PKC
信号通路图
研究领域
- 抑制剂选择性比较
- 溶解性比较
| 目录号 | 产品目录 | 溶解度(25°C) | ||
|---|---|---|---|---|
| 水 | DMSO | 酒精 | ||
| 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抑制剂（15）
- 新PKC产品
| 产品目录 | 产品描述 | 文献引用 | 实验数据 |
|---|---|---|---|
| S1055 |
Enzastaurin (LY317615)Enzastaurin (LY317615)是一种有效的PKCβ选择性抑制剂，无细胞试验中IC50为6 nM，比作用于PKCα，PKCγ和PKCε选择性高6到20倍。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是一种有效的，选择性的泛PKC抑制剂，最有效作用于PKCθ，无细胞试验中Ki为0.22 nM；对PKCζ没有活性。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是一种有效的PKC抑制剂，在无细胞试验中作用于PKCα，PKCγ 和PKCη，IC50分别为2 nM，5 nM 和 4 nM，对PKCδ(20 nM)和PKCε(73 nM作用较弱，对PKCζ (1086 nM)的活性很低。同时 对其他的激酶PKA, PKG, S6K, CaMKII, 等也显示抑制活性。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是一种pan-PKC抑制剂，作用于PKCα， PKCβ， PKCγ和PKCδ，IC50分别为7 nM， 7 nM， 6 nM和10 nM，对PKCζ作用稍弱，抑制PKCμ活性。 |
(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)是一种有效的PKC抑制剂，作用于PKCα，PKCβI，PKCβII和PKCγ，无细胞试验中IC50分别为20 nM， 17 nM， 16nM和20 nM，作用于PKC比作用于EGFR，PDGFR和胰岛素受体选择性高3000倍以上。 |
(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)是一种pan-PKC抑制剂，作用于PKC-α， PKC-βI， PKC-βII， PKC-γ和PKC-ε，IC50分别为5 nM， 24 nM， 14 nM， 27 nM和24 nM，也有效抑制MAPKAP-K1b， MSK1， GSK3β和S6K1。 |
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| S2554 |
DaphnetinDaphnetin是天然香豆素衍生物，是一种蛋白激酶抑制剂，抑制EGFR， PKA和PKC，IC50分别为7.67 μM， 9.33 μM和25.01 μM，且具有抗炎和抗氧化剂活动性。 |
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是一种PKC抑制剂，IC50为7-18 μM，同时也是一种选择性蜂毒明肽敏感型钾离子通道阻断剂，IC50为1.1 μM. |
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| S2391 |
QuercetinQuercetin是蔬菜水果和白酒中的天然黄酮类化合物，是一种体外重组Sirt1蛋白的激活剂同时也是PI3K抑制剂，IC50为2.4 – 5.4 μM。 |
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是一种化学化合物，可从Myrica cerifera (Bayberry属, 小乔木，原产于北美)的根皮中分离得到。 |
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| S7663 |
Ruboxistaurin (LY333531 HCl)LY333531是特异性β-蛋白激酶C的抑制剂。能竞争性地、可逆地抑制PKCβ1和PKCβ2，IC50分别为4.7和5.9 nM。 |
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| S7119 |
Go6976Go6976是一种强效的PKC抑制剂，其对PKC (老鼠大脑), PKCα, and PKCβ1的IC50分别为7.9nM，2.3 nM, 和 6.2 nM 。此外，也是JAK2 和 Flt3的强抑制剂。 |
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)是一种多靶点激酶抑制剂，作用于PKCα/β/γ， Syk， Flk-1， Akt， PKA， c-Kit， c-Fgr， c-Src， FLT3， PDFRβ和VEGFR1/2，IC50为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. |
