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 NV3Kb5YzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4DqdGlEPTB;Mz6yO|M2OiEQvF2= NHjn[VRUSU6JRWK=
HuO-3N1 NHPs[XRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXTJR|UxRTRwMUexOFIh|ryP NH\QdXhUSU6JRWK=
LAMA-84 M3nPTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUXJR|UxRTRwNUi0OlUh|ryP Mn;oV2FPT0WU
CAL-72 M1fIeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYTJR|UxRTVwNEiwPFQh|ryP NE\sPWtUSU6JRWK=
LoVo MkT6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{Hre2lEPTB;Nj65N|I{QSEQvF2= MVfTRW5ITVJ?
HH NIjvO3pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX7JR|UxRThwMke2O|Eh|ryP MnLGV2FPT0WU
SK-MEL-3 NXWzO4pvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3HOU2lEPTB;OD6yPFU4PSEQvF2= MVLTRW5ITVJ?
KM12 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3jTVmlEPTB;OT6yNVE1OiEQvF2= MknjV2FPT0WU
NCI-H1437 M3vpR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NELWXFRKSzVyPUmuPFA6PyEQvF2= NVf5co5mW0GQR1XS
NCI-H1838 NVnwdot1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYfJR|UxRTFzLkG4OlUh|ryP NYHye5FyW0GQR1XS
J-RT3-T3-5 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3r5[WlEPTB;MUGuNlQyPyEQvF2= M17rUnNCVkeHUh?=
GOTO NX\PO4lXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYPJR|UxRTFzLk[5PVYh|ryP NVHJXWFWW0GQR1XS
LB2241-RCC NXe1NWhDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHvZOWdKSzVyPUGxMlcyQDZizszN MXvTRW5ITVJ?
ES7 M4HjV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmS0TWM2OD1zMT63PFgh|ryP M4rjZ3NCVkeHUh?=
KP-N-YS M2HqZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGrDSJhKSzVyPUGyMlY{PTRizszN NVnoNGp3W0GQR1XS
CAL-12T NX;ieFBqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYDJR|UxRTF|Lk[xO{DPxE1? MV\TRW5ITVJ?
COLO-684 MlTXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV7IbZhXUUN3ME2xOE4yPTZ7IN88US=> M4TDNXNCVkeHUh?=
DOK MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mo\nTWM2OD1zNT6zN|I6KM7:TR?= MnHXV2FPT0WU
Hs-578-T MnTkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXvJR|UxRTF3LkSxPFIh|ryP NHTId4xUSU6JRWK=
D-423MG MmnBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFjkZ3NKSzVyPUG1MlUzOzZizszN NXfhUJk1W0GQR1XS
DBTRG-05MG NHry[WFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWjJR|UxRTF3Lk[xNVEh|ryP NF;QRndUSU6JRWK=
VM-CUB-1 NGm0OY5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3;EeGlEPTB;MUWuPVg1QSEQvF2= NWLXT4JlW0GQR1XS
KG-1 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGLCXHdKSzVyPUG2MlA6QTZizszN M2P3V3NCVkeHUh?=
8305C MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH\IWYRKSzVyPUG2MlE5QDlizszN NG\sbHVUSU6JRWK=
HuH-7 M2XlXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M13zPWlEPTB;MU[uNlY4PCEQvF2= NHm2d4ZUSU6JRWK=
LXF-289 M17GSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3\LUGlEPTB;MU[uNlc1PyEQvF2= Mom4V2FPT0WU
NCI-H1793 M{PZOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUnPXnA6UUN3ME2xOk41PzF{IN88US=> M2ftbnNCVkeHUh?=
ChaGo-K-1 M{jVOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnfoTWM2OD1zNj62OVY5KM7:TR?= M2HHfHNCVkeHUh?=
GCIY MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkTtTWM2OD1zNj63PVA2KM7:TR?= MWDTRW5ITVJ?
