Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T2433 |
NU 7026
NU7026,DNA-PK Inhibitor II,LY293646 |
Apoptosis; ATM/ATR; DNA-PK; PI3K | Apoptosis; DNA Damage/DNA Repair; PI3K/Akt/mTOR signaling |
NU 7026 (DNA-PK Inhibitor II) 是一种新型特异性的DNA-PK 抑制剂,IC50为 0.23 μM,也抑制PI3K,IC50为 13 μM。 | |||
T4339 |
YU238259
|
DNA-PK; Others | DNA Damage/DNA Repair; Others; PI3K/Akt/mTOR signaling |
YU238259 是一种新型的同源依赖性 DNA 修复 (HDR) 抑制剂,在基于细胞的 GFP 报告基因检测中不抑制非同源末端连接 (NHEJ),可研究癌症。 | |||
T15789 |
LTURM34
|
DNA-PK; PI3K; PI4K | DNA Damage/DNA Repair; PI3K/Akt/mTOR signaling |
LTURM34 是一种 DNA-PK 抑制剂,IC50 为 34 nM。它在广泛的肿瘤细胞系中显示出有效的抗增殖活性,对 DNA-PK 的选择性比 PI3K 高 170 倍。 | |||
T2461 |
PIK-90
|
DNA-PK; PI3K | DNA Damage/DNA Repair; PI3K/Akt/mTOR signaling |
PIK90 PIK-90 是一种 DNA-PK 和 PI3K 抑制剂,抑制 p110α、p110γ和DNA-PK,IC50分别为 11、18 和 13 nM。 | |||
T6100 |
Torin 2
|
Apoptosis; ATM/ATR; DNA-PK; mTOR; Autophagy | Apoptosis; Autophagy; DNA Damage/DNA Repair; PI3K/Akt/mTOR signaling |
Torin 2 是一种特异性 mTOR 抑制剂,IC50值为0.25 nM,并改善了药代动力学特性。它抑制 ATM/ATR/DNA-PK 的 EC50 分别为 28 nM/35 nM/118 nM。 | |||
T3541 |
CC-115
CC 115 |
DNA-PK; PI3K; mTOR | DNA Damage/DNA Repair; PI3K/Akt/mTOR signaling |
CC-115 是一种双重 mTOR/DNA-PK 的抑制剂,IC50分别为 21 nM 和 13 nM,可阻断mTORC1和mTORC2信号通路。 | |||
T3986 |
SF2523
|
DNA-PK; Epigenetic Reader Domain; PI3K; mTOR | Chromatin/Epigenetic; DNA Damage/DNA Repair; PI3K/Akt/mTOR signaling |
SF2523 是一种选择性PI3K 抑制剂,抑制DNA-PK、PI3Kα、PI3Kγ、BRD4 和 mTOR,IC50分别为 9 nM、34 nM、158 nM、241 nM 和 280 nM。 | |||
T4459 |
PK11000
|
DNA Alkylator/Crosslinker | DNA Damage/DNA Repair |
PK11000 是一种烷化剂,可通过共价半胱氨酸修饰来稳定野生型和突变型p53的 DNA 结合结构域。 | |||
T9760 |
IC 86621
|
DNA-PK | DNA Damage/DNA Repair; PI3K/Akt/mTOR signaling |
IC 86621 是一种选择性和可逆的 ATP 竞争性 DNA-PK 抑制剂,IC50 为 120 nM。 IC 86621 增加 DNA 双链断裂 (DSB) 诱导的抗肿瘤活性,其 EC50 为 68 µM,用于 DNA-PK 介导的细胞 DSB 修复。 | |||
T6557 |
KU-0060648
KU0060648 |
DNA-PK; PI3K; mTOR | DNA Damage/DNA Repair; PI3K/Akt/mTOR signaling |
KU-0060648 是一种 PI3K 和 DNA-PK 的双重抑制剂,对 PI3Kα、PI3Kβ、PI3Kδ、PI3Kγ 和 DNA-PK 的 IC50值分别为 4 nM、0.5 nM、0.1 nM、0.59 nM 和 8.6 nM。 | |||
T6143 |
PI-103
PI103,PI 103 |
Apoptosis; DNA-PK; PI3K; mTOR; Autophagy | Apoptosis; Autophagy; DNA Damage/DNA Repair; PI3K/Akt/mTOR signaling |
PI-103 是一种 PI3K 和 mTOR 抑制剂,抑制 p110α、p110β、p110δ、p110γ、mTORC1和 mTORC2,IC50分别为 8 nM、88 nM、48 nM、150 nM、20 nM 和 83 nM。它可诱导自噬,还抑制 DNA-PK,IC50为 2 nM。 | |||
T2667 |
PIK-75
|
