KU-55933 (ATM Kinase Inhibitor)

Catalog No.S1092

KU-55933 (ATM Kinase Inhibitor) Chemical Structure

Molecular Weight(MW): 395.49

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.

Size Price Stock Quantity  
In DMSO USD 112 In stock
USD 70 In stock
USD 120 In stock
USD 370 In stock

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Cited by 35 Publications

4 Customer Reviews

  •  

    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.

    Cancer Discov 2012 2, 1048-1063. KU-55933 (ATM Kinase Inhibitor) purchased from Selleck.

    Confocal immunostaining (left panel) graphical representation (right panel) for phosphorylation of S25-53BP1, which is known to be ATM dependent, at different time points following irradiation of HEK 293T parental and p18CycE-expressing cells in the absence or presence of the ATM inhibitor, KU55933. Error bars represent SD (n=3).

    Nucleic Acids Res 2011 41, 10157-69. KU-55933 (ATM Kinase Inhibitor) purchased from Selleck.

  •  

    59PDb2 repression is restored in c22 by inhibition of DNAPKcs. Shown are representative ChIP QPCR of USF-1 binding at Db2 (A) and Db2 mRNA levels (B) in P5424-c22 1 d after treatment with the indicated kinase inhibitors.

    J Immunol 2012 188, 2266-2275. KU-55933 (ATM Kinase Inhibitor) purchased from Selleck.

    effect of ATM inhibitor in etoposide-induced cell death. The cells were pretreated with KU55933 (2 μM) for 1 h before etoposide treatment.

     

     

    J Biol Chem 2011 286, 8394-8404. KU-55933 (ATM Kinase Inhibitor) purchased from Selleck.

Purity & Quality Control

Choose Selective ATM/ATR Inhibitors

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Notes:

2. For more details, such as half maximal inhibitory concentrations (IC50s) and working concentrations of each inhibitor, please click on the link of the inhibitor of interest.
3. "+" indicates inhibitory effect. Increased inhibition is marked by a higher "+" designation.
4. Orange "√" refers to compounds which do inhibitory effects on the related isoform, but without specific value.

Biological Activity

Description 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.
Targets
ATM [1]
(Cell-free assay)
DNA-PK [1]
(Cell-free assay)
mTOR [1]
(Cell-free assay)
PI3K [1]
(Cell-free assay)
ATR [1]
(Cell-free assay)
12.9 nM 2.5 μM 9.3 μM 16.6 μM >100 μM
In vitro

