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抑制剂选择性比较

特异性亚型抑制剂

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所有产品 PKC抑制剂(17) PKC激活剂(3) 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。	Cancer Cell, 2019, 36(2):179-193 Am J Cancer Res, 2019, 9(5):906-926 J Pharm Pharmacol, 2019, 71(3):338-347	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.
S2791	Sotrastaurin Sotrastaurin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K_i为0.22 nM；对PKCζ没有活性。Phase 2。	J Diabetes Res, 2019, 2019:9582714 PLoS One, 2019, 14(3):e0211309 Biochem Biophys Res Commun, 2018, 10.1016/j.bbrc.2018.07.049	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.
S1421	Staurosporine Staurosporine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。	Nephrol Dial Transplant, 2019, 34(6):934-941 Biochem Pharmacol, 2018, 150:9-23 Mol Carcinog, 2018, 57(7):886-895
S2911	Go 6983 Go 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。	Cancer Res, 2019, 10.1158/0008-5472.CAN-18-2486 FASEB J, 2019, 33(1):1468-1481 J Cell Mol Med, 2019, 10.1111/jcmm.14522	(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.
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。	Front Physiol, 2019, 10:167 Onco Targets Ther, 2019, 12:1137-1146 Cereb Cortex, 2018, 10.1093/cercor/bhy007	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)
S6723^New	LXS-196 LXS-196是PKC的选择性抑制剂。
S6577^New	PKC-theta inhibitor PKC-theta inhibitor可抑制PKC-θ，IC50为12 nM。
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。	Int J Biochem Cell Biol, 2019, 110:111-121 Free Radic Res, 2019, 53(3):348-358 Cell Physiol Biochem, 2017, 41(3):1011-1019
S2554	Daphnetin Daphnetin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。	Int Immunopharmacol, 2019, 72:195-203 Inflamm Res, 2017, 66(7):579-589	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.
S4066	Dequalinium Chloride Dequalinium 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.
S1292	Chelerythrine Chloride Chelerythrine是一种有效的，选择性的PKC拮抗剂， IC50为0.66 μM。
S2391	Quercetin Quercetin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。	Front Cell Neurosci, 2019, 13:316 Clin Cancer Res, 2018, 10.1158/1078-0432 Mol Nutr Food Res, 2017, 61(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.
S3661	2-Methoxy-1,4-naphthoquinone 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.
S2327	Myricitrin Myricitrin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。
S7663	Ruboxistaurin HCl(LY333531 ) 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。	PLoS One, 2019, 14(3):e0211309 FEBS Lett, 2014, 588(18):3409-16
S7119	Go6976 Go6976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。	Acta Physiol, 2018, 223(3):e13055 Biochim Biophys Acta Mol Basis Dis, 2018, 1864(9 Pt B):2957-2971 J Biol Chem, 2018, 10.1074/jbc.RA118.002191	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.
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。	Cancer Res, 2019, 10.1158/0008-5472 Cancer Lett, 2019, 445:34-44 Leukemia, 2018, 32(1):139-148	(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.
S7791^New	Phorbol 12-myristate 13-acetate (PMA) Phorbol 12-myristate 13-acetate (PMA)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。	Clin Exp Immunol, 2016, 184(2):147-58
S3819	Decursinol angelate Decursinol angelate is a cytotoxic and protein kinase C activating agent from the root of Angelica gigas.
s9101	Ingenol Ingenol, a plant-derived diterpenoid, is a weak PKC activator and possesses important anticancer activity.

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。	Cancer Cell,2019, 36(2):179-193 Am J Cancer Res,2019, 9(5):906-926 J Pharm Pharmacol,2019, 71(3):338-347	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.
S2791	Sotrastaurin Sotrastaurin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K_i为0.22 nM；对PKCζ没有活性。Phase 2。	J Diabetes Res,2019, 2019:9582714 PLoS One,2019, 14(3):e0211309 Biochem Biophys Res Commun,2018, 10.1016/j.bbrc.2018.07.049	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.
S1421	Staurosporine Staurosporine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。	Nephrol Dial Transplant,2019, 34(6):934-941 Biochem Pharmacol,2018, 150:9-23 Mol Carcinog,2018, 57(7):886-895
S2911	Go 6983 Go 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。	Cancer Res,2019, 10.1158/0008-5472.CAN-18-2486 FASEB J,2019, 33(1):1468-1481 J Cell Mol Med,2019, 10.1111/jcmm.14522	(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.
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。	Front Physiol,2019, 10:167 Onco Targets Ther,2019, 12:1137-1146 Cereb Cortex,2018, 10.1093/cercor/bhy007	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)
S6723^New	LXS-196 LXS-196是PKC的选择性抑制剂。
S6577^New	PKC-theta inhibitor PKC-theta inhibitor可抑制PKC-θ，IC50为12 nM。
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。	Int J Biochem Cell Biol,2019, 110:111-121 Free Radic Res,2019, 53(3):348-358 Cell Physiol Biochem,2017, 41(3):1011-1019
S2554	Daphnetin Daphnetin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。	Int Immunopharmacol,2019, 72:195-203 Inflamm Res,2017, 66(7):579-589	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.
S4066	Dequalinium Chloride Dequalinium 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.
S1292	Chelerythrine Chloride Chelerythrine是一种有效的，选择性的PKC拮抗剂， IC50为0.66 μM。
S2391	Quercetin Quercetin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。	Front Cell Neurosci,2019, 13:316 Clin Cancer Res,2018, 10.1158/1078-0432 Mol Nutr Food Res,2017, 61(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.
S3661	2-Methoxy-1,4-naphthoquinone 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.
S2327	Myricitrin Myricitrin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。
S7663	Ruboxistaurin HCl(LY333531 ) 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。	PLoS One,2019, 14(3):e0211309 FEBS Lett,2014, 588(18):3409-16
S7119	Go6976 Go6976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。	Acta Physiol,2018, 223(3):e13055 Biochim Biophys Acta Mol Basis Dis,2018, 1864(9 Pt B):2957-2971 J Biol Chem,2018, 10.1074/jbc.RA118.002191	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.
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。	Cancer Res,2019, 10.1158/0008-5472 Cancer Lett,2019, 445:34-44 Leukemia,2018, 32(1):139-148	(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.

产品目录	产品描述	文献引用
S7791^New	Phorbol 12-myristate 13-acetate (PMA) Phorbol 12-myristate 13-acetate (PMA)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。	Clin Exp Immunol, 2016, 184(2):147-58
S3819	Decursinol angelate Decursinol angelate is a cytotoxic and protein kinase C activating agent from the root of Angelica gigas.
s9101	Ingenol Ingenol, a plant-derived diterpenoid, is a weak PKC activator and possesses important anticancer activity.

产品目录

产品描述

文献引用

实验数据

S7791^New