Apoptosis; DNA-PK; PI3K | Apoptosis; DNA Damage/DNA Repair; PI3K/Akt/mTOR signaling |
PIK75 是一种可逆的DNA-PK 和p110α-选择性的抑制剂,抑制 DNA-PK、p110α 和 p110γ,IC50分别为 2、5.8 和 76 nM。它诱导凋亡,抑制 p110α 效果比抑制 p110β 高 200 多倍,p110β的IC50为 1.3 μM。 | |||
T7122 |
AZD-7648
|
DNA-PK | DNA Damage/DNA Repair; PI3K/Akt/mTOR signaling |
AZD-7648 是一种 DNA 依赖性蛋白激酶 (DNA-PK) 抑制剂,在酶试验中 IC50 为 0.63 nM,具有抗肿瘤活性。 | |||
T25399 |
ETP-45658
ETP45658,ETP 45658 |
DNA-PK; PI3K; mTOR | DNA Damage/DNA Repair; PI3K/Akt/mTOR signaling |
ETP-45658 (ETP45658) 是一种PI3K 抑制剂,抑制PI3Kα、PI3Kδ、PI3Kβ和PI3Kγ的IC50值分别为 22.0、39.8、129.0 和 717.3 nM。它可研究癌症,还抑制DNA-PK 和mTOR,IC50分别为70.6 和 152 nM。 | |||
T6276 |
KU-57788
NU7441 |
DNA-PK; CRISPR/Cas9 | DNA Damage/DNA Repair; PI3K/Akt/mTOR signaling |
KU-57788 (NU7441) 是一种 NHEJ 通路抑制剂,抑制 PI3K 和 mTOR,IC50分别为 5.0 和 1.7 μM。 它是高效的选择性DNA-PK 抑制剂,IC50为 14 nM。 | |||
T6883 |
Samotolisib
GTPL8918,LY3023414 |
DNA-PK; PI3K; mTOR; Autophagy | Autophagy; DNA Damage/DNA Repair; PI3K/Akt/mTOR signaling |
Samotolisib (LY3023414) 在低纳摩尔浓度下,有效抑制mTORC1/2。它选择性地有效抑制PI3Kα、PI3Kβ、PI3Kδ、PI3Kγ、DNA-PK 和mTOR,IC50分别为 6.07 nM、77.6 nM、38 nM、23.8 nM、4.24 nM 和 165 nM。它可用于多种肿瘤和癌症的试验。 | |||
T3586 |
Compound 401
2-morpholino-4H-pyrimido[2,1-a]isoquinolin-4-one |
DNA-PK | DNA Damage/DNA Repair; PI3K/Akt/mTOR signaling |
Compound 401 (2-morpholino-4H-pyrimido[2,1-a]isoquinolin-4-one) 是一种可靶向 mTOR 的合成 DNA-PK 抑制剂,IC50为0.28 μM。 | |||
T13017 |
STL127705
Compound L,7-[[2-(3,4-Dimethoxyphenyl)ethyl]amino]-3-(3-fluorophenyl)pyrimido[4,5-d]pyrimidine-2,4(1H,3H)-dione |
DNA-PK; Others | DNA Damage/DNA Repair; Others; PI3K/Akt/mTOR signaling |
STL127705 (Compound L) 是一种有效的 Ku 70/80 异二聚体蛋白抑制剂,抑制 Ku70/80-DNA 相互作用,IC50 为 3.5 μM。 它抑制 Ku 依赖性 DNA-PKCS 激酶的激活,IC50 为 2.5 μM。 | |||
T25069 |
AMA-37
DNA-PK Inhibitor V,ArylMorpholine Analog 37,AMA 37 |
||
AMA-37 is a selective, reversible, and ATP-competitive DNA-PK inhibitor. | |||
T2008 |
LY294002
LY 294002,NSC 697286,SF 1101 |
Apoptosis; DNA-PK; Casein Kinase; PI3K; Autophagy | Apoptosis; Autophagy; DNA Damage/DNA Repair; Metabolism; PI3K/Akt/mTOR signaling; Stem Cells |
LY294002 (SF 1101) 是一种 PI3K 的广谱抑制剂,抑制 PI3Kα、PI3Kδ 和 PI3Kβ (IC50=0.5/0.57/0.97 μM)。LY294002 也是 DNA-PK 抑制剂 (IC50=1.4 μM) 和 CK2 抑制剂 (IC50=98 nM)。LY294002 可以激活凋亡和自噬。 | |||
T61828 |
DNA-PK-IN-8
|
||
DNA-PK-IN-8(化合物DK1)是一种高效、选择性且口服活性的DNA依赖蛋白激酶 (DNA-PK) 抑制剂,其IC50值为0.8 nM。与Doxorubicin联合应用时,该化合物能在多种癌细胞中展现出协同的抗增殖效应,并能显著地抑制HL-60肿瘤生长。 | |||
T62034 | DNA-PK-IN-7 | ||
