PKC
信号通路图
研究领域
抑制剂选择性比较
特异性亚型抑制剂
PKC产品
| 目录号 | 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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| S1113 |
GSK690693GSK690693 是一种泛Akt抑制剂，靶向作用于Akt1/2/3，在无细胞试验中IC50为2 nM/13 nM/9 nM，也对AGC激酶家族:PKA，PrkX和PKC同工酶敏感。GSK690693 也能有效地抑制CAMK家族的 AMPK 和 DAPK3，对应的IC50值分别为50 nM和81 nM。GSK690693 可影响 Unc-51-like autophagy activating kinase 1 (ULK1) 的活性并有效地抑制 STING-dependent IRF3 的激活。Phase 1。 |
UPN cells were treated with GSK690693 or MK2206 (1 uM) for 1h followed by LPA (10 uM), EGF or IGF-1 (10 ng/ml) for another 1h and Western blot was performed. Band intensities of phospho-AKT (p-AKTS473), phospho-S6 (p-S6S240/S244), phospho-YB-1 (p-YB-1S102) and YB-1 were quantified and normalized to the intensity of ERK2. It directly determined the role of AKT using two potent, AKT inhibitors with distinct actions—a catalytic domain inhibitor, GSK690693, and an allosteric inhibitor, MK2206 -in UPN and SKOV3 cells, which showed appreciable AKT and YB-1 phosphorylation upon growth factor stimulation. GSK690693 increased basal and growth factor-induced AKT phosphorylation due to blocking a negative feedback loop downstream of AKT, whereas MK2206 abolished both basal and growth-factor-induced AKT phosphorylation. |
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| S1573 |
Fasudil (HA-1077) HClFasudil (HA-1077, AT-877)是一种有效的、具有选择性的Rho抑制剂（ROCK2, Ki=0.33 μM），同时对PKA、PKG、PKC和MLCK也具有抑制活性，Ki值分别为1.6 μM、1.6 μM、3.3 μM、36 μM。Fasudil 也是calcium channel的阻滞剂。 |
The ROCK inhibitors fasudil and Y27632 prevented SCP2 cell bone metastasis in nude mice (n = 10 per group). Shown are BLI images of bone metastases, IHC analyses of SMAD3 C-tail phosphorylation and PTHLH, osteoclast TRAP staining, and BLI quantitation. |
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| S2791 |
Sotrastaurin (AEB071)Sotrastaurin (AEB071) 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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| S2485 |
Mitoxantrone (NSC-301739) 2HClMitoxantrone 2HCl (NSC-301739) 是Mitoxantrone的盐酸盐形式。Mitoxantrone 是一种 type II topoisomerase 和 protein kinase C (PKC)的抑制剂，对于PKC的IC50值为 8.5 μM。Mitoxantrone 可抑制MCF-7/wt cells的细胞增殖，对应的IC50值为0.42 μM。Mitoxantrone 还可诱导细胞凋亡。 |
Immunohistochemistry and quantification of cleaved caspase 3 expression in DU145-DR tumor xenografts from (D). Scale bar, 100 mm. Data represent the mean ± SD. *p < 0.05.
