 mM).
TN4271 Isochamaejasmine Isochamaejasmine has inhibition of NF-kappaB activation, which could reverse the anti-apoptotic effect; it induces apoptosis in leukemia cells by inhibiting the ...
T17148 TPPB TPPB is a kinase C activator of cell-permeable benzolactam-derived protein (Ki: 11.9 nM).
T17299 (-)-Indolactam V (-)-Indolactam V is a PKC activator (Kis: 3.36 nM, 1.03 μM for η-CRD2 , γ-CRD2). (-)-Indolactam V also has the Kds are 5.5 nM (η-C1B), 7.7 nM (ε-C1B), 8.3 n...
T4001 Euxanthone Euxanthone has vasorelaxation effect, may be through multiple pathways involved PKC-mediated signal pathway and calcium-independent pathway, it induces its vasod...
TN2799 20-Deoxyingenol 3-angelate 20-Deoxyingenol 3-angelate and ingenol 20-acetate 3-angelate are known as promoters of tumors of mouse skin. 20-Deoxyingenol 3-angelate can induce significant pl...
TN2844 (2R,3S)-Dihydrodehydroconiferyl alcohol (2R,3S)-Dihydrodehydroconiferyl alcohol can induce neurite outgrowth and enhance NGF-induced neurite outgrowth from PC12 cells by amplifying up-stream steps such...
TN3160 6-Deoxyisojacareubin 6-Deoxyisojacareubin shows moderate inhibitory activity against the QGY-7703 cell line, with the IC50 value of 9.65 uM; it also possesses potency in the inhibiti...
TN3517 Bisacurone Bisacurone has anti-oxidant, anti-inflammatory, and anti-metastatic activities, it may have a protective effect against ethanol-induced liver injury by suppressi...
TN3655 Cimiside E Cimiside E has anti-inflammatory activity, it selectively inhibits TNF-α-induced expression of VCAM-1 at least by upregulation of PPAR-γ, and signals for ERK1/...
TN3694 Coniferaldehyde Coniferaldehyde exerts anti-inflammatory properties by inducing heme oxygenase-1(HO-1), it inhibits LPS-induced apoptosis through the PKC α/β II/Nrf-2/HO-1 dep...
TN4114 Gardenin A Gardenin A has antihyperlipidemic and hepatoprotective effects , it also promotes neuritogenesis through the activation of MAPK/ERK-, PKC-, and PKA-dependent, bu...
TN4300 Isojacareubin Isojacareubin displays potent activity against H. pylori HP40 clinical isolate with MIC 23.9 uM, which is approximately two times greater than that of the standa...
T16848 SB-218078 SB-218078 is less potently inhibits Cdc2 (IC50: 250 nM) and PKC (IC50: 1000 nM). SB-218078 is a potent, ATP-competitive, and cell-permeable checkpoint kinase 1 i...
TN4431 Leucosceptoside A Leucosceptoside A shows inhibitory activity against PKCalpha with the IC50 value of 19.0 microM; it also exhibits strong inhibitory capacity against α-glucosida...
T8764 PKC-iota inhibitor 1 PKC-iota inhibitor 1 is an inhibitor of protein kinase C-iota (PKC-ι ; IC50 : 0.34 μM)
T6139L A-674563 2HCl(552325-73-2(fb-2hcl)) A-674563 is an Akt1 inhibitor with Ki of 11 nM, modest potent to PKA and >30-fold selective for Akt1 over PKC.
T8681 HA-1004 dihydrochloride HA-1004 dihydrochloride is an inhibitor of PKA, PKC, cGKI, MYLK, and calcium channel protein
T8681 HA-1004 dihydrochloride HA-1004 dihydrochloride is an inhibitor of PKA, PKC, cGKI, MYLK, and calcium channel protein
T20168 Sodium aurothiomalate Sodium aurothiomalate is a gold compound that is used for its immunosuppressive anti-rheumatic effects. Aurothiomalate sodium is a potent and selective inhibitor...
