KU-55933 (ATM Kinase Inhibitor)

製品コード:S1092

For research use only.

KU-55933 (ATM Kinase Inhibitor) is a potent and specific ATM inhibitor with IC50/Ki of 12.9 nM/2.2 nM in cell-free assays, and is highly selective for ATM as compared to DNA-PK, PI3K/PI4K, ATR and mTOR. KU‑55933 (ATM Kinase Inhibitor) inhibits the activation of autophagy‑initiating kinase ULK1 and results in a significant decrease of autophagy.

KU-55933 (ATM Kinase Inhibitor)化学構造

CAS No. 587871-26-9

サイズ 価格(税別)
10mM (1mL in DMSO) JPY 20500
JPY 13600
JPY 21900
JPY 63400

代表番号: 03-5615-9297|電子メール:[email protected]
よく尋ねられる質問

文献中Selleckの製品使用例(285)

製品安全説明書

ATM/ATR阻害剤の選択性比較

相関ATM/ATR製品

生物活性

製品説明 KU-55933 (ATM Kinase Inhibitor) is a potent and specific ATM inhibitor with IC50/Ki of 12.9 nM/2.2 nM in cell-free assays, and is highly selective for ATM as compared to DNA-PK, PI3K/PI4K, ATR and mTOR. KU‑55933 (ATM Kinase Inhibitor) inhibits the activation of autophagy‑initiating kinase ULK1 and results in a significant decrease of autophagy.
ターゲット
ATM [1]
(Cell-free assay)
12.9 nM
体外試験

KU-55933 inhibits DNA-PK and PI3K with IC50 of 2.5 μM and 16.6 μM, respectively. Besides, KU-55933 also prevents the activity of mTOR with IC50 of 9.3 μM. KU-55933 is active at the cellular level in ablating a well-characterized ATM-dependent phosphorylation event. KU-55933 has a dose-dependent effect in inhibiting this ATM-dependent phosphorylation event with IC50 of 300 nM. KU-58050 does not prevent the ATM-dependent phosphorylation of p53 serine 15 until a dose of 30 μM. Addition of KU-55933 has no appreciable effects on UV-induced phosphorylation of H2AX on serine 139, NBS1 on serine 343, CHK1 on serine 345, and SMC1 on serine 966. In stark contrast to the UV responses, KU-55933 ablates the ionizing radiation-induced phosphorylation of these ATM substrates. KU-55933 sensitizes HeLa cells to a range of ionizing radiation doses. [1] KU-55933 inhibits the phosphorylation of Akt induced by growth factors in cancer cells. KU-55933 suppresses the proliferation of cancer cells. Furthermore, suppression of ATM by KU-55933 improves survival, probably via prevention of downstream activation of TAp63α. [2]

