S1421 |
Staurosporine (STS)
|
Staurosporine (STS) is a potent PKC inhibitor for PKCα, PKCγ and PKCη with IC50 of 2 nM, 5 nM and 4 nM, less potent to PKCδ (20 nM), PKCε (73 nM) and little active to PKCζ (1086 nM) in cell-free assays. Also shows inhibitory activities on other kinases, such as PKA, PKG, S6K, CaMKII, etc. Phase 3. |
-
Nat Commun, 2024, 15(1):489
-
Nat Commun, 2024, 15(1):3816
-
Nat Commun, 2024, 15(1):3816
|
|
S1113 |
GSK690693
|
GSK690693 is a pan-Akt inhibitor targeting Akt1/2/3 with IC50 of 2 nM/13 nM/9 nM in cell-free assays, also sensitive to the AGC kinase family: PKA, PrkX and PKC isozymes. GSK690693 also potently inhibits AMPK and DAPK3 from the CAMK family with IC50 of 50 nM and 81 nM, respectively. GSK690693 affects Unc-51-like autophagy activating kinase 1 (ULK1) activity, robustly inhibits STING-dependent IRF3 activation. Phase 1. |
-
EMBO J, 2024, 10.1038/s44318-024-00244-9
-
EMBO Mol Med, 2024, 10.1038/s44321-024-00136-9
-
CNS Neurosci Ther, 2024, 30(8):e14913
|
|
S2911 |
Go 6983
|
Go 6983 (GOE 6983, Gö 6983) is a pan-PKC inhibitor against for PKCα, PKCβ, PKCγ and PKCδ with IC50 of 7 nM, 7 nM, 6 nM and 10 nM, respectively; less potent to PKCζ and inactive to PKCμ. |
-
Cell Rep Med, 2023, 10.1016/j.xcrm.2023.101244
-
Cell Rep, 2023, 42(3):112273
-
Elife, 2023, 12e83345
|
|
S2791 |
Sotrastaurin (AEB071)
|
Sotrastaurin (AEB071) is a potent and selective pan-PKC inhibitor, mostly for PKCθ with Ki of 0.22 nM in a cell-free assay; inactive to PKCζ. Phase 2. |
-
Cell Rep, 2024, 43(3):113944
-
Cell Rep, 2024, 43(3):113929
-
bioRxiv, 2024, 2024.09.16.613344
|
|
S1573 |
Fasudil HCl
|
Fasudil HCl, a potent and selective inhibitor of Rho kinase, displays less potent inhibiton over PKA, PKG, PKC and MLCK with Ki of 1.6, 1.6, 3.3, and 36 μM in cell-free assays, respectively. Fasudil is also a calcium channel blocker. |
-
Sci China Life Sci, 2024, 67(8):1549-1562
-
Ren Fail, 2024, 46(2):2396455
-
PeerJ, 2023, 11:e15494
|
|
S1055 |
Enzastaurin
|
Enzastaurin is a potent PKCβ selective inhibitor with IC50 of 6 nM in cell-free assays, 6- to 20-fold selectivity against PKCα, PKCγ and PKCε. Phase 3. |
-
Nat Cell Biol, 2022, 24(1):88-98
-
Oncogene, 2022, 10.1038/s41388-022-02179-z
-
Cancers (Basel), 2022, 14(21)5215
|
|
S7208 |
Bisindolylmaleimide I (GF109203X)
|
Bisindolylmaleimide I (GF109203X, GO 6850) is a potent PKC inhibitor with IC50 of 20 nM, 17 nM, 16 nM, and 20 nM for PKCα, PKCβI, PKCβII, and PKCγ in cell-free assays, respectively, showing more than 3000-fold selectivity for PKC as compared to EGFR, PDGFR and insulin receptor. |
-
Cell Death Dis, 2024, 15(4):274
-
Front Cell Dev Biol, 2024, 12:1356589
-
Nat Commun, 2023, 14(1):4062
|
|
S7791 |
PMA (Phorbol 12-myristate 13-acetate)
|
PMA (Phorbol 12-myristate 13-acetate), a potent activator of PKC, is active at nanomolar concentrations. Phorbol 12-myristate 13-acetate (PMA) induces sphingosine-1-phosphate (S1P).PMA has strong excitability on the skin and mucous membrane. Special protection is required when using PMA. Wear gloves and mask to avoid direct contact in any way. |