TP1789L Malantide acetate(86555-35-3 free base) Malantide acetate is a dodecapeptide phosphorylated by cyclic AMP-dependent protein kinase (PKA), and increases PKA activity.Malantide is a synthetic peptide tha...
TP1053L Protein Kinase C 19-31 acetate(121545-65-1 free base) Protein Kinase C 19-31 acetate, a peptide inhibitor of protein kinase C (PKC), derived from the pseudo-substrate regulatory domain of PKCa (residues 19-31) with ...
TP1945L1 Pep2m, myristoylated acetate(1423381-07-0 free base) Pep2m, myristoylated acetate is a Cell-permeable, myristoylated form of pep2m. Peptide inhibitor of the interaction between the C-terminus of the GluA2 (AMPA rec...
TP1924L1 ZIP acetate(863987-12-6 free base) ZIP acetate is a novel, cell-permeable inhibitor of protein kinase Mζ (PKMζ), a constitutively active, atypical PKC isozyme involved in LTP maintenance. Select...
T17019 TCS 21311 TCS 21311 is an effective and highly selective inhibitor of JAK3 (IC50: 8 nM). TCS 21311 inhibits PKCα, PKCθ, and GSK3β (IC50s: 13, 68, and 3 nM, respectivel...
T16791 Rottlerin Rottlerin 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,...
TN1542 Cycloheterophyllin Cycloheterophyllin has an antioxidant effect, it is a photoprotective agent that inhibits ultraviolet A (UVA)-induced oxidative stress and damage, and could be u...
T14943 CGP60474 CGP60474 is an inhibitor of VEGFR-2 (IC50: 84 nM) and an ATP-competitive inhibitor of PKC.
TN1557 Decursinol angelate Decursinol angelate has anti-tumor, anti-inflammatory, anti-oxidant, and hepatoprotective activities, it inhibits VEGF-induced angiogenesis via suppression of th...
TN2326 (Z)-Butylidenephthalide (Z)-Butylidenephthalide has antitumor effect, can effectively inhibit the tumor growth in the glioma.
T12494 PKC-IN-1 PKC-IN-1 is a ATP-competitive and reversible conventional PKC enzymes inhibitor (PKCα, PKCβI, PKCβII, PKCθ, PKCγ, PKC mu and PKCε with IC50s of 2.3, 8.1, 7...
T12496 PKC-theta inhibitor 1 PKC-theta inhibitor 1 is an inhibitor of PKCθ (Ki of 6 nM)
T10888 CRT0066854 hydrochloride CRT0066854 hydrochloride is an effective selective atypical PKCs inhibitor. CRT0066854 is against full-length (FL) PKCι, PKCζ, and ROCK-II kinases with IC50 va...
T13637 DCP-LA DCP-LA (FR236924), linoleic acid derivatives, selective and direct activation of PKCε.
T10980 DCPLA-ME DCPLA-ME is the methyl ester form of DCPLA and can be used to treat neurodegenerative diseases. It is an effective PKCε activator.
T14069 A-3 hydrochloride A-3 hydrochloride is a potent, cell-permeable, reversible, ATP-competitive non-selective antagonist of various kinases. A-3 hydrochloride also inhibits PKC and c...
T14328 AS2521780 AS2521780 is an inhibitor of PKCθ (IC50: 0.48 nM).
T14831 Bryostatin 1 Bryostatin 1 is a natural macrolide isolated from the bryozoan Bugula neritina and is a CNS)permeable PKC modulator. Bryostatin 1 binds to the isolated C1 domain...
T14989 CMPD101 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 ...
T16671 PS315 PS315 inhibits the full-length and catalytic domain constructs of PKCζ (IC50=10 μM) and PKCη (IC50=30 μM). PS315 has anti-cancer activity. PS315 is a derivat...
T10549 Bisindolylmaleimide VIII acetate Bisindolylmaleimide VIII acetate is a potent and selective PKC inhibitor (IC50: 158 nM for rat brain PKC). It has IC50s of 53, 195, 163, 213, and 175 nM for PKC-...
