S6キナーゼ
シグナル伝達経路
研究分野
阻害剤の選択性比較
| カタログ番号 | 製品カタログ | 溶解度(25°C) | ||
|---|---|---|---|---|
| 水 | DMSO | アルコール | ||
| S2843 | BI-D1870 | <1 mg/mL | 78 mg/mL | <1 mg/mL |
| S1558 | AT7867 | <1 mg/mL | 68 mg/mL | 5 mg/mL |
| S2163 | PF-4708671 | <1 mg/mL | 30 mg/mL | 8 mg/mL |
| S1582 | H 89 2HCl | 6 mg/mL | 104 mg/mL | <1 mg/mL |
| S7704 | LY2584702 Tosylate | <1 mg/mL | 7 mg/mL | <1 mg/mL |
| S8518 | AD80 | <1 mg/mL | 94 mg/mL | 94 mg/mL |
| S7871 | LJI308 | <1 mg/mL | 73 mg/mL | <1 mg/mL |
| S7870 | LJH685 | <1 mg/mL | 76 mg/mL | 20 mg/mL |
| S7563 | AT13148 | <1 mg/mL | 62 mg/mL | <1 mg/mL |
| S7698 | LY2584702 | <1 mg/mL | 1 mg/mL | <1 mg/mL |
亜型選択性的な製品
S6 Kinase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 |
|---|---|---|---|
| S2843 |
BI-D1870BI-D1870 is an ATP-competitive inhibitor of S6 ribosome for RSK1/2/3/4 with IC50 of 31 nM/24 nM/18 nM/15 nM in cell-free assays, respectively; 10- to 100-fold selectivity for RSK than MST2, GSK-3β, MARK3, CK1 and Aurora B. |
Expressions of active forms of all p90RSK isoforms were assessed by immunoblotting in Control vs. GR cells following treatment with increasing concentrations of BI-D1870 for 24 hours. Actin was included as a loading control.
|
|
| S1558 |
AT7867AT7867 is a potent ATP-competitive inhibitor of Akt1/2/3 and p70S6K/PKA with IC50 of 32 nM/17 nM/47 nM and 85 nM/20 nM in cell-free assays, respectively; little activity outside the AGC kinase family. |
(B) Treatment of HEK293T cells with the AKT inhibitors MK2206 or AT7867 abolished EGF (20 ng, 15 min)-induced binding of AKT and pT308AKT to CNK1 and also their residual interaction found in non-stimulated cells.
|
|
| S2163 |
PF-4708671PF-4708671 is a cell-permeable inhibitor of p70 ribosomal S6 kinase (S6K1 isoform) with Ki/IC50 of 20 nM/160 nM in cell-free assays, 400-fold greater selectivity for S6K1 than S6K2, and 4- and >20-fold selectivity for S6K1 than MSK1 and RSK1/2, respectively. First S6K1-specific inhibitor to be reported. |
(F) EGR-2 and GFI-1 abundance (n = 5).
|
|
| S1582 |
H 89 2HClH 89 2HCl is a potent PKA inhibitor with Ki of 48 nM in a cell-free assay, 10-fold selective for PKA than PKG,500-fold greater selectivity than PKC, MLCK, calmodulin kinase II and casein kinase I/II. |
The effects of H89 on bTSH-induced FASN downregulation in 3T3-L1 adipocytes. Differentiated 3T3-L1 adipocytes were pretreated with either 20 µmol/L H89 or vehicle for 1 h, then treated with 0.2 µM bTSH for 8 h. Levels of FASN, pCREB, pERK1/2 and pJNK were determined by Western blotting.
|
|
| S7704 |
LY2584702 TosylateLY2584702 Tosylate is a selective, ATP-competitive p70S6K inhibitor with IC50 of 4 nM. Phase 1. |
Samples were processed and analyzed for S6 and phospho-S6 content as described in methods.
|
|
| S8518 |
AD80AD80, a multikinase inhibitor, shows strong activity against human RET, BRAF, S6K, and SRC but were much less active than either AD57 or AD58 against mTOR. The IC50 value for RET is 4 nM. |
||
| S7871 |
LJI308LJI308 is a potent, and pan-RSK (p90 ribosomal S6 kinase) inhibitor with IC50 of 6 nM, 4 nM, and 13 nM for RSK1, RSK2, and RSK3, respectively. |
||
| S7870 |
LJH685LJH685 is a potent pan-RSK inhibitor with IC50 of 6 nM, 5 nM and 4 nM for RSK1, RSK2, and RSK3, respectively. |
In (E), single (left panel) and double resistant (right panel) SKMel28 cells were treated with vemurafenib, the RSK inhibitor LJH-685 or the combination.
|
|
| S7563 |
AT13148AT13148 is an oral, ATP-competitive, multi-AGC kinase inhibitor with IC50 of 38 nM/402 nM/50 nM, 8 nM, 3 nM, and 6 nM/4 nM for Akt1/2/3, p70S6K, PKA, and ROCKI/II, respectively. Phase 1. |
AT13148 exerts cytotoxic and anti-proliferative activity against human gastric cancer cells. Human gastric cancer cells (HGC-27, AGS, SNU-601, N87 and MKN-28 lines) or GEC-1 gastric epithelial cells were treated with applied concentration of AT13148 for indicated time, cell survival (A and E), cell proliferation (B and F), cell cycle distribution (C, for HGC-27 cells) and cell death (D, for HGC-27 cells) were tested by the described assays, separately. Data were presented as mean ± SD. “Ctrl” stands for untreated control cells (For all figures). “hr/hrs” stands for hour/hours (For all figures). Experiments in this figure were repeated for five times. *p < 0.05 vs. “Ctrl” group.
