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抑制剂选择性比较

DNA-PK产品

所有产品 DNA-PK抑制剂(13) 新DNA-PK产品

目录号	产品描述	文献引用	实验数据
S1038	PI-103 PI-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。	Cancer Cell, 2019, 36(2):179-193 Cell, 2019, 36(2):179-193 Gastroenterology, 2019, 157(6):1615-1629	We treated all of drugs in T47D which has a PI3KCA H1044R mutation with the concentration shown below for 1 hour and performed western blot analysis using antibodies to phospho-AKT(SERINE 472), and total AKT.
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。	Nucleic Acids Res, 2020, 48(2):736-747 Nature, 2019, 74(7779):571-574 Cancer Cell, 2019, 36(2):179-193	Validation of activity and specificity of chemical inhibitors of; ATM, ATR, and DNAPK. H460 cells were treated with 1 uM camptothecin (CPT) or 20 ug/ml bleomycin for 1 h in the presence of the indicated inhibitors: DNAPK-i1—NU7026, DNAPK-i2—NU7441. MSH6, fibrillarin, and tubulin were used as loading controls.Effects of DNAPK inhibitors on its autophosphorylation in bleomycin-treated cells.
S1205	PIK-75 HCl PIK-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。	Cancer Cell, 2019, 35(5):752-766 Cell Metab, 2019, 29(6):1400-1409 J Thorac Oncol, 2019, 10.1016/j.jtho.2019.10.009	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	NU7026 NU7026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	Nat Commun, 2019, 10(1):5718 Nucleic Acids Res, 2019, 47(7):3503-3520 Cancer Res, 2019, 10.1158/0008-5472.CAN-18-3388	DNA damage-induced inhibition of rRNA synthesis is dependent on DNA-PK and PARP-1 activity. Representative nuclei stained by EU are shown 22 h after 2 h treatment with 25 µg/ml cisplatin. Cells were treated with cisplatin under the following conditions: pretreatment with Nu7026 (Nu7026, 26) or Nu7441 (Nu7441, 41)
S2622	PP121 PP121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。	Biochem Biophys Res Commun, 2015, 465(1):137-44 Tumour Biol, 2014, 35(9):8659-64 Int J Clin Exp Pathol, 2013, 6(10):2082-91	PP121 induces apoptosis in ATC cells. CAL62 cells were treated with PP121 at the indicated concentrations for 48 h, followed by PI staining. The nuclei were stained with Hoechst and analyzed using a fluorescent microscope. The representative images are shown.
S8843^New	AZD7648 AZD7648是DNA-PK的有效抑制剂，IC50为0.6 nM，其选择性比对所检测激酶库中其他的396种激酶高100倍以上。
S6506^New	Compound 401 Compound 401是DNA-PK和mTOR抑制剂（IC50为5.3 μM）。它对p110α/p85α PI3K没有明显抑制作用，在COS7细胞中抑制S6激酶在Thr389位的磷酸化和Akt在Ser473位的磷酸化。
S8045	KU-0060648 KU-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。	Cell, 2019, 176(3):505-519 Cancer Res, 2019, 79(1):99-113 Mol Cancer Ther, 2018, 17(2):419-431	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-115 CC-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	SF2523 SF2523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。	Oncotarget, 2017, 8(58):98471-98481
S8322	LY3023414(Samotolisib) LY3023414是一种口服的ATP竞争性抑制剂，抑制I类PI3K亚型、mTOR和DNA-PK。	Oncotarget, 2017, 8(58):98964-98973	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	YU238259 YU238259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	LTURM34 LTURM34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。

目录号	产品描述	文献引用	实验数据
S1038	PI-103 PI-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。	Cancer Cell,2019, 36(2):179-193 Cell,2019, 36(2):179-193 Gastroenterology,2019, 157(6):1615-1629	We treated all of drugs in T47D which has a PI3KCA H1044R mutation with the concentration shown below for 1 hour and performed western blot analysis using antibodies to phospho-AKT(SERINE 472), and total AKT.
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。	Nucleic Acids Res,2020, 48(2):736-747 Nature,2019, 74(7779):571-574 Cancer Cell,2019, 36(2):179-193	Validation of activity and specificity of chemical inhibitors of; ATM, ATR, and DNAPK. H460 cells were treated with 1 uM camptothecin (CPT) or 20 ug/ml bleomycin for 1 h in the presence of the indicated inhibitors: DNAPK-i1—NU7026, DNAPK-i2—NU7441. MSH6, fibrillarin, and tubulin were used as loading controls.Effects of DNAPK inhibitors on its autophosphorylation in bleomycin-treated cells.
S1205	PIK-75 HCl PIK-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。	Cancer Cell,2019, 35(5):752-766 Cell Metab,2019, 29(6):1400-1409 J Thorac Oncol,2019, 10.1016/j.jtho.2019.10.009	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	NU7026 NU7026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	Nat Commun,2019, 10(1):5718 Nucleic Acids Res,2019, 47(7):3503-3520 Cancer Res,2019, 10.1158/0008-5472.CAN-18-3388	DNA damage-induced inhibition of rRNA synthesis is dependent on DNA-PK and PARP-1 activity. Representative nuclei stained by EU are shown 22 h after 2 h treatment with 25 µg/ml cisplatin. Cells were treated with cisplatin under the following conditions: pretreatment with Nu7026 (Nu7026, 26) or Nu7441 (Nu7441, 41)
S2622	PP121 PP121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。	Biochem Biophys Res Commun,2015, 465(1):137-44 Tumour Biol,2014, 35(9):8659-64 Int J Clin Exp Pathol,2013, 6(10):2082-91	PP121 induces apoptosis in ATC cells. CAL62 cells were treated with PP121 at the indicated concentrations for 48 h, followed by PI staining. The nuclei were stained with Hoechst and analyzed using a fluorescent microscope. The representative images are shown.
S8843^New	AZD7648 AZD7648是DNA-PK的有效抑制剂，IC50为0.6 nM，其选择性比对所检测激酶库中其他的396种激酶高100倍以上。
S6506^New	Compound 401 Compound 401是DNA-PK和mTOR抑制剂（IC50为5.3 μM）。它对p110α/p85α PI3K没有明显抑制作用，在COS7细胞中抑制S6激酶在Thr389位的磷酸化和Akt在Ser473位的磷酸化。
S8045	KU-0060648 KU-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。	Cell,2019, 176(3):505-519 Cancer Res,2019, 79(1):99-113 Mol Cancer Ther,2018, 17(2):419-431	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-115 CC-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	SF2523 SF2523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。	Oncotarget,2017, 8(58):98471-98481
S8322	LY3023414(Samotolisib) LY3023414是一种口服的ATP竞争性抑制剂，抑制I类PI3K亚型、mTOR和DNA-PK。	Oncotarget,2017, 8(58):98964-98973	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	YU238259 YU238259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	LTURM34 LTURM34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。

Tags: DNA-PK activation | DNA-PK phosphorylation | DNA-PK assay | DNA-PK activity | DNA-PK activation | DNA-PK pathway | DNA-PK inhibitor clinical trial | DNA-PKcs phosphorylation | DNA-PK function | DNA-PK inhibitor review