T10550 Bisindolylmaleimide X hydrochloride Bisindolylmaleimide X hydrochloride (BIM-X hydrochloride) is a potent and selective PKC inhibitor. It is also a potent CDK2 antagonist (IC50: 200 nM).
T10555 BJE6-106 BJE6-106 (B106) is a potent, selective PKCδ inhibitor (IC50: 0.05 μM) and targets selectivity over classical PKCα (IC50: 50 μM). BJE6-106 induces caspase-dep...
T13314 VTX-27 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).
T13605 Cercosporin Cercosporin is produced by a plant pathogen, Cercosporakikuchii, and the elsinochromes. Cercosporin is a potent photosensitizer with a short activation wavelengt...
T15637 K-252b K-252b is an indolocarbazole isolated from the actinomycete Nocardiopsis and is a PKC inhibitor. K-252b can be used to inhibit extracellular kinases of cells in ...
T15638 K-252c K-252c is a staurosporine analog isolated from Nocardiopsis sp. and is a cell-permeable PKC inhibitor (IC50: 2.45 µM). K-252c also inhibits β-lactamase, chymot...
T13384 Y-33075 Y-33075 is a selective inhibitor of ROCK derived from Y-27632, and is more potent than Y-27632, with an IC50 of 3.6 nM.
T13363 Y06137 Y06137 is a potent and selective inhibitor of BET, and used for treatment of castration-resistant prostate cancer (CRPC). Y06137 binds to the BRD4(1) bromodomain...
T11740 Delcasertib Delcasertib is a potent and selective inhibitor of δ-protein kinase C (δPKC).
T16526 Phorbol 12,13-dibutyrate Phorbol 12,13-dibutyrate is a PKC activator. It also is a potent skin tumor promoter.
T0610 Piceatannol Piceatannol is an anti-inflammatory, immunomodulatory and antiproliferative agent. It inhibits p56lck and syk protein tyrosine kinases and inhibits NF-κB activa...
Sotrastaurin HOT
T6278CAS 425637-18-9
Sotrastaurin is a potent pan-PKC inhibitor (Kis: 0.95/0.64/2.1/3.2/1.8/0.22 nM for PKCα/βI/δ/ε/η/θ).
PKC ζ pseudosubstrate acetate
TP1956LCAS TP1956L
PKC ζ pseudosubstrate acetate is an inhibitor of protein kinase C (PKC) ζ; attached to cell permeabilisation Antennapedia domain vector peptide. Consists of am...
PKC-theta inhibitor hcl
T5817CAS 2253640-49-0
PKC-theta inhibitor is a selective PKC-θinhibitor(IC50:12 nM).
GSK690693
T6285CAS 937174-76-0
GSK690693 is a pan-Akt inhibitor targeting Akt1/2/3 with IC50 of 2 nM/13 nM/9 nM, also sensitive to the AGC kinase family: PKA, PrkX and PKC isozymes. Phase 1.
Phorbol
T4037CAS 17673-25-5
Phorbol, a plant-derived diterpene, is a tumor promoter through the activation of protein kinase C.
Syk Inhibitor II (hydrochloride)
T4391CAS 227449-73-2
Spleen tyrosine kinase (Syk) is a non-receptor tyrosine kinase that, upon phosphorylation, binds to immunoreceptor tyrosine-based activation motifs of FcRγ chai...
Chelerythrine
T6S0052CAS 34316-15-9
1. Chelerythrine may have antimanic effect . 2. Chelerythrine can inhibit telomerase activity. 3. Chelerythrine is a well-known protein kinase C inhibitor . 4. C...
Iso-H7 dihydrochloride
T7501CAS 140663-38-3
Iso-H7 dihydrochloride is a less potent inhibitor of phosphokinase C than H-7.
Ingenol
T5S2017CAS 30220-46-3
1. Ingenol mebutate is an effective treatment for actinic keratosis. 2. Formulating novel derivatives from Ingenol esters may be an innovative approach to develo...
Decursin
T3S1416CAS 5928-25-6
1. Decursin is able to attenuate kainic acid-induced seizures and could have potential as an antiepileptic drug. 2. Decursin exhibits hepatoprotective effects , ...