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| E0010New |
Hypocrellin AHypocrellin A (HA) 是一种从 Shiraia bambusicola 中分离的苝醌，显示出抗病毒、抗菌和抗癌的活性。Hypocrellin A 还是 PKC 的选择性和有效抑制剂。 |
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| S6214New |
H-1152 dihydrochlorideH-1152 dihydrochloride (2HCl) 是一种膜渗透性和选择性的 Rho-associated protein kinase (ROCK) 的抑制剂。 H-1152 可抑制 ROCK2、PKA、PKC、PKG、Aurora A 和 CaMK2 的IC50值分别为 0.0120 μM、3.03 μM、5.68 μM、0.360 μM、0.745 μM 和 0.180 μM。 |
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| S1421 |
Staurosporine (AM-2282)Staurosporine (AM-2282, Antibiotic AM-2282, STS)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。 |
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| S2911 |
Go 6983Go 6983 (GOE 6983, Gö 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, GO 6850)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。 |
Effect of PKC inhibitor on DHPG-stimulated Cx43 and ERK1/2 phosphorylation response and GJIC inhibition. Cells were treated with the PKC inhibitor GF109203X (different concentrations indicated) for 30 min prior to DHPG (100 lM, 15 min) treatment. a Representative immunoblots with an anti-Cx43 antibody are shown. b Representative immunoblots with a phospho-specific antibody recognizing the dually phosphorylated form of ERK1/2 (Thr202/Tyr204) and an antibody recognizing total ERK1/2 are shown. Quantitative analysis of the Cx43-P2/Cx43-P0?1 ratio and the phospho-ERK1/2 (p-ERK1/2)/total-ERK1/2 (t-ERK1/2) ratio are shown below the representative immunoblots, respectively. C Cells were incubated without (a) or with 100 lM DHPG (b) or with 100 μM DHPG in combination with 10 μM GF109203X (c) and scrape loaded (9100). d Cells were exposed to GF109203X (different concentrations indicated) alone (filled square) or 100 μM DHPG and GF109203X (filled diamond) prior to measurement of GJIC by scrape loading. Data are shown as mean ± SEM for three separate experiments performed in triplicate (*p<0.05 vs. NC, n = 3, +GF109203X for 0.1, 1, 5 or 10 μM) |
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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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| S1292 |
Chelerythrine Chloride (NSC 646662)Chelerythrine Chloride (NSC 646662, Broussonpapyrine)是一种有效的，选择性的PKC拮抗剂， IC50为0.66 μM。 |
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| S3273 |
HypericinHypericin (Hyp, HY) 是一种在 common St. John's Wort (Hypericum species) 中发现的天然物质，具有抗抑郁、抗肿瘤和抗病毒 (人类免疫缺陷病毒HIV和丙型肝炎病毒HCV) 活性。Hypericin 对 MAO (monoaminoxidase)、PKC (protein kinase C)、dopamine-beta-hydroxylase、reverse transcriptase、telomerase 和 CYP (cytochrome P450)。 |
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| S9522 |
ValrubicinValrubicin 是一种化疗药物，用于治疗膀胱癌。Valrubicin 可抑制 TPA- 和 PDBu- 诱导的 PKC 活化，对应的IC50值分别为0.85 μM 和 1.25 μM。 |
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| S8388 |
ML-7 HClML-7 是平滑肌肌球蛋白轻链激酶MLCK抑制剂，Ki值为0.3 μM。对钙离子-钙调蛋白依赖性或非依赖性的平滑肌MLCKs具有可逆的、ATP竞争性抑制作用。ML-7 还可抑制 PKA 和 PKC，对应的Ki值分别为21 μM和42 μM。 |
Platelets (3 × 108/mL) were treated with ML-7 (5 µM) for 20 minutes, followed by stimulation with oxLDL (50 µg/mL) for 15 seconds. Samples were then lysed, separated by SDS-PAGE, and immunoblotted for phospho-MLCSer19 followed by reprobing for β-tubulin. (Ai) Representative blots. (Aii) Densitometric analysis of 5 independent experiments. *P < .05.
