IκB/IKK

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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 IκB/IKK抑制剂(20) IκB/IKK调节剂(2) 新IκB/IKK产品

目录号	产品描述	文献引用	实验数据
S1274	BX-795 BX-795是一种有效的，特异性的PDK1抑制剂，在无细胞试验中IC50为6 nM，作用于PDK1比作用于PKA和PKC选择性分别高140和1600倍。同时，相比于 GSK3β，作用于PDK1的选择性高出100多倍。	Nature, 2019, 567(7747):262-266 Cell, 2019, 176(6):1447-1460 Nat Immunol, 2019, 20(1):18-28	Induction of basal p62 Ser403 phosphorylation in ULK1/2-deﬁcient MEF was suppressed by BX-795, an inhibitor of TBK1. WT ( Ulk1 +/+/Ulk2 +/+) and Ulk1 -/- /Ulk2 -/-(KO) MEF were treated with NaCl/Pi (Con) or 10 uM BX-795 for 6 h, and subjected to immunoblotting with indicated antibodies.
S2913	BAY 11-7082 BAY 11-7082是一种NF-κB抑制剂，抑制TNFα诱导的IκBα磷酸化，在肿瘤细胞中IC50为10 μM。同时对泛素化系统的组分也有抑制作用。	Eur J Pharmacol, 2020, 873:172981 Exp Ther Med, 2020, 19(2):871-882 Blood, 2019, 134(13):1084-1094	Immunofluorescence images of Ishikawa cells showing the increase in the nuclear colocalization of ERa (red) and p65 (green) after E2 incubation. Nuclear colocalization is yellow. Treatment with ICI 182,780, PDTC or Bay inhibited the nuclear localization of both ERa and p65. Blue, DAPI-stained nuclei. All pictures were obtained the same day using the same microscope settings. Original magnification 3200, bar =50 um. Arrows, cytoplasmic ERa and p65 staining. ICI, ICI 182,780; Bay, Bay 11-7082.
S2882	IKK-16 (IKK Inhibitor VII) IKK-16 (IKK Inhibitor VII)是一种选择性的IκB激酶(IKK)抑制剂，作用于IKK-2，IKK complex和IKK-1，无细胞试验中IC50分别为40 nM，70 nM和200 nM。	Eur J Pharmacol, 2020, 873:172981 Cancer Cell, 2019, 35(2):191-203 Immunity, 2019, 50(2):348-361	Reduction in IFN-g production in TcREG by IKK-16 coincides with decrease in T-bet and Eomes expression levels. Flow cytometry plots showing cellular analysis for T-bet and Eomes in CD45+CD3+CD8+ population.
S2824	TPCA-1 TPCA-1是一种IKK-2抑制剂，无细胞试验中IC50为17.9 nM，抑制NF-κB通路，比作用于IKK-1选择性高22倍。	Eur J Pharmacol, 2020, 873:172981 Nature, 2019, 567(7747):262-266 Cancer Cell, 2019, 35(2):191-203	AGS cells were treated with cwith IL-1β in the presence of the IKK inhibitor TPCA-1, the p38 MAPK inhibitor BIX02188 and the JNK inhibitor SP600125. Cell lysates were obtained 24 h after IL-1β treatment and immunoblotted with PTEN antibodies.