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]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
DU-145 NHXhTmVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M33aT2lEPTB;Mz6yO|M2OiEQvF2= MnXWV2FPT0WU
HuO-3N1 NWH0dYVWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVXJR|UxRTRwMUexOFIh|ryP M4XrPHNCVkeHUh?=
LAMA-84 NFfrVJVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M37KWmlEPTB;ND61PFQ3PSEQvF2= NF7YO4tUSU6JRWK=
CAL-72 NHTsTYFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1vCcGlEPTB;NT60PFA5PCEQvF2= M4LC[HNCVkeHUh?=
LoVo Mnz5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MofTTWM2OD14LkmzNlM6KM7:TR?= NITRV4RUSU6JRWK=
HH NE\HOoZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NILNTFlKSzVyPUiuNlc3PzFizszN MXXTRW5ITVJ?
SK-MEL-3 NYHUUndLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVvJR|UxRThwMki1O|Uh|ryP NHOyNpVUSU6JRWK=
KM12 MmrQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH3DWndKSzVyPUmuNlEyPDJizszN NWPybIZPW0GQR1XS
NCI-H1437 NIfpcmdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEXmZWlKSzVyPUmuPFA6PyEQvF2= M3vBfHNCVkeHUh?=
NCI-H1838 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4DvdWlEPTB;MUGuNVg3PSEQvF2= MWXTRW5ITVJ?
J-RT3-T3-5 M{XGXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUfJR|UxRTFzLkK0NVch|ryP NXL1S4VIW0GQR1XS
GOTO MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3WyfGlEPTB;MUGuOlk6PiEQvF2= NIfEVWdUSU6JRWK=
LB2241-RCC NX;3fFRiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2fZb2lEPTB;MUGuO|E5PiEQvF2= NF7UcJFUSU6JRWK=
ES7 NUPFUVZ[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXjGepViUUN3ME2xNU44QDhizszN NXjvUGlCW0GQR1XS
KP-N-YS M2DQdmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV;pV3B1UUN3ME2xNk43OzV2IN88US=> NUTidoVDW0GQR1XS
CAL-12T NIjwN4VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIPzZ2RKSzVyPUGzMlYyPyEQvF2= MV7TRW5ITVJ?
COLO-684 NVuzcJZET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4fWVGlEPTB;MUSuNVU3QSEQvF2= Ml\WV2FPT0WU
DOK M2HzTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIXvS5lKSzVyPUG1MlM{OjlizszN MXXTRW5ITVJ?
Hs-578-T NIfDb3BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3\R[mlEPTB;MUWuOFE5OiEQvF2= MUHTRW5ITVJ?
D-423MG NV7ueIN4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWrJR|UxRTF3LkWyN|Yh|ryP NUTpPJJrW0GQR1XS
DBTRG-05MG MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYf5bFh4UUN3ME2xOU43OTFzIN88US=> NWiwV5REW0GQR1XS
VM-CUB-1 MnGxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2e2S2lEPTB;MUWuPVg1QSEQvF2= NWTlRpdNW0GQR1XS
KG-1 M3nQNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXjJR|UxRTF4LkC5PVYh|ryP M2HwN3NCVkeHUh?=
8305C M2fDUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF33W21KSzVyPUG2MlE5QDlizszN MWDTRW5ITVJ?
HuH-7 M{LCSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2fSSmlEPTB;MU[uNlY4PCEQvF2= NI[0WZhUSU6JRWK=
LXF-289 M2PhUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXXJR|UxRTF4LkK3OFch|ryP MWfTRW5ITVJ?
NCI-H1793 NUDOdWp[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUfxfHFuUUN3ME2xOk41PzF{IN88US=> M2fmUnNCVkeHUh?=
ChaGo-K-1 NITVZYdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NITGUWxKSzVyPUG2MlY2PjhizszN MnPLV2FPT0WU
GCIY NUnueHpMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHfHO21KSzVyPUG2Mlc6ODVizszN MkfkV2FPT0WU
SK-MEL-28 M4HEeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHj4dWVKSzVyPUG3MlA1PzVizszN M1q4PXNCVkeHUh?=
NCI-SNU-1 Mn6xS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3XRcWlEPTB;MUeuNVI3QSEQvF2= MYDTRW5ITVJ?
