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KU-55933
別名: ATM Kinase Inhibitor
KU-55933是一種有效的，特異性ATM抑制劑，在無細胞試驗中IC50/Ki為12.9 nM/2.2 nM，與DNA-PK， PI3K/PI4K， ATR和mTOR相比，對ATM具有高度選擇性。KU?55933 (ATM Kinase Inhibitor)可抑制 autophagy?initiating kinase ULK1 的激活從而導致自噬的顯著減少。
KU-55933 Chemical Structure
CAS: 587871-26-9
產(chǎn)品質(zhì)控
批次：
純度：
99.95%
99.95
KU-55933相關產(chǎn)品
相關信號通路圖
細胞實驗數(shù)據(jù)示例
| 細胞系 | 實驗類型 | 給藥濃度 | 孵育時間 | 活性描述 | 文獻信息 |
|---|---|---|---|---|---|
| HepG2? | Growth Inhibition Assay | 10?μM | 24 h | blocks SC-III3-induced S phase arrest | 25527123 |
| HepG2? | Function Assay | 10?μM | 24 h | suppresses the phosphorylations of ATM on Ser1981, Chk1 on Ser345, Chk2 on Thr68, and Cdk2 on Tyr15 induced by SC-III3 | 25527123 |
| MCF10A | Growth Inhibition Assay | 10 μM | 24 h | potentiates the cytotoxicity of GA | 24150595 |
| HL-60? | Function Assay | 10 μM | 0.5 h | reduces phosphorylation of Chk2? | 23934411 |
| MCF-7 | Growth Inhibition Assay | 1-100μM | 24 h | inhibits the cell proliferation | 23185347 |
| HeLa? | Growth Inhibition Assay | 1-100μM | 24 h | inhibits the cell proliferation | 23185347 |
| SH-SY5Y | Function Assay | 10?μM? | 24 h | inhibits clioquinol-induced phosphorylation of p53 | 22627294 |
| IMR-32 | Function Assay | 10?μM? | 24 h | inhibits clioquinol-induced phosphorylation of p53 | 22627294 |
| A549 | Function Assay | 10?μM? | 1 h | suppresses Nano-Co-induced p53 accumulation | 22559321 |
| T47D? | Function Assay | 20?mM | 24 h | prevents IR-induced degradation of IκBα | 21144805 |
| A29 MEF | Function Assay | 10?μM? | 1h | blocks?the phosphorylation of Akt at Ser473? | 20053781 |
| MDA-MB-453? | Growth Inhibition Assay | 5-40 μM | 72 h | IC50 of 10 μM | 20053781 |
| PC-3 | Growth Inhibition Assay | 5-40 μM | 72 h | IC50 of 10 μM | 20053781 |
| BJ | Function assay | 10 uM | 10 days | Suppression of senescence in human BJ cells assessed as increase in cell number at 10 uM after 10 days by senescence reversal assay | 16767085 |
| BJ | Function assay | 10 uM | 10 days | Inhibition of ataxia telangiectasia-mutated in human BJ cells assessed as increase in cell number at 10 uM after 10 days by senescence reversal assay | 16767085 |
| MCF7 | Function assay | 10 uM | 10 mins | Sensitization of infrared-induced DNA damage in human MCF7 cells assessed as reduction in colony formation at 10 uM pretreated for 10 mins followed by irradiation for 4 hrs measured after 10 days by crystal violet staining analysis | 26632965 |
| KATO III? | Growth Inhibition Assay | 2.5/5/7.5 μM | enhances the toxicity of olaparib | 24841718 | |
| hTCEpi | Growth Inhibition Assay | 10 μM | prevents the cytopathic effect of HSV-1 | 24370835 | |
