PKC
Signaling Pathway Map
Research Area
- Inhibitory Selectivity
- Solubility
| Catalog No. | Product Name | Solubility(25°C) | ||
|---|---|---|---|---|
| Water | DMSO | Alcohol | ||
| S1055 | Enzastaurin (LY317615) | <1 mg/mL | 30 mg/mL | <1 mg/mL |
| S2791 | Sotrastaurin | <1 mg/mL | 87 mg/mL | 2 mg/mL |
| S1421 | Staurosporine | <1 mg/mL | 4 mg/mL | <1 mg/mL |
| S2911 | Go 6983 | <1 mg/mL | 59 mg/mL | <1 mg/mL |
| S7208 | Bisindolylmaleimide I (GF109203X) | <1 mg/mL | 82 mg/mL | <1 mg/mL |
| S3661 | 2-Methoxy-1,4-naphthoquinone | <1 mg/mL | 37 mg/mL | 3 mg/mL |
| S7207 | Bisindolylmaleimide IX (Ro 31-8220 Mesylate) | <1 mg/mL | 100 mg/mL | <1 mg/mL |
| S2554 | Daphnetin | <1 mg/mL | 35 mg/mL | <1 mg/mL |
| S4066 | Dequalinium Chloride | <1 mg/mL | 0.025 mg/mL | <1 mg/mL |
| S2391 | Quercetin | <1 mg/mL | 61 mg/mL | 10 mg/mL |
| S2327 | Myricitrin | <1 mg/mL | 93 mg/mL | 1 mg/mL |
| S7663 | Ruboxistaurin (LY333531 HCl) | <1 mg/mL | 50 mg/mL | <1 mg/mL |
| S7119 | Go6976 | <1 mg/mL | 18 mg/mL | <1 mg/mL |
| S8064 | Midostaurin (PKC412) | <1 mg/mL | 100 mg/mL | 20 mg/mL |
| S3819 | Decursinol angelate | -1 mg/mL | 65 mg/mL | -1 mg/mL |
- PKC Inhibitors (15)
- New PKC Products
| Catalog No. | Information | Product Use Citations | Product Validations |
|---|---|---|---|
| S1055 |
Enzastaurin (LY317615)Enzastaurin (LY317615) 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. |
The protein kinase C (PKC)–specific inhibitor enzastaurin
induces apoptosis of lupus B cells and prevents lupus development
in Sle mice. C, Levels of serum IgG anti–double-stranded DNA
(anti-dsDNA) and antihistone/anti-dsDNA autoantibodies from
vehicle-treated control mice and enzastaurin-treated mice, as analyzed
by enzyme-linked immunosorbent assay. Bars in A–C show the mean
SD of 3 independent experiments. D, Representative immunofluorescent
images of IgG deposition (top) and glomeruli (bottom) in kidney
sections from Sle1.Sle3 mice treated with vehicle or enzastaurin. Original
magnification 20 (top); 40 (bottom). PAS periodic acid–Schiff.
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|
| S2791 |
SotrastaurinSotrastaurin 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. |
Lysates from H3122 and MGH006 cells treated with 1 µM PMA in the presence or absence of 0.3 µM sotrastaurin (SOT) were fractionated. Immunoblotting was performed with the indicated antibodies.
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|
| S1421 |
StaurosporineStaurosporine 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. |
Intracellular concentration of HSF1-phosphoserine 326, total HSF1, S6 kinase-phosphothreonine-389, total S6 kinase and β-actin, without or with heat shock in HeLa cells pretreated with mTOR inhibitors rapamycin (30 nM) and KU0063794 (2 uM) and kinase inhibitor staurosporine (100 nM) for 2 hr. Relative levels of HSF1-phosphoserine 326 in cells after the various treatments were determined by densitometric analysis of X-ray films, normalized to untreated cells (lane 1), and are indicated below the representation of the immunoblots.
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| S2911 |
Go 6983Go 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. |
(a) In vitro kinase reactions were performed by using GSTp531-64 (FP267) as substrate and GST-CK1δ (FP449) as enzyme, or using (b) GST-CK1δ375–428 (FP1183) as substrate and recombinant PKCα as enzyme in combination with one of three PKC-specific inhibitors (Go-6983, enzastaurin, and bisindolylmaleimide I (BIM I), respectively). Data are presented as normalized bar graph.
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| S7208 |
Bisindolylmaleimide I (GF109203X)Bisindolylmaleimide I (GF109203X) 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. |
(b) Western blotting showing that PKC inhibitor increased GLT-1 and GLAST expression in MPP+-treated astrocytes. Results are expressed as the mean±S.E. of at least three experiments. One-way ANOVA. **P<0.01, *P<0.05, #P<0.05. *Represents a significant difference between other group and control group; while #represents a significant difference between the indicated group and MPP+-treated astrocytes for 24 h.
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| S3661New |
2-Methoxy-1,4-naphthoquinone2-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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| 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. |
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| S2554 |
DaphnetinDaphnetin, 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. |
C57/BL6 mice (5 mice/group) were intraperitoneally injected with daphnetin (DFN, 5 mg/kg) or DMSO, and then challenged with LPS (37.5 mg/kg) or saline. 16 h after LPS challenge, mice were sacrificed, and then lung and serum were collected. c, Representative photomicrographs showed H&E staining of lung tissue.
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| S4066 |
Dequalinium ChlorideDequalinium 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. |
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| S2391 |
QuercetinQuercetin, 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. Phase 4. |
After starved in serum-free medium for 24h,A549 cells incubated with the indicated concentrations of Quercetin for 3h,followed by 20-minute stimolation of 100ng/ml EGF. |
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| S2327 |
MyricitrinMyricitrin, a flavonoid compound isolated from the root bark of Myrica cerifera, which exerts antinociceptive effects. |
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| S7663 |
Ruboxistaurin (LY333531 HCl)LY333531 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. |
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| S7119 |
Go6976Go6976 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. |
Erk5 activation depends on Mek5, classical PKC and Mek1/2. MOVAS cells were serum-starved overnight and then treated for 1 h if not indicated otherwise with inhibitors targeting Jnk (SP600125, 10 μM), p38 (SB203580, 10 μM), Mek1/2 (CI-1040, 3 μM), Jak2 (AG490, 10 μM), Src (SU6656, 0.5 μM), Go6983 (PKC, 1 μM), Gö6976 (classical PKC, 1 μM), proteasomes (MG132, 25 μM), TPA (100 ng/ml for 15 min to activate PKCs or overnight to inhibit) and Mek5 (BIX02189, 1 μM), as well as Ca2 + chelators (EDTA, 2 mM; BAPTA-AM, 10 μM; both with 30 min preincubation), followed by stimulation with 20 ng/ml PDGF-BB for 10 min. Total cell lysates (TCL) were prepared and subjected to SDS-PAGE. Erk5 and PDGFRβ activities were measured by band shift and Tyr857 phosphorylation, respectively, using immunoblotting. Panel E and G show representative immunoblots. |
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| S8064 |
Midostaurin (PKC412)Midostaurin (pkc412) 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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| S3819New |
Decursinol angelateDecursinol angelate is a cytotoxic and protein kinase C activating agent from the root of Angelica gigas. |
