ATM/ATR
信号通路图
研究领域
- 抑制剂选择性比较
- 溶解性比较
| 目录号 | 产品目录 | 溶解度(25°C) | ||
|---|---|---|---|---|
| 水 | DMSO | 酒精 | ||
| S1009 | Dactolisib (BEZ235, NVP-BEZ235) | <1 mg/mL | 0.01 mg/mL | <1 mg/mL |
| S1092 | KU-55933 (ATM Kinase Inhibitor) | <1 mg/mL | 33 mg/mL | <1 mg/mL |
| S1570 | KU-60019 | <1 mg/mL | 18 mg/mL | <1 mg/mL |
| S8007 | VE-821 | <1 mg/mL | 74 mg/mL | <1 mg/mL |
| S2758 | Wortmannin | <1 mg/mL | 85 mg/mL | <1 mg/mL |
| S8680 | AZD1390 | <1 mg/mL | 14 mg/mL | 95 mg/mL |
| S8666 | BAY 1895344 (BAY-1895344) | 82 mg/mL | 82 mg/mL | 82 mg/mL |
| S2817 | Torin 2 | <1 mg/mL | 20 mg/mL | <1 mg/mL |
| S2245 | CP-466722 | <1 mg/mL | 0.28 mg/mL | <1 mg/mL |
| S7102 | VE-822 | <1 mg/mL | 36 mg/mL | <1 mg/mL |
| S8050 | ETP-46464 | <1 mg/mL | 6 mg/mL | <1 mg/mL |
| S7136 | CGK 733 | <1 mg/mL | 100 mg/mL | <1 mg/mL |
| S7050 | AZ20 | <1 mg/mL | 83 mg/mL | 3 mg/mL |
| S7693 | AZD6738 | <1 mg/mL | 82 mg/mL | 41 mg/mL |
| S3600 | Schisandrin B (Sch B) | <1 mg/mL | 80 mg/mL | 10 mg/mL |
| S8096 | Mirin | <1 mg/mL | 44 mg/mL | <1 mg/mL |
| S8375 | AZD0156 | <1 mg/mL | 0.3 mg/mL | 2 mg/mL |
| S4157 | Chloroquine Phosphate | 100 mg/mL | <1 mg/mL | <1 mg/mL |
特异性亚型抑制剂
- ATM/ATR抑制剂（18）
- 新ATM/ATR产品
| 产品目录 | 产品描述 | 文献引用 | 实验数据 |
|---|---|---|---|
| S1009 |
Dactolisib (BEZ235, NVP-BEZ235)Dactolisib (BEZ235, NVP-BEZ235) 是一种双重ATP竞争性 PI3K 和 mTOR 抑制剂，在无细胞试验中，抑制 p110α/γ/δ/β 和 mTOR(p70S6K) 的 IC50 分别为 4 nM /5 nM /7 nM /75 nM /6 nM。 在 3T3TopBP1-ER 细胞中抑制 ATR，IC50 为 21 nM，而对 Akt 和 PDK1 的抑制作用很弱。Phase 2。 |
Level of phospho-proteins in RTK and PI3K–Akt–mTOR pathways in treated tumours, detected with western blot.
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| S1092 |
KU-55933 (ATM Kinase Inhibitor)KU-55933 (ATM Kinase Inhibitor)是一种有效的，特异性ATM抑制剂，在无细胞试验中IC50/Ki为12.9 nM/2.2 nM，与DNA-PK， PI3K/PI4K， ATR和mTOR相比，对ATM具有高度选择性。 |
Effects of NVP-BKM120 and KU-55933 and their combination on the DNA damage response. A, HCC1937 cells were treated for 18 hours with NVP-BKM120 at 2.5 μmol/L, KU-55933 at 10 μmol/L, or their combination, subjected to ionizing radiation(IR) with 10 Gy or mock, lysed 6 hours later, and subjected to immunoblotting with antibodies as indicated. |
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| S1570 |
KU-60019KU-60019是一种改进的KU-55933类似物，在无细胞试验中作用于ATM，IC50为6.3 nM，作用于ATM比作用于DNA-PK和ATR的选择性分别高270和1600倍，并且是高度有效的放射增敏剂。 |
The ATM-dependent Ser15-p53 phosphorylation was monitored by Western blotting. Protein loading levels were monitored by probing for actin.
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| S8007 |
VE-821VE-821是一种有效的，选择性的，ATP竞争性ATR抑制剂，在无细胞试验中Ki/IC50为13 nM/26 nM，抑制H2AX磷酸化，对PIKKs ATM， DNA-PK， mTOR和PI3Kγ具有很低的抑制活性。 |
Cell viability response to ATR inhibitor.