| MCF7 | Function assay | 1 hr | Inhibition of ATM kinase in human MCF7 cells after 1 hr by immunofluorescence assay, IC50 = 0.3 μM. | 26632965 | |
| KOSC-2 | Growth Inhibition Assay | IC50=26.9075 μM | SANGER | ||
| DEL | Growth Inhibition Assay | IC50=26.8356 μM | SANGER | ||
| GT3TKB | Growth Inhibition Assay | IC50=26.5342 μM | SANGER | ||
| MDA-MB-415 | Growth Inhibition Assay | IC50=26.5033 μM | SANGER | ||
| GI-1 | Growth Inhibition Assay | IC50=25.7055 μM | SANGER | ||
| BFTC-905 | Growth Inhibition Assay | IC50=25.5944 μM | SANGER | ||
| QIMR-WIL | Growth Inhibition Assay | IC50=25.1858 μM | SANGER | ||
| PANC-08-13 | Growth Inhibition Assay | IC50=25.0938 μM | SANGER | ||
| SK-MEL-30 | Growth Inhibition Assay | IC50=24.4662 μM | SANGER | ||
| CHL-1 | Growth Inhibition Assay | IC50=23.7292 μM | SANGER | ||
| Ramos-2G6-4C10 | Growth Inhibition Assay | IC50=22.96 μM | SANGER | ||
| SNU-449 | Growth Inhibition Assay | IC50=22.8748 μM | SANGER | ||
| HCC2157 | Growth Inhibition Assay | IC50=22.8054 μM | SANGER | ||
| LB1047-RCC | Growth Inhibition Assay | IC50=22.5879 μM | SANGER | ||
| YH-13 | Growth Inhibition Assay | IC50=22.5123 μM | SANGER | ||
| Mewo | Growth Inhibition Assay | IC50=22.5073 μM | SANGER | ||
| JVM-3 | Growth Inhibition Assay | IC50=22.506 μM | SANGER | ||
| HSC-3 | Growth Inhibition Assay | IC50=21.1835 μM | SANGER | ||
| U031 | Growth Inhibition Assay | IC50=21.1489 μM | SANGER | ||
| D-283MED | Growth Inhibition Assay | IC50=20.5339 μM | SANGER | ||
| A704 | Growth Inhibition Assay | IC50=19.8305 μM | SANGER | ||
| HCC70 | Growth Inhibition Assay | IC50=19.489 μM | SANGER | ||
| MLMA | Growth Inhibition Assay | IC50=19.0557 μM | SANGER | ||
| 697 | Growth Inhibition Assay | IC50=19.0201 μM | SANGER | ||
| HuP-T3 | Growth Inhibition Assay | IC50=18.5888 μM | SANGER | ||
| NCI-H2030 | Growth Inhibition Assay | IC50=18.1997 μM | SANGER | ||
| HCC2998 | Growth Inhibition Assay | IC50=17.6733 μM | SANGER | ||
| NCI-H82 | Growth Inhibition Assay | IC50=17.4573 μM | SANGER | ||
| CTB-1 | Growth Inhibition Assay | IC50=17.2259 μM | SANGER | ||
| NCI-SNU-1 | Growth Inhibition Assay | IC50=17.1269 μM | SANGER | ||
| SK-MEL-28 | Growth Inhibition Assay | IC50=17.0475 μM | SANGER | ||
| GCIY | Growth Inhibition Assay | IC50=16.7905 μM | SANGER | ||
| ChaGo-K-1 | Growth Inhibition Assay | IC50=16.6568 μM | SANGER | ||
| NCI-H1793 | Growth Inhibition Assay | IC50=16.4712 μM | SANGER | ||
| LXF-289 | Growth Inhibition Assay | IC50=16.2747 μM | SANGER | ||
| HuH-7 | Growth Inhibition Assay | IC50=16.2674 μM | SANGER | ||
| 8305C | Growth Inhibition Assay | IC50=16.1889 μM | SANGER | ||
| KG-1 | Growth Inhibition Assay | IC50=16.0996 μM | SANGER | ||
| VM-CUB-1 | Growth Inhibition Assay | IC50=15.9849 μM | SANGER | ||