DNA-PK-IN-7 是有效的 DNA-PK 抑制剂,IC50为 1 nM (WO2021104277A1, compound 5)。 | |||
T62191 | DNA-PK-IN-5 | ||
DNA-PK-IN-5 是一种 DNA-PK 的有效抑制剂。DNA-PK-IN-5 能够抑制 DNA-PKcs 活性,明显降低肿瘤 DNA 修复,并诱导细胞凋亡。DNA-PK-IN-5 能够提高肿瘤组织对放疗的敏感性,克服耐药问题,提高对多种实体瘤和血液肿瘤的抑制效果。 | |||
T61533 | DNA-PK-IN-9 | ||
DNA-PK-IN-9 (also known as compound YK6) is a highly potent inhibitor of DNA-dependent protein kinase (DNA-PK), displaying an IC50 value of 10.47 nM. DNA-PK-IN-9 holds significant potential in anticancer research [1]. | |||
T79165 |
DNA-PK-IN-10
|
DNA-PK | DNA Damage/DNA Repair; PI3K/Akt/mTOR signaling |
DNA-PK-IN-10是一种DNA-PK抑制剂, 主要应用于乳腺癌与非小细胞肺癌的研究。 | |||
T61857 | DNA-PK-IN-4 | ||
DNA-PK-IN-4 (WO2021209055A1, compound 27), an imidazolinone derivative compound, is a highly effective inhibitor of DNA-PK, specifically targeting DNA-PKcs activity. By inhibiting DNA-PKcs, the compound significantly impairs tumor DNA repair mechanisms and triggers apoptosis in cells. With its potential application in cancer research, DNA-PK-IN-4 holds promise for further investigation [1]. | |||
T61370 |
DNA-PK-IN-6
|
||
DNA-PK-IN-6, a robust DNA-PK inhibitor, effectively hampers the activity of DNA-PKcs, thereby significantly impairing the DNA repair mechanism in tumors and instigating apoptosis in cells. Additionally, DNA-PK-IN-6 amplifies the responsiveness of tumor tissues to radiotherapy, overcomes the challenge of drug resistance, and augments its inhibitory impact on a diverse range of solid and hematological tumors[1]. | |||
T62648 | DNA-PK-IN-1 | ||
DNA-PK-IN-1 是一种 DNA-PK 的有效抑制剂。DNA 依赖性蛋白激酶 (DNA-PK) 是一种由 Ku70/Ku80 异二聚体和 DNA 依赖性蛋白激酶催化亚基 (DNA-PKcs) 组成的 DNA-PK 酶复合物。DNA-PK-IN-1 具有潜力进行癌症疾病的研究。 | |||
T61633 | DNA-PK-IN-2 | ||
DNA-PK-IN-2 is a highly effective inhibitor of DNA-dependent protein kinase (DNA-PK), which is a complex enzyme composed of Ku70/Ku80 heterodimer and DNA-PK catalytic subunit (DNA-PKcs). With its potential applications in cancer research, DNA-PK-IN-2 demonstrates promise as a valuable tool for studying cancer diseases [1]. | |||
T61751 |
DNA-PK-IN-3
|
||
DNA-PK-IN-3 is a highly potent inhibitor of DNA-PK. This compound exerts a synergistic effect when combined with radiotherapy and chemotherapy, resulting in enhanced therapeutic outcomes and significant inhibition of tumor growth. Furthermore, DNA-PK-IN-3 demonstrates remarkable efficacy in reducing damage to normal cells, effectively minimizing adverse side effects. Due to these compelling properties, DNA-PK-IN-3 holds great potential for cancer research applications[1]. | |||