SK-MEL-28 NYjpNVh{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX7XUZQ3UUN3ME2xO{4xPDd3IN88US=> Mk[xV2FPT0WU
NCI-SNU-1 M2W3Omdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWHJR|UxRTF5LkGyOlkh|ryP M1rkN3NCVkeHUh?=
CTB-1 NXLqNottT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGrMdJdKSzVyPUG3MlIzPTlizszN NInpcZZUSU6JRWK=
NCI-H82 MoTYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3XQWWlEPTB;MUeuOFU4OyEQvF2= NGTFTZNUSU6JRWK=
HCC2998 NHjzUJFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXXRRWRNUUN3ME2xO{43PzN|IN88US=> M{X5PXNCVkeHUh?=
NCI-H2030 MnPLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGTvOldKSzVyPUG4MlE6QTdizszN NXvqZpdnW0GQR1XS
HuP-T3 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUfkTIVsUUN3ME2xPE42QDh6IN88US=> MVXTRW5ITVJ?
697 MnvMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnvSTWM2OD1zOT6wNlAyKM7:TR?= M3nlUHNCVkeHUh?=
MLMA M1rqemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYTTPFJPUUN3ME2xPU4xPTV5IN88US=> NV7YNGxyW0GQR1XS
HCC70 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX7JR|UxRTF7LkS4PUDPxE1? NVL1W49YW0GQR1XS
A704 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV73foFPUUN3ME2xPU45OzB3IN88US=> MmPoV2FPT0WU
D-283MED NYW5TVVYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWHJR|UxRTJyLkWzN|kh|ryP MojwV2FPT0WU
U031 MnfGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3\rS2lEPTB;MkGuNVQ5QSEQvF2= MWDTRW5ITVJ?
HSC-3 MoK3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVq5PWVKUUN3ME2yNU4yQDN3IN88US=> MlXoV2FPT0WU
JVM-3 M32wZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXzJR|UxRTJ{LkWwOkDPxE1? M3uw[3NCVkeHUh?=
Mewo MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4DwTmlEPTB;MkKuOVA4OyEQvF2= M1T0PXNCVkeHUh?=
YH-13 Mn7PS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFPWfYZKSzVyPUKyMlUyOjNizszN NXfhUIRzW0GQR1XS
LB1047-RCC MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnPJTWM2OD1{Mj61PFc6KM7:TR?= NGLqTZJUSU6JRWK=
HCC2157 MnvBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmXzTWM2OD1{Mj64NFU1KM7:TR?= MoHqV2FPT0WU
SNU-449 MoLWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M37PdWlEPTB;MkKuPFc1QCEQvF2= MmK5V2FPT0WU
Ramos-2G6-4C10 MlvKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1fLcGlEPTB;MkKuPVYh|ryP MlvrV2FPT0WU
CHL-1 NFTyW2lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NULGWmtQUUN3ME2yN{44Ojl{IN88US=> MVzTRW5ITVJ?
SK-MEL-30 Ml\zS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MonaTWM2OD1{ND60OlYzKM7:TR?= M1zCdHNCVkeHUh?=
PANC-08-13 Mn3hS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFvvXZNKSzVyPUK1MlA6OzhizszN MWnTRW5ITVJ?
QIMR-WIL MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX7JR|UxRTJ3LkG4OVgh|ryP M1\GXnNCVkeHUh?=
BFTC-905 NV7ocpVJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVHGPVV6UUN3ME2yOU42QTR2IN88US=> MXjTRW5ITVJ?
GI-1 MmP1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmrWTWM2OD1{NT63NFU2KM7:TR?= MWXTRW5ITVJ?
MDA-MB-415 NYXSUnI1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkfkTWM2OD1{Nj61NFM{KM7:TR?= M3zUT3NCVkeHUh?=
GT3TKB M3yzNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH7vSXdKSzVyPUK2MlU{PDJizszN NEnOOlZUSU6JRWK=
DEL M1nmWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIjOZohKSzVyPUK2Mlg{PTZizszN Mn2wV2FPT0WU
KOSC-2 M{Xy[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVPJR|UxRTJ4LkmwO|Uh|ryP NYT0fXBvW0GQR1XS
RVH-421 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXnJR|UxRTJ5LkK5NlEh|ryP M3nU[nNCVkeHUh?=
EW-13 MonvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYT6fmpPUUN3ME2yO{41OzB6IN88US=> MkjrV2FPT0WU
639-V MlW4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWW3TGdwUUN3ME2yO{42OTF7IN88US=> MVXTRW5ITVJ?
A2780 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWjwfJloUUN3ME2yO{43PDFizszN MXzTRW5ITVJ?