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| S0754 |
Bisindolylmaleimide IVBisindolylmaleimide IV (Arcyriarubin A, BIM IV, Compound 5/1a) 是一种有效的 protein kinase C (PKC) 的抑制剂，其IC50值为0.55 μM。Bisindolylmaleimide IV 也可抑制 PKA，对应的IC50值为11.8 μM。 Bisindolylmaleimide IV 是一种有效的、选择性的细胞培养中针对人巨细胞病毒 human cytomegalovirus (HCMV) 复制的抑制剂，IC50值为0.2 μM。 |
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| S0069 |
VTX-27VTX-27 (Compound 27) 是一种有效的、选择性的 protein kinase C θ (PKC θ) 的抑制剂，其PKCθ和PKCδ的Ki值分别为0.08 nM和16 nM。 |
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| S0780 |
Oncrasin-1Oncrasin-1 (Onc-1) 是一种有效的具有抗肿瘤活性的 RNA polymerase II 的抑制剂，可杀死具有 K-Ras 突变的多种人类肺癌细胞。Oncrasin-1 可驱动敏感细胞核（非耐药细胞）中的 protein kinase C iota (PKCι) 的异常聚集。 |
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| S6577 |
PKC-theta inhibitorPKC-theta inhibitor (compound 20) 可抑制PKC-θ，IC50值为18 nM。 |
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| S2391 |
Quercetin (NSC 9221)Quercetin (NSC 9221, Sophoretin, C.I. 75720)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。Quercetin 可诱导凋亡和保护性的自噬。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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| S7862 |
RottlerinRottlerin (Mallotoxin, NSC 56346, NSC 94525)是一种从 Mallotus Philippinensis 纯化出来的天然化合物，一种特效的 Protein kinase 的抑制剂，对PKCδ(来自杆状病毒感染的Sf9昆虫细胞)、PKCδ(来自猪脾)和CaM kinase III的IC50值分别为3 μM、6 μM和5.3 μM。Rottlerin 还可以抑制PKCα、PKCγ、PKCβ、PKCη、CKII和PKA，其IC50值分别为30 μM、40 μM、42 μM、82 μM、30 μM和78 μM。 |
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| S3661 |
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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| S6424 |
TAS-301TAS-301是平滑肌细胞迁移和增殖的抑制剂，在大鼠颈动脉球囊损伤后抑制内膜增厚。TAS-301 可抑制PDGF诱导的 PKC 激活。 |
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| S2327 |
MyricitrinMyricitrin (Myricitrine) 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) HClRuboxistaurin (LY333531) HCl 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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| S2964 |
HA-100 dihydrochlorideHA-100 dihydrochloride 是 cGMP-dependent protein kinase (PKG)、cAMP-dependent protein kinase (PKA)、protein kinase C (PKC) 和 MLC-kinase 的抑制剂，对应的IC50值分别为4 μM、8 μM、12 μM和240 μM。 |
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| S7119 |
Go6976Go6976 (PD406976)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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| S6723 |
Darovasertib (LXS-196)Darovasertib (LXS-196, IDE-196)是PKC的选择性抑制剂。 |
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| S8064 |
Midostaurin (PKC412)Midostaurin (pkc412, CGP 41251) 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。 |
(f and g) Induction of apoptosis in HMC-1.1 and -1.2, respectively. Columns represent the mean of three independent experiments and the bars represent the standard error. ctrl, control; mido, midostaurin.
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| S7791 |
Phorbol 12-myristate 13-acetate (PMA)Phorbol 12-myristate 13-acetate (PMA, 12-O-Tetradecanoylphorbol-13-acetate, TPA, Phorbol myristate acetate)是一种有效的PKC激活剂，在纳摩尔浓度范围内具有活性作用。Phorbol 12-myristate 13-acetate (PMA)可诱导sphingosine-1-phosphate (S1P)。 |
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| S3289 |