-
Cell Rep Med, 2024, 5(8):101686
-
J Exp Clin Cancer Res, 2024, 43(1):105
-
Cell Mol Biol Lett, 2024, 29(1):77
|
|
S2485 |
Mitoxantrone 2HCl
|
Mitoxantrone 2HCl is a dihydrochloride salt of Mitoxantrone. Mitoxantrone is an inhibitor of type II topoisomerase and protein kinase C (PKC) with IC50 of 8.5 μM for PKC. Mitoxantrone inhibits cell proliferative growth of MCF-7/wt cells with IC50 of 0.42 μM. Mitoxantrone also induces apoptosis. |
-
Mol Metab, 2024, 80:101873
-
Blood Adv, 2024, 8(15):4017-4024
-
BMC Pharmacol Toxicol, 2024, 25(1):25
|
|
S8064 |
Midostaurin
|
Midostaurin 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. |
-
Elife, 2024, 12RP90532
-
Blood, 2023, 141(9):1023-1035
-
Nat Commun, 2023, 14(1):5709
|
|
S2391 |
Quercetin
|
Quercetin, a natural flavonoid present in vegetables, fruit and wine, is a stimulator of recombinant SIRT1 and also a PI3K inhibitor with IC50 of 2.4-5.4 μM. Quercetin induces mitophagy, apoptosis and protective autophagy. Phase 4. |
-
Cell Metab, 2024, S1550-4131(24)00371-1
-
Nucleic Acids Res, 2024, gkae322
-
Clin Transl Med, 2024, 14(5):e1660
|
|
S7119 |
Go6976
|
Go6976 (PD406976) is a potent PKC inhibitor with IC50 of 7.9 nM, 2.3 nM, and 6.2 nM for PKC (Rat brain), PKCα, and PKCβ1, respectively. Also a potent inhibitor of JAK2 and Flt3.
|
-
J Cell Sci, 2023, 136(4)jcs259788
-
Sci Adv, 2023, 9(34):eadi5168
-
Sci Adv, 2023, 9(34):eadi5168
|
|
S7207 |
Bisindolylmaleimide IX (Ro 31-8220) Mesylate
|
Bisindolylmaleimide IX (Ro 31-8220 Mesylate) is a pan-PKC inhibitor with IC50 of 5 nM, 24 nM, 14 nM, 27 nM, and 24 nM for PKC-α, PKC-βI, PKC-βII, PKC-γ, and PKC-ε, respectively, and also shows potent inhibition against MAPKAP-K1b, MSK1, GSK3β and S6K1. |
-
Cell Rep, 2023, 42(3):112273
-
Nat Cardiovasc Res, 2023, 2(6):550-571
-
Elife, 2022, 11e80953
|
|
S7663 |
Ruboxistaurin (LY333531) HCl
|
Ruboxistaurin (LY333531) HCl is a β-specific protein kinase C inhibitor. It competitively and reversibly inhibits PKCβ1 and PKCβ2 with IC50 values of 4.7 and 5.9 nM respectively. |
-
Life Sci, 2023, 329:121972
-
bioRxiv, 2023, 10.1101/2023.12.07.570359
-
Cell Rep Methods, 2023, 3(10):100599
|
|
S8388 |
ML-7 HCl
|
ML-7 is an inhibitor of smooth muscle myosin light chain kinase (MLCK) with a Ki value of 0.3 µM and displays reversible, ATP-competitive inhibition of Ca2+-calmodulin-dependent and -independent smooth muscle MLCKs. ML-7 also inhibits PKA and PKC with Ki of 21 μM and 42 μM, respectively. |
-
Ecotoxicol Environ Saf, 2023, 257:114940
-
Mol Biol Cell, 2023, 34(8):ar79
-
Nat Commun, 2022, 13(1):1768
|
|
S7862 |
Rottlerin
|
Rottlerin (Mallotoxin, NSC 56346, NSC 94525), a natural compound purified from Mallotus Philippinensis, is a specific Protein kinase inhibitor with IC50 of 3 μM, 6 μM and 5.3 μM for PKCδ(from baculovirus-infected Sf9 insect cells), PKCδ(from porcine spleen) and CaM kinase III, respectively. Rottlerin also inhibits PKCα, PKCγ, PKCβ, PKCη, CKII and PKA with IC50 of 30 μM, 40 μM, 42 μM, 82 μM, 30 μM and 78 μM, respectively. |