SW982 Mn\ZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnOzTWM2OD1{Nz65NFUzKM7:TR?= NHHGUW1USU6JRWK=
SW1710 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIfU[YVKSzVyPUK4MlA6QDFizszN NVzVXnRbW0GQR1XS
HCC1569 NGq3RYxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MULJR|UxRTJ6LkS4PVch|ryP NVnVcoR5W0GQR1XS
MV-4-11 MlXHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWHtNFRKUUN3ME2yPE42PzN3IN88US=> NIjmcW1USU6JRWK=
BHT-101 M4\sR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUfJR|UxRTJ6Lk[1O|Ih|ryP NYmwUXBNW0GQR1XS
Ca9-22 M1TWXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MljFTWM2OD1{OD63NVQh|ryP NWHXd3Q6W0GQR1XS
HAL-01 NVXhWGhkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWHOOHVCUUN3ME2yPE44PjF3IN88US=> NX3jWZFmW0GQR1XS
D-263MG MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH\ENpVKSzVyPUK5MlM1PCEQvF2= M{TzUHNCVkeHUh?=
NEC8 NWHBfWRPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYC2N2g6UUN3ME2yPU42PTR6IN88US=> M1zqeXNCVkeHUh?=
EKVX M{WxfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NW\ER|NWUUN3ME2zNU42QDR5IN88US=> MYXTRW5ITVJ?
EM-2 M1rwWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVrJR|UxRTNzLk[zNFQh|ryP MWXTRW5ITVJ?
MFM-223 MknSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX\JR|UxRTNzLkiwPVgh|ryP MW\TRW5ITVJ?
SK-PN-DW MnznS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXfJR|UxRTN{LkG0NFYh|ryP M{\LcnNCVkeHUh?=
HuO9 MnzBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH;o[4lKSzVyPUOyMlUzQDJizszN MlnEV2FPT0WU
MHH-PREB-1 NETlVHVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH;K[ItKSzVyPUOyMlYzOzRizszN MoTOV2FPT0WU
OVCAR-4 NVTW[VlDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIXUcVBKSzVyPUOyMlg{PjNizszN MkK4V2FPT0WU
NCI-H1648 NGX2b5ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEDLUoVKSzVyPUOyMlg3PTFizszN NYKxN4M6W0GQR1XS
MKN1 NW\oVo5CT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4jvZ2lEPTB;M{SuNVExOSEQvF2= NFPSVFdUSU6JRWK=
KYSE-450 NIjkT|dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUTJR|UxRTN2Lk[0OFQh|ryP Ml3pV2FPT0WU
ES8 MnXXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NImwbGNKSzVyPUO0Mlg6PzVizszN MXrTRW5ITVJ?
MS-1 NFzEfFhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIHI[3BKSzVyPUO0Mlk2PTRizszN NUnpVJFCW0GQR1XS
HOP-92 NFmzTXVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVnzb2k3UUN3ME2zOU46Ojd5IN88US=> NF[1PFVUSU6JRWK=
SKG-IIIa NX7oZ3IyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX\kelhJUUN3ME2zOk4zPTZzIN88US=> NYn5dXo3W0GQR1XS
TE-11 NHfiOohIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M13SPGlEPTB;M{[uOVI1OyEQvF2= NULwN3d1W0GQR1XS
SK-NEP-1 M2rmb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2XoZmlEPTB;M{euOlc1PCEQvF2= MYrTRW5ITVJ?
DB M2Gwc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NY\jb|N7UUN3ME2zO{46OTh3IN88US=> NILnR2RUSU6JRWK=
IA-LM M2Tj[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1LlTGlEPTB;M{iuNFI{QSEQvF2= MoXzV2FPT0WU
COLO-829 NIPQdnhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIPxN4xKSzVyPUO4MlQyPTlizszN Mn;mV2FPT0WU
TGBC11TKB MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2jpVmlEPTB;M{muNVQxQCEQvF2= NIKwUIdUSU6JRWK=
CAL-51 NIHWW4dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mln6TWM2OD12MD6wOlEzKM7:TR?= MlXtV2FPT0WU
NCI-H2228 M3vyfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1Twb2lEPTB;NECuN|Y3OiEQvF2= NEnhcINUSU6JRWK=
C32 NHHEW|dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXHaXlN[UUN3ME20NE41ODJ2IN88US=> MWjTRW5ITVJ?