S2864	IMD 0354 IMD 0354是一种IKKβ抑制剂，作用于NF-κβ通路，抑制IκBα磷酸化。	Mucosal Immunol, 2020, 13(1):86-95 Stem Cell Res Ther, 2019, 10(1):375 Cancer Cell Int, 2019, 19:241	(B) Histological examinations of xenograft lesions produced by A549 cells. We stained the lesions with H&E, TUNEL and staining for Ki-67. (C, D) The histogram shows percentage of A549 cells that were positive for proliferation marker Ki-67 and apoptosis marker TUNEL in 3 representative fields. Results are expressed as the mean ± SD. ns. P > 0.05, P < 0.01 and *P < 0.001 for the indicated comparisons by 1-way A OVA or Student’s t test.
S8935^New	BAY-985 BAY-985是一种有效、高选择性的TBK1/IKKε抑制剂。 BAY-985对TBK1 (IC50 = 2 nM, low ATP assay; 30 nM, high ATP assay)和IKKε (IC50 = 2 nM)具有高效力，在机械性细胞phosphorylation of interferon regulatory factor 3(pIRF3)分析中也具有高效力(IC50 = 74 nM)，并且对SK-MEL-2细胞具有抗增殖作用(IC50 = 900 nM)。
S6714^New	INH14 INH14是TLR2介导的NF-kB激活抑制剂，对IKKα和IKKβ的IC50值分别为8.975 μM和3.598 μM。
S8872^New	GSK8612 GSK8612是高效选择性TBK1抑制剂，pKd为8。
S8078	Bardoxolone Methyl Bardoxolone Methyl是一种IKK抑制剂，具有强的促凋亡和抗炎活性。同时还是有效的Nrf2激活剂和NF-κB抑制剂。	Sci Rep, 2018, 8(1):14702 Mol Cell Biol, 2018, 38(22) Metab Eng, 2017, 42:185-193	Renal Nrf2 activity was shown in RTA402-treated acFSGS (RTA402 + acFSGS) mice as early as day 7 (RTA402 + acFSGS) and persisted to day 28, compared to vehicle + acFSGS mice. Kidney in situ ROS production demonstrated by DHE detection.
S8044	BMS-345541 BMS-345541是一种催化亚基的高选择性抑制剂，作用于IKK-2和IKK-1，无细胞试验中IC50分别为0.3 μM和4 μM。	Oncogene, 2019, 38(30):5873-5889 J Exp Clin Cancer Res, 2019, 38(1):140 Vascul Pharmacol, 2019, 121:106579	(E) After transfection with control or catalase siRNAs for 24 h, A375 and G361 cells were treated with vehicle or 2.5 µM BMS-345541, 20 µM PS-1145 and/or 50 µM of fotemustine for an additional 48 h. Cell viability was then assessed. , p<0.05. (F) A375 and G361 cells were treated with vehicle or 2.5 µM BMS-345541, 20 µM PS-1145 and/or 50 µM of fotemustine, in the presence or absence of catalase inhibitor 3-Amino-1,2,4-triazole (ATZ, 50 µM) for 48 h. Cell viability was then assessed. , p<0.05.
S4907	SC-514 SC-514是一种口服有效的，ATP竞争性的IKK-2抑制剂，IC50为3-12 μM，抑制NF-κB依赖性的基因表达，不抑制其他IKK异构体或其他丝-苏氨酸和酪氨酸激酶。	Cell Signal, 2019, 55:17-25 Lab Invest, 2018, 98(10):1311-1319 Mol Cells, 2018, 41(8):762-770
S1681	Mesalamine Mesalamine是一种抗炎化合物。
S7352	Bay 11-7085 BAY 11-7085 是TNFα诱导的IκBα磷酸化的不可逆抑制剂，其IC50为10 μM。	Eur J Pharmacol, 2020, 873:172981 Gastroenterology, 2019, 10.1053/j.gastro.2019.11.013 J Allergy Clin Immunol, 2019, 143(1):229-244.e9	VSMCs were pretreated with BAY 11-7085 (BAY, 10μmol/L) for 1h and further treated with or without 10^-7mol/L salusin-β for 30min. A, Cytoplasmic extracts (Cy) were obtained and the phosphorylated IκBα, IκBα and HDCA3 protein levels were measured by western blot analysis. B, nuclear extracts (Nu) were obtained and the nuclear p50, p65 and HDAC3 protein levels were measured by western blot analysis. Data are expressed as means ± SD (n=3). *P< 0.05 versus the control with no treatment; #P< 0.05 versus 10^-7mol/L salusin-β treatment alone.