細胞データ
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
DU-145 NEnlPJBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEDmOm1KSzVyPUOuNlc{PTJizszN MWC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyNlIyODJxJ{7TRW5ITVJ:L3G+
HuO-3N1 NHWwNYVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4rJU2lEPTB;ND6xO|E1OiEQvF2= MlHlQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlIzOTB{Lze+V2FPT0WUPD;hQi=>
LAMA-84 NYDo[GJFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF\neoVKSzVyPUSuOVg1PjVizszN NYPyVnJtRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjJ{MUCyM{c,W0GQR1XSQE9iRg>?
CAL-72 NGPtd|FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MY\JR|UxRTVwNEiwPFQh|ryP MontQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlIzOTB{Lze+V2FPT0WUPD;hQi=>
LoVo NUj3c5pNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWnJR|UxRTZwOUOyN|kh|ryP M4\ZSFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFIzOjFyMj:nQnNCVkeHUkyvZV4>
HH NW\SWXBlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYflNpE4UUN3ME24MlI4PjdzIN88US=> M2LFO|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFIzOjFyMj:nQnNCVkeHUkyvZV4>
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LB2241-RCC NHPTW2NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn;tTWM2OD1zMT63NVg3KM7:TR?= Mn7hQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlIzOTB{Lze+V2FPT0WUPD;hQi=>
ES7 Mlq0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2P0UGlEPTB;MUGuO|g5KM7:TR?= NIrnb2s9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzOjJzMEKvK|5USU6JRWK8M4E,
KP-N-YS MoXFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX3JR|UxRTF{Lk[zOVQh|ryP M3e5SFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFIzOjFyMj:nQnNCVkeHUkyvZV4>
CAL-12T Mk\4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYfJR|UxRTF|Lk[xO{DPxE1? NHvJWGU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzOjJzMEKvK|5USU6JRWK8M4E,
COLO-684 M4T5bWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{jYZmlEPTB;MUSuNVU3QSEQvF2= NUDaOopURGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjJ{MUCyM{c,W0GQR1XSQE9iRg>?
DOK NWrrSZNWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{G1S2lEPTB;MUWuN|MzQSEQvF2= NIr4WYo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzOjJzMEKvK|5USU6JRWK8M4E,
Hs-578-T NYjzSmo2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXPJR|UxRTF3LkSxPFIh|ryP NFPyd3U9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzOjJzMEKvK|5USU6JRWK8M4E,
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DBTRG-05MG M{C4NWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoDTTWM2OD1zNT62NVEyKM7:TR?= MkfYQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlIzOTB{Lze+V2FPT0WUPD;hQi=>
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KG-1 NHHFR5pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlL0TWM2OD1zNj6wPVk3KM7:TR?= MWO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyNlIyODJxJ{7TRW5ITVJ:L3G+
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LXF-289 NYPZOW5lT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1XIOWlEPTB;MU[uNlc1PyEQvF2= MV[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyNlIyODJxJ{7TRW5ITVJ:L3G+
NCI-H1793 M324[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUDOVodXUUN3ME2xOk41PzF{IN88US=> NF\lbo49[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzOjJzMEKvK|5USU6JRWK8M4E,
ChaGo-K-1 NVizOJJHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHHGPYNKSzVyPUG2MlY2PjhizszN NEX2NVY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzOjJzMEKvK|5USU6JRWK8M4E,
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HDLM-2 MlTKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVni[nlzUUN3ME20Nk46ODh2IN88US=> NEXCUVU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzOjJzMEKvK|5USU6JRWK8M4E,
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HCC1806 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYDJR|UxRTR|LkSxNUDPxE1? NWjK[HUxRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjJ{MUCyM{c,W0GQR1XSQE9iRg>?
VMRC-RCZ MmLPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXrk[JZwUUN3ME20N{41PTh4IN88US=> M{P5Z|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFIzOjFyMj:nQnNCVkeHUkyvZV4>
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BB30-HNC MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn;PTWM2OD12OT65OFk5KM7:TR?= M1T0SFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFIzOjFyMj:nQnNCVkeHUkyvZV4>
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HepG2  M330eGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV6wSFNxOTEEoN88US=> NXPsbGZYOjRiaB?= NWnxcZFi[myxY3vzJHNENUmLSUOtbY5lfWOnZDDTJJBp[XOnIHHydoV{fA>? NVfjbFZxRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW1NlcyOjNpPkK1OVI4OTJ|PD;hQi=>
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アッセイ
Methods Test Index PMID
Western blot p-AKT(Ser473) / p-AKT(Thr308) ; PARP / Cleaved PARP / Caspase-3 / Cleaved caspase-3 ; ATM-S1981 / ATM / p-p53(S15) / p53 ; p21 / p27 / p53 22739265 20639198 20177072
Immunofluorescence p-S824 KAP1 / ZEBRA 28249048
体内試験 Suppression of ATM-dependent STAT3 activation by KU-55933 enhances TRAIL-mediated apoptosis through up-regulation of surface DR5 expression, whereas suppression of both STAT3 and NF-κB appeares to be involved in down-regulation of cFLIP accompanied by an additional increase in apoptotic levels. The ATM inhibitor KU-55933 affectes TRAIL-mediated apoptosis more strongly than the JAK2 inhibitor, AG490, or overexpression of STAT3β. [3]

お薦めの試験操作(参考用のみ)

キナーゼ試験:

[1]

  • Purified enzyme assays:

    ATM for use in the in vitro assay is obtained from HeLa nuclear extract by immunoprecipitation with rabbit polyclonal antiserum raised to the COOH-terminal 400 amino acids of ATM in buffer containing 25 mM HEPES (pH 7.4), 2 mM MgCl2, 250 mM KCl, 500 μM EDTA, 100 μM Na3VO4, 10% v/v glycerol, and 0.1% v/v Igepal. ATM-antibody complexes are isolated from nuclear extract by incubating with protein A-Sepharose beads for 1 hour and then through centrifugation to recover the beads. In the well of a 96-well plate, ATM-containing Sepharose beads are incubated with 1 μg of substrate glutathione S-transferase–p53N66 (NH2-terminal 66 amino acids of p53 fused to glutathione S-transferase) in ATM assay buffer [25 mM HEPES (pH 7.4), 75 mM NaCl, 3 mM MgCl2, 2 mM MnCl2, 50 μM Na3VO4, 500 μM DTT, and 5% v/v glycerol] at 37 °C in the presence or absence of inhibitor. After 10 minutes with gentle shaking, ATP is added to a final concentration of 50 μM and the reaction continued at 37 °C for an additional 1 hour. The plate is centrifuged at 250 × g for 10 minutes (4 °C) to remove the ATM-containing beads, and the supernatant is removed and transferred to a white opaque 96-well plate and incubated at room temperature for 1.5 hours to allow glutathione S-transferase-p53N66 binding. This plate is then washed with PBS, blotted dry, and analyzed by a standard ELISA technique with a phospho-serine 15 p53 antibody. The detection of phosphorylated glutathione S-transferase-p53N66 substrate is performed in combination with a goat antimouse horseradish peroxidase-conjugated secondary antibody. Enhanced chemiluminescence solution is used to produce a signal and chemiluminescent detection is carried out.