KU-19-19 MkjnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVL0N2VUUUN3ME20NE44Pjh|IN88US=> MkTmV2FPT0WU
KNS-62 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1fzcGlEPTB;NECuPFM5OSEQvF2= Ml\kV2FPT0WU
FADU NVrT[G55T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml7xTWM2OD12MT6yOVAzKM7:TR?= M161SHNCVkeHUh?=
CAL-33 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1HYcmlEPTB;NEKuOlc1QSEQvF2= NFnEdHdUSU6JRWK=
CHP-134 MojJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXTJR|UxRTR{Lki0PVYh|ryP MWjTRW5ITVJ?
HDLM-2 NH\yOVhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVHMeI54UUN3ME20Nk46ODh2IN88US=> NULBXGVYW0GQR1XS
NBsusSR MnLaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGO1eVVKSzVyPUSzMlA4OjVizszN MmjjV2FPT0WU
SW954 NIL1cpZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIq1Z29KSzVyPUSzMlExPTNizszN MkTnV2FPT0WU
HCC1806 MlPvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmLrTWM2OD12Mz60NVEh|ryP MYHTRW5ITVJ?
VMRC-RCZ MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXPuXmZbUUN3ME20N{41PTh4IN88US=> MmfiV2FPT0WU
A549 MkXhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnizTWM2OD12Mz65N|Eh|ryP MmTqV2FPT0WU
NKM-1 M4rZV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXnJR|UxRTR|Lkm1OVgh|ryP M{HiS3NCVkeHUh?=
DMS-273 M2C0SGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFG3WlVKSzVyPUS0Mlc2PjdizszN NXTSeVVSW0GQR1XS
TYK-nu NVjJfnJtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXPJR|UxRTR3LkGyN|Qh|ryP NYL2NHBbW0GQR1XS
KALS-1 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUjJR|UxRTR3LkG0OkDPxE1? M3\jU3NCVkeHUh?=
A101D NXz4c|dxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEjiTXVKSzVyPUS1MlQ1PTZizszN M2jIW3NCVkeHUh?=
G-361 MlLVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4jwVmlEPTB;NE[uNlE{QCEQvF2= MnTqV2FPT0WU
KARPAS-299 M1\lNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnTCTWM2OD12Nj6zOVE3KM7:TR?= NXvvR2NrW0GQR1XS
RS4-11 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MY\JR|UxRTR4LkW0NkDPxE1? MWnTRW5ITVJ?
HT-1376 NH3PT4xIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkTzTWM2OD12Nj63OFI3KM7:TR?= MlnmV2FPT0WU
SK-N-AS M3rTNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3W2bmlEPTB;NE[uO|gzOiEQvF2= MUTTRW5ITVJ?
MG-63 M3rC[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFPJboFKSzVyPUS2MlkxOzZizszN MXzTRW5ITVJ?
EPLC-272H MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NY\vb2tjUUN3ME20Ok46PTB|IN88US=> MVXTRW5ITVJ?
BALL-1 MoqyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{TWcmlEPTB;NEeuPFMzKM7:TR?= M1fGUnNCVkeHUh?=
LCLC-97TM1 M321Rmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2jyXGlEPTB;NEiuNlAzKM7:TR?= MnXJV2FPT0WU
HO-1-N-1 M{fLZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3ryWmlEPTB;NEiuPVY4PiEQvF2= NGLvfJFUSU6JRWK=
MFE-280 NXmyT|lpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlHITWM2OD12OT60OlE4KM7:TR?= Ml7GV2FPT0WU
NCI-H526 M1f2d2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV;VTZBmUUN3ME20PU45OTZ|IN88US=> NV71cWxEW0GQR1XS
D-566MG MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIT1ZZFKSzVyPUS5MlkxQTZizszN MYLTRW5ITVJ?