1,2-Dipalmitoyl-sn-glycerol
T4950CAS 30334-71-5
1,2-Dipalmitoyl-sn-glycerol is an analog of the PKC-activating second messenger diacylglycerol (DAG). It weakly activates PKC.
Cholesterol 3-Sulfate Sodium Salt
T5239CAS 2864-50-8
Cholesterol sulfate is a sterol sulfate in human plasma. It is a component of cell membrane and has a regulatory function. It also activates multiple protein kin...
LXS196
T5600CAS 1874276-76-2
LXS196 is a potent, selective and orally active protein kinase C (PKC) inhibitor(IC50 values of 1.9 nM, 0.4 nM and 3.1 μM for PKCα, PKCθ and GSK3β, respectiv...
Mitoxantrone
T6588CAS 65271-80-9
Mitoxantrone is an anthracenedione antibiotic with antineoplastic activity. Mitoxantrone intercalates into and crosslinks DNA, thereby disrupting DNA and RNA rep...
Hypocrellin A
T5771CAS 77029-83-5
Hypocrellin A is PKC inhibitor, has light-induced antitumor,antifungal and antiviral activities, it also exerts immunomodulatory effects on MHC-restricted presen...
D-ERYTHRO-SPHINGOSINE
T5891CAS 123-78-4
D-erythro-Sphingosine is a protein kinase C (PKC) inhibitor. D-erythro-Sphingosine (Erythrosphingosine) is also a PP2A activator
Plantainoside D
T5796CAS 147331-98-4
Plantainoside D shows potent antioxidative effects as those of ascorbic acid, it shows angiotensin-converting enzyme (ACE) inhibitory inhibitory activity in vitr...
Bisindolylmaleimide IV
T7659CAS 119139-23-0
Bisindolylmaleimide IV is a protein kinase C (PKC)  cell permeable inhibitor( IC50 : 0.10 - 0.55 µM)
Phorbol 12-myristate 13-acetate
TQ0198CAS 16561-29-8
Phorbol 12-myristate 13-acetate (PMA) is a dual SphK and PKC activator.
Valrubicin
T7604CAS 56124-62-0
Valrubicin (AD 32) inhibits TPA- and PDBu-induced PKC activation (IC50s: 0.85 and 1.25 μM) and has antitumor and anti-inflammatory activity.
Bisindolylmaleimide V
T7790CAS 113963-68-1
Bisindolylmaleimide V (BIM V) is a weak protein kinase C (PKC)inhibitor( IC50 >100 µM)
Hispidin
T7792CAS 555-55-5
Hispidin is a polyphenol originally, including antioxidant, anti-inflammatory, and cytoprotective properties
PKCβ inhibitor 1
T8376CAS 257879-35-9
PKCβ inhibitor 1(KUN79359) is a potent, selective and ATP-competitive inhibitor of PKCß isozymes(IC50s of 21 and 5 nM for human PKCβ1 and PKCβ2, respectivel...
Ingenol mebutate
TN1047CAS 75567-37-2
Ingenol mebutate shows anticancer activity, and P-gp-mediated absorptive transport, dermal penetration, and vascular damage contribute to the anticancer activity...
Ro 3306
T2356CAS 872573-93-8
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...
Verbascoside
T3375CAS 61276-17-3
Verbascoside is a protein kinase C inhibitor with antimicrobial, anti-inflammatory activities.
Staurosporine
T6680CAS 62996-74-1
Staurosporine is a potent PKC inhibitor for PKCα/γ/η (IC50: 2/5/4 nM), less potent to PKCε (73 nM), PKCδ (20 nM) and little action to PKCζ (1086 nM).
Enzastaurin
T6280CAS 170364-57-5
Enzastaurin (LY317615) is an effective PKCβ selective inhibitor (IC50: 6 nM), 6- to 20-fold selectivity against PKCα/γ/ε.
Fasudil
T1606CAS 103745-39-7
Fasudil is a potent inhibitor of ROCK1, PKA, PKC, and MLCK.