細胞試験:

[1]

  • 細胞株:U2OS cells
  • 濃度: 10 μM
  • 反応時間:2 hours
  • 実験の流れ:

    U2OS cells are exposed to ionizing radiation (3, 5, or 15 Gy) or UV (5 or 50 J/m2) and the ATM response determined by Western blot analysis of p53 serine 15 phosphorylation and stabilization of wild-type p53. Whole cell extracts are obtained from each time point, proteins separated by SDS-PAGE, and the ATM-specific increase in phosphorylated serine 15 measured with a p53 phospho-serine 15 specific antibody. Overall p53 stabilization with time is also observed with a p53-specific antibody (DO-1). Similarly, for studying ATM-dependent phosphorylations on H2AX, CHK1, NBS1, and SMC1, the following antibodies are used: CHK1 phospho-serine 345 and NBS1 phospho-serine 343 antibodies. Histone H2A (H-124) and CHK1 antibodies are also used, as well as SMC1 and SMC1 phospho-serine 966 antibodies. For determination of a cellular IC50 for KU-55933, the peak response time for p53 serine 15 phosphorylation of 2 hours is used to monitor inhibition of ATM. KU-55933 is titrated onto cells and preincubated for 1 hour before ionizing radiation. Using scanning densitometry, the percentage inhibition relative to vehicle control is calculated, and the IC50 value is calculated as for the in vitro determinations.

動物試験:

[3]

  • 動物モデル:BALB/c nu/nu nude mice bearing LU1205 cells
  • 投薬量:10 μM
  • 投与方法:--

溶解度 (25°C)

体外

体内

左から(NMPから)右の順に溶剤を製品に加えます(文献ではなく、Selleckの実験によるデータ):
5%DMSO+40%PEG300+5%Tween80+50%ddH2O
混合させたのち直ちに使用することを推奨します。

3.95 mg/mL

化学情報

分子量 395.49
化学式

C21H17NO3S2

CAS No. 587871-26-9
Storage 3年 -20°C
2年 -80°C in solvent
Smiles C1COCCN1C2=CC(=O)C=C(O2)C3=C4C(=CC=C3)SC5=CC=CC=C5S4

投与溶液組成計算機(クリア溶液)

ステップ1:実験データを入力してください。(実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します)

mg/kg g μL

ステップ2:投与溶媒の組成を入力してください。(ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください)

% DMSO % % Tween 80 % ddH2O
%DMSO %

計算結果:

投与溶媒濃度: mg/ml;

DMSOストック溶液調製方法: mg 試薬を μL DMSOに溶解する(濃度 mg/mL, 注:濃度が当該ロットのDMSO溶解度を超える場合はご連絡ください。 )

投与溶媒調製方法:Take μL DMSOストック溶液に μL PEG300,を加え、完全溶解後μL Tween 80,を加えて完全溶解させた後 μL ddH2O,を加え完全に溶解させます。

投与溶媒調製方法:μL DMSOストック溶液に μL Corn oil,を加え、完全溶解。

注意:1.ストック溶液に沈殿、混濁などがないことをご確認ください;
2.順番通りに溶剤を加えてください。次のステップに進む前に溶液に沈殿、混濁などがないことを確認してから加えてください。ボルテックス、ソニケーション、水浴加熱など物理的な方法で溶解を早めることは可能です。

便利ツール

質量 濃度 体積 分子量

技術サポート

ストックの作り方、阻害剤の保管方法、細胞実験や動物実験の際に注意すべき点など、製品を取扱う時に問い合わせが多かった質問に対しては取扱説明書でお答えしています。

Handling Instructions

他に質問がある場合は、お気軽にお問い合わせください。

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Tags: KU-55933 (ATM Kinase Inhibitor)を買う | KU-55933 (ATM Kinase Inhibitor) ic50 | KU-55933 (ATM Kinase Inhibitor)供給者 | KU-55933 (ATM Kinase Inhibitor)を購入する | KU-55933 (ATM Kinase Inhibitor)費用 | KU-55933 (ATM Kinase Inhibitor)生産者 | オーダーKU-55933 (ATM Kinase Inhibitor) | KU-55933 (ATM Kinase Inhibitor)化学構造 | KU-55933 (ATM Kinase Inhibitor)分子量 | KU-55933 (ATM Kinase Inhibitor)代理店