-
Cell Death Discov, 2024, 10(1):263
-
Mol Metab, 2023, 70:101694
-
ACS Appl Mater Interfaces, 2022, 14(21):24144-24159
|
|
S6577 |
PKC-theta inhibitor
|
PKC-theta inhibitor (compound 20) inhibits PKC-θ with an IC50 of 18 nM. |
-
JCI Insight, 2023, 8(4)e164793
-
Int J Mol Sci, 2023, 24(15)11970
-
Commun Biol, 2022, 5(1):795
|
|
S2554 |
Daphnetin
|
Daphnetin, a natural coumarin derivative, is a protein kinase inhibitor, inhibits EGFR, PKA and PKC with IC50 of 7.67 μM, 9.33 μM and 25.01 μM, respectively, also known to exhibit anti-inflammatory and anti-oxidant activities. |
-
Sci Rep, 2021, 11(1):11491
-
Acta Neuropathol, 2020, 10.1007/s00401-020-02226-7
-
Int Immunopharmacol, 2019, 72:195-203
|
|
S1292 |
Chelerythrine Chloride (NSC 646662)
|
Chelerythrine Chloride (NSC 646662, Broussonpapyrine) is a potent, selective antagonist of PKC with IC50 of 0.66 μM. |
-
J Headache Pain, 2023, 24(1):49
-
Nutr Neurosci, 2022, 1-19
-
J Biol Chem, 2015, 290(34):20841-55
|
|
S6723 |
Darovasertib (LXS-196)
|
Darovasertib (LXS-196, IDE-196) is a selective inhibitor of protein kinase C (PKC). |
-
Cell Rep Med, 2023, 10.1016/j.xcrm.2023.101244
-
Cell Mol Biol Lett, 2023, 28(1):24
-
Commun Biol, 2022, 5(1):795
|
|
S4066 |
Dequalinium Chloride
|
Dequalinium Chloride is a PKC inhibitor with IC50 of 7-18 μM, and also a selective blocker of apamin-sensitive K+ channels with IC50 of 1.1 μM. |
-
Nat Commun, 2024, 15(1):686
-
Neoplasia, 2020, 22(10):470-483
-
Vet Microbiol, 2020, 251:108913
|
|
S2327 |
Myricitrin
|
Myricitrin (Myricitrine), a flavonoid compound isolated from the root bark of Myrica cerifera, which exerts antinociceptive effects. |
-
Front Pharmacol, 2024, 15:1372094
-
Molecules, 2023, 28(3)1444
-
Molecules, 2021, 26(5)1210
|
|
S0754 |
Bisindolylmaleimide IV
|
Bisindolylmaleimide IV (Arcyriarubin A, BIM IV, Compound 5/1a) is a potent inhibitor of protein kinase C (PKC) with IC50 of 0.55 μM. Bisindolylmaleimide IV also inhibits PKA with IC50 of 11.8μM. Bisindolylmaleimide IV is a potent, selective inhibitor of human cytomegalovirus (HCMV) replication in cell culture with IC50 of 0.2 μM. |
-
Elife, 2021, 10e68473
|
|
S9101 |
Ingenol
|
Ingenol, a plant-derived diterpenoid, is a weak PKC activator and possesses important anticancer activity. |
-
Sci Rep, 2020, 10(1):13124
|
|
S0069 |
VTX-27
|
VTX-27 (Compound 27) is a potent and selective inhibitor of protein kinase C θ (PKC θ) with Ki of 0.08 nM and 16 nM for PKC θ and PKC δ, respectively. |
-
Elife, 2021, 10e68473
|
|
E0124 |
Chelerythrine
|
Chelerythrine (Toddaline, Broussonpapyrine) is a potent, selective antagonist of PKC with an IC50 of 0.66 μM. Chelerythrine also inhibits the BclXL-Bak BH3 peptide binding with an IC50 of 1.5 μM. Chelerythrine shows antitumor, antidiabetic and anti-inflammatory activity.