T2287 |
PIK-75 hydrochloride
PIK-75 HCl,2-甲基-5-硝基苯磺酸 [(6-溴咪唑并[1,2-a]吡啶-3-基)亚甲基]甲基肼盐酸盐,PIK-75 |
Apoptosis; DNA-PK; PI3K | Apoptosis; DNA Damage/DNA Repair; PI3K/Akt/mTOR signaling |
PIK-75 hydrochloride (PIK-75 HCl) 是一种可逆的 DNA-PK 和 p110α-选择性抑制剂,抑制 DNA-PK,p110α和 p110γ,可诱导凋亡。 | |||
T4079 |
LY-294002 hydrochloride
SF 1101,LY 294002,NSC 697286 |
PI3K | PI3K/Akt/mTOR signaling |
LY-294002 hydrochloride (NSC 697286) 是一种合成的 PI3Kα/δ/β 分子抑制剂(IC50:0.5/0.57/0.97 μM,在无细胞试验中);在溶液中比 Wortmannin 更稳定,也是自噬体形成的阻断剂。 | |||
T9498 |
BAY-8400
|
DNA-PK | DNA Damage/DNA Repair; PI3K/Akt/mTOR signaling |
BAY-8400是一种具有口服活性、有效和选择性 DNA 依赖蛋白激酶 (DNA-PK) 抑制剂(IC50=81 nM),与靶向α疗法联合使用显示协同疗效。BAY-8400 可用于癌症研究。 | |||
T1826 |
PI3K-IN-1
Voxtalisib Analogue,Voxtalisib (SAR245409, XL765) Analogue,XL765,SAR245409 |
DNA-PK; PI3K | DNA Damage/DNA Repair; PI3K/Akt/mTOR signaling |
PI3K-IN-1 (Voxtalisib Analogue) 是 PI3K 抑制剂,PI3K-IN-1(25 μM) 能够阻断 PI3K/Akt 信号通路。 | |||
T6612 |
NU6027
|
ATM/ATR; DNA-PK; CDK | Cell Cycle/Checkpoint; DNA Damage/DNA Repair; PI3K/Akt/mTOR signaling |
NU6027 是一种有效的 ATR/CDK 抑制剂,抑制 CDK1/2、ATR 和 DNA-PK,Ki 为 2.5 μM/1.3 μM、0.4 μM 和 2.2 μM。它以 ATR 依赖性方式增强羟基脲和顺铂的细胞毒性。 | |||
T7014 |
Voxtalisib
XL765,SAR245409 |
DNA-PK; PI3K; mTOR | DNA Damage/DNA Repair; PI3K/Akt/mTOR signaling |
Voxtalisib (XL765) 是一种PI3K 抑制剂,抑制p110α,p110β,p110γ和p110δ。它抑制mTORC1和mTORC2,IC50s 分别为 160 和 910 nM。它也抑制 DNA-PK (其 IC50=150 nM) 和 mTOR (其 IC50=157 nM)。 | |||
T62083 |
Camonsertib
ATR inhibitor 4,RP-3500 |
ATM/ATR | DNA Damage/DNA Repair; PI3K/Akt/mTOR signaling |
Camonsertib (RP-3500) 是一种选择性的、口服具有活力的 ATR 激酶抑制剂 (ATRi),在生化试验中的 IC50: 1.00 nM,表现出有效的抗肿瘤作用。RP-3500 对 ATR 的选择性是 mTOR 的 30 倍 (IC50: 120 nM),是 ATM、DNA-PK 和 PI3Kα 激酶的 2,000 倍以上。 | |||
T8637 |
DMNB
6-Nitroveratraldehyde,6-硝基藜芦醛 |
DNA-PK | DNA Damage/DNA Repair; PI3K/Akt/mTOR signaling |
DMNB (6-Nitroveratraldehyde) 可用于合成no-carrier-added 6-[18F]fluoro-L-DOPA (6-FDOPA)。它可用于研究多巴胺能系统的PET。 | |||
T8651 |
CAL-101
(S)-2-(1-(9H-Purin-6-ylamino)ethyl)-5-fluoro-3-phenylquinazolin-4(3H)-one,GS-1101,Idelalisib |
PI3K | PI3K/Akt/mTOR signaling |
CAL-101 (Idelalisib) 是 p110δ 的选择性抑制剂(IC50:2.5 nM;在无细胞试验中);显示对 p110δ 的选择性比 p110α/β/γ 高 40 到 300 倍,对 p110δ 的选择性比 C2β、hVPS34、DNA-PK 和 mTOR 高 400 到 4000 倍。 | |||
T2415 |
PP121
|