CTB-1 Mn3DS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYnJR|UxRTF5LkKyOVkh|ryP MUnTRW5ITVJ?
NCI-H82 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHjScmhKSzVyPUG3MlQ2PzNizszN NXPXfmhXW0GQR1XS
HCC2998 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MofFTWM2OD1zNz62O|M{KM7:TR?= MoDuV2FPT0WU
NCI-H2030 NF3lRWJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoLaTWM2OD1zOD6xPVk4KM7:TR?= NXHw[WdCW0GQR1XS
HuP-T3 NXL6TGx3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX\JR|UxRTF6LkW4PFgh|ryP MYHTRW5ITVJ?
697 M2mw[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUn5XmdJUUN3ME2xPU4xOjBzIN88US=> NYXKW3c3W0GQR1XS
MLMA M{nZWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWjJR|UxRTF7LkC1OVch|ryP NYi0fmVRW0GQR1XS
HCC70 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4DNbmlEPTB;MUmuOFg6KM7:TR?= NYr0O4h7W0GQR1XS
A704 MmnBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2PPRmlEPTB;MUmuPFMxPSEQvF2= NIHLVWNUSU6JRWK=
D-283MED MnnIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHzNSJFKSzVyPUKwMlU{OzlizszN MlP3V2FPT0WU
U031 NWnLeohPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mlf3TWM2OD1{MT6xOFg6KM7:TR?= M4roO3NCVkeHUh?=
HSC-3 NH3xU4ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFrHTpJKSzVyPUKxMlE5OzVizszN M2HqRnNCVkeHUh?=
JVM-3 NYGwcmR3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYLJR|UxRTJ{LkWwOkDPxE1? NInHcWpUSU6JRWK=
Mewo MknWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGjOdlZKSzVyPUKyMlUxPzNizszN MkDEV2FPT0WU
YH-13 NEPzboRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYTqPINVUUN3ME2yNk42OTJ|IN88US=> NELOUGtUSU6JRWK=
LB1047-RCC MlPqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXvGdVlEUUN3ME2yNk42QDd7IN88US=> MkHzV2FPT0WU
HCC2157 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NITJ[ZlKSzVyPUKyMlgxPTRizszN MWDTRW5ITVJ?
SNU-449 NFjZbZdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NG\aSm1KSzVyPUKyMlg4PDhizszN NX;JSWdXW0GQR1XS
Ramos-2G6-4C10 NICwbHdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWLJR|UxRTJ{Lkm2JO69VQ>? MojoV2FPT0WU
CHL-1 M{nhfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmOzTWM2OD1{Mz63NlkzKM7:TR?= NVPLUVA3W0GQR1XS
SK-MEL-30 NUXLZmp6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmnZTWM2OD1{ND60OlYzKM7:TR?= MWPTRW5ITVJ?
PANC-08-13 NY\3do9bT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlHKTWM2OD1{NT6wPVM5KM7:TR?= NEXCRVNUSU6JRWK=
QIMR-WIL NHW1SGNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXi4OpBsUUN3ME2yOU4yQDV6IN88US=> MXvTRW5ITVJ?
BFTC-905 MnTYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NY\ibo1TUUN3ME2yOU42QTR2IN88US=> NES0ZmdUSU6JRWK=
GI-1 NHLuUJNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mlu4TWM2OD1{NT63NFU2KM7:TR?= NYnLS|diW0GQR1XS
MDA-MB-415 M{LBN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4jpUmlEPTB;Mk[uOVA{OyEQvF2= NW[wXoRbW0GQR1XS
GT3TKB M2WxWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NELiRlBKSzVyPUK2MlU{PDJizszN MlzYV2FPT0WU
DEL NVj1clF[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX3EVHlLUUN3ME2yOk45OzV4IN88US=> MX;TRW5ITVJ?
KOSC-2 M3XNRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWCydVBzUUN3ME2yOk46ODd3IN88US=> NYq3TmxPW0GQR1XS
RVH-421 NGnaXFhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoP4TWM2OD1{Nz6yPVIyKM7:TR?= M3TQUnNCVkeHUh?=
EW-13 M361Xmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFK1do1KSzVyPUK3MlQ{ODhizszN MkDaV2FPT0WU