Fasudil hydrochloride
T3060CAS 105628-07-7
Fasudil Hydrochloride 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.
Methyl hesperidin
T0228CAS 11013-97-1
Methyl Hesperidin, a flavanone glycoside (flavonoid) (C28H34O15), is abundant in citrus fruits. Its aglycone form is called hesperetin.
ML-7 hydrochloride
T3050CAS 110448-33-4
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-musc...
Midostaurin
T3211CAS 120685-11-2
PKC412(Midostaurin; CGP41231; CGP41251) is a broad spectrum protein kinase inhibitor. Midostaurin inhibits protein kinase C alpha (PKCalpha), vascular endothelia...
CP21R7
T3684CAS 125314-13-8
CP21R7 is an effective and specific GSK3β inhibitor. It is used as an activator of stem cells prior to the induction of differentiation of stem cells to smooth...
Bisindolylmaleimide I
T6513CAS 133052-90-1
GF109203X is a potent and highly selective protein kinase C (PKC) inhibitor with a Ki of 14 nM.
Go 6983
T6313CAS 133053-19-7
Go 6983 is a pan-PKC inhibitor against for PKCα, PKCβ, PKCγ, PKCδ and PKCζ with IC50 of 7 nM, 7 nM, 6 nM, 10 nM and 60 nM, respectively.
Ro 31-8220 Mesylate
T6643CAS 138489-18-6
Ro 31-8220 is a pan-PKC inhibitor for PKC-α/βI/βII/γ/ε (IC50: 5/24/14/27/24 nM), and also shows potent inhibition against MSK1, MAPKAP-K1b, S6K1, and GSK3β...
Ruboxistaurin hydrochloride
T3689CAS 169939-93-9
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). S...
Myricetrin
T2757CAS 17912-87-7
Myricitrin, a flavonoid compound isolated from the root bark of Myrica cerifera, exerts antinociceptive effects.
6,7,4'-Trihydroxyisoflavone
TN1299CAS 17817-31-1
6,7,4'-Trihydroxyisoflavone, is a novel inhibitor of PKCα in suppressing solar UV-induced matrix metalloproteinase 1, which has antioxidant, and anti-cancer act...
TAS301
T2441CAS 193620-69-8
TAS-301, an inhibitor of smooth muscle cell migration and proliferation, inhibits intimal thickening after balloon injury to rat carotid arteries.
PD168393
T6932CAS 194423-15-9
PD168393 is an irreversible EGFR inhibitor (IC50: 0.70 nM), irreversibly alkylate Cys-773; inactive against PKC, FGFR, PDGFR, and insulin.
NH125
T6605CAS 278603-08-0
NH125 is a selective eEF-2 kinase inhibitor with IC50 of 60 nM, >125-fold selectivity over PKC, PKA, and CaMKII, and also a potent histidine kinase inhibitor.
SU9516
T6167CAS 377090-84-1
SU9516 is a potent CDK2 inhibitor, with an IC50 of 22 nM, and also has inhibitory effects on CDK1 and CDK4, with IC50s of 40 nM and 200 nM, respectively.
Chelerythrine chloride
T3419CAS 3895-92-9
Chelerythrine Chloride is a cell-permeable inhibitor of protein kinase C, competitive with respect to the phosphate acceptor and non-competitive with respect to ...
Ellagic acid
T0465CAS 476-66-4
Ellagic acid is a fused four ring compound isolated from the kino of Eucalyptus maculata Hook and E. Hemipholia F. Muell. Activates Factor XII of the blood clott...
Daphnetin
T2851CAS 486-35-1
Daphnetin, 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...
Dequalinium chloride
T0979CAS 522-51-0
Dequalinium Chloride, a topical bacteriostat, is a selective blocker of apamin-sensitive K+ channels. It is used in wound dressings and mouth infections and may ...
Miltefosine
T0033CAS 58066-85-6
Miltefosine is the treatment of visceral and cutaneous leishmaniasis drug , and is proceeding clinical trials for this in several countries. Several medical agen...