Apoptosis; VEGFR; Bcr-Abl; PDGFR; Src; mTOR; Hck | Angiogenesis; Apoptosis; Cytoskeletal Signaling; PI3K/Akt/mTOR signaling; Tyrosine Kinase/Adaptors |
PP121是一种多靶点激酶抑制剂,抑制 PDGFR、Hck、mTOR、VEGFR2、Src、Abl、DNK-PK 的 IC50值分别为2、8、10、12、14、18、60 nM。 | |||
T11067 |
VX-984
M9831 |
DNA-PK | DNA Damage/DNA Repair; PI3K/Akt/mTOR signaling |
VX-984 (M9831) 是一种可口服的、具有选择性的的、可透过血脑屏障的 DNA-PK 抑制剂。VX-984 对非同源性末端 NHEJ 的接合具有抑制作用,可作用于 DSBs 使 DNA 双链断裂。VX-984常见于对胶质母细胞瘤 (GBM) 和非小细胞肺癌 (NSC-LC) 的研究。 | |||
T6319 |
OSI-027
ASP4786,OSI027 |
DNA-PK; PI3K; mTOR; Autophagy | Autophagy; DNA Damage/DNA Repair; PI3K/Akt/mTOR signaling |
OSI-027 (ASP4786) 是一种选择性、可口服和 ATP 竞争性的mTOR 激酶活性抑制剂,IC50为 4 nM。它抑制mTORC1和mTORC2,IC50分别为 22 nM 和 65 nM。 | |||
T2685 |
KU-55933
ATM Kinase Inhibitor |
ATM/ATR; DNA-PK; PI3K; mTOR; Autophagy | Autophagy; DNA Damage/DNA Repair; PI3K/Akt/mTOR signaling |
KU-55933 (ATM Kinase Inhibitor) 是一种 ATM 抑制剂,IC50和 Ki 值分别为 12.9 和 2.2 nM。它对 ATM 的选择性比对 PI3K/PI4K、 DNA-PK、ATR 和 mTOR 高。 | |||
T12672 |
(Rac)-Nedisertib
(Rac)-M3814 |
DNA-PK | DNA Damage/DNA Repair; PI3K/Akt/mTOR signaling |
(Rac)-Nedisertib is a racemate of Nedisertib, a potent inhibitor of DNA-PK(IC50 of <3 nM). | |||
T6283 |
Wortmannin
SL-2052,渥曼青霉素,KY-12420 |
ATM/ATR; DNA-PK; Serine/threonin kinase; PLK; PI3K; Antibiotic; Autophagy | Autophagy; Cell Cycle/Checkpoint; DNA Damage/DNA Repair; Metabolism; Microbiology/Virology; PI3K/Akt/mTOR signaling |
Wortmannin (SL-2052) 是一种 PI3K 抑制剂 (IC50=3 nM),具有共价性和不可逆性。Wortmannin 也是一种 PlK1 和 PlK3 的抑制剂 (IC50=5.8/48 nM),可以阻断自噬。 | |||
T13444 |
(R)-Nedisertib
(R)-M3814 |
Others | Others |
(R)-Nedisertib is a less active R-enantiomer of Nedisertib(IC50 in the range of 7-30 nM for DNA-PK). | |||
T68192 | OK-1035 | ||
OK-1035 is a potent and selective DNA-PK inhibitor. When a synthetic peptide was used as a substrate, OK-1035 caused 50% inhibition of DNA-PK activity at 8 microM. OK-1035 inhibited the phosphorylation by DNA-PK of consensus peptide as well as that of recombinant human wild type-p53. Kinetic studies indicated that OK-1035 inhibited DNA-PK activity in an ATP-competitive manner. | |||
T24559 |
NU-7163
NU 7163,NU7163 |
||
NU-7163 is a potent and selective inhibitor of ATP-competitive DNA-PK. | |||
T68978 |
KU-0058684
|
||
KU-0058684 is a potent PARP and DNA-PK inhibitors. | |||
T68691 | NU-7031 | ||
NU-7031 is a potent DNA-PK inhibitor with potential anticancer activity. |