IκB/IKK
シグナル伝達経路
研究分野
- 阻害剤の選択性比較
- 溶解度
| カタログ番号 | 製品カタログ | 溶解度(25°C) | ||
|---|---|---|---|---|
| 水 | DMSO | アルコール | ||
| S1274 | BX-795 | <1 mg/mL | 100 mg/mL | <1 mg/mL |
| S2882 | IKK-16 (IKK Inhibitor VII) | <1 mg/mL | 97 mg/mL | <1 mg/mL |
| S2824 | TPCA-1 | <1 mg/mL | 56 mg/mL | <1 mg/mL |
| S2864 | IMD 0354 | <1 mg/mL | 10 mg/mL | 77 mg/mL |
| S8044 | BMS-345541 | <1 mg/mL | 9 mg/mL | <1 mg/mL |
| S9042 | Wedelolactone | -1 mg/mL | 63 mg/mL | -1 mg/mL |
| S4907 | SC-514 | <1 mg/mL | 45 mg/mL | <1 mg/mL |
| S1681 | Mesalamine | <1 mg/mL | 31 mg/mL | 31 mg/mL |
| S3615 | Dehydrocostus Lactone | <1 mg/mL | 46 mg/mL | 46 mg/mL |
| S7851 | AZD3264 | <1 mg/mL | 88 mg/mL | 2 mg/mL |
| S7697 | LY2409881 | <1 mg/mL | 20 mg/mL | <1 mg/mL |
| S7691 | PS-1145 | <1 mg/mL | 64 mg/mL | 2 mg/mL |
| S7948 | MRT67307 HCl | 92 mg/mL | 92 mg/mL | 92 mg/mL |
| S3612 | Rosmarinic acid | 24 mg/mL | 72 mg/mL | 72 mg/mL |
| S7441 | WS3 | <1 mg/mL | 100 mg/mL | 80 mg/mL |
| S7442 | WS6 | <1 mg/mL | 100 mg/mL | 100 mg/mL |
亜型選択性的な製品
IκB/IKK製品
| 製品コード | 製品説明 | 文献中Selleckの製品使用例 | お客様のフィードバック |
|---|---|---|---|
| S1274 |
BX-795BX795 is a potent and specific PDK1 inhibitor with IC50 of 6 nM, 140- and 1600-fold more selective for PDK1 than PKA and PKC in cell-free assays, respectively. Meanwhile, in comparison to GSK3β more than 100-fold selectivity observed for PDK1. |
(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.
|
|
| S2882 |
IKK-16 (IKK Inhibitor VII)IKK-16 (IKK Inhibitor VII) is a selective IκB kinase (IKK) inhibitor for IKK-2, IKK complex and IKK-1 with IC50 of 40 nM, 70 nM and 200 nM in cell-free assays, respectively. |
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 is an inhibitor of IKK-2 with IC50 of 17.9 nM in a cell-free assay, inhibits NF-κB pathway, exhibits 22-fold selectivity over IKK-1. |
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 is an IKKβ inhibitor and blocks IκBα phosphorylation in NF-κB pathway. |
(C) ELISA showed that the elevated IL-8 was significantly inhibited in HUVEC-shCD109 when pretreated with SB525334, LY294002, or IMD 0354. GAPDH served as a loading control for WB. Data shown as mean ± SD were from triplicates of three independent experiments. **P < 0.01 by t test. CM, conditioned media; NC, negative control.
|
|
| S8044 |
BMS-345541BMS-345541 is a highly selective inhibitor of the catalytic subunits of IKK-2 and IKK-1 with IC50 of 0.3 μM and 4 μM in cell-free assays, respectively. |
(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.