| DBTRG-05MG | Growth Inhibition Assay | IC50=15.6111 μM | SANGER | ||
| D-423MG | Growth Inhibition Assay | IC50=15.5236 μM | SANGER | ||
| Hs-578-T | Growth Inhibition Assay | IC50=15.4182 μM | SANGER | ||
| DOK | Growth Inhibition Assay | IC50=15.3329 μM | SANGER | ||
| COLO-684 | Growth Inhibition Assay | IC50=14.1569 μM | SANGER | ||
| CAL-12T | Growth Inhibition Assay | IC50=13.617 μM | SANGER | ||
| KP-N-YS | Growth Inhibition Assay | IC50=12.6354 μM | SANGER | ||
| ES7 | Growth Inhibition Assay | IC50=11.788 μM | SANGER | ||
| LB2241-RCC | Growth Inhibition Assay | IC50=11.7186 μM | SANGER | ||
| GOTO | Growth Inhibition Assay | IC50=11.6996 μM | SANGER | ||
| J-RT3-T3-5 | Growth Inhibition Assay | IC50=11.2417 μM | SANGER | ||
| NCI-H1838 | Growth Inhibition Assay | IC50=11.1865 μM | SANGER | ||
| NCI-H1437 | Growth Inhibition Assay | IC50=9.8097 μM | SANGER | ||
| KM12 | Growth Inhibition Assay | IC50=9.21142 μM | SANGER | ||
| SK-MEL-3 | Growth Inhibition Assay | IC50=8.28575 μM | SANGER | ||
| HH | Growth Inhibition Assay | IC50=8.27671 μM | SANGER | ||
| LoVo | Growth Inhibition Assay | IC50=6.93239 μM | SANGER | ||
| CAL-72 | Growth Inhibition Assay | IC50=5.48084 μM | SANGER | ||
| LAMA-84 | Growth Inhibition Assay | IC50=4.58465 μM | SANGER | ||
| HuO-3N1 | Growth Inhibition Assay | IC50=4.17142 μM | SANGER | ||
| DU-145 | Growth Inhibition Assay | IC50=3.27352 μM | SANGER | ||
| RVH-421 | Growth Inhibition Assay | IC50=27.2921 μM | SANGER | ||
| EW-13 | Growth Inhibition Assay | IC50=27.4308 μM | SANGER | ||
| 639-V | Growth Inhibition Assay | IC50=27.5119 μM | SANGER | ||
| A2780 | Growth Inhibition Assay | IC50=27.641 μM | SANGER | ||
| SW982 | Growth Inhibition Assay | IC50=27.9052 μM | SANGER | ||
| SW1710 | Growth Inhibition Assay | IC50=28.0981 μM | SANGER | ||
| HCC1569 | Growth Inhibition Assay | IC50=28.4897 μM | SANGER | ||
| MV-4-11 | Growth Inhibition Assay | IC50=28.5735 μM | SANGER | ||
| BHT-101 | Growth Inhibition Assay | IC50=28.6572 μM | SANGER | ||
| Ca9-22 | Growth Inhibition Assay | IC50=28.714 μM | SANGER | ||
| HAL-01 | Growth Inhibition Assay | IC50=28.7615 μM | SANGER | ||
| D-263MG | Growth Inhibition Assay | IC50=29.344 μM | SANGER | ||
| NEC8 | Growth Inhibition Assay | IC50=29.5548 μM | SANGER | ||
| EKVX | Growth Inhibition Assay | IC50=31.5847 μM | SANGER | ||
| EM-2 | Growth Inhibition Assay | IC50=31.6304 μM | SANGER | ||
| MFM-223 | Growth Inhibition Assay | IC50=31.8098 μM | SANGER | ||
| SK-PN-DW | Growth Inhibition Assay | IC50=32.1406 μM | SANGER | ||
| HuO9 | Growth Inhibition Assay | IC50=32.5282 μM | SANGER | ||
| MHH-PREB-1 | Growth Inhibition Assay | IC50=32.6234 μM | SANGER | ||