|
-
Nutr Neurosci, 2022, 1-19
|
|
S7074 |
Ionomycin
|
Ionomycin (SQ23377) is a potent and selective calcium ionophore and an antibiotic produced by Streptomyces conglobatus. It induces the activation of protein kinase C (PKC) and promotes apoptosis. |
-
Diabetes, 2024, db231000
-
Am J Physiol Cell Physiol, 2020, 10.1152/ajpcell.00290.2020
|
|
S3289 |
Daphnoretin
|
Daphnoretin (Dephnoretin, Thymelol), a biologically active compound isolated from Wikstroemia indica C.A. Mey., is a protein kinase C (PKC) activator. Daphnoretin inhibits the proliferation, invasion, and migration of tumor cells and promote its apoptosis by regulating the activity of Akt signal pathway. |
|
|
S3273 |
Hypericin
|
Hypericin (Hyp, HY) is a naturally occurring substance found in the common St. John's Wort (Hypericum species) with antidepressive, antineoplastic and antiviral (human immunodeficiency and hepatitis C virus) activities. Hypericin has inhibitory effects on MAO (monoaminoxidase), PKC (protein kinase C), dopamine-beta-hydroxylase, reverse transcriptase, telomerase and CYP (cytochrome P450). |
-
Eur J Pharmacol, 2021, 900:174071
|
|
S9522 |
Valrubicin
|
Valrubicin(AD-32) is a chemotherapy drug used to treat bladder cancer. Valrubicin is a chemotherapy agent, inhibits TPA- and PDBu-induced PKC activation with IC50s of 0.85 and 1.25 μM, respectively. |
|
|
S3819 |
Decursinol angelate
|
Decursinol angelate is a cytotoxic and protein kinase C activating agent from the root of Angelica gigas. |
|
|
E2368 |
N-Desmethyltamoxifen hydrochloride
|
N-Desmethyltamoxifen hydrochloride (N-Desmethyl tamoxifen HCl), the primary metabolite of tamoxifen, is an estrogen response modifer and protein kinase C inhibitor with IC50 of 25 µM. |
|
|
S0780 |
Oncrasin-1
|
Oncrasin-1 (Onc-1) is a potent RNA polymerase II inhibitor with antitumor activity that kills various human lung cancer cells with K-Ras mutations. Oncrasin-1 drives abnormal aggregation of protein kinase C iota (PKCι) in nucleus of sensitive cells but not in resistant cells. |
|
|
E0010 |
Hypocrellin A
|
Hypocrellin A (HA) is a perylenequinone isolated from Shiraia bambusicola that shows antiviral, antimicrobial and anticancer activity through mediating multiple signaling pathways. Hypocrellin A also is a selective and potent inhibitor of PKC. |
|
|
E2403 |
ζ-Stat (NSC37044)
|
ζ-Stat (NSC37044) is a specific and atypical protein kinase Cζ (PKCζ) inhibitor, with an IC50 of 5 μM. |
|
|
E0067New |
Hispidin
|
Hispidin is a phenolic compound from Phellinus linteus (a medicinal mushroom) and a potent inhibitor of protein kinase Cβ(PKC) with an IC50 of 2 μM, respectively. It also inhibits beta-secretase (BACE1) and prolyl endopeptidase(PE) with IC50 values of 4.9 μM and 16 μM respectively. It exhibits strong anti-oxidant, anti-cancer, anti-diabetic, anti-dementia, anti-inflammatory, anti-apoptotic, and antiviral properties. |
|
|
S3661 |
2-Methoxy-1,4-naphthoquinone
|
2-Methoxy-1,4-naphthoquinone, isolated from the leaves of Impatiens glandulifera, specifically suppressed the expression of PKC βI, δ, and ζ in a concentration-dependent manner in Raji cells. |
|
|
S6424 |
TAS-301
|
TAS-301 is an inhibitor of smooth muscle cell migration and proliferation. TAS-301 inhibits intimal thickening after balloon injury to rat carotid arteries, and inhibits PKC activation induced by PDGF. |
|
|
E2510 |
WAY-301398
|
WAY-301398 (6-methoxynaphthalene) can bind to protein kinase C (PKC). |
|
|
S7859 |
WAY-354831
|
WAY-354831 exhibits antibacterial activity. |
|
|
E3408 |
Radix Euphorbiae Ebracteolatae Extract
|
Radix Euphorbiae Ebracteolatae Extract is extracted from Radix Euphorbiae Ebracteolatae, which modulates aquaporins via inhibiting PKC activity in the kidney. |
|
|
S2323 |
Methyl-Hesperidin
|
Methyl Hesperidin is a flavanone glycoside (flavonoid) (C28H34O15) found abundantly in citrus fruits. Its aglycone form is called hesperetin. |
