IκB/IKK
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
IκB/IKK产品
| 产品目录 | 产品描述 | 文献引用 | 实验数据 |
|---|---|---|---|
| S1274 |
BX-795BX-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。 |
(A) Washed human platelets were untreated or pretreated with the PDK1 inhibitor BX-795 (1 μM) for 5 min, and this was followed by stimulation with 2-methylthio-ADP (2MeSADP) (50 nM) under stirring for 5 min. Western blots were then probed for phosphorylated Akt (Thr308), Akt (Ser473), glycogen synthase kinase 3b (GSK3b) (Ser9), mitogen-activated protein kinase kinase 1/2 (MEK1/2) (Ser217/221), extracellular signal-regulated kinase 1/2 (ERK1/2) (Thr202/Tyr204), and cytosolic phospholipase A2 (cPLA2) (Ser505). The western blots shown are representative of three independent experiments.
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| S2913 |
BAY 11-7082BAY 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。 |
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.
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| 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。 |
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.
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| S2824 |
TPCA-1TPCA-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。 |
GAB2-induced chemokine expression is dependent on IKKβ-NF-κB activity. (a) Effect of small-molecule inhibitors against PI3K (GDC-0941), PI3K/mTOR (BEZ235), MEK (AZD6288) or IKKβ (TPCA-1, IKK16 and Bay 65–1942) on CXCL1, CXCL2 and CXCL8 mRNA levels in GAB2-overexpressing FTSECs. Cells were treated with 2 μm of each inhibitor or DMSO control for 6 h before collected for quantitative PCR analyses. Data are averages±s.e.m. of four independent experiments. Comparison between DMSO- or inhibitor-treated GAB2-overexpressing FTSECs were used for statistical analyses. n.s., not significant; *P<0.05; **P<0.01. (b) Effect of suppressing IKKβ (encoded by IKBKB) or NF-κB p65 (encoded by RELA) on CXCL1, CXCL2 and CXCL8 mRNA levels in GAB2-overexpressing FTSECs. Cells were infected with a control shRNA targeting LacZ or shRNAs targeting IKBKB or RELA and cultured for 48 h before collected for quantitative PCR analyses. Data are averages±s.e.m. of three independent experiments. *P<0.05; **P<0.01.
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| S2864 |
IMD 0354IMD 0354是一种IKKβ抑制剂，作用于NF-κβ通路，抑制IκBα磷酸化。 |
(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.
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| S9042New |
WedelolactoneWedelolactone, 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. |
||
| S8078 |
Bardoxolone MethylBardoxolone 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。 |
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.
|
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| S8044 |
BMS-345541BMS-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。 |
(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.
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| S4907 |
SC-514SC-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。 |
||
| S1681 |
MesalamineMesalamine是一种抗炎化合物。 |
||
| S7352 |
Bay 11-7085BAY 11-7085 是TNFα诱导的IκBα磷酸化的不可逆抑制剂，其IC50为10 μM。 |
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 LactoneDehydrocostus 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。 |
||
| S7851 |
AZD3264AZD3264是一种新型IKK2抑制剂。 |
(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.
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| S7697 |
LY2409881LY2409881 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。 |
A549 cells were treated with NF-kB inhibitor LY2409881 (30 nM) for 2 h, followed by western blot analysis of p-NF-kB.
|
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| S7691 |
PS-1145PS-1145是一种特异性IKK抑制剂，IC50 为 88 nM。 |
(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.
|
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| S7948 |
MRT67307 HClMRT67307是一种高效的双重的IKKϵ /TBK1抑制剂，其IC50分别为160和19 nM。 |
|
|
| S3612 |
Rosmarinic acidRosmarinic 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 |
WS3WS3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 |
WS6WS6通过调节Erb3 binding protein-1 (EBP1)和IκB kinase通路诱导β细胞增殖。 |
| 产品目录 | 产品描述 | 文献引用 | 实验数据 |
|---|---|---|---|
| S1274 |
BX-795BX-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。 |
(A) Washed human platelets were untreated or pretreated with the PDK1 inhibitor BX-795 (1 μM) for 5 min, and this was followed by stimulation with 2-methylthio-ADP (2MeSADP) (50 nM) under stirring for 5 min. Western blots were then probed for phosphorylated Akt (Thr308), Akt (Ser473), glycogen synthase kinase 3b (GSK3b) (Ser9), mitogen-activated protein kinase kinase 1/2 (MEK1/2) (Ser217/221), extracellular signal-regulated kinase 1/2 (ERK1/2) (Thr202/Tyr204), and cytosolic phospholipase A2 (cPLA2) (Ser505). The western blots shown are representative of three independent experiments.
|
|
| S2913 |
BAY 11-7082BAY 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。 |
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。 |
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-1TPCA-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。 |
GAB2-induced chemokine expression is dependent on IKKβ-NF-κB activity. (a) Effect of small-molecule inhibitors against PI3K (GDC-0941), PI3K/mTOR (BEZ235), MEK (AZD6288) or IKKβ (TPCA-1, IKK16 and Bay 65–1942) on CXCL1, CXCL2 and CXCL8 mRNA levels in GAB2-overexpressing FTSECs. Cells were treated with 2 μm of each inhibitor or DMSO control for 6 h before collected for quantitative PCR analyses. Data are averages±s.e.m. of four independent experiments. Comparison between DMSO- or inhibitor-treated GAB2-overexpressing FTSECs were used for statistical analyses. n.s., not significant; *P<0.05; **P<0.01. (b) Effect of suppressing IKKβ (encoded by IKBKB) or NF-κB p65 (encoded by RELA) on CXCL1, CXCL2 and CXCL8 mRNA levels in GAB2-overexpressing FTSECs. Cells were infected with a control shRNA targeting LacZ or shRNAs targeting IKBKB or RELA and cultured for 48 h before collected for quantitative PCR analyses. Data are averages±s.e.m. of three independent experiments. *P<0.05; **P<0.01.
|
|
| S2864 |
IMD 0354IMD 0354是一种IKKβ抑制剂，作用于NF-κβ通路，抑制IκBα磷酸化。 |
(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.
|
|
| S9042New |
WedelolactoneWedelolactone, 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. |
||
| S8078 |
Bardoxolone MethylBardoxolone 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。 |
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-345541BMS-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。 |
(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-514SC-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。 |
||
| S1681 |
MesalamineMesalamine是一种抗炎化合物。 |
||
| S7352 |
Bay 11-7085BAY 11-7085 是TNFα诱导的IκBα磷酸化的不可逆抑制剂，其IC50为10 μM。 |
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 LactoneDehydrocostus 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。 |
||
| S7851 |
AZD3264AZD3264是一种新型IKK2抑制剂。 |
(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 |
LY2409881LY2409881 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。 |
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-1145PS-1145是一种特异性IKK抑制剂，IC50 为 88 nM。 |
(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 HClMRT67307是一种高效的双重的IKKϵ /TBK1抑制剂，其IC50分别为160和19 nM。 |
|
|
| S3612 |
Rosmarinic acidRosmarinic 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。 |
| 产品目录 | 产品描述 | 文献引用 | 实验数据 |
|---|---|---|---|
| S7441 |
WS3WS3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 |
WS6WS6通过调节Erb3 binding protein-1 (EBP1)和IκB kinase通路诱导β细胞增殖。 |
