DNA-PK
信号通路图
研究领域
抑制剂选择性比较
DNA-PK产品
| 产品目录 | 产品描述 | 文献引用 | 实验数据 |
|---|---|---|---|
| S1038 |
PI-103PI-103是一种多靶点 PI3K 抑制剂，在无细胞试验中作用于p110α/β/δ/γ的IC50为 2 nM/3 nM/3 nM/15 nM，对 mTOR/DNA-PK的作用较小，IC50为30 nM/23 nM。 |
(D) IGROV parental, shControl (two independent clones) and ShPKCiota (two independent clones) were treated with 5 μM GDC-0941 and 1.5 μM PI-103 for 24 hours and subjected to western blot analysis with the indicated antibodies. Each experiment was performed in triplicate.
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| S2638 |
NU7441 (KU-57788)NU7441 (KU-57788)是一种高度有效的，选择性DNA-PK抑制剂，在无细胞试验中IC50为14 nM，也会抑制PI3K，IC50为5 μM。它可降低NHEJ的频率，而增强Cas9介导DNA剪接后发生的同源重组修复率。 |
Cells were treated with cisplatin under the following conditions: pretreatment with Nu7026 (Nu7026, 26) or Nu7441 (Nu7441, 41). Before DNA damage, wortmannin was applied at 100 nM for 30 min, Nu7026 at 10 uM for 1 h, Nu7441 at 1 uM for 1 h. Accompanying quantifications of the adjusted nucleolar EU fluorescence are shown. Each condition was normalized to cells treated with DMSO or indicated inhibitors without DNA damaging treatment. Two-way ANOVA was followed by Holm-Sidak's test for the comparison of cells with and without inhibitors. *, **, *** represent P ≤ 0.05, 0.01, 0.001, respectively.
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| S1205 |
PIK-75 HClPIK-75 HCl是一种p110α抑制剂，IC50为5.8 nM (比作用于p110β效果强200倍)，在Ser773处功能特异性突变，也有效抑制DNA-PK，无细胞试验中IC50为2 nM。 |
A549 cells were treated with DMSO or PIK-75 (200 nM) for 1 h and subsequently stimulated with izTRAIL for 24 h. Long-term survival was visualized after 7 days by crystal violet staining. One of two independent experiments is shown.
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| S2893 |
NU7026NU7026是一种有效的DNA-PK抑制剂，在无细胞试验中IC50为0.23 μM，作用于DNA-PK比作用于PI3K选择性高60倍，对ATM和ATR没有抑制活性 |
M059K cells were transfected with Scrambled, ERCC1, EGFR, or EGFR–ERCC1 siRNA. Following 48 hours of siRNA transfection, Scrambled siRNA and ERCC1 siRNA-transfected cells were treated with 1 µmol/L gefitinib or 125 nMol/L NU7026, or both, while EGFR siRNA and EGFR–ERCC1 siRNA-transfected cells were treated with 125 nMol/L of NU7026 1 hour prior 4 Gy IR treatment. Survival of these cells was then assessed 72 hours following IR treatment via MTT assay.
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| S2622 |
PP121PP121是一种作用于PDGFR， Hck， mTOR， VEGFR2， Src和Abl的多靶点抑制剂，IC50分别为2 nM， 8 nM， 10 nM， 12 nM， 14 nM和18 nM，也抑制DNA-PK，IC50为60 nM。 |
After starved in serum-free medium for 24 h,A549 cells incubated with the indicated concentrations of PP-121 for 3 h,followed by 20-minute stimolation of 100ng/ml EGF. |
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| S8045 |
KU-0060648KU-0060648是DNA-PK和PI3Kα/β/δ双重抑制剂，IC50分别为8.6 nM和4 nM/0.5 nM/0.1 nM，对PI3Kγ抑制作用稍弱，IC50为0.59 μM。 |
a/ Western blot showing knock down efficiency obtained with the siRNAs targeting either Ku70 or Ku80. b/ Quantitation of genome editing events from cells transfected with pQCiG-TLR and ΔeGFP donor in the presence of 2 μM NU7441, 250 nM KU-0060648, siRNAs targeting Ku70, Ku80, DNA-PKcs or DNA ligase IV, 1 μM Scr7, or a combination of Scr7 and 2 μM NU7441 or 250 nM KU-0060648. The HDR and NHEJ values are relative to those obtained with Cas9, sgRNA, and ΔeGFP donor in the presence of vehicle (DMSO). Results are from biological replicates performed in technical duplicates. Significance (relative to vehicle) was calculated using the Student’s t-test: *p ≤0.05; **p ≤0.01; ns, not significant.