|
|
E2506 |
A-3 hydrochloride
|
A-3 hydrochloride, a potent, cell-permeable, reversible, ATP-competitive non-selective antagonist of various kinases, againsts cAMP-dependent protein kinase (PKA) (Ki=4.3 µM), casein kinase II (CK2) (Ki=5.1 µM) and myosin light chain kinase (MLCK) (Ki=7.4 µM), also inhibits Protein Kinase C (PKC) and casein kinase I (CK1) with Ki values of 47 µM and 80 µM, respectively. |
|
|
S6214 |
H-1152 dihydrochloride
|
H-1152 dihydrochloride (2HCl) is a membrane-permeable and selective inhibitor of Rho-associated protein kinase (ROCK). H-1152 inhibits ROCK2, PKA, PKC, PKG, AuroraA and CaMK2 with IC50 of 0.0120 μM, 3.03 μM, 5.68 μM, 0.360 μM, 0.745 μM and 0.180 μM, respectively. |
|
|
S2964 |
HA-100 dihydrochloride
|
HA-100 dihydrochloride is an inhibitor of cGMP-dependent protein kinase (PKG), cAMP-dependent protein kinase (PKA), protein kinase C (PKC) and MLC-kinase with IC50 of 4 μM, 8 μM, 12 μM and 240 μM, respectively. |
-
Adv Sci (Weinh), 2024, 11(4):e2304987
|
|
E2839 |
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, also exerting IC50s of 53, 195, 163, 213, and 175 nM for PKC-α, PKC-βI, PKC-βII, PKC-γ, PKC-ε, respectively. |
|
|
E0786 |
N-Desmethyltamoxifen
|
N-Desmethyltamoxifen, the major metabolite of Tamoxifen in humans and a ten-fold more potent protein kinase C (PKC) inhibitor than Tamoxifen, also is a potent regulator of ceramide metabolism in human AML cells, limiting ceramide glycosylation, hydrolysis, and sphingosine phosphorylation. |
|
|
S1421 |
Staurosporine (STS)
|
Staurosporine (STS) is a potent PKC inhibitor for PKCα, PKCγ and PKCη with IC50 of 2 nM, 5 nM and 4 nM, less potent to PKCδ (20 nM), PKCε (73 nM) and little active to PKCζ (1086 nM) in cell-free assays. Also shows inhibitory activities on other kinases, such as PKA, PKG, S6K, CaMKII, etc. Phase 3. |
- Nat Commun, 2024, 15(1):489
- Nat Commun, 2024, 15(1):3816
- Nat Commun, 2024, 15(1):3816
|
|
S1113 |
GSK690693
|
GSK690693 is a pan-Akt inhibitor targeting Akt1/2/3 with IC50 of 2 nM/13 nM/9 nM in cell-free assays, also sensitive to the AGC kinase family: PKA, PrkX and PKC isozymes. GSK690693 also potently inhibits AMPK and DAPK3 from the CAMK family with IC50 of 50 nM and 81 nM, respectively. GSK690693 affects Unc-51-like autophagy activating kinase 1 (ULK1) activity, robustly inhibits STING-dependent IRF3 activation. Phase 1. |
- EMBO J, 2024, 10.1038/s44318-024-00244-9
- EMBO Mol Med, 2024, 10.1038/s44321-024-00136-9
- CNS Neurosci Ther, 2024, 30(8):e14913
|
|
S2911 |
Go 6983
|
Go 6983 (GOE 6983, Gö 6983) is a pan-PKC inhibitor against for PKCα, PKCβ, PKCγ and PKCδ with IC50 of 7 nM, 7 nM, 6 nM and 10 nM, respectively; less potent to PKCζ and inactive to PKCμ. |
- Cell Rep Med, 2023, 10.1016/j.xcrm.2023.101244
- Cell Rep, 2023, 42(3):112273
- Elife, 2023, 12e83345
|
|
S2791 |
Sotrastaurin (AEB071)
|
Sotrastaurin (AEB071) is a potent and selective pan-PKC inhibitor, mostly for PKCθ with Ki of 0.22 nM in a cell-free assay; inactive to PKCζ. Phase 2. |
- Cell Rep, 2024, 43(3):113944
- Cell Rep, 2024, 43(3):113929
- bioRxiv, 2024, 2024.09.16.613344
|
|
S1573 |
Fasudil HCl
|
Fasudil HCl, a potent and selective inhibitor of Rho kinase, displays less potent inhibiton over PKA, PKG, PKC and MLCK with Ki of 1.6, 1.6, 3.3, and 36 μM in cell-free assays, respectively. Fasudil is also a calcium channel blocker. |
- Sci China Life Sci, 2024, 67(8):1549-1562
- Ren Fail, 2024, 46(2):2396455
- PeerJ, 2023, 11:e15494
|
|
S1055 |
Enzastaurin
|
Enzastaurin is a potent PKCβ selective inhibitor with IC50 of 6 nM in cell-free assays, 6- to 20-fold selectivity against PKCα, PKCγ and PKCε. Phase 3. |
- Nat Cell Biol, 2022, 24(1):88-98
- Oncogene, 2022, 10.1038/s41388-022-02179-z
- Cancers (Basel), 2022, 14(21)5215
|
|
S7208 |