639-V NU\0NXVUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIXEfpFKSzVyPUK3MlUyOTlizszN NGPrc5lUSU6JRWK=
A2780 Mo\iS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVXJR|UxRTJ5Lk[0NUDPxE1? NVe5T4xFW0GQR1XS
SW982 MlPJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NI\KO2dKSzVyPUK3MlkxPTJizszN NVPwfIdYW0GQR1XS
SW1710 M{HVNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIfBeoZKSzVyPUK4MlA6QDFizszN M4nUPXNCVkeHUh?=
HCC1569 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHTt[plKSzVyPUK4MlQ5QTdizszN NIX3VZBUSU6JRWK=
MV-4-11 MknZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUCwSWMxUUN3ME2yPE42PzN3IN88US=> Mo\JV2FPT0WU
BHT-101 NHrLdHRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV3hWW5{UUN3ME2yPE43PTd{IN88US=> MYLTRW5ITVJ?
Ca9-22 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVTJR|UxRTJ6LkexOEDPxE1? Mm\lV2FPT0WU
HAL-01 NYDDUnlvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3TlfmlEPTB;MkiuO|YyPSEQvF2= M{jSPHNCVkeHUh?=
D-263MG NWLt[4VKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWr1dGxFUUN3ME2yPU4{PDRizszN MWHTRW5ITVJ?
NEC8 MkXiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVXx[oFnUUN3ME2yPU42PTR6IN88US=> NWfUfFY1W0GQR1XS
EKVX Ml7FS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUPFWYhGUUN3ME2zNU42QDR5IN88US=> M4O4PHNCVkeHUh?=
EM-2 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3naeWlEPTB;M{GuOlMxPCEQvF2= MXLTRW5ITVJ?
MFM-223 NETFVWpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWfSfmtPUUN3ME2zNU45ODl6IN88US=> M1PMVnNCVkeHUh?=
SK-PN-DW MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFvoXo5KSzVyPUOyMlE1ODZizszN NWH6fmhkW0GQR1XS
HuO9 NXL2XWU3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2KxW2lEPTB;M{KuOVI5OiEQvF2= NY\jUYllW0GQR1XS
MHH-PREB-1 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH7aOXZKSzVyPUOyMlYzOzRizszN Mm\6V2FPT0WU
OVCAR-4 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVfJR|UxRTN{LkizOlMh|ryP MkPIV2FPT0WU
NCI-H1648 NXX3fY9zT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX\2[FZjUUN3ME2zNk45PjVzIN88US=> M4m0UXNCVkeHUh?=
MKN1 MkTiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUTWdXRSUUN3ME2zOE4yOTBzIN88US=> M2nLbHNCVkeHUh?=
KYSE-450 NYH3OJFwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkjqTWM2OD1|ND62OFQ1KM7:TR?= MX;TRW5ITVJ?
ES8 NGPHdHpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2Pke2lEPTB;M{SuPFk4PSEQvF2= M2nKWnNCVkeHUh?=
MS-1 NV;ZXpNnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M17iS2lEPTB;M{SuPVU2PCEQvF2= MlrzV2FPT0WU
HOP-92 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUfJR|UxRTN3LkmyO|ch|ryP MYTTRW5ITVJ?
SKG-IIIa M4rFSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4HD[GlEPTB;M{[uNlU3OSEQvF2= NYe4ZYd3W0GQR1XS
TE-11 NF3HW3NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3XmWmlEPTB;M{[uOVI1OyEQvF2= MUnTRW5ITVJ?
SK-NEP-1 M{LNXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{fid2lEPTB;M{euOlc1PCEQvF2= NEjSSmtUSU6JRWK=
DB M4\VXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3vFTWlEPTB;M{euPVE5PSEQvF2= MWrTRW5ITVJ?
IA-LM M4T3dGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4TPdmlEPTB;M{iuNFI{QSEQvF2= NH\WcnNUSU6JRWK=
COLO-829 NFjBNoJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF;0d2VKSzVyPUO4MlQyPTlizszN NWCybm9xW0GQR1XS
TGBC11TKB MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1vvdmlEPTB;M{muNVQxQCEQvF2= M2PoR3NCVkeHUh?=
CAL-51 NV64PJRkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MULJR|UxRTRyLkC2NVIh|ryP MWTTRW5ITVJ?
