There are 5 isoforms in the Ser/Thr PKC family which is involved in cell proliferation, differentiation, apoptosis, angiogenesis and tumor promotion. The priming of PKC isoforms seems to require two upstream kinases which are phosphoinositide-dependent protein kinase 1 (PDK1) and mammalian target of rapamycin 2 complex (mTORC2). PKCs can also be activated directly by G proteins (GPCR). PKC is involved in cell migration by regulating cytoskeletal dynamics, and PKC can regulate CD44, a cell surface protein, in cell -ECM interaction. PKC is involved in the activation of the transcription factors nuclear factor-κB (NF-κB), nuclear factor of activated T cells (NFAT) activator protein 1 (AP1), and MET signaling. When MET is activated by HGF, MET is depend on PKC and microtubule network to accumulate and promote the entry of STAT3 into nucleus.
PKC inhibitors
Other TGF-beta/Smad Inhibitors
| Cat.No. | Product Name | Information | Product Use Citations | Product Validations |
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| S6723 | Darovasertib (LXS196) | Darovasertib (LXS-196, IDE-196) is a selective inhibitor of protein kinase C (PKC). |
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| S7791 | PMA chemical (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 a mask to avoid direct contact in any way. |
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| 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. |
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| S2911 | Go 6983 | Go 6983 (GOE 6983, Gö 6983) is a pan-PKC inhibitor against 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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| 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. This compound also shows inhibitory activities on other kinases, such as PKA, PKG, S6K, CaMKII, etc. Phase 3. |
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| S2391 | Quercetin (Sophoretin) | 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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| S2791 | Sotrastaurin (AEB071) | 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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| S7208 | Bisindolylmaleimide I (GF109203X) | Bisindolylmaleimide I (GF109203X, GO 6850) is a potent PKC inhibitor with IC50 values of 20 nM, 17 nM, 16 nM, and 20 nM for PKC , PKC I, PKC II, and PKC 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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| S8064 | Midostaurin (PKC412) | 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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| 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. |
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