|
|
| S7698 |
LY2584702LY2584702 is a selective, ATP-competitive p70S6K inhibitor with IC50 of 4 nM. Phase 1. |
Murine DCs were pretreated with PBS or kinase inhibitors (10 μmol/l) wortmanni LY2584702 2 h prior to nicotine (10−7 mol/l) 12~15 h stimulation. MR expression was determined via western blot analyses (C, F). β-actin was used as an internal control.
|
| 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 |
|---|---|---|---|
| S2843 |
BI-D1870BI-D1870 is an ATP-competitive inhibitor of S6 ribosome for RSK1/2/3/4 with IC50 of 31 nM/24 nM/18 nM/15 nM in cell-free assays, respectively; 10- to 100-fold selectivity for RSK than MST2, GSK-3β, MARK3, CK1 and Aurora B. |
Expressions of active forms of all p90RSK isoforms were assessed by immunoblotting in Control vs. GR cells following treatment with increasing concentrations of BI-D1870 for 24 hours. Actin was included as a loading control.
|
|
| S1558 |
AT7867AT7867 is a potent ATP-competitive inhibitor of Akt1/2/3 and p70S6K/PKA with IC50 of 32 nM/17 nM/47 nM and 85 nM/20 nM in cell-free assays, respectively; little activity outside the AGC kinase family. |
(B) Treatment of HEK293T cells with the AKT inhibitors MK2206 or AT7867 abolished EGF (20 ng, 15 min)-induced binding of AKT and pT308AKT to CNK1 and also their residual interaction found in non-stimulated cells.
|
|
| S2163 |
PF-4708671PF-4708671 is a cell-permeable inhibitor of p70 ribosomal S6 kinase (S6K1 isoform) with Ki/IC50 of 20 nM/160 nM in cell-free assays, 400-fold greater selectivity for S6K1 than S6K2, and 4- and >20-fold selectivity for S6K1 than MSK1 and RSK1/2, respectively. First S6K1-specific inhibitor to be reported. |
(F) EGR-2 and GFI-1 abundance (n = 5).
|
|
| S1582 |
H 89 2HClH 89 2HCl is a potent PKA inhibitor with Ki of 48 nM in a cell-free assay, 10-fold selective for PKA than PKG,500-fold greater selectivity than PKC, MLCK, calmodulin kinase II and casein kinase I/II. |
The effects of H89 on bTSH-induced FASN downregulation in 3T3-L1 adipocytes. Differentiated 3T3-L1 adipocytes were pretreated with either 20 µmol/L H89 or vehicle for 1 h, then treated with 0.2 µM bTSH for 8 h. Levels of FASN, pCREB, pERK1/2 and pJNK were determined by Western blotting.
|
|
| S7704 |
LY2584702 TosylateLY2584702 Tosylate is a selective, ATP-competitive p70S6K inhibitor with IC50 of 4 nM. Phase 1. |
Samples were processed and analyzed for S6 and phospho-S6 content as described in methods.
|
|
| S8518 |
AD80AD80, a multikinase inhibitor, shows strong activity against human RET, BRAF, S6K, and SRC but were much less active than either AD57 or AD58 against mTOR. The IC50 value for RET is 4 nM. |
||
| S7871 |
LJI308LJI308 is a potent, and pan-RSK (p90 ribosomal S6 kinase) inhibitor with IC50 of 6 nM, 4 nM, and 13 nM for RSK1, RSK2, and RSK3, respectively. |
||
| S7870 |
LJH685LJH685 is a potent pan-RSK inhibitor with IC50 of 6 nM, 5 nM and 4 nM for RSK1, RSK2, and RSK3, respectively. |
In (E), single (left panel) and double resistant (right panel) SKMel28 cells were treated with vemurafenib, the RSK inhibitor LJH-685 or the combination.
|
|
| S7563 |
AT13148AT13148 is an oral, ATP-competitive, multi-AGC kinase inhibitor with IC50 of 38 nM/402 nM/50 nM, 8 nM, 3 nM, and 6 nM/4 nM for Akt1/2/3, p70S6K, PKA, and ROCKI/II, respectively. Phase 1. |
AT13148 exerts cytotoxic and anti-proliferative activity against human gastric cancer cells. Human gastric cancer cells (HGC-27, AGS, SNU-601, N87 and MKN-28 lines) or GEC-1 gastric epithelial cells were treated with applied concentration of AT13148 for indicated time, cell survival (A and E), cell proliferation (B and F), cell cycle distribution (C, for HGC-27 cells) and cell death (D, for HGC-27 cells) were tested by the described assays, separately. Data were presented as mean ± SD. “Ctrl” stands for untreated control cells (For all figures). “hr/hrs” stands for hour/hours (For all figures). Experiments in this figure were repeated for five times. *p < 0.05 vs. “Ctrl” group.
|
|
| S7698 |
LY2584702LY2584702 is a selective, ATP-competitive p70S6K inhibitor with IC50 of 4 nM. Phase 1. |
Murine DCs were pretreated with PBS or kinase inhibitors (10 μmol/l) wortmanni LY2584702 2 h prior to nicotine (10−7 mol/l) 12~15 h stimulation. MR expression was determined via western blot analyses (C, F). β-actin was used as an internal control.
|