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| S7891 |
CC-115CC-115是DNA依赖性的蛋白激酶DNA-PK和哺乳动物雷帕霉素靶标mTOR的双重抑制剂，IC50分别为0.013 μM 和 0.021 μM。具有潜在的抗肿瘤活性。 |
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| S8589 |
SF2523SF2523是一种有效的、具有高度选择性的PI3K抑制剂，对PI3Kα, PI3Kγ, DNA-PK, BRD4 和 mTOR的IC50分别为34 nM, 158 nM, 9 nM, 241 nM 和 280 nM。 |
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| S8322 |
LY3023414LY3023414是一种口服的ATP竞争性抑制剂，抑制I类PI3K亚型、mTOR和DNA-PK。 |
The structure and formula weight of LY3023414 were presented (A). Established human glioma cells (U251MG and A172 lines), primary human astrocytes (“Astrocytes”) or primary human glioma cells [three lines, “Glioma (L1/2/3)”], were either left untreated (“Ctrl”) or treated with LY3023414 at 1-1000 nM, cells were further cultured for indicated time; Cell survival was tested (B, C, and E) (n=5). Cell proliferation was also tested by the BrdU ELISA assay (D and F) (n=5). *p < 0.05 vs. “Ctrl”. Experiments in this figure were repeated three times.
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| S8379 |
YU238259YU238259是一种新型的homology-dependent DNA repair(HDR)抑制剂，在细胞GFP报告基因实验中，发现其不抑制非同源性末端接合NHEJ。 |
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| S8427 |
LTURM34LTURM34是特异性的DNA-PK抑制剂，对DNA-PK活性的抑制选择性比对PI3K活性的抑制高170倍，IC50为0.034 μM。 |
| 产品目录 | 产品描述 | 文献引用 | 实验数据 |
|---|---|---|---|
| S1038 |
PI-103PI-103是一种多靶点 PI3K 抑制剂，在无细胞试验中作用于p110α/β/δ/γ的IC50为 2 nM/3 nM/3 nM/15 nM，对 mTOR/DNA-PK的作用较小，IC50为30 nM/23 nM。 |
(D) IGROV parental, shControl (two independent clones) and ShPKCiota (two independent clones) were treated with 5 μM GDC-0941 and 1.5 μM PI-103 for 24 hours and subjected to western blot analysis with the indicated antibodies. Each experiment was performed in triplicate.
|
|
| S2638 |
NU7441 (KU-57788)NU7441 (KU-57788)是一种高度有效的，选择性DNA-PK抑制剂，在无细胞试验中IC50为14 nM，也会抑制PI3K，IC50为5 μM。它可降低NHEJ的频率，而增强Cas9介导DNA剪接后发生的同源重组修复率。 |
Cells were treated with cisplatin under the following conditions: pretreatment with Nu7026 (Nu7026, 26) or Nu7441 (Nu7441, 41). Before DNA damage, wortmannin was applied at 100 nM for 30 min, Nu7026 at 10 uM for 1 h, Nu7441 at 1 uM for 1 h. Accompanying quantifications of the adjusted nucleolar EU fluorescence are shown. Each condition was normalized to cells treated with DMSO or indicated inhibitors without DNA damaging treatment. Two-way ANOVA was followed by Holm-Sidak's test for the comparison of cells with and without inhibitors. *, **, *** represent P ≤ 0.05, 0.01, 0.001, respectively.
|
|
| S1205 |
PIK-75 HClPIK-75 HCl是一种p110α抑制剂，IC50为5.8 nM (比作用于p110β效果强200倍)，在Ser773处功能特异性突变，也有效抑制DNA-PK，无细胞试验中IC50为2 nM。 |
A549 cells were treated with DMSO or PIK-75 (200 nM) for 1 h and subsequently stimulated with izTRAIL for 24 h. Long-term survival was visualized after 7 days by crystal violet staining. One of two independent experiments is shown.