Vitamin E
T1648CAS 59-02-9
(+)-α-Tocopherol is a naturally-occurring form of vitamin E, a fat-soluble vitamin with potent antioxidant properties.
Procyanidin A1
TN1136CAS 103883-03-0
Procyanidin A1 has antiallergic effects, it inhibits degranulation downstream of protein kinase C activation or Ca2+; influx from an internal store in RBL-2H3 ce...
Clitorin
TN1513CAS 55804-74-5
Clitorin has free radical scavenging property. It shows significant interactions with CD38, it may have anti-hyperglycemic potential.
[Ala107]-MBP (104-118) acetate(99026-77-4 free base)
TP1887L1CAS TP1887L1
[Ala107]-MBP (104-118) acetate is synthetic peptide analog of bovine myelin basic protein (MBP). Non-competitive inhibitor of PKC (IC50 = 46 - 145 mM).
Isochamaejasmine
TN4271CAS 93859-63-3
Isochamaejasmine has inhibition of NF-kappaB activation, which could reverse the anti-apoptotic effect; it induces apoptosis in leukemia cells by inhibiting the ...
TPPB
T17148CAS 497259-23-1
TPPB is a kinase C activator of cell-permeable benzolactam-derived protein (Ki: 11.9 nM).
(-)-Indolactam V
T17299CAS 90365-57-4
(-)-Indolactam V is a PKC activator (Kis: 3.36 nM, 1.03 μM for η-CRD2 , γ-CRD2). (-)-Indolactam V also has the Kds are 5.5 nM (η-C1B), 7.7 nM (ε-C1B), 8.3 n...
Euxanthone
T4001CAS 529-61-3
Euxanthone has vasorelaxation effect, may be through multiple pathways involved PKC-mediated signal pathway and calcium-independent pathway, it induces its vasod...
20-Deoxyingenol 3-angelate
TN2799CAS 75567-38-3
20-Deoxyingenol 3-angelate and ingenol 20-acetate 3-angelate are known as promoters of tumors of mouse skin. 20-Deoxyingenol 3-angelate can induce significant pl...
(2R,3S)-Dihydrodehydroconiferyl alcohol
TN2844CAS 126253-41-6
(2R,3S)-Dihydrodehydroconiferyl alcohol can induce neurite outgrowth and enhance NGF-induced neurite outgrowth from PC12 cells by amplifying up-stream steps such...
6-Deoxyisojacareubin
TN3160CAS 26486-92-0
6-Deoxyisojacareubin shows moderate inhibitory activity against the QGY-7703 cell line, with the IC50 value of 9.65 uM; it also possesses potency in the inhibiti...
Bisacurone
TN3517CAS 120681-81-4
Bisacurone has anti-oxidant, anti-inflammatory, and anti-metastatic activities, it may have a protective effect against ethanol-induced liver injury by suppressi...
Cimiside E
TN3655CAS 154822-57-8
Cimiside E has anti-inflammatory activity, it selectively inhibits TNF-α-induced expression of VCAM-1 at least by upregulation of PPAR-γ, and signals for ERK1/...
Coniferaldehyde
TN3694CAS 20649-42-7
Coniferaldehyde exerts anti-inflammatory properties by inducing heme oxygenase-1(HO-1), it inhibits LPS-induced apoptosis through the PKC α/β II/Nrf-2/HO-1 dep...
Gardenin A
TN4114CAS 21187-73-5
Gardenin A has antihyperlipidemic and hepatoprotective effects , it also promotes neuritogenesis through the activation of MAPK/ERK-, PKC-, and PKA-dependent, bu...
Isojacareubin
TN4300CAS 50597-93-8
Isojacareubin displays potent activity against H. pylori HP40 clinical isolate with MIC 23.9 uM, which is approximately two times greater than that of the standa...
SB-218078
T16848CAS 135897-06-2
SB-218078 is less potently inhibits Cdc2 (IC50: 250 nM) and PKC (IC50: 1000 nM). SB-218078 is a potent, ATP-competitive, and cell-permeable checkpoint kinase 1 i...
