| T0033 |
Miltefosine |
Miltefosine is the treatment of visceral and cutaneous leishmaniasis drug , and is proceeding clinical trials for this in several countries. Several medical agents produce some po |
| T0228 |
Methyl hesperidin |
Methyl Hesperidin, a flavanone glycoside (flavonoid) (C28H34O15), is abundant in citrus fruits. Its aglycone form is called hesperetin. |
| 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 clotting system which al |
| T0610 |
Piceatannol |
Piceatannol is an anti-inflammatory, immunomodulatory and antiproliferative agent. It inhibits p56lck and syk protein tyrosine kinases and inhibits NF-κB activation and gene expre |
| 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 also have antifunga |
| T1648 |
Vitamin E |
(+)-α-Tocopherol is a naturally-occurring form of vitamin E, a fat-soluble vitamin with potent antioxidant properties. |
| 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. |
| T2441 |
TAS-301 |
TAS-301, an inhibitor of smooth muscle cell migration and proliferation, inhibits intimal thickening after balloon injury to rat carotid arteries. |
| T2757 |
Myricetrin |
Myricitrin, a flavonoid compound isolated from the root bark of Myrica cerifera, exerts antinociceptive effects. |
| 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), also exhibit ant |
| 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-muscle myosin light cha |
| 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. |
| T3211 |
Midostaurin |
PKC412(Midostaurin; CGP41231; CGP41251) is a broad spectrum protein kinase inhibitor. Midostaurin inhibits protein kinase C alpha (PKCalpha), vascular endothelial growth factor rec |
| T3375 |
Verbascoside |
Verbascoside is a protein kinase C inhibitor with antimicrobial, anti-inflammatory activities. |
| 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 ATP. |
| T4037 |
Phorbol |
Phorbol, a plant-derived diterpene, is a tumor promoter through the activation of protein kinase C. |
| 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. |
| T6223 |
U0126-EtOH |
U0126-EtOH is a non-ATP competitive specific inhibitor of MEK1/2 (IC50: 0.07/0.06 μM). |
| T6278 |
Sotrastaurin |
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). |
| T6280 |
Enzastaurin |
Enzastaurin (LY317615) is an effective PKCβ selective inhibitor (IC50: 6 nM), 6- to 20-fold selectivity against PKCα/γ/ε. |
| 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. |
| 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. |
| T6513 |
Bisindolylmaleimide I |
GF109203X is a potent and highly selective protein kinase C (PKC) inhibitor with a Ki of 14 nM. |
| 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. |
| 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. |
| 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). |
| T6932 |
PD168393 |
PD168393 is an irreversible EGFR inhibitor (IC50: 0.70 nM), irreversibly alkylate Cys-773; inactive against PKC, FGFR, PDGFR, and insulin. |
| 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. Chelerythrine has po |
| 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 , potentially by inhi |
| 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 develop new lead compoun |
| 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 kinase C (PKC) iso-enz |
| T5817 |
PKC-theta inhibitor |
PKC-theta inhibitor is a selective PKC-θinhibitor(IC50:12 nM). |
| 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, respectively). |
| T5771 |
Hypocrellin A |
Hypocrellin A is PKC inhibitor, has light-induced antitumor,antifungal and antiviral activities, it also exerts immunomodulatory effects on MHC-restricted presentation of antigen. |
| 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 vitro with the IC(50) v |
| T7659 |
Bisindolylmaleimide IV |
Bisindolylmaleimide IV is a protein kinase C (PKC) cell permeable inhibitor( IC50 : 0.10 - 0.55 µM) |
| 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. |
| TQ0198 |
Phorbol 12-myristate 13-acetate |
Phorbol 12-myristate 13-acetate (PMA) is a dual SphK and PKC activator. |
| 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 |
| 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 muscle and endothe |
| 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 chains and mediates dow |
| T6588 |
Mitoxantrone |
Mitoxantrone is an anthracenedione antibiotic with antineoplastic activity. Mitoxantrone intercalates into and crosslinks DNA, thereby disrupting DNA and RNA replication. This agen |