Bisindolylmaleimide I (GF109203X)
|
Bisindolylmaleimide I (GF109203X, GO 6850) is a potent PKC inhibitor with IC50 of 20 nM, 17 nM, 16 nM, and 20 nM for PKCα, PKCβI, PKCβII, and PKCγ in cell-free assays, respectively, showing more than 3000-fold selectivity for PKC as compared to EGFR, PDGFR and insulin receptor. |
- Cell Death Dis, 2024, 15(4):274
- Front Cell Dev Biol, 2024, 12:1356589
- Nat Commun, 2023, 14(1):4062
|
|
S2485 |
Mitoxantrone 2HCl
|
Mitoxantrone 2HCl is a dihydrochloride salt of Mitoxantrone. Mitoxantrone is an inhibitor of type II topoisomerase and protein kinase C (PKC) with IC50 of 8.5 μM for PKC. Mitoxantrone inhibits cell proliferative growth of MCF-7/wt cells with IC50 of 0.42 μM. Mitoxantrone also induces apoptosis. |
- Mol Metab, 2024, 80:101873
- Blood Adv, 2024, 8(15):4017-4024
- BMC Pharmacol Toxicol, 2024, 25(1):25
|
|
S8064 |
Midostaurin
|
Midostaurin 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. |
- Elife, 2024, 12RP90532
- Blood, 2023, 141(9):1023-1035
- Nat Commun, 2023, 14(1):5709
|
|
S2391 |
Quercetin
|
Quercetin, a natural flavonoid present in vegetables, fruit and wine, is a stimulator of recombinant SIRT1 and also a PI3K inhibitor with IC50 of 2.4-5.4 μM. Quercetin induces mitophagy, apoptosis and protective autophagy. Phase 4. |
- Cell Metab, 2024, S1550-4131(24)00371-1
- Nucleic Acids Res, 2024, gkae322
- Clin Transl Med, 2024, 14(5):e1660
|
|
S7119 |
Go6976
|
Go6976 (PD406976) is a potent PKC inhibitor with IC50 of 7.9 nM, 2.3 nM, and 6.2 nM for PKC (Rat brain), PKCα, and PKCβ1, respectively. Also a potent inhibitor of JAK2 and Flt3.
|
- J Cell Sci, 2023, 136(4)jcs259788
- Sci Adv, 2023, 9(34):eadi5168
- Sci Adv, 2023, 9(34):eadi5168
|
|
S7207 |
Bisindolylmaleimide IX (Ro 31-8220) Mesylate
|
Bisindolylmaleimide IX (Ro 31-8220 Mesylate) is a pan-PKC inhibitor with IC50 of 5 nM, 24 nM, 14 nM, 27 nM, and 24 nM for PKC-α, PKC-βI, PKC-βII, PKC-γ, and PKC-ε, respectively, and also shows potent inhibition against MAPKAP-K1b, MSK1, GSK3β and S6K1. |
- Cell Rep, 2023, 42(3):112273
- Nat Cardiovasc Res, 2023, 2(6):550-571
- Elife, 2022, 11e80953
|
|
S7663 |
Ruboxistaurin (LY333531) HCl
|
Ruboxistaurin (LY333531) HCl is a β-specific protein kinase C inhibitor. It competitively and reversibly inhibits PKCβ1 and PKCβ2 with IC50 values of 4.7 and 5.9 nM respectively. |
- Life Sci, 2023, 329:121972
- bioRxiv, 2023, 10.1101/2023.12.07.570359
- Cell Rep Methods, 2023, 3(10):100599
|
|
S8388 |
ML-7 HCl
|
ML-7 is an inhibitor of smooth muscle myosin light chain kinase (MLCK) with a Ki value of 0.3 µM and displays reversible, ATP-competitive inhibition of Ca2+-calmodulin-dependent and -independent smooth muscle MLCKs. ML-7 also inhibits PKA and PKC with Ki of 21 μM and 42 μM, respectively. |
- Ecotoxicol Environ Saf, 2023, 257:114940
- Mol Biol Cell, 2023, 34(8):ar79
- Nat Commun, 2022, 13(1):1768
|
|
S7862 |
Rottlerin
|
Rottlerin (Mallotoxin, NSC 56346, NSC 94525), a natural compound purified from Mallotus Philippinensis, is a specific Protein kinase inhibitor with IC50 of 3 μM, 6 μM and 5.3 μM for PKCδ(from baculovirus-infected Sf9 insect cells), PKCδ(from porcine spleen) and CaM kinase III, respectively. Rottlerin also inhibits PKCα, PKCγ, PKCβ, PKCη, CKII and PKA with IC50 of 30 μM, 40 μM, 42 μM, 82 μM, 30 μM and 78 μM, respectively. |
- Cell Death Discov, 2024, 10(1):263
- Mol Metab, 2023, 70:101694
- ACS Appl Mater Interfaces, 2022, 14(21):24144-24159
|
|
S6577 |
PKC-theta inhibitor
|
PKC-theta inhibitor (compound 20) inhibits PKC-θ with an IC50 of 18 nM. |
- JCI Insight, 2023, 8(4)e164793
- Int J Mol Sci, 2023, 24(15)11970
- Commun Biol, 2022, 5(1):795
|
|
S2554 |
Daphnetin
|
Daphnetin, a natural coumarin derivative, is a protein kinase inhibitor, inhibits EGFR, PKA and PKC with IC50 of 7.67 μM, 9.33 μM and 25.01 μM, respectively, also known to exhibit anti-inflammatory and anti-oxidant activities. |