DaphnoretinDaphnoretin (Dephnoretin, Thymelol) 是一种从Wikstroemia indica C.A. Mey.中提取的具有生物活性的化合物，是 protein kinase C (PKC) 的激活剂。Daphnoretin 通过调节 Akt 信号通路的活性，来抑制肿瘤细胞的增殖、侵袭和迁移，促进其凋亡。 |
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| S3819 |
Decursinol angelateDecursinol angelate is a cytotoxic and protein kinase C activating agent from the root of Angelica gigas. |
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| S9101 |
IngenolIngenol, a plant-derived diterpenoid, is a weak PKC activator and possesses important anticancer activity. |
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| E0124New |
ChelerythrineChelerythrine (Toddaline, Broussonpapyrine) 是一种有效的选择性 PKC 拮抗剂，IC50 为 0.66 μM。 Chelerythrine 还抑制 BclXL-Bak BH3 肽结合，IC50 为 1.5 μM。 Chelerythrine 具有抗肿瘤、抗糖尿病和抗炎活性。 |
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| S2323 |
Methyl-HesperidinMethyl-Hesperidin 是一种在柑橘类水果中广泛存在的黄酮苷（黄酮）（C28H34O15），其苷元形式被称为橙皮素。 |
| 目录号 | 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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| S1113 |
GSK690693GSK690693 是一种泛Akt抑制剂，靶向作用于Akt1/2/3，在无细胞试验中IC50为2 nM/13 nM/9 nM，也对AGC激酶家族:PKA，PrkX和PKC同工酶敏感。GSK690693 也能有效地抑制CAMK家族的 AMPK 和 DAPK3，对应的IC50值分别为50 nM和81 nM。GSK690693 可影响 Unc-51-like autophagy activating kinase 1 (ULK1) 的活性并有效地抑制 STING-dependent IRF3 的激活。Phase 1。 |
UPN cells were treated with GSK690693 or MK2206 (1 uM) for 1h followed by LPA (10 uM), EGF or IGF-1 (10 ng/ml) for another 1h and Western blot was performed. Band intensities of phospho-AKT (p-AKTS473), phospho-S6 (p-S6S240/S244), phospho-YB-1 (p-YB-1S102) and YB-1 were quantified and normalized to the intensity of ERK2. It directly determined the role of AKT using two potent, AKT inhibitors with distinct actions—a catalytic domain inhibitor, GSK690693, and an allosteric inhibitor, MK2206 -in UPN and SKOV3 cells, which showed appreciable AKT and YB-1 phosphorylation upon growth factor stimulation. GSK690693 increased basal and growth factor-induced AKT phosphorylation due to blocking a negative feedback loop downstream of AKT, whereas MK2206 abolished both basal and growth-factor-induced AKT phosphorylation. |
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| S1573 |
Fasudil (HA-1077) HClFasudil (HA-1077, AT-877)是一种有效的、具有选择性的Rho抑制剂（ROCK2, Ki=0.33 μM），同时对PKA、PKG、PKC和MLCK也具有抑制活性，Ki值分别为1.6 μM、1.6 μM、3.3 μM、36 μM。Fasudil 也是calcium channel的阻滞剂。 |
The ROCK inhibitors fasudil and Y27632 prevented SCP2 cell bone metastasis in nude mice (n = 10 per group). Shown are BLI images of bone metastases, IHC analyses of SMAD3 C-tail phosphorylation and PTHLH, osteoclast TRAP staining, and BLI quantitation. |
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| S2791 |
Sotrastaurin (AEB071)Sotrastaurin (AEB071) 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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| S2485 |
Mitoxantrone (NSC-301739) 2HClMitoxantrone 2HCl (NSC-301739) 是Mitoxantrone的盐酸盐形式。Mitoxantrone 是一种 type II topoisomerase 和 protein kinase C (PKC)的抑制剂，对于PKC的IC50值为 8.5 μM。Mitoxantrone 可抑制MCF-7/wt cells的细胞增殖，对应的IC50值为0.42 μM。Mitoxantrone 还可诱导细胞凋亡。 |
Immunohistochemistry and quantification of cleaved caspase 3 expression in DU145-DR tumor xenografts from (D). Scale bar, 100 mm. Data represent the mean ± SD. *p < 0.05.
