S6 Kinase
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
S6 Kinase产品
| 产品目录 | 产品描述 | 文献引用 | 实验数据 |
|---|---|---|---|
| S2843 |
BI-D1870BI-D1870是一种ATP-竞争性S6 ribosome抑制剂，在无细胞试验中作用于RSK1/2/3/K4，IC50分别为31 nM/24 nM/18 nM/15 nM，作用于RSK比作用于MST2，GSK-3β，MARK3，CK1和Aurora B选择性高10到100倍。 |
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.
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| S1558 |
AT7867AT7867是一种有效的，ATP竞争性的Akt1/2/3和p70S6K/PKA抑制剂，无细胞试验中IC50分别为32 nM/17 n/47 nM和85 nM/20 nM，对AGC激酶家族以外几乎没有抑制活性。 |
(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.
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| S2163 |
PF-4708671PF-4708671是一种细胞渗透性p70 ribosomal S6 kinase(S6K1亚型)抑制剂，在无细胞试验中Ki/IC50为20 nM/160 nM，作用于S6K1比作用于S6K2选择性高400倍，作用于S6K1比作用于MSK1和RSK1/2选择性分别高4和20倍以上，是第一个报道的S6K1特异性抑制剂。 |
(F) EGR-2 and GFI-1 abundance (n = 5).
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| S1582 |
H 89 2HClH 89 2HCl是一种有效的PKA抑制剂，无细胞试验中Ki为48 nM，作用于PKA比作用于PKG选择性高10倍，比作用于PKC，MLCK，钙调蛋白激酶II和酪蛋白激I/II选择性高500倍。 |
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.
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| S7704 |
LY2584702 TosylateLY2584702 Tosylate是一种选择性的，ATP竞争性p70S6K抑制剂，IC50为 4 nM。Phase 1。 |
Samples were processed and analyzed for S6 and phospho-S6 content as described in methods.
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| S8518 |
AD80AD80，一种多激酶抑制剂，对人源RET、BRAF、S6K和SRC活性较强，但对mTOR的活性比AD57或AD58弱。其对RET的IC50值为4 nM。 |
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| S7871 |
LJI308LJI308是一种有效的，泛-RSK (p90核糖体S6激酶)抑制剂，对RSK1，RSK2，和 RSK3的 IC50 分别为 6 nM，4 nM 和 13 nM。 |
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| S7870 |
LJH685LJH685是一种高效的RSK抑制剂，其对RSK1, RSK2和RSK3的IC50分别为6 nM, 5 nM和4 nM。 |
In (E), single (left panel) and double resistant (right panel) SKMel28 cells were treated with vemurafenib, the RSK inhibitor LJH-685 or the combination.
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| S7563 |
AT13148AT13148是一种口服的，ATP竞争性的，多AGC kinase抑制剂，对Akt1/2/3，p70S6K，PKA，和ROCKI/II的IC50分别为38 nM/402 nM/50 nM，8 nM，3 nM，和6 nM/4 nM。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.
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| S7698 |
LY2584702LY2584702是一种选择性的，ATP竞争性的p70S6K抑制剂，IC50为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.
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| 产品目录 | 产品描述 | 文献引用 | 实验数据 |
|---|---|---|---|
| S2843 |
BI-D1870BI-D1870是一种ATP-竞争性S6 ribosome抑制剂，在无细胞试验中作用于RSK1/2/3/K4，IC50分别为31 nM/24 nM/18 nM/15 nM，作用于RSK比作用于MST2，GSK-3β，MARK3，CK1和Aurora B选择性高10到100倍。 |
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是一种有效的，ATP竞争性的Akt1/2/3和p70S6K/PKA抑制剂，无细胞试验中IC50分别为32 nM/17 n/47 nM和85 nM/20 nM，对AGC激酶家族以外几乎没有抑制活性。 |
(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是一种细胞渗透性p70 ribosomal S6 kinase(S6K1亚型)抑制剂，在无细胞试验中Ki/IC50为20 nM/160 nM，作用于S6K1比作用于S6K2选择性高400倍，作用于S6K1比作用于MSK1和RSK1/2选择性分别高4和20倍以上，是第一个报道的S6K1特异性抑制剂。 |
(F) EGR-2 and GFI-1 abundance (n = 5).
|
|
| S1582 |
H 89 2HClH 89 2HCl是一种有效的PKA抑制剂，无细胞试验中Ki为48 nM，作用于PKA比作用于PKG选择性高10倍，比作用于PKC，MLCK，钙调蛋白激酶II和酪蛋白激I/II选择性高500倍。 |
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是一种选择性的，ATP竞争性p70S6K抑制剂，IC50为 4 nM。Phase 1。 |
Samples were processed and analyzed for S6 and phospho-S6 content as described in methods.
|
|
| S8518 |
AD80AD80，一种多激酶抑制剂，对人源RET、BRAF、S6K和SRC活性较强，但对mTOR的活性比AD57或AD58弱。其对RET的IC50值为4 nM。 |
||
| S7871 |
LJI308LJI308是一种有效的，泛-RSK (p90核糖体S6激酶)抑制剂，对RSK1，RSK2，和 RSK3的 IC50 分别为 6 nM，4 nM 和 13 nM。 |
||
| S7870 |
LJH685LJH685是一种高效的RSK抑制剂，其对RSK1, RSK2和RSK3的IC50分别为6 nM, 5 nM和4 nM。 |
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是一种口服的，ATP竞争性的，多AGC kinase抑制剂，对Akt1/2/3，p70S6K，PKA，和ROCKI/II的IC50分别为38 nM/402 nM/50 nM，8 nM，3 nM，和6 nM/4 nM。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.
|
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| S7698 |
LY2584702LY2584702是一种选择性的，ATP竞争性的p70S6K抑制剂，IC50为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.
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