BB30-HNC M1z4RWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV3JR|UxRTR7Lkm0PVgh|ryP NF7ET2JUSU6JRWK=
SK-N-DZ Mnf0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGPqTmdKSzVyPUWwMlA1QDFizszN MkXBV2FPT0WU
HepG2  Moi2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{jQVVExyqEQvF2= NFvtfmczPCCq MVjicI9kc3NiU1OtTWlKOy2rbnT1Z4VlKFNicHjhd4Uh[XK{ZYP0 NFz3R2kzPTV{N{GyNy=>
HepG2  NHi0S5lHfW6ldHnvckBCe3OjeR?= NXzEUItiOTEEoN88US=> MXOyOEBp Mn[2d5VxeHKnc4Pld{B1cGVicHjvd5Bpd3K7bHH0bY9veyCxZjDBWG0hd25iU3XyNVk5OSxiQ3jrNUBwdiCVZYKzOFUtKEOqa{Kgc44hXGi{NkisJIFv\CCFZHuyJI9vKFS7ckG1JIlv\HWlZXSgZpkhW0NvSVnJNy=> MlLsNlU2OjdzMkO=
KATO III  MnXoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1jZOlIvPS93L{euOUDPxE1? M1:4UmROW09? M2XROYVvcGGwY3XzJJRp\SC2b4jpZ4l1gSCxZjDvcIFx[XKrYh?= M{j4[VI1QDRzN{G4
hTCEpi NUnvc|QxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVvJWmV4OTBizszN Mk\kSG1UVw>? NFzZPVBxemW4ZX70d{B1cGViY4n0c5BifGirYzDl[oZm[3Rib3[gTHNXNTF? NXnOcHJFOjR|N{C4N|U>
MCF10A NGDUbHRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGXjeXkyOCEQvF2= Mn\FNlQhcA>? MXfEUXNQ M3\HfpBwfGWwdHnheIV{KHSqZTDjfZRwfG:6aXPpeJkhd2ZiR1G= MUeyOFE2ODV7NR?=
HL-60  NVTpTWNoTnWwY4Tpc44hSXO|YYm= MVexNEDPxE1? M1TvVlAvPSCq NGj0eoRFVVOR MWXy[YR2[2W|IIDoc5NxcG:{eXzheIlwdiCxZjDDbIszyqB? M4q0T|I{QTN2NEGx
MCF-7 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M122VFEuOTByzszN M3PTSFI1KGh? NV\2SZhjTkKV NGPYPZhqdmirYnn0d{B1cGViY3XscEBxem:uaX\ldoF1cW:w NH33fWkzOzF6NUO0Oy=>
HeLa  NWewbIhOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{LBNVEuOTByzszN NXnjdnRlOjRiaB?= M1nZd2ZDWw>? NI\jWWVqdmirYnn0d{B1cGViY3XscEBxem:uaX\ldoF1cW:w NVHF[JA2OjNzOEWzOFc>
SH-SY5Y NWfD[o06TnWwY4Tpc44hSXO|YYm= NY\hSIlzOTEEoN88UeKh M1r3NlI1KGh? NEnJU3dqdmirYnn0d{BkdGmxcYXpco9tNWmwZIXj[YQheGixc4Doc5J6dGG2aX;uJI9nKHB3Mx?= MVSyNlYzPzJ7NB?=
IMR-32 MXXGeY5kfGmxbjDBd5NigQ>? MoPQNVDDqM7:TdMg MlrLNlQhcA>? MVfpcohq[mm2czDjcIlweXWrbn;sMYlv\HWlZXSgdIhwe3Cqb4L5cIF1cW:wIH;mJJA2Ow>? MmLYNlI3Ojd{OUS=
A549 NU\2OmI1TnWwY4Tpc44hSXO|YYm= MlSwNVDDqM7:TdMg MYGxJIg> NYDrR2Rne3WycILld5NmeyCQYX7vMWNwNWmwZIXj[YQheDV|IHHjZ5VufWyjdHnvci=> NXK3emVHOjJ3NUmzNlE>
T47D  NUHvbotrTnWwY4Tpc44hSXO|YYm= MnLCNlDDqG2P M13xW|I1KGh? NUfMc|JRTE2VTx?= MYPwdoV3\W62czDJVk1qdmS3Y3XkJIRm\3KjZHH0bY9vKG:oIFpOvmLPuQ>? MWmyNVE1PDhyNR?=
A29 MEF NEDzfHpHfW6ldHnvckBCe3OjeR?= MkWyNVDDqM7:TdMg M{\uZlFp MWricI9kc3QEoITo[UBxcG:|cHjvdplt[XSrb36gc4YhSWu2