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KU-60019

CAS No. : 925701-46-8

MCE 国际站：KU-60019

产品活性：KU-60019 是一种 ATM 激酶特异性的抑制剂，IC₅₀ 为 6.3 nM。

研究领域：Cell Cycle/DNA Damage  |  PI3K/Akt/mTOR

作用靶点：ATM/ATR

In Vitro: KU-60019 is an improved analogue of KU-55933. KU-55933 has an IC₅₀ of 13 nM and K_i of 2.2 nM in vitro and is highly specific for the ATM kinase using a panel of 60 protein kinases. KU-60019 is an improved inhibitor of the ATM kinase with an IC₅₀ of 6.3 nM, approximately half that of KU-55933. The IC₅₀ values for DNA-PKcs and ATR are 1.7 and >10 μM, respectively, almost 270-and 1600-fold higher than for ATM. KU-60019 is 10-fold more effective than KU-55933 at blocking radiation-induced phosphorylation of key ATM targets in human glioma cells. In human U87 glioma cells, KU-55933 completely inhibits phosphorylation of p53 (S15) at 10 μM but not at 3 μM, whereas γ-H2AX levels are only partly reduced with 10 μM 1 h after irradiation. By comparison, 3 μM KU-60019 completely inhibits p53 phosphorylation and partial inhibits at 1 μM.

In Vivo: Despite PTEN-deficient control tumors reaching a 4-fold increase in size before PTEN wild-type controls, KU-60019-treated PTEN-deficient tumors display a statistically significant slowing in growth. This growth inhibition is especially evident at the start of the experiment (days 5-12) just after KU-60019 is administered (days 1-5).

相关产品：Bioactive Compound Library Plus  |  Cell Cycle/DNA Damage Compound Library  |  Kinase Inhibitor Library  |  PI3K/Akt/mTOR Compound Library  |  Anti-Cancer Compound Library  |  Anti-Aging Compound Library  |  Oxygen Sensing Compound Library  |  Glycolysis Compound Library  |  Cytoskeleton Compound Library  |  Anti-Pancreatic Cancer Compound Library  |  Anti-Cancer Metabolism Compound Library  |  Anti-Obesity Compound Library  |  Glucose Metabolism Compound Library  |  Cancer Stem Cells Compound Library  |  Highly Selective Inhibitors Library  |  Tuvusertib  |  Elimusertib  |  CGK733  |  AZD1390  |  Ceralasertib  |  AZD-7648  |  KU 59403  |  VE-821  |  KU-55933  |  ATM Inhibitor-3  |  Elimusertib-d₃  |  ATR-IN-22  |  ATR-IN-6  |  AZD0156  |  CP-466722  |  Antitumor agent-28  |  ATR-IN-12  |  ATR-IN-18  |  ATR-IN-13  |  ATR-IN-5  |  ATR-IN-20  |  ATR-IN-21  |  AZ32  |  ATM Inhibitor-2  |  ATM Inhibitor-6  |  Ro 90-7501  |  ATR-IN-17  |  A011  |  ATR-IN-4

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