| S2911 |
Go 6983
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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; this compound is less potent to PKCζ and inactive to PKCμ.
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Nat Biotechnol, 2025, 10.1038/s41587-025-02833-3
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Nat Commun, 2025, 16(1):3874
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Nucleic Acids Res, 2025, 53(8)gkaf349
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| S1055 |
Enzastaurin
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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.
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Nat Commun, 2025, 16(1):3874
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Neuro Oncol, 2025, noaf200
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Cell Rep Med, 2025, S2666-3791(25)00102-8
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| S7791 |
PMA chemical (Phorbol 12-myristate 13-acetate)
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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.
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Protein Cell, 2025, pwaf020
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Nat Commun, 2025, 16(1):8054
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Cancer Commun (Lond), 2025, 10.1002/cac2.70036
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| S6723 |
Darovasertib (LXS196)
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Darovasertib (LXS-196, IDE-196) is a selective inhibitor of protein kinase C (PKC).
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bioRxiv, 2024, 2024.09.26.615160
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Cell Rep Med, 2023, 10.1016/j.xcrm.2023.101244
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Cell Mol Biol Lett, 2023, 28(1):24
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| S1421 |
Staurosporine (STS)
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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. This compound also shows inhibitory activities on other kinases, such as PKA, PKG, S6K, CaMKII, etc. Phase 3.
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Cell Metab, 2025, S1550-4131(25)00149-4
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Mol Cell, 2025, 85(19):3711-3728.e11
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EMBO J, 2025, 10.1038/s44318-025-00526-w
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| S2391 |
Quercetin (Sophoretin)
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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.
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Alzheimers Res Ther, 2025, 17(1):176
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Cell Mol Life Sci, 2025, 82(1):164
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Virol Sin, 2025, S1995-820X(25)00102-6
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| S2791 |
Sotrastaurin (AEB071)
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A potent and selective pan-PKC inhibitor, Sotrastaurin (AEB071) mostly targets PKCθ with a Ki of 0.22 nM in a cell-free assay; it is inactive to PKCζ. This compound has reached Phase 2.
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Proc Natl Acad Sci U S A, 2025, 122(8):e2421717122
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iScience, 2025, 28(6):112753
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Cell Signal, 2025, 135:112051
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| S7208 |
Bisindolylmaleimide I (GF109203X)
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Bisindolylmaleimide I (GF109203X, GO 6850) is a potent PKC inhibitor with IC50 values of 20 nM, 17 nM, 16 nM, and 20 nM for PKCα, PKCβI, PKCβII, and PKCγ in cell-free assays, respectively. This compound shows more than 3000-fold selectivity for PKC as compared to EGFR, PDGFR and insulin receptor.
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J Neuroinflammation, 2025, 22(1):121
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Commun Biol, 2025, 8(1):1267
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Cell Death Dis, 2024, 15(4):274
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| S8064 |
Midostaurin (PKC412)
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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.
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Blood Adv, 2025, bloodadvances.2024015427
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Onco Targets Ther, 2025, 18:489-501
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Blood Cancer J, 2024, 14(1):207
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| S7119 |
Go6976
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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.
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FASEB J, 2025, 39(12):e70768
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FASEB J, 2025, 39(12):e70768
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bioRxiv, 2025, 2025.02.02.636139
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