S3615	Dehydrocostus Lactone Dehydrocostus lactone (DHE)是一种天然的倍半萜内酯，抑制IKKβ活性、IκBα的磷酸化和降解、共激活子p300的招募、p50/p65 NF-κB的核转位及它们结合于COX2启动子上的能力。DHE具有抗炎、抗溃疡、抗肿瘤作用和免疫调节活性。	J Cell Mol Med, 2019, 23(8):5762-5770
S7851	AZD3264 AZD3264是一种新型IKK2抑制剂。	Redox Biol, 2017, 11:562-576	(C) G361 cells were loaded with DCF (ROS probe) and further stimulated with vehicle or indicated IKKβ inhibitors for 3 h. Fluorescence was measured using a fluorescence microplate reader. *, p<0.05 versus control.
S7697	LY2409881 LY2409881 是一种有效的选择性 IKK2 抑制剂，IC50 为 30 nM，选择性比IKK1和其他常见激酶高10倍多。	Nat Commun, 2019, 10(1):2924 J Biol Chem, 2018, 293(30):11913-11927 Biochem Biophys Res Commun, 2018, 503(1):94-101	A549 cells were treated with NF-kB inhibitor LY2409881 (30 nM) for 2 h, followed by western blot analysis of p-NF-kB.
S7691	PS-1145 PS-1145是一种特异性IKK抑制剂，IC50 为 88 nM。	J Biol Chem, 2018, 293(19):7268-7280 Redox Biol, 2017, 562-576 Blood, 2016, 128(1):82-92	(E) After transfection with control or catalase siRNAs for 24 h, A375 and G361 cells were treated with vehicle or 2.5 µM BMS-345541, 20 µM PS-1145 and/or 50 µM of fotemustine for an additional 48 h. Cell viability was then assessed. , p<0.05. (F) A375 and G361 cells were treated with vehicle or 2.5 µM BMS-345541, 20 µM PS-1145 and/or 50 µM of fotemustine, in the presence or absence of catalase inhibitor 3-Amino-1,2,4-triazole (ATZ, 50 µM) for 48 h. Cell viability was then assessed. , p<0.05.
S7948	MRT67307 HCl MRT67307是一种高效的双重的IKKϵ /TBK1抑制剂，其IC50分别为160和19 nM。	Mol Cell, 2019, 74(2):347-362.e6 Cell Death Differ, 2019, 26(6):1077-1088 Cell, 2018, 174(6):1477-1491
S9042	Wedelolactone Wedelolactone, a medicinal plant-derived natural compound, is an inhibitor of IKK that is critical for activation of NF-κB by mediating phosphorylation and degradation of IκBα.	Int Immunopharmacol, 2019, 73:17-22
S3612	Rosmarinic acid Rosmarinic acid (RA)是一种天然的羟化化合物。它具有阻止补体结合、抑制脂肪氧合酶和环氧煤活性的功能，通过抑制NF-κB激活信号中IKK-β的活性、抑制CCL11和CCR3的表达。
S7441	WS3 WS3是一种β细胞增殖诱导剂，通过调节Erb3 binding protein-1 (EBP1)和IκB kinase通路发挥作用。
S7442	WS6 WS6通过调节Erb3 binding protein-1 (EBP1)和IκB kinase通路诱导β细胞增殖。