- Sci Rep, 2021, 11(1):11491
- Acta Neuropathol, 2020, 10.1007/s00401-020-02226-7
- Int Immunopharmacol, 2019, 72:195-203
|
|
S1292 |
Chelerythrine Chloride (NSC 646662)
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Chelerythrine Chloride (NSC 646662, Broussonpapyrine) is a potent, selective antagonist of PKC with IC50 of 0.66 μM. |
- J Headache Pain, 2023, 24(1):49
- Nutr Neurosci, 2022, 1-19
- J Biol Chem, 2015, 290(34):20841-55
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S6723 |
Darovasertib (LXS-196)
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Darovasertib (LXS-196, IDE-196) is a selective inhibitor of protein kinase C (PKC). |
- Cell Rep Med, 2023, 10.1016/j.xcrm.2023.101244
- Cell Mol Biol Lett, 2023, 28(1):24
- Commun Biol, 2022, 5(1):795
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S4066 |
Dequalinium Chloride
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Dequalinium Chloride is a PKC inhibitor with IC50 of 7-18 μM, and also a selective blocker of apamin-sensitive K+ channels with IC50 of 1.1 μM. |
- Nat Commun, 2024, 15(1):686
- Neoplasia, 2020, 22(10):470-483
- Vet Microbiol, 2020, 251:108913
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S2327 |
Myricitrin
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Myricitrin (Myricitrine), a flavonoid compound isolated from the root bark of Myrica cerifera, which exerts antinociceptive effects. |
- Front Pharmacol, 2024, 15:1372094
- Molecules, 2023, 28(3)1444
- Molecules, 2021, 26(5)1210
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S0754 |
Bisindolylmaleimide IV
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Bisindolylmaleimide IV (Arcyriarubin A, BIM IV, Compound 5/1a) is a potent inhibitor of protein kinase C (PKC) with IC50 of 0.55 μM. Bisindolylmaleimide IV also inhibits PKA with IC50 of 11.8μM. Bisindolylmaleimide IV is a potent, selective inhibitor of human cytomegalovirus (HCMV) replication in cell culture with IC50 of 0.2 μM. |
- Elife, 2021, 10e68473
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S0069 |
VTX-27
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VTX-27 (Compound 27) is a potent and selective inhibitor of protein kinase C θ (PKC θ) with Ki of 0.08 nM and 16 nM for PKC θ and PKC δ, respectively. |
- Elife, 2021, 10e68473
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S3273 |
Hypericin
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Hypericin (Hyp, HY) is a naturally occurring substance found in the common St. John's Wort (Hypericum species) with antidepressive, antineoplastic and antiviral (human immunodeficiency and hepatitis C virus) activities. Hypericin has inhibitory effects on MAO (monoaminoxidase), PKC (protein kinase C), dopamine-beta-hydroxylase, reverse transcriptase, telomerase and CYP (cytochrome P450). |
- Eur J Pharmacol, 2021, 900:174071
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S9522 |
Valrubicin
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Valrubicin(AD-32) is a chemotherapy drug used to treat bladder cancer. Valrubicin is a chemotherapy agent, inhibits TPA- and PDBu-induced PKC activation with IC50s of 0.85 and 1.25 μM, respectively. |
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E2368 |
N-Desmethyltamoxifen hydrochloride
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N-Desmethyltamoxifen hydrochloride (N-Desmethyl tamoxifen HCl), the primary metabolite of tamoxifen, is an estrogen response modifer and protein kinase C inhibitor with IC50 of 25 µM. |
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S0780 |
Oncrasin-1
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Oncrasin-1 (Onc-1) is a potent RNA polymerase II inhibitor with antitumor activity that kills various human lung cancer cells with K-Ras mutations. Oncrasin-1 drives abnormal aggregation of protein kinase C iota (PKCι) in nucleus of sensitive cells but not in resistant cells. |