Leucosceptoside A
TN4431CAS 83529-62-8
Leucosceptoside A shows inhibitory activity against PKCalpha with the IC50 value of 19.0 microM; it also exhibits strong inhibitory capacity against α-glucosida...
PKC-iota inhibitor 1
T8764CAS 2328094-11-5
PKC-iota inhibitor 1 is an inhibitor of protein kinase C-iota (PKC-ι ; IC50 : 0.34 μM)
A-674563 2HCl(552325-73-2(fb-2hcl))
T6139LCAS T6139L
A-674563 is an Akt1 inhibitor with Ki of 11 nM, modest potent to PKA and >30-fold selective for Akt1 over PKC.
HA-1004 dihydrochloride
T8681CAS 92564-34-6
HA-1004 dihydrochloride is an inhibitor of PKA, PKC, cGKI, MYLK, and calcium channel protein
HA-1004 dihydrochloride
T8681CAS 92564-34-6
HA-1004 dihydrochloride is an inhibitor of PKA, PKC, cGKI, MYLK, and calcium channel protein
Sodium aurothiomalate
T20168CAS 12244-57-4
Sodium aurothiomalate is a gold compound that is used for its immunosuppressive anti-rheumatic effects. Aurothiomalate sodium is a potent and selective inhibitor...
Malantide acetate(86555-35-3 free base)
TP1789LCAS TP1789L
Malantide acetate is a dodecapeptide phosphorylated by cyclic AMP-dependent protein kinase (PKA), and increases PKA activity.Malantide is a synthetic peptide tha...
Protein Kinase C 19-31 acetate(121545-65-1 free base)
TP1053LCAS TP1053L
Protein Kinase C 19-31 acetate, a peptide inhibitor of protein kinase C (PKC), derived from the pseudo-substrate regulatory domain of PKCa (residues 19-31) with ...
Pep2m, myristoylated acetate(1423381-07-0 free base)
TP1945L1CAS TP1945L1
Pep2m, myristoylated acetate is a Cell-permeable, myristoylated form of pep2m. Peptide inhibitor of the interaction between the C-terminus of the GluA2 (AMPA rec...
ZIP acetate(863987-12-6 free base)
TP1924L1CAS TP1924L1
ZIP acetate is a novel, cell-permeable inhibitor of protein kinase Mζ (PKMζ), a constitutively active, atypical PKC isozyme involved in LTP maintenance. Select...
TCS 21311
T17019CAS 1260181-14-3
TCS 21311 is an effective and highly selective inhibitor of JAK3 (IC50: 8 nM). TCS 21311 inhibits PKCα, PKCθ, and GSK3β (IC50s: 13, 68, and 3 nM, respectivel...
Rottlerin
T16791CAS 82-08-6
Rottlerin 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,...
Cycloheterophyllin
TN1542CAS 36545-53-6
Cycloheterophyllin has an antioxidant effect, it is a photoprotective agent that inhibits ultraviolet A (UVA)-induced oxidative stress and damage, and could be u...
CGP60474
T14943CAS 164658-13-3
CGP60474 is an inhibitor of VEGFR-2 (IC50: 84 nM) and an ATP-competitive inhibitor of PKC.
Decursinol angelate
TN1557CAS 130848-06-5
Decursinol angelate has anti-tumor, anti-inflammatory, anti-oxidant, and hepatoprotective activities, it inhibits VEGF-induced angiogenesis via suppression of th...
(Z)-Butylidenephthalide
TN2326CAS 72917-31-8
(Z)-Butylidenephthalide has antitumor effect, can effectively inhibit the tumor growth in the glioma.
PKC-IN-1
T12494CAS 1046787-18-1
PKC-IN-1 is a ATP-competitive and reversible conventional PKC enzymes inhibitor (PKCα, PKCβI, PKCβII, PKCθ, PKCγ, PKC mu and PKCε with IC50s of 2.3, 8.1, 7...