NCI-H2228 NF3BfY1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkfmTWM2OD12MD6zOlYzKM7:TR?= MoTnV2FPT0WU
C32 NGrSOHlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnfTTWM2OD12MD60NFI1KM7:TR?= MXfTRW5ITVJ?
KU-19-19 NWHBc4FET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYDJR|UxRTRyLke2PFMh|ryP NHO0ZpRUSU6JRWK=
KNS-62 M{DGdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2jqfGlEPTB;NECuPFM5OSEQvF2= NUSybHBlW0GQR1XS
FADU MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnTMTWM2OD12MT6yOVAzKM7:TR?= MkDYV2FPT0WU
CAL-33 MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnntTWM2OD12Mj62O|Q6KM7:TR?= M3n1UXNCVkeHUh?=
CHP-134 M4f1NWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2rpUmlEPTB;NEKuPFQ6PiEQvF2= MYnTRW5ITVJ?
HDLM-2 MmPXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWfZc25lUUN3ME20Nk46ODh2IN88US=> Ml\2V2FPT0WU
NBsusSR M3PPOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVjJR|UxRTR|LkC3NlUh|ryP NVmydodbW0GQR1XS
SW954 NXvvXmx2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVjJR|UxRTR|LkGwOVMh|ryP NVz5Xpk{W0GQR1XS
HCC1806 M4jOOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUnJR|UxRTR|LkSxNUDPxE1? Mn7FV2FPT0WU
VMRC-RCZ M1WwUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYDD[4NQUUN3ME20N{41PTh4IN88US=> NGTHc|BUSU6JRWK=
A549 NWDnOnBxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml\qTWM2OD12Mz65N|Eh|ryP MnKzV2FPT0WU
NKM-1 Moq0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYDaZXlxUUN3ME20N{46PTV6IN88US=> NYDtXmFiW0GQR1XS
DMS-273 NXzhSYQ5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWXhOIM5UUN3ME20OE44PTZ5IN88US=> MonhV2FPT0WU
TYK-nu NF;nRpJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEjrOGdKSzVyPUS1MlEzOzRizszN NVH1Z4JUW0GQR1XS
KALS-1 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV;JR|UxRTR3LkG0OkDPxE1? NWrOTpQ5W0GQR1XS
A101D NILNV5BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXW2Nph4UUN3ME20OU41PDV4IN88US=> NHS5OXhUSU6JRWK=
G-361 M1r6Xmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{m5T2lEPTB;NE[uNlE{QCEQvF2= NFf6bGlUSU6JRWK=
KARPAS-299 M4jSSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmjzTWM2OD12Nj6zOVE3KM7:TR?= NFu1ZoVUSU6JRWK=
RS4-11 NU\WOVhHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlL2TWM2OD12Nj61OFIh|ryP MlzpV2FPT0WU
HT-1376 NUXQcYpjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{TpOmlEPTB;NE[uO|QzPiEQvF2= NX;VdFF[W0GQR1XS
SK-N-AS M2exO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWj5SY9CUUN3ME20Ok44QDJ{IN88US=> Mn3aV2FPT0WU
MG-63 NVH5U|BFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWrJR|UxRTR4LkmwN|Yh|ryP MX3TRW5ITVJ?
EPLC-272H MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVPjOW01UUN3ME20Ok46PTB|IN88US=> M4HrenNCVkeHUh?=
BALL-1 NVPSSItGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlPyTWM2OD12Nz64N|Ih|ryP NGXSenBUSU6JRWK=
LCLC-97TM1 M{HTSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1r3[WlEPTB;NEiuNlAzKM7:TR?= MmPwV2FPT0WU
HO-1-N-1 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NILlSXVKSzVyPUS4Mlk3PzZizszN NVX6Z5ZIW0GQR1XS
MFE-280 NX;NO4RST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkL5TWM2OD12OT60OlE4KM7:TR?= NGjTUpJUSU6JRWK=
NCI-H526 M2fGWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX24R|NzUUN3ME20PU45OTZ|IN88US=> MVrTRW5ITVJ?
D-566MG NHHY[XdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVjJR|UxRTR7LkmwPVYh|ryP M{PwNXNCVkeHUh?=
BB30-HNC MnvCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWTJR|UxRTR7Lkm0PVgh|ryP M3HXVXNCVkeHUh?=