|
|
| S2893 |
NU7026NU7026是一种有效的DNA-PK抑制剂，在无细胞试验中IC50为0.23 μM，作用于DNA-PK比作用于PI3K选择性高60倍，对ATM和ATR没有抑制活性 |
M059K cells were transfected with Scrambled, ERCC1, EGFR, or EGFR–ERCC1 siRNA. Following 48 hours of siRNA transfection, Scrambled siRNA and ERCC1 siRNA-transfected cells were treated with 1 µmol/L gefitinib or 125 nMol/L NU7026, or both, while EGFR siRNA and EGFR–ERCC1 siRNA-transfected cells were treated with 125 nMol/L of NU7026 1 hour prior 4 Gy IR treatment. Survival of these cells was then assessed 72 hours following IR treatment via MTT assay.
|
|
| S2622 |
PP121PP121是一种作用于PDGFR， Hck， mTOR， VEGFR2， Src和Abl的多靶点抑制剂，IC50分别为2 nM， 8 nM， 10 nM， 12 nM， 14 nM和18 nM，也抑制DNA-PK，IC50为60 nM。 |
After starved in serum-free medium for 24 h,A549 cells incubated with the indicated concentrations of PP-121 for 3 h,followed by 20-minute stimolation of 100ng/ml EGF. |
|
| S8045 |
KU-0060648KU-0060648是DNA-PK和PI3Kα/β/δ双重抑制剂，IC50分别为8.6 nM和4 nM/0.5 nM/0.1 nM，对PI3Kγ抑制作用稍弱，IC50为0.59 μM。 |
a/ Western blot showing knock down efficiency obtained with the siRNAs targeting either Ku70 or Ku80. b/ Quantitation of genome editing events from cells transfected with pQCiG-TLR and ΔeGFP donor in the presence of 2 μM NU7441, 250 nM KU-0060648, siRNAs targeting Ku70, Ku80, DNA-PKcs or DNA ligase IV, 1 μM Scr7, or a combination of Scr7 and 2 μM NU7441 or 250 nM KU-0060648. The HDR and NHEJ values are relative to those obtained with Cas9, sgRNA, and ΔeGFP donor in the presence of vehicle (DMSO). Results are from biological replicates performed in technical duplicates. Significance (relative to vehicle) was calculated using the Student’s t-test: *p ≤0.05; **p ≤0.01; ns, not significant.
|
|
| S7891 |
CC-115CC-115是DNA依赖性的蛋白激酶DNA-PK和哺乳动物雷帕霉素靶标mTOR的双重抑制剂，IC50分别为0.013 μM 和 0.021 μM。具有潜在的抗肿瘤活性。 |
||
| S8589 |
SF2523SF2523是一种有效的、具有高度选择性的PI3K抑制剂，对PI3Kα, PI3Kγ, DNA-PK, BRD4 和 mTOR的IC50分别为34 nM, 158 nM, 9 nM, 241 nM 和 280 nM。 |
||
| S8322 |
LY3023414LY3023414是一种口服的ATP竞争性抑制剂，抑制I类PI3K亚型、mTOR和DNA-PK。 |
The structure and formula weight of LY3023414 were presented (A). Established human glioma cells (U251MG and A172 lines), primary human astrocytes (“Astrocytes”) or primary human glioma cells [three lines, “Glioma (L1/2/3)”], were either left untreated (“Ctrl”) or treated with LY3023414 at 1-1000 nM, cells were further cultured for indicated time; Cell survival was tested (B, C, and E) (n=5). Cell proliferation was also tested by the BrdU ELISA assay (D and F) (n=5). *p < 0.05 vs. “Ctrl”. Experiments in this figure were repeated three times.
|
|
| S8379 |
YU238259YU238259是一种新型的homology-dependent DNA repair(HDR)抑制剂，在细胞GFP报告基因实验中，发现其不抑制非同源性末端接合NHEJ。 |
||
| S8427 |
LTURM34LTURM34是特异性的DNA-PK抑制剂，对DNA-PK活性的抑制选择性比对PI3K活性的抑制高170倍，IC50为0.034 μM。 |