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| E0010New |
Hypocrellin AHypocrellin A (HA) 是一种从 Shiraia bambusicola 中分离的苝醌，显示出抗病毒、抗菌和抗癌的活性。Hypocrellin A 还是 PKC 的选择性和有效抑制剂。 |
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| S6214New |
H-1152 dihydrochlorideH-1152 dihydrochloride (2HCl) 是一种膜渗透性和选择性的 Rho-associated protein kinase (ROCK) 的抑制剂。 H-1152 可抑制 ROCK2、PKA、PKC、PKG、Aurora A 和 CaMK2 的IC50值分别为 0.0120 μM、3.03 μM、5.68 μM、0.360 μM、0.745 μM 和 0.180 μM。 |
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| S1421 |
Staurosporine (AM-2282)Staurosporine (AM-2282, Antibiotic AM-2282, STS)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。 |
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| S2911 |
Go 6983Go 6983 (GOE 6983, Gö 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, GO 6850)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。 |
Effect of PKC inhibitor on DHPG-stimulated Cx43 and ERK1/2 phosphorylation response and GJIC inhibition. Cells were treated with the PKC inhibitor GF109203X (different concentrations indicated) for 30 min prior to DHPG (100 lM, 15 min) treatment. a Representative immunoblots with an anti-Cx43 antibody are shown. b Representative immunoblots with a phospho-specific antibody recognizing the dually phosphorylated form of ERK1/2 (Thr202/Tyr204) and an antibody recognizing total ERK1/2 are shown. Quantitative analysis of the Cx43-P2/Cx43-P0?1 ratio and the phospho-ERK1/2 (p-ERK1/2)/total-ERK1/2 (t-ERK1/2) ratio are shown below the representative immunoblots, respectively. C Cells were incubated without (a) or with 100 lM DHPG (b) or with 100 μM DHPG in combination with 10 μM GF109203X (c) and scrape loaded (9100). d Cells were exposed to GF109203X (different concentrations indicated) alone (filled square) or 100 μM DHPG and GF109203X (filled diamond) prior to measurement of GJIC by scrape loading. Data are shown as mean ± SEM for three separate experiments performed in triplicate (*p<0.05 vs. NC, n = 3, +GF109203X for 0.1, 1, 5 or 10 μM) |
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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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| S1292 |
Chelerythrine Chloride (NSC 646662)Chelerythrine Chloride (NSC 646662, Broussonpapyrine)是一种有效的，选择性的PKC拮抗剂， IC50为0.66 μM。 |
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| S3273 |
HypericinHypericin (Hyp, HY) 是一种在 common St. John's Wort (Hypericum species) 中发现的天然物质，具有抗抑郁、抗肿瘤和抗病毒 (人类免疫缺陷病毒HIV和丙型肝炎病毒HCV) 活性。Hypericin 对 MAO (monoaminoxidase)、PKC (protein kinase C)、dopamine-beta-hydroxylase、reverse transcriptase、telomerase 和 CYP (cytochrome P450)。 |
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| S9522 |
ValrubicinValrubicin 是一种化疗药物，用于治疗膀胱癌。Valrubicin 可抑制 TPA- 和 PDBu- 诱导的 PKC 活化，对应的IC50值分别为0.85 μM 和 1.25 μM。 |
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| S8388 |
ML-7 HClML-7 是平滑肌肌球蛋白轻链激酶MLCK抑制剂，Ki值为0.3 μM。对钙离子-钙调蛋白依赖性或非依赖性的平滑肌MLCKs具有可逆的、ATP竞争性抑制作用。ML-7 还可抑制 PKA 和 PKC，对应的Ki值分别为21 μM和42 μM。 |
Platelets (3 × 108/mL) were treated with ML-7 (5 µM) for 20 minutes, followed by stimulation with oxLDL (50 µg/mL) for 15 seconds. Samples were then lysed, separated by SDS-PAGE, and immunoblotted for phospho-MLCSer19 followed by reprobing for β-tubulin. (Ai) Representative blots. (Aii) Densitometric analysis of 5 independent experiments. *P < .05.
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| S0754 |
Bisindolylmaleimide IVBisindolylmaleimide IV (Arcyriarubin A, BIM IV, Compound 5/1a) 是一种有效的 protein kinase C (PKC) 的抑制剂，其IC50值为0.55 μM。Bisindolylmaleimide IV 也可抑制 PKA，对应的IC50值为11.8 μM。 Bisindolylmaleimide IV 是一种有效的、选择性的细胞培养中针对人巨细胞病毒 human cytomegalovirus (HCMV) 复制的抑制剂，IC50值为0.2 μM。 |
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| S0069 |