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E0010 |
Hypocrellin A
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Hypocrellin A (HA) is a perylenequinone isolated from Shiraia bambusicola that shows antiviral, antimicrobial and anticancer activity through mediating multiple signaling pathways. Hypocrellin A also is a selective and potent inhibitor of PKC. |
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E2403 |
ζ-Stat (NSC37044)
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ζ-Stat (NSC37044) is a specific and atypical protein kinase Cζ (PKCζ) inhibitor, with an IC50 of 5 μM. |
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E0067New |
Hispidin
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Hispidin is a phenolic compound from Phellinus linteus (a medicinal mushroom) and a potent inhibitor of protein kinase Cβ(PKC) with an IC50 of 2 μM, respectively. It also inhibits beta-secretase (BACE1) and prolyl endopeptidase(PE) with IC50 values of 4.9 μM and 16 μM respectively. It exhibits strong anti-oxidant, anti-cancer, anti-diabetic, anti-dementia, anti-inflammatory, anti-apoptotic, and antiviral properties. |
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S3661 |
2-Methoxy-1,4-naphthoquinone
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2-Methoxy-1,4-naphthoquinone, isolated from the leaves of Impatiens glandulifera, specifically suppressed the expression of PKC βI, δ, and ζ in a concentration-dependent manner in Raji cells. |
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S6424 |
TAS-301
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TAS-301 is an inhibitor of smooth muscle cell migration and proliferation. TAS-301 inhibits intimal thickening after balloon injury to rat carotid arteries, and inhibits PKC activation induced by PDGF. |
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E3408 |
Radix Euphorbiae Ebracteolatae Extract
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Radix Euphorbiae Ebracteolatae Extract is extracted from Radix Euphorbiae Ebracteolatae, which modulates aquaporins via inhibiting PKC activity in the kidney. |
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S6214 |
H-1152 dihydrochloride
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H-1152 dihydrochloride (2HCl) is a membrane-permeable and selective inhibitor of Rho-associated protein kinase (ROCK). H-1152 inhibits ROCK2, PKA, PKC, PKG, AuroraA and CaMK2 with IC50 of 0.0120 μM, 3.03 μM, 5.68 μM, 0.360 μM, 0.745 μM and 0.180 μM, respectively. |
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S2964 |
HA-100 dihydrochloride
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HA-100 dihydrochloride is an inhibitor of cGMP-dependent protein kinase (PKG), cAMP-dependent protein kinase (PKA), protein kinase C (PKC) and MLC-kinase with IC50 of 4 μM, 8 μM, 12 μM and 240 μM, respectively. |
- Adv Sci (Weinh), 2024, 11(4):e2304987
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E2839 |
Bisindolylmaleimide VIII (acetate)
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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, also exerting IC50s of 53, 195, 163, 213, and 175 nM for PKC-α, PKC-βI, PKC-βII, PKC-γ, PKC-ε, respectively. |
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E0786 |
N-Desmethyltamoxifen
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N-Desmethyltamoxifen, the major metabolite of Tamoxifen in humans and a ten-fold more potent protein kinase C (PKC) inhibitor than Tamoxifen, also is a potent regulator of ceramide metabolism in human AML cells, limiting ceramide glycosylation, hydrolysis, and sphingosine phosphorylation. |
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