PKC-theta inhibitor 1
T12496CAS 1160501-81-4
PKC-theta inhibitor 1 is an inhibitor of PKCθ (Ki of 6 nM)
CRT0066854 hydrochloride
T10888CAS 2250019-91-9
CRT0066854 hydrochloride is an effective selective atypical PKCs inhibitor. CRT0066854 is against full-length (FL) PKCι, PKCζ, and ROCK-II kinases with IC50 va...
DCP-LA
T13637CAS 28399-31-7
DCP-LA (FR236924), linoleic acid derivatives, selective and direct activation of PKCε.
DCPLA-ME
T10980CAS 56687-67-3
DCPLA-ME is the methyl ester form of DCPLA and can be used to treat neurodegenerative diseases. It is an effective PKCε activator.
A-3 hydrochloride
T14069CAS 78957-85-4
A-3 hydrochloride is a potent, cell-permeable, reversible, ATP-competitive non-selective antagonist of various kinases. A-3 hydrochloride also inhibits PKC and c...
AS2521780
T14328CAS 1214726-89-2
AS2521780 is an inhibitor of PKCθ (IC50: 0.48 nM).
Bryostatin 1
T14831CAS 83314-01-6
Bryostatin 1 is a natural macrolide isolated from the bryozoan Bugula neritina and is a CNS)permeable PKC modulator. Bryostatin 1 binds to the isolated C1 domain...
CMPD101
T14989CAS 865608-11-3
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 ...
PS315
T16671CAS 1221964-50-6
PS315 inhibits the full-length and catalytic domain constructs of PKCζ (IC50=10 μM) and PKCη (IC50=30 μM). PS315 has anti-cancer activity. PS315 is a derivat...
Bisindolylmaleimide VIII acetate
T10549CAS 138516-31-1
Bisindolylmaleimide VIII acetate is a potent and selective PKC inhibitor (IC50: 158 nM for rat brain PKC). It has IC50s of 53, 195, 163, 213, and 175 nM for PKC-...
Bisindolylmaleimide X hydrochloride
T10550CAS 145317-11-9
Bisindolylmaleimide X hydrochloride (BIM-X hydrochloride) is a potent and selective PKC inhibitor. It is also a potent CDK2 antagonist (IC50: 200 nM).
BJE6-106
T10555CAS 1564249-38-2
BJE6-106 (B106) is a potent, selective PKCδ inhibitor (IC50: 0.05 μM) and targets selectivity over classical PKCα (IC50: 50 μM). BJE6-106 induces caspase-dep...
VTX-27
T13314CAS 1321924-70-2
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).
Cercosporin
T13605CAS 35082-49-6
Cercosporin is produced by a plant pathogen, Cercosporakikuchii, and the elsinochromes. Cercosporin is a potent photosensitizer with a short activation wavelengt...
K-252b
T15637CAS 99570-78-2
K-252b is an indolocarbazole isolated from the actinomycete Nocardiopsis and is a PKC inhibitor. K-252b can be used to inhibit extracellular kinases of cells in ...
K-252c
T15638CAS 85753-43-1
K-252c is a staurosporine analog isolated from Nocardiopsis sp. and is a cell-permeable PKC inhibitor (IC50: 2.45 µM). K-252c also inhibits β-lactamase, chymot...
Y-33075
T13384CAS 199433-58-4
Y-33075 is a selective inhibitor of ROCK derived from Y-27632, and is more potent than Y-27632, with an IC50 of 3.6 nM.
Y06137
T13363CAS 2226534-49-0
Y06137 is a potent and selective inhibitor of BET, and used for treatment of castration-resistant prostate cancer (CRPC). Y06137 binds to the BRD4(1) bromodomain...
Delcasertib
T11740CAS 949100-39-4
Delcasertib is a potent and selective inhibitor of δ-protein kinase C (δPKC).
Phorbol 12,13-dibutyrate
T16526CAS 37558-16-0
Phorbol 12,13-dibutyrate is a PKC activator. It also is a potent skin tumor promoter.
Piceatannol
T0610CAS 10083-24-6
Piceatannol is an anti-inflammatory, immunomodulatory and antiproliferative agent. It inhibits p56lck and syk protein tyrosine kinases and inhibits NF-κB activa...