| OVCAR-4 | Growth Inhibition Assay | IC50=32.8363 μM | SANGER | ||
| NCI-H1648 | Growth Inhibition Assay | IC50=32.8651 μM | SANGER | ||
| MKN1 | Growth Inhibition Assay | IC50=34.1101 μM | SANGER | ||
| KYSE-450 | Growth Inhibition Assay | IC50=34.6444 μM | SANGER | ||
| ES8 | Growth Inhibition Assay | IC50=34.8975 μM | SANGER | ||
| MS-1 | Growth Inhibition Assay | IC50=34.9554 μM | SANGER | ||
| HOP-92 | Growth Inhibition Assay | IC50=35.9277 μM | SANGER | ||
| SKG-IIIa | Growth Inhibition Assay | IC50=36.2561 μM | SANGER | ||
| TE-11 | Growth Inhibition Assay | IC50=36.5243 μM | SANGER | ||
| SK-NEP-1 | Growth Inhibition Assay | IC50=37.6744 μM | SANGER | ||
| DB | Growth Inhibition Assay | IC50=37.9185 μM | SANGER | ||
| IA-LM | Growth Inhibition Assay | IC50=38.0239 μM | SANGER | ||
| COLO-829 | Growth Inhibition Assay | IC50=38.4159 μM | SANGER | ||
| TGBC11TKB | Growth Inhibition Assay | IC50=39.1408 μM | SANGER | ||
| CAL-51 | Growth Inhibition Assay | IC50=40.0612 μM | SANGER | ||
| NCI-H2228 | Growth Inhibition Assay | IC50=40.3662 μM | SANGER | ||
| C32 | Growth Inhibition Assay | IC50=40.4024 μM | SANGER | ||
| KU-19-19 | Growth Inhibition Assay | IC50=40.7683 μM | SANGER | ||
| KNS-62 | Growth Inhibition Assay | IC50=40.8381 μM | SANGER | ||
| FADU | Growth Inhibition Assay | IC50=41.2502 μM | SANGER | ||
| CAL-33 | Growth Inhibition Assay | IC50=42.6749 μM | SANGER | ||
| CHP-134 | Growth Inhibition Assay | IC50=42.8496 μM | SANGER | ||
| HDLM-2 | Growth Inhibition Assay | IC50=42.9084 μM | SANGER | ||
| NBsusSR | Growth Inhibition Assay | IC50=43.0725 μM | SANGER | ||
| SW954 | Growth Inhibition Assay | IC50=43.1053 μM | SANGER | ||
| HCC1806 | Growth Inhibition Assay | IC50=43.411 μM | SANGER | ||
| VMRC-RCZ | Growth Inhibition Assay | IC50=43.4586 μM | SANGER | ||
| A549 | Growth Inhibition Assay | IC50=43.931 μM | SANGER | ||
| NKM-1 | Growth Inhibition Assay | IC50=43.9558 μM | SANGER | ||
| DMS-273 | Growth Inhibition Assay | IC50=44.7567 μM | SANGER | ||
| TYK-nu | Growth Inhibition Assay | IC50=45.1234 μM | SANGER | ||
| KALS-1 | Growth Inhibition Assay | IC50=45.146 μM | SANGER | ||
| A101D | Growth Inhibition Assay | IC50=45.4456 μM | SANGER | ||
| G-361 | Growth Inhibition Assay | IC50=46.2138 μM | SANGER | ||
| KARPAS-299 | Growth Inhibition Assay | IC50=46.3516 μM | SANGER | ||
| RS4-11 | Growth Inhibition Assay | IC50=46.542 μM | SANGER | ||
| HT-1376 | Growth Inhibition Assay | IC50=46.7426 μM | SANGER | ||
| SK-N-AS | Growth Inhibition Assay | IC50=46.7822 μM | SANGER | ||
| MG-63 | Growth Inhibition Assay | IC50=46.9036 μM | SANGER | ||
| EPLC-272H | Growth Inhibition Assay | IC50=46.9503 μM | SANGER | ||
| BALL-1 | Growth Inhibition Assay | IC50=47.832 μM | SANGER | ||
| LCLC-97TM1 | Growth Inhibition Assay | IC50=48.202 μM | SANGER | ||
| HO-1-N-1 | Growth Inhibition Assay | IC50=48.9676 μM | SANGER | ||
| MFE-280 | Growth Inhibition Assay | IC50=49.4617 μM | SANGER | ||
| NCI-H526 | Growth Inhibition Assay | IC50=49.8163 μM | SANGER | ||
| D-566MG | Growth Inhibition Assay | IC50=49.9096 μM | SANGER | ||
| BB30-HNC | Growth Inhibition Assay | IC50=49.9498 μM | SANGER | ||
| SK-N-DZ | Growth Inhibition Assay | IC50=50.0481 μM | SANGER | ||
| U2OS | Function assay | Inhibition of ATM in human U2OS cells assessed as inhibition of p53 phosphorylation at Ser15 residue, IC50 = 0.25 μM. | 26632965 | ||
| SK-N-MC | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells | 29435139 | ||
| 點擊查看更多細胞系數(shù)據(jù) | |||||
生物活性
| 產(chǎn)品描述 | KU-55933是一種有效的，特異性ATM抑制劑，在無細胞試驗中IC50/Ki為12.9 nM/2.2 nM，與DNA-PK， PI3K/PI4K， ATR和mTOR相比，對ATM具有高度選擇性。KU?55933 (ATM Kinase Inhibitor)可抑制 autophagy?initiating kinase ULK1 的激活從而導致自噬的顯著減少。 | ||
|---|---|---|---|
| 靶點 |
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| 體外研究(In Vitro) | ||||
| 體外研究活性 | KU-55933是有效的特定ATM抑制劑，IC50為13 nM，Ki值為2.2 nM。KU-55933也抑制DNA-PK和PI3K，IC50分別為2.5和16.6 μM。KU-55933也抑制mTOR活性，IC50為9.3 μM。KU-55933有效作用于ATM依賴的磷酸化作用。KU-55933抑制ATM依賴的磷酸化作用，存在劑量依賴性，IC50為300 nM。小于30 μM時，KU-58050不能抑制p53的ATM-依賴性磷酸化作用（位點為第15位絲氨酸）。在UV-誘導的H2AX（位點為第139位絲氨酸）, NBS1（位點為第343為絲氨酸）, CHK1（位點為第345位絲氨酸）,及SMC1（位點為第966位絲氨酸）中，加入KU-55933沒有明顯作用效果。紫外處理時，KU-55933切除由電離輻射誘導的ATM磷酸化底物。KU-55933使HeLa細胞對電離輻射敏感。在癌細胞中，KU-55933抑制生長因子誘導的Akt的磷酸化作用。KU-55933抑制癌細胞增殖。KU-55933抑制ATM，通過阻斷下游TAp63α的激活，提高存活力。[2] | |||
|---|---|---|---|---|
| 激酶實驗 | 純化的酶實驗 | |||
| 通過免疫沉淀反應從HeLa核蛋白萃取中獲得用于體外研究的ATM，在反應buffer中，把兔多克隆抗血清加到ATM羧基端第400個氨基酸處，buffer包含25 mM HEPES (pH為7.4), 2 mM MgCl2, 250 mM KCl, 500 μM EDTA, 100 μM Na3VO4, 10% v/v 甘油, 及0.1% v/v Igepal。和蛋白A凝膠溫育1小時，然后進行離心作用，從核蛋白中分離ATM抗體復合物。在96孔板中，包含ATM的凝膠珠和1 μg 底物GST-p53N66 (p53的氮端第66位氨基酸與GST融合)在ATM實驗buffer中37oC下溫育，buffer包括25 mM HEPES (pH 為7.4), 75 mM NaCl, 3 mM MgCl2, 2 mM MnCl2, 50 μM Na3VO4, 500 μM DTT, 及5% v/v甘油。震蕩10分鐘后，加入ATP，最終濃度為50 μM，在37oC反應持續(xù)1小時。按250×g轉(zhuǎn)速4oC下離心10分鐘，除去ATM凝膠珠，上清液轉(zhuǎn)移到96孔板上，在室溫下溫育1.5小時。然后用PBS沖洗，烘干，加入p-p53(Ser15)抗體用于ELISA分析。使用增強的化學發(fā)光溶液產(chǎn)生信號和化學發(fā)光。 | ||||
| 細胞實驗 | 細胞系 | U2OS細胞 | ||
| 濃度 | 10 μM | |||
| 孵育時間 | 2小時 | |||
| 方法 | U2OS細胞經(jīng)過電離輻射(3, 5, 或15 Gy) 或者UV處理(5或50 J/m2)，通過p-p53（Ser15）和p53 的Western blot分析而測定ATM反應。在不同時間點獲得細胞萃取物，SDS-PAGE分離蛋白，加入p-p53(Ser15)抗體，ATM增多。加入p53抗體觀察到p53隨著時間變化趨于穩(wěn)定。為了測定KU-55933的IC50值，使用p-p53(Ser15)抗體檢測KU-55933抑制ATM的效果。KU-55933加到細胞中，預溫育1小時，然后進行電離輻射。在體外，使用掃描密度測定法測定IC50值。 |
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| 實驗圖片 | 檢測方法 | 檢測指標 | 實驗圖片 | PMID |
| Western blot |
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