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KU-60019 {[allProObj[0].p_purity_real_show]}

货号：A231772

KU-60019是一种改良的 ATM 激酶抑制剂，IC50 为 6.3 nM，具有高特异性抑制作用。

KU-60019 化学结构 CAS号：925701-46-8
KU-60019 化学结构
CAS号：925701-46-8
KU-60019 3D分子结构
CAS号：925701-46-8
KU-60019 化学结构 CAS号：925701-46-8
KU-60019 3D分子结构 CAS号：925701-46-8
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KU-60019 纯度/质量文件 产品仅供科研

货号：A231772 标准纯度： {[allProObj[0].p_purity_real_show]}
批次查询： 批次纯度:

全球学术期刊中引用的产品

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产品名称 ATM ↓ ATR ↓ 其他靶点 纯度
Wortmannin ++

ATM, IC50: 150 nM

 		DNA-PK,PI3K,MLCK 99%+
CP-466722 +

ATM, IC50: 410 nM

 		99%+
Torin 2 ++

ATM, EC50: 28 nM

 		++

ATR, EC50: 35 nM

 		DNA-PK,mTOR 99%+
KU-55933 +++

ATM, IC50: 12.9 nM

 		96%
ETP-46464 +

ATM, IC50: 545 nM

 		+++

ATR, IC50: 14 nM

 		DNA-PK,mTOR 98%
CGK733 ++

ATM, IC50: 200 nM

 		++

ATR, IC50: 200 nM

 		99%+
AZD0156 ✔ 99%+
Dactolisib +++

ATR, IC50: 21 nM

 		98+%
Ceralasertib ++++

ATR, IC50: 1 nM

 		99%+
Berzosertib +++

ATR, IC50: 19 nM

 		99%+
VE-821 +++

ATR, Ki: 13 nM

 		99%+
AZ20 ++++

ATR, IC50: 5 nM

 		mTOR 99%+
Schizandrin B +

ATR, IC50: 7.25 μM

 		P-gp 98%
m-PEG25-NHS ester ++++

ATR, IC50: 7 nM

 		95%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

KU-60019 生物活性

描述 The serine/threonine protein kinase ATM signals can regulate cell cycle and DNA repair components through phosphorylation on the targets such as p53, CHK2, NBS1, and BRCA1, thus playing a central role in the maintenance of genome integrity. KU-60019 is an improved inhibitor of the ATM kinase (compared with KU-55933) with an IC50 of 6.3 nM. Pre-treatment with KU-60019 can inhibit the downstream targets p53 phosphorylation at Ser15 site, as well as CHK2 at T68 site, induced by 5Gy of ionizing radiation in U1242 cells. Compared with KU-55933, KU-60019 acts as a more potent radiosensitizer at concentration>1 μM in U87 and U1242 human glioma cells but not A-T fibroblasts. Treatment with KU-60019 resulted in inhibited migration of U87 cells ≥70% in a dose-dependent manner and inhibited invasion of U1242 cells by ∼60%, which may due to the impaired AKT signaling[1]. In in vivo study, combination of radiation and KU-60019 administrated by pump implantation at dose of 10μM, significantly increase survival of mice 2- to 3-fold over controls in orthotopic human glioma xenograft models[2].
作用机制 KU-60019 is an improved form of KU-55933, which is an ATP-competitive ATM inhibitor.[1]

KU-60019 细胞实验

Cell Line
Concentration Treated Time Description References
human osteosarcoma cells (U2OS) 2 µM 72 hours increase 1-bp insertion frequency Nat Commun. 2021 Aug 25;12(1):5111
mouse embryonic stem cells (mESC) 2 µM 72 hours increase 1-bp insertion frequency Nat Commun. 2021 Aug 25;12(1):5111
C4–2 cells 2 μM 72 hours KU-60019 in combination with Enzalutamide re-sensitized C4–2/N-Myc cells to Enzalutamide. Mol Cancer. 2019 Jan 18;18(1):11
human diploid fibroblasts (HDFs) 0.5 μM 15 days Co-inhibition of ATM and ROCK by KU-60019 and Y-27632 synergistically increases the proliferation of HDFs undergoing replicative senescence through activation of transcription factors E2F1 and FOXM1 Commun Biol. 2022 Jul 14;5(1):702
HEK293FT cells 1 μM 48 hours Inhibition of ATM activity, leading to accumulation of cytoplasmic DNA. J Neurosci. 2019 Aug 7;39(32):6378-6394
LNCaP cells 10 μM KU-60019 significantly reduced the percentage of ADT-induced SA-β-gal positive senescent cells, indicating the involvement of ATM in ADT-induced senescence. Mol Cancer. 2019 Jan 18;18(1):11
RKOΔHDAC2 cells 0.5-3 µM 48 hours KU-60019 inhibits ATM kinase, sensitizing RKOΔHDAC2 cells to cytotoxic effects of 5-FU, inducing cell cycle arrest and apoptosis. Cell Biol Toxicol. 2023 Oct;39(5):2401-2419
RKO cells 0.5-3 µM 48 hours KU-60019 inhibits ATM kinase, sensitizing RKO cells to cytotoxic effects of 5-FU, inducing cell cycle arrest and apoptosis. Cell Biol Toxicol. 2023 Oct;39(5):2401-2419
WT cortical neurons 1 µM 24 hours Inhibition of ATM kinase activity, leading to increased SQSTM1 puncta Autophagy. 2021 Aug;17(8):1998-2010
HT22 cells 1 µM 24 hours Inhibition of ATM kinase activity, leading to increased ATM protein levels Autophagy. 2021 Aug;17(8):1998-2010
MC38 1 μM 24 hours Enhanced radiosensitivity through H2O2-dependent oxidative damage and increased DNA damage Int J Radiat Oncol Biol Phys. 2023 Mar 15;115(4):933-944
CT26 1 μM 24 hours Enhanced radiosensitivity through H2O2-dependent oxidative damage and increased DNA damage Int J Radiat Oncol Biol Phys. 2023 Mar 15;115(4):933-944
HT29 1 μM 24 hours Enhanced radiosensitivity through H2O2-dependent oxidative damage and increased DNA damage Int J Radiat Oncol Biol Phys. 2023 Mar 15;115(4):933-944
SW480 1 μM 24 hours Enhanced radiosensitivity through H2O2-dependent oxidative damage and increased DNA damage Int J Radiat Oncol Biol Phys. 2023 Mar 15;115(4):933-944
HCT116 1 μM 24 hours Enhanced radiosensitivity through H2O2-dependent oxidative damage and increased DNA damage Int J Radiat Oncol Biol Phys. 2023 Mar 15;115(4):933-944
Peripheral blood mononuclear cells (PBMCs) 3 µM 1 hour To investigate the inhibitory effect of KU-60019 on ATM activation and validate its suppression of p53 downstream targets. Results showed that KU-60019 inhibited radiation-induced p53 accumulation, thereby preventing the upregulation of miR-34a-5p in PBMCs and EVs. Cell Commun Signal. 2024 Oct 2;22(1):471
KP6 and KPP4 0.3 µM and 3 µM 3 hours pre-treatment Restored radiation sensitivity in PTEN-deficient cells Cell Biosci. 2022 Apr 27;12(1):50
BEAS-2B PTENhomo 0.3 µM and 3 µM 3 hours pre-treatment Restored radiation sensitivity in PTEN-deficient cells Cell Biosci. 2022 Apr 27;12(1):50
PBLCs 3 µM 24 hours Inhibition of ATM significantly protected unstimulated PBLCs from radiation-induced cell death Cell Death Dis. 2018 Oct 15;9(11):1053
microglia 1 μM 48 hours Inhibition of ATM kinase activity, leading to microglial activation and morphological changes, and increased production of pro-inflammatory cytokines. J Neurosci. 2019 Aug 7;39(32):6378-6394

KU-60019 动物实验

Species
Animal Model
Administration Dosage Frequency Description References
Mice HCT116 and MC38 tumor models Tail vein injection 0.5 mg/kg 3 hours before radiation Enhanced tumor radiosensitivity while reducing intestinal toxicity Int J Radiat Oncol Biol Phys. 2023 Mar 15;115(4):933-944
Mice KP6 and KPP4 cell transplantation model In vitro culture 3 µM 8 days observation KU-60019 combined with radiation led to regression of PTEN-deficient tumors Cell Biosci. 2022 Apr 27;12(1):50

KU-60019 动物研究

Dose Mice: 10 mg/kg[3] (i.p.), 100 mg/kg[4]
Administration i.p.

KU-60019 参考文献

[1]Golding SE, Rosenberg E, et al. Improved ATM kinase inhibitor KU-60019 radiosensitizes glioma cells, compromises insulin, AKT and ERK prosurvival signaling, and inhibits migration and invasion. Mol Cancer Ther. 2009 Oct;8(10):2894-902.

[2]Biddlestone-Thorpe L, Sajjad M, et al. ATM kinase inhibition preferentially sensitizes p53-mutant glioma to ionizing radiation. Clin Cancer Res. 2013 Jun 15;19(12):3189-200.

KU-60019 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.83mL

0.37mL

0.18mL

9.13mL

1.83mL

0.91mL

18.26mL

3.65mL

1.83mL

KU-60019 技术信息

CAS号925701-46-8
分子式C30H33N3O5S
分子量 547.67
SMILES Code O=C(NC1=CC(CC2=C(C(C3=CC(C=C(N4CCOCC4)O3)=O)=CC=C2)S5)=C5C=C1)CN6C[C@@H](C)O[C@@H](C)C6
MDL No. MFCD18384974
别名
运输蓝冰
InChI Key SCELLOWTHJGVIC-BGYRXZFFSA-N
Pubchem ID 15953870
存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Sealed in dry, store in freezer, under -20°C
溶解方案

DMSO: 105 mg/mL(191.72 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

无水乙醇: 8 mg/mL(14.61 mM)，配合低频超声助溶，注意：无水乙醇开封后，易挥发，也会吸收空气中的水分，导致溶解能力下降，请避免使用开封较久的乙醇

请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议现用现配，当天使用； 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶
方案 一
方案 二

Tags: KU-60019 | 925701-46-8 | KU60019 | KU 60019 | ATM/ATR Inhibitor | Cell Cycle/DNA Damage | PI3K/Akt/mTOR | ATM/ATR | 仅供科研使用 | AmBeed-信号通路专用抑制剂 | KU-60019 纯度/质量文件 | KU-60019 亚型比较 | KU-60019 生物活性 | KU-60019 动物研究 | KU-60019 参考文献 | KU-60019 实验方案 | KU-60019 技术信息

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