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| S2758 |
WortmanninWortmannin是一种首次命名的PI3K抑制剂，在无细胞试验中IC50为3 nM，对 PI3K 家族的选择性较低。也会抑制自噬体的形成，并有效抑制DNA-PK/ATM，在无细胞试验中IC50为16 nM和150 nM。 |
L3.6pl cells at 6,000 cells per well were incubated in MEM with 5% FBS in triplicate in a 96-well culture plate and then treated alone with 5 umol/L BMS-777607, 10 umol/L wortmannin, or with BMS-777607 in combination with individual inhibitors. Polyploidy was examined under BK71 Olympus microscope and photographed 72 hours after treatment. |
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| S8680New |
AZD1390AZD1390 is a first-in-class orally available and CNS penetrant ATM inhibitor with an IC50 of 0.78 nM in cells and >10,000-fold selectivity over closely related members of the PIKK family of enzymes and excellent selectivity across a broad panel of kinases. |
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| S8666New |
BAY 1895344 (BAY-1895344)BAY 1895344是有效的、高选择性的、具有口服生物活性的ATR抑制剂，IC50为7 nM。 |
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| S2817 |
Torin 2Torin 2 是一种有效的选择性mTOR抑制剂，在p53−/− MEFs细胞系中IC50为0.25 nM；作用于mTOR比作用于PI3K选择性高800倍，并且改善了药代动力学性能。抑制ATM/ATR/DNA-PK，在PC3细胞系中EC50分别为28 nM/35 nM/118 nM。 |
A. Western Blot analysis in the ALL-SIL cell line treated with single administration of Imatinib, Nilotinib, GZD824, Torin-2 and BGT226 for 24 h. An increase of expression of fast-migrating (lipidated) LC3A/B after drug treatments is shown. Twenty-five μg of protein were blotted on each lane. β-Actin documented equal lane loading. B. Flow cytometric analysis of autophagy in the ALL-SIL and PEER cell lines treated with single or combined administration of Imatinib, Nilotinib, GZD824 with Torin-2 or BGT226 for 24 h. CTRL, control (untreated) cells. Asterisks indicate significant differences in comparison to single drug treated samples (*p< 0.05). Imatinib, Nilotinib, GZD824, Torin-2 and BGT226 were abbreviated in IMA, NIL, GZD, TOR and BGT.
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| S2245 |
CP-466722CP-466722是一种有效的，可逆的ATM抑制剂，不影响ATR，且抑制PI3K或PIKK家族成员。 |
HCT116 cells expressing the DDR-Act reporter were treated with Etoposide 20 μM (E20) for 24 hours, in the absence or in the presence of KU-55933 or CP-466722 at the indicated concentration. (A) Western blot analysis of p53 and actin as control.
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| S7102 |
VE-822VE-822是一种ATR抑制剂，在HT29细胞中IC50 为 19 nM。 |
Flow cytometry analysis of E14.5 FL lineage negative cells from indicated genotypes treated with ATMi (KU-55933; 1nM), ATRi (VE-822; 1nM) or both inhibitors or DMSO as a negative control for 24 hours in culture before AnnexinV and PI levels were measured.
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| S8050 |
ETP-46464ETP-46464是一种有效的，选择性ATR抑制剂，IC50为25 nM。 |
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| S7136 |
CGK 733CGK 733是一种有效的ATM/ATR选择性抑制剂，IC50约为200 nM。 |
K562 and K562R cells were pre-treated for 1 h with CGK733 (5 μM), then treated with CTD (10 μM) for 24 h, and protein levels of cleaved PARP, Mcl-1, and phosphorylated H3 were determined by Western blotting. GAPDH served as a normal control.
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| S7050 |
AZ20AZ20是一种新型有效的选择性ATR激酶抑制剂，无细胞试验中IC50为5 nM，比作用于mTOR的选择性高8倍。 |
(B) SAHA treatment impairs the HR capacity of GBM03 cells. AZ20(ATRi) as a positive control.
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| S7693 |
AZD6738AZD6738是一种口服具有活性的，选择性 ATR 激酶抑制剂，IC50 为 1 nM。Phase 1/2。 |
AZD6738 (AZD) synergizes with cytarabine (ara-C) to induce apoptosis and proliferation inhibition in AML cells. (a) OCI-AML3 cells were treated with cytarabine and AZD6738, alone or in combination, for 24 h and then subjected to annexin V-FITC/PI staining and flow cytometry analyses. CI values were calculated using CompuSyn software. Combined drug treatments were compared to single drug treatment using 1-way ANOVA with Bonferroni post hoc test. ***indicates p < 0.001. (b and c) OCI-AML3 cells were treated with cytarabine and AZD-6738, alone or in combination, for 24 h. Whole cell lysates were subjected to Western blotting and probed with the indicated antibodies.
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| S3600 |
Schisandrin B (Sch B)Schisandrin B (Sch B)是中草药五味子(Turcz.)中含量最丰富的二苯并环辛二烯木酚素。它是一种安全的ATR和P-gp抑制剂。 |
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| S8096 |
MirinMirin是有效的Mre11–Rad50–Nbs1（MRN）复合体抑制剂，能够抑制Mre11相关的外切酶活性。 |
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| S8375 |
AZD0156AZD0156是有效的、选择性的ATM激酶抑制剂，具有潜在的化疗/辐射增敏和抗肿瘤活性。 |
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| S4157 |
Chloroquine PhosphateChloroquine Phosphate是一种4-氨基喹啉的抗疟疾和抗风湿药，也是一种ATM激活剂。 |
NCI-H929 EV and miR-137 OE cells were treated with ATM activator Chloroquine Phosphate (CQ), specific ATM inhibitor KU-55933, and ATR inhibitor AZ20 for 12 hr. Immunoblotting showed the expression of p-ATM, p-Chk2, p-BRCA1, p-ATR and p-Chk1. |