| 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, respectively). |
| 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 cells. |
| 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 activities. |
| TN1513 |
Clitorin |
Clitorin has free radical scavenging property. It shows significant interactions with CD38, it may have anti-hyperglycemic potential. |
| TN2225 |
Soyasapogenol B |
Soyasapogenol B has anti-cancer, hypocholesterolemic, anticomplementary, hepatoprotective effects, it inhibits proliferation of cultured Hep-G2. |
| TN2326 |
(Z)-Butylidenephthalide |
(Z)-Butylidenephthalide has antitumor effect, can effectively inhibit the tumor growth in the glioma. |
| 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 used in the research |
| TN1047 |
Ingenol mebutate |
Ingenol mebutate shows anticancer activity, and P-gp-mediated absorptive transport, dermal penetration, and vascular damage contribute to the anticancer activity of ingenol-3-angel |
| 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, 7.6, 25.6, 57.5, 314 |
| 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 values of 132 nM, 639 |
| 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. |
| 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 of Munc13-1 and th |
| T14943 |
CGP60474 |
CGP60474 is an inhibitor of VEGFR-2 (IC50: 84 nM) and an ATP-competitive inhibitor of PKC. |
| T14989 |
CMPD101 |
CMPD101 is a membrane-permeable inhibitor of GRK2/3 (IC50: 18 nM and 5.4 nM) used for the study of heart failure. CMPD101 exhibits less selectively against GRK1, GRK5, ROCK-2 and P |
| T10549 |
Bisindolylmaleimide VIII acetate |
Bisindolylmaleimide VIII acetate (Ro 31-7549 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 PK |
| 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-dependent apoptosis w |
| T13314 |
VTX-27 |
VTX-27 is a selective inhibitor of protein kinase C θ (PKC θ)(Kis of 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 wavelength. Cercosporin cont |
| 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 culture because it |
| 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, chymotrypsin, and malate |
| 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 with a Kd of 81 nM |
| T16276 |
NBD-556 |
NBD-556 is a small molecule mimetic of CD4. NBD-556 recognizes the HIV-1 envelope protein gp120 and induces restructuring of gp120 analogous to CD4 binding. |
| T16526 |
Phorbol 12,13-dibutyrate |
Phorbol 12,13-dibutyrate is a PKC activator. It also is a potent skin tumor promoter. |
| 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 derivative of PS48 and is |
| 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,ζ of 80-100 μM). |
| 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 inhibitor that inhi |
| 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 nM (δ-C1B), 18.9 nM |
| T2S0501 |
Ilexgenin A |
Ilexgenin A exerts anti-inflammation and anti-angiogenesis effects through inhibition of STAT3 and PI3K pathways and exhibits synergistic effects with Sorafenib on hepatoma growth. |
| T4001 |
Euxanthone |
Euxanthone has vasorelaxation effect, may be through multiple pathways involved PKC-mediated signal pathway and calcium-independent pathway, it induces its vasodilator effect throu |
| 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 platelet aggregation |
| 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 as MAPK and PKC. |
| 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 inhibition of protein kinas |
| TN3517 |
Bisacurone |
Bisacurone has anti-oxidant, anti-inflammatory, and anti-metastatic activities, it may have a protective effect against ethanol-induced liver injury by suppressing hepatic oxidatio |
| 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 ERK1/2, PI3K, and PKC ar |
| 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 dependent pathway in R |
| TN4114 |
Gardenin A |
Gardenin A has antihyperlipidemic and hepatoprotective effects , it also promotes neuritogenesis through the activation of MAPK/ERK-, PKC-, and PKA-dependent, but not TrkA-dependen |
| 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 activity of Bcl-2 f |
| 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 standard drug amoxicillin |
| 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-glucosidase. Leucosceptoside |