VTX-27VTX-27 (Compound 27) 是一种有效的、选择性的 protein kinase C θ (PKC θ) 的抑制剂，其PKCθ和PKCδ的Ki值分别为0.08 nM和16 nM。 |
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| S0780 |
Oncrasin-1Oncrasin-1 (Onc-1) 是一种有效的具有抗肿瘤活性的 RNA polymerase II 的抑制剂，可杀死具有 K-Ras 突变的多种人类肺癌细胞。Oncrasin-1 可驱动敏感细胞核（非耐药细胞）中的 protein kinase C iota (PKCι) 的异常聚集。 |
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| S6577 |
PKC-theta inhibitorPKC-theta inhibitor (compound 20) 可抑制PKC-θ，IC50值为18 nM。 |
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| S2391 |
Quercetin (NSC 9221)Quercetin (NSC 9221, Sophoretin, C.I. 75720)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。Quercetin 可诱导凋亡和保护性的自噬。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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| S7862 |
RottlerinRottlerin (Mallotoxin, NSC 56346, NSC 94525)是一种从 Mallotus Philippinensis 纯化出来的天然化合物，一种特效的 Protein kinase 的抑制剂，对PKCδ(来自杆状病毒感染的Sf9昆虫细胞)、PKCδ(来自猪脾)和CaM kinase III的IC50值分别为3 μM、6 μM和5.3 μM。Rottlerin 还可以抑制PKCα、PKCγ、PKCβ、PKCη、CKII和PKA，其IC50值分别为30 μM、40 μM、42 μM、82 μM、30 μM和78 μM。 |
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| S3661 |
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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| S6424 |
TAS-301TAS-301是平滑肌细胞迁移和增殖的抑制剂，在大鼠颈动脉球囊损伤后抑制内膜增厚。TAS-301 可抑制PDGF诱导的 PKC 激活。 |
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| S2327 |
MyricitrinMyricitrin (Myricitrine) 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) HClRuboxistaurin (LY333531) HCl 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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| S2964 |
HA-100 dihydrochlorideHA-100 dihydrochloride 是 cGMP-dependent protein kinase (PKG)、cAMP-dependent protein kinase (PKA)、protein kinase C (PKC) 和 MLC-kinase 的抑制剂，对应的IC50值分别为4 μM、8 μM、12 μM和240 μM。 |
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| S7119 |
Go6976Go6976 (PD406976)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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| S6723 |
Darovasertib (LXS-196)Darovasertib (LXS-196, IDE-196)是PKC的选择性抑制剂。 |
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| S8064 |
Midostaurin (PKC412)Midostaurin (pkc412, CGP 41251) 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。 |
(f and g) Induction of apoptosis in HMC-1.1 and -1.2, respectively. Columns represent the mean of three independent experiments and the bars represent the standard error. ctrl, control; mido, midostaurin.
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| 目录号 | 产品描述 | 文献引用 | 实验数据 |
|---|---|---|---|
| S7791 |
Phorbol 12-myristate 13-acetate (PMA)Phorbol 12-myristate 13-acetate (PMA, 12-O-Tetradecanoylphorbol-13-acetate, TPA, Phorbol myristate acetate)是一种有效的PKC激活剂，在纳摩尔浓度范围内具有活性作用。Phorbol 12-myristate 13-acetate (PMA)可诱导sphingosine-1-phosphate (S1P)。 |
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| S3289 |
DaphnoretinDaphnoretin (Dephnoretin, Thymelol) 是一种从Wikstroemia indica C.A. Mey.中提取的具有生物活性的化合物，是 protein kinase C (PKC) 的激活剂。Daphnoretin 通过调节 Akt 信号通路的活性，来抑制肿瘤细胞的增殖、侵袭和迁移，促进其凋亡。 |
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| S3819 |
Decursinol angelateDecursinol angelate is a cytotoxic and protein kinase C activating agent from the root of Angelica gigas. |
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| S9101 |
IngenolIngenol, a plant-derived diterpenoid, is a weak PKC activator and possesses important anticancer activity. |
| 目录号 | 产品描述 | 文献引用 | 实验数据 |
|---|---|---|---|
| E0124New |
ChelerythrineChelerythrine (Toddaline, Broussonpapyrine) 是一种有效的选择性 PKC 拮抗剂，IC50 为 0.66 μM。 Chelerythrine 还抑制 BclXL-Bak BH3 肽结合，IC50 为 1.5 μM。 Chelerythrine 具有抗肿瘤、抗糖尿病和抗炎活性。 |
| 目录号 | 产品描述 | 文献引用 | 实验数据 |
|---|---|---|---|
| S2323 |
Methyl-HesperidinMethyl-Hesperidin 是一种在柑橘类水果中广泛存在的黄酮苷（黄酮）（C28H34O15），其苷元形式被称为橙皮素。 |
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