|
|
| S9042新 |
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. |
||
| S4907 |
SC-514SC-514 is an orally active, ATP-competitive IKK-2 inhibitor with IC50 of 3-12 μM, blocks NF-κB-dependent gene expression, does not inhibit other IKK isoforms or other serine-threonine and tyrosine kinases. |
||
| S1681 |
MesalamineMesalamine is a specific inhibitor of TNFα-induced IKK activity, used to treat inflammatory bowel disease. |
||
| S3615 |
Dehydrocostus LactoneDehydrocostus lactone (DHE), a natural sesquiterpene lactone, inhibits IKKβ activity, IκBα phosphorylation and degradation, coactivators p300 recruitments and p50/p65 NF-κB nuclear translocation, and their DNA binding activity on COX-2 promoter. It has anti-inflammatory, anti-ulcer, immunomodulatory and anti-tumor properties. |
||
| S7851 |
AZD3264AZD3264 is a novel IKK2 inhibitor. |
(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 is a potent and selective IKK2 inhibitor with IC50 of 30 nM, >10-fold selectivity over IKK1 and other common kinases. |
||
| S7691 |
PS-1145PS-1145 is a specific IKK inhibitor with IC50 of 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 is a potent and dual IKKϵ and TBK1 inhibitor with IC50 of 160 and 19 nM, respectively. |
|
|
| S3612 |
Rosmarinic acidRosmarinic acid (RA) is a naturally occurring hydroxylated compound. It has the ability to block complement fixation, inhibit lipoxygenase and cyclooxygenase activity and inhibit the expression of CCL11 and CCR3 by suppressing the IKK-β activity in NF-κB activation signaling. |
||
| S7441 |
WS3WS3 is a β cell proliferation inducer via modulation of Erb3 binding protein-1 (EBP1) and the IκB kinase pathway. |
||
| S7442 |
WS6WS6 is a β cell proliferation inducer via modulation of Erb3 binding protein-1 (EBP1) and the IκB kinase pathway. |
| 製品コード | 製品説明 | 文献中Selleckの製品使用例 | お客様のフィードバック |
|---|---|---|---|
| S1274 |
BX-795BX795 is a potent and specific PDK1 inhibitor with IC50 of 6 nM, 140- and 1600-fold more selective for PDK1 than PKA and PKC in cell-free assays, respectively. Meanwhile, in comparison to GSK3β more than 100-fold selectivity observed for PDK1. |
(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.
|
|
| S2882 |
IKK-16 (IKK Inhibitor VII)IKK-16 (IKK Inhibitor VII) is a selective IκB kinase (IKK) inhibitor for IKK-2, IKK complex and IKK-1 with IC50 of 40 nM, 70 nM and 200 nM in cell-free assays, respectively. |
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 is an inhibitor of IKK-2 with IC50 of 17.9 nM in a cell-free assay, inhibits NF-κB pathway, exhibits 22-fold selectivity over IKK-1. |
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 is an IKKβ inhibitor and blocks IκBα phosphorylation in NF-κB pathway. |
(C) ELISA showed that the elevated IL-8 was significantly inhibited in HUVEC-shCD109 when pretreated with SB525334, LY294002, or IMD 0354. GAPDH served as a loading control for WB. Data shown as mean ± SD were from triplicates of three independent experiments. **P < 0.01 by t test. CM, conditioned media; NC, negative control.
|
|
| S8044 |
BMS-345541BMS-345541 is a highly selective inhibitor of the catalytic subunits of IKK-2 and IKK-1 with IC50 of 0.3 μM and 4 μM in cell-free assays, respectively. |
(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.
|
|
| S9042新 |
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. |
||
| S4907 |
SC-514SC-514 is an orally active, ATP-competitive IKK-2 inhibitor with IC50 of 3-12 μM, blocks NF-κB-dependent gene expression, does not inhibit other IKK isoforms or other serine-threonine and tyrosine kinases. |
||
| S1681 |
MesalamineMesalamine is a specific inhibitor of TNFα-induced IKK activity, used to treat inflammatory bowel disease. |
||
| S3615 |
Dehydrocostus LactoneDehydrocostus lactone (DHE), a natural sesquiterpene lactone, inhibits IKKβ activity, IκBα phosphorylation and degradation, coactivators p300 recruitments and p50/p65 NF-κB nuclear translocation, and their DNA binding activity on COX-2 promoter. It has anti-inflammatory, anti-ulcer, immunomodulatory and anti-tumor properties. |
||
| S7851 |
AZD3264AZD3264 is a novel IKK2 inhibitor. |
(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 is a potent and selective IKK2 inhibitor with IC50 of 30 nM, >10-fold selectivity over IKK1 and other common kinases. |
||
| S7691 |
PS-1145PS-1145 is a specific IKK inhibitor with IC50 of 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 is a potent and dual IKKϵ and TBK1 inhibitor with IC50 of 160 and 19 nM, respectively. |
|
|
| S3612 |
Rosmarinic acidRosmarinic acid (RA) is a naturally occurring hydroxylated compound. It has the ability to block complement fixation, inhibit lipoxygenase and cyclooxygenase activity and inhibit the expression of CCL11 and CCR3 by suppressing the IKK-β activity in NF-κB activation signaling. |
| 製品コード | 製品説明 | 文献中Selleckの製品使用例 | お客様のフィードバック |
|---|---|---|---|
| S7441 |
WS3WS3 is a β cell proliferation inducer via modulation of Erb3 binding protein-1 (EBP1) and the IκB kinase pathway. |
||
| S7442 |
WS6WS6 is a β cell proliferation inducer via modulation of Erb3 binding protein-1 (EBP1) and the IκB kinase pathway. |