目录号	产品描述	文献引用	实验数据
S1274	BX-795 BX-795是一种有效的，特异性的PDK1抑制剂，在无细胞试验中IC50为6 nM，作用于PDK1比作用于PKA和PKC选择性分别高140和1600倍。同时，相比于 GSK3β，作用于PDK1的选择性高出100多倍。	Nature,2019, 567(7747):262-266 Cell,2019, 176(6):1447-1460 Nat Immunol,2019, 20(1):18-28	Induction of basal p62 Ser403 phosphorylation in ULK1/2-deﬁcient MEF was suppressed by BX-795, an inhibitor of TBK1. WT ( Ulk1 +/+/Ulk2 +/+) and Ulk1 -/- /Ulk2 -/-(KO) MEF were treated with NaCl/Pi (Con) or 10 uM BX-795 for 6 h, and subjected to immunoblotting with indicated antibodies.
S2913	BAY 11-7082 BAY 11-7082是一种NF-κB抑制剂，抑制TNFα诱导的IκBα磷酸化，在肿瘤细胞中IC50为10 μM。同时对泛素化系统的组分也有抑制作用。	Eur J Pharmacol,2020, 873:172981 Exp Ther Med,2020, 19(2):871-882 Blood,2019, 134(13):1084-1094	Immunofluorescence images of Ishikawa cells showing the increase in the nuclear colocalization of ERa (red) and p65 (green) after E2 incubation. Nuclear colocalization is yellow. Treatment with ICI 182,780, PDTC or Bay inhibited the nuclear localization of both ERa and p65. Blue, DAPI-stained nuclei. All pictures were obtained the same day using the same microscope settings. Original magnification 3200, bar =50 um. Arrows, cytoplasmic ERa and p65 staining. ICI, ICI 182,780; Bay, Bay 11-7082.
S2882	IKK-16 (IKK Inhibitor VII) IKK-16 (IKK Inhibitor VII)是一种选择性的IκB激酶(IKK)抑制剂，作用于IKK-2，IKK complex和IKK-1，无细胞试验中IC50分别为40 nM，70 nM和200 nM。	Eur J Pharmacol,2020, 873:172981 Cancer Cell,2019, 35(2):191-203 Immunity,2019, 50(2):348-361	Reduction in IFN-g production in TcREG by IKK-16 coincides with decrease in T-bet and Eomes expression levels. Flow cytometry plots showing cellular analysis for T-bet and Eomes in CD45+CD3+CD8+ population.
S2824	TPCA-1 TPCA-1是一种IKK-2抑制剂，无细胞试验中IC50为17.9 nM，抑制NF-κB通路，比作用于IKK-1选择性高22倍。	Eur J Pharmacol,2020, 873:172981 Nature,2019, 567(7747):262-266 Cancer Cell,2019, 35(2):191-203	AGS cells were treated with cwith IL-1β in the presence of the IKK inhibitor TPCA-1, the p38 MAPK inhibitor BIX02188 and the JNK inhibitor SP600125. Cell lysates were obtained 24 h after IL-1β treatment and immunoblotted with PTEN antibodies.
S2864	IMD 0354 IMD 0354是一种IKKβ抑制剂，作用于NF-κβ通路，抑制IκBα磷酸化。	Mucosal Immunol,2020, 13(1):86-95 Stem Cell Res Ther,2019, 10(1):375 Cancer Cell Int,2019, 19:241	(B) Histological examinations of xenograft lesions produced by A549 cells. We stained the lesions with H&E, TUNEL and staining for Ki-67. (C, D) The histogram shows percentage of A549 cells that were positive for proliferation marker Ki-67 and apoptosis marker TUNEL in 3 representative fields. Results are expressed as the mean ± SD. ns. P > 0.05, P < 0.01 and *P < 0.001 for the indicated comparisons by 1-way A OVA or Student’s t test.
S8935^New	BAY-985 BAY-985是一种有效、高选择性的TBK1/IKKε抑制剂。 BAY-985对TBK1 (IC50 = 2 nM, low ATP assay; 30 nM, high ATP assay)和IKKε (IC50 = 2 nM)具有高效力，在机械性细胞phosphorylation of interferon regulatory factor 3(pIRF3)分析中也具有高效力(IC50 = 74 nM)，并且对SK-MEL-2细胞具有抗增殖作用(IC50 = 900 nM)。
S6714^New	INH14 INH14是TLR2介导的NF-kB激活抑制剂，对IKKα和IKKβ的IC50值分别为8.975 μM和3.598 μM。
S8872^New	GSK8612 GSK8612是高效选择性TBK1抑制剂，pKd为8。
S8078	Bardoxolone Methyl Bardoxolone Methyl是一种IKK抑制剂，具有强的促凋亡和抗炎活性。同时还是有效的Nrf2激活剂和NF-κB抑制剂。	Sci Rep,2018, 8(1):14702 Mol Cell Biol,2018, 38(22) Metab Eng,2017, 42:185-193	Renal Nrf2 activity was shown in RTA402-treated acFSGS (RTA402 + acFSGS) mice as early as day 7 (RTA402 + acFSGS) and persisted to day 28, compared to vehicle + acFSGS mice. Kidney in situ ROS production demonstrated by DHE detection.