SK-N-DZ MnLnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYjJR|UxRTVyLkC0PFEh|ryP MkW4V2FPT0WU
HepG2  MoHyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHnLe5gyOMLizszN M1XXeVI1KGh? NUnWTHky[myxY3vzJHNENUmLSUOtbY5lfWOnZDDTJJBp[XOnIHHydoV{fA>? MV[yOVUzPzF{Mx?=
HepG2  NIXNZmxHfW6ldHnvckBCe3OjeR?= MlHoNVDDqM7:TR?= MojnNlQhcA>? MmTod5VxeHKnc4Pld{B1cGVicHjvd5Bpd3K7bHH0bY9veyCxZjDBWG0hd25iU3XyNVk5OSxiQ3jrNUBwdiCVZYKzOFUtKEOqa{Kgc44hXGi{NkisJIFv\CCFZHuyJI9vKFS7ckG1JIlv\HWlZXSgZpkhW0NvSVnJNy=> NYLpZ29OOjV3MkexNlM>
KATO III  NYHFUW42T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoTHNk42NzVxNz61JO69VQ>? M33zbWROW09? M3T5SoVvcGGwY3XzJJRp\SC2b4jpZ4l1gSCxZjDvcIFx[XKrYh?= NVPvVoVCOjR6NEG3NVg>
hTCEpi NGHQXnZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2C4TVExKM7:TR?= MkfKSG1UVw>? MXXwdoV3\W62czD0bIUh[3m2b4DheIhq[yCnZn\lZ5Qhd2ZiSGPWMVE> NVG2dHNlOjR|N{C4N|U>
MCF10A MmfxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4S3UVExKM7:TR?= MYSyOEBp MUPEUXNQ NVHiRmx6eG:2ZX70bYF1\XNidHjlJIN6fG:2b4jpZ4l1gSCxZjDHRS=> NWGyUW94OjRzNUC1PVU>
HL-60  M4LMXmZ2dmO2aX;uJGF{e2G7 M3rUdVExKM7:TR?= MUSwMlUhcA>? Mo\6SG1UVw>? M1f2RZJm\HWlZYOgdIhwe3Cqb4L5cIF1cW:wIH;mJGNpczMEoB?= MXeyN|k{PDRzMR?=
MCF-7 MoPoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnXGNU0yODEQvF2= NEDLUlUzPCCq MVTGRnM> M4TDSolvcGmkaYTzJJRp\SClZXzsJJBzd2yrZnXyZZRqd25? NVnCRW5POjNzOEWzOFc>
HeLa  MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NITQSGsyNTFyMN88US=> MUKyOEBp Ml3ySmJU MY\pcohq[mm2czD0bIUh[2WubDDwdo9tcW[ncnH0bY9v NUDafZBnOjNzOEWzOFc>
SH-SY5Y NIO5cG1HfW6ldHnvckBCe3OjeR?= MmTyNVDDqM7:TdMg NF7N[40zPCCq NUToNFlvcW6qaXLpeJMh[2yrb4H1bY5wdC2rbnT1Z4VlKHCqb4PwbI9zgWyjdHnvckBw\iCyNUO= NIPzVWIzOjZ{N{K5OC=>
IMR-32 M{nP[WZ2dmO2aX;uJGF{e2G7 NH[1cIIyOMLizszNxsA> MlLSNlQhcA>? M2D4bolvcGmkaYTzJINtcW:zdXnuc4wucW6mdXPl[EBxcG:|cHjvdplt[XSrb36gc4YheDV| NWXzNGREOjJ4MkeyPVQ>
A549 NWDCfWlpTnWwY4Tpc44hSXO|YYm= MnvBNVDDqM7:TdMg MYOxJIg> NFr5NHd{fXCycnXzd4V{KE6jbn:tR48ucW6mdXPl[EBxPTNiYXPjeY12dGG2aX;u MVuyNlU2QTN{MR?=
T47D  M2\Z[mZ2dmO2aX;uJGF{e2G7 Mom3NlDDqG2P MmLXNlQhcA>? M{HHXWROW09? NUXGRVRseHKndnXueJMhUVJvaX7keYNm\CCmZXfyZYRifGmxbjDv[kBK|rqEzsG= NFXhdJMzOTF2NEiwOS=>
A29 MEF NVL6fVlWTnWwY4Tpc44hSXO|YYm= MWKxNOKh|ryPwrC= MX:xbC=> NWTlPZI3[myxY3vzxsB1cGVicHjvd5Bpd3K7bHH0bY9vKG:oIFHreEBifCCVZYK0O|PDqA>? NFnJcYwzODB3M{e4NS=>
MDA-MB-453  MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYG1MVQxKM7:TR?= M1XwU|czKGh? M3LuVGlEPTBib3[gNVAh|ryP NGPGWlUzODB3M{e4NS=>
PC-3 NVHxUVdST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlvHOU01OCEQvF2= NF70W3M4OiCq M4LtRmlEPTBib3[gNVAh|ryP MWiyNFA2Ozd6MR?=

... Click to View More Cell Line Experimental Data

In vivo 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]

Protocol

Kinase Assay:[1]
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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.
Cell Research:[1]
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  • Cell lines: U2OS cells
  • Concentrations: 10 μM
  • Incubation Time: 2 hours
  • Method: 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.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 33 mg/mL (83.44 mM)
Water <1 mg/mL
Ethanol <1 mg/mL
In vivo 5% DMSO and 47.5% PEG300 10 mg/mL

* 1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 395.49
Formula

C21H17NO3S2

CAS No. 587871-26-9
Storage powder
in solvent
Synonyms N/A

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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID