- Inhibitory Selectivity
|Catalog No.||Product Name||Solubility(25°C)|
|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|
|S1292||Chelerythrine Chloride||<1 mg/mL||3 mg/mL||<1 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|
|S3661||2-Methoxy-1,4-naphthoquinone||<1 mg/mL||37 mg/mL||3 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|
|S9101||Ingenol||<1 mg/mL||69 mg/mL||70 mg/mL|
|S3819||Decursinol angelate||-1 mg/mL||65 mg/mL||-1 mg/mL|
- PKC Inhibitors (17)
- New PKC Products
|Catalog No.||Information||Product Use Citations||Product Validations|
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.
Sotrastaurin 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.
Staurosporine 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.
Caspase-8, 9, 3, 6, PARP, and cleaved PARP were detected in POTEG overexpressed cells and control cells with or without STS treatment.
Go 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.
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.
Chelerythrine is a potent, selective antagonist of PKC with IC50 of 0.66 mM.
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.
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.
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.
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.
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. 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.
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.
Myricitrin, a flavonoid compound isolated from the root bark of Myrica cerifera, which exerts antinociceptive effects.
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.
Go6976 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.
Go6976 abolished the anticalcification activity of CST by promoting the ossification of cultured VSMCs. Rat VSMCs werecultured in growth medium or calcification medium in the presence or absence of 10 7mol/L of CST or in calcification medium containing10 7mol/L of CST and pretreated with different doses of Go6976 (0.01, 0.1 and 0.5lmol/L) for 30 min. On day 7 (A, n=4) and 12 (B,n=4), VSMCs were harvested for the determination of ALP activity (A) using an ALP assay kit and calcium content (B) using the OCPCmethod. The VSMCs cultured with calcification medium containing 10 7mol/L of CST were pretreated with different doses of Go6976 (0.01and 0.1lmol/L) for 30 min. On day 6, VSMCs were harvested for the detection of expression of OCN (C, D, n=6). Data from at least threeindependent experiments are presented as the mean SEM, and representative images are shown.*P<.05 and †P<.01. Ctrl, control groupin vitro;b-GP,b-glycerophosphate group;b-GP+CST,b-glycerophosphate plus 10 7mol/L cortistatin group;b-GP+CST+Go6976,b-glycerophosphate plus 10 7mol/L cortistatin plus Go6976 group.
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.
Ingenol, a plant-derived diterpenoid, is a weak PKC activator and possesses important anticancer activity.
Decursinol angelate is a cytotoxic and protein kinase C activating agent from the root of Angelica gigas.