S8044	BMS-345541 BMS-345541是一种催化亚基的高选择性抑制剂，作用于IKK-2和IKK-1，无细胞试验中IC50分别为0.3 μM和4 μM。	Oncogene,2019, 38(30):5873-5889 J Exp Clin Cancer Res,2019, 38(1):140 Vascul Pharmacol,2019, 121:106579	(E) After transfection with control or catalase siRNAs for 24 h, A375 and G361 cells were treated with vehicle or 2.5 µM BMS-345541, 20 µM PS-1145 and/or 50 µM of fotemustine for an additional 48 h. Cell viability was then assessed. , p<0.05. (F) A375 and G361 cells were treated with vehicle or 2.5 µM BMS-345541, 20 µM PS-1145 and/or 50 µM of fotemustine, in the presence or absence of catalase inhibitor 3-Amino-1,2,4-triazole (ATZ, 50 µM) for 48 h. Cell viability was then assessed. , p<0.05.
S4907	SC-514 SC-514是一种口服有效的，ATP竞争性的IKK-2抑制剂，IC50为3-12 μM，抑制NF-κB依赖性的基因表达，不抑制其他IKK异构体或其他丝-苏氨酸和酪氨酸激酶。	Cell Signal,2019, 55:17-25 Lab Invest,2018, 98(10):1311-1319 Mol Cells,2018, 41(8):762-770
S1681	Mesalamine Mesalamine是一种抗炎化合物。
S7352	Bay 11-7085 BAY 11-7085 是TNFα诱导的IκBα磷酸化的不可逆抑制剂，其IC50为10 μM。	Eur J Pharmacol,2020, 873:172981 Gastroenterology,2019, 10.1053/j.gastro.2019.11.013 J Allergy Clin Immunol,2019, 143(1):229-244.e9	VSMCs were pretreated with BAY 11-7085 (BAY, 10μmol/L) for 1h and further treated with or without 10^-7mol/L salusin-β for 30min. A, Cytoplasmic extracts (Cy) were obtained and the phosphorylated IκBα, IκBα and HDCA3 protein levels were measured by western blot analysis. B, nuclear extracts (Nu) were obtained and the nuclear p50, p65 and HDAC3 protein levels were measured by western blot analysis. Data are expressed as means ± SD (n=3). *P< 0.05 versus the control with no treatment; #P< 0.05 versus 10^-7mol/L salusin-β treatment alone.
S3615	Dehydrocostus Lactone Dehydrocostus lactone (DHE)是一种天然的倍半萜内酯，抑制IKKβ活性、IκBα的磷酸化和降解、共激活子p300的招募、p50/p65 NF-κB的核转位及它们结合于COX2启动子上的能力。DHE具有抗炎、抗溃疡、抗肿瘤作用和免疫调节活性。	J Cell Mol Med,2019, 23(8):5762-5770
S7851	AZD3264 AZD3264是一种新型IKK2抑制剂。	Redox Biol,2017, 11:562-576	(C) G361 cells were loaded with DCF (ROS probe) and further stimulated with vehicle or indicated IKKβ inhibitors for 3 h. Fluorescence was measured using a fluorescence microplate reader. *, p<0.05 versus control.
S7697	LY2409881 LY2409881 是一种有效的选择性 IKK2 抑制剂，IC50 为 30 nM，选择性比IKK1和其他常见激酶高10倍多。	Nat Commun,2019, 10(1):2924 J Biol Chem,2018, 293(30):11913-11927 Biochem Biophys Res Commun,2018, 503(1):94-101	A549 cells were treated with NF-kB inhibitor LY2409881 (30 nM) for 2 h, followed by western blot analysis of p-NF-kB.
S7691	PS-1145 PS-1145是一种特异性IKK抑制剂，IC50 为 88 nM。	J Biol Chem,2018, 293(19):7268-7280 Redox Biol,2017, 562-576 Blood,2016, 128(1):82-92	(E) After transfection with control or catalase siRNAs for 24 h, A375 and G361 cells were treated with vehicle or 2.5 µM BMS-345541, 20 µM PS-1145 and/or 50 µM of fotemustine for an additional 48 h. Cell viability was then assessed. , p<0.05. (F) A375 and G361 cells were treated with vehicle or 2.5 µM BMS-345541, 20 µM PS-1145 and/or 50 µM of fotemustine, in the presence or absence of catalase inhibitor 3-Amino-1,2,4-triazole (ATZ, 50 µM) for 48 h. Cell viability was then assessed. , p<0.05.
S7948	MRT67307 HCl MRT67307是一种高效的双重的IKKϵ /TBK1抑制剂，其IC50分别为160和19 nM。	Mol Cell,2019, 74(2):347-362.e6 Cell Death Differ,2019, 26(6):1077-1088 Cell,2018, 174(6):1477-1491
S9042	Wedelolactone Wedelolactone, a medicinal plant-derived natural compound, is an inhibitor of IKK that is critical for activation of NF-κB by mediating phosphorylation and degradation of IκBα.	Int Immunopharmacol,2019, 73:17-22
S3612	Rosmarinic acid Rosmarinic acid (RA)是一种天然的羟化化合物。它具有阻止补体结合、抑制脂肪氧合酶和环氧煤活性的功能，通过抑制NF-κB激活信号中IKK-β的活性、抑制CCL11和CCR3的表达。

目录号	产品描述	文献引用	实验数据
S7441	WS3 WS3是一种β细胞增殖诱导剂，通过调节Erb3 binding protein-1 (EBP1)和IκB kinase通路发挥作用。
S7442	WS6 WS6通过调节Erb3 binding protein-1 (EBP1)和IκB kinase通路诱导β细胞增殖。

目录号

产品描述

文献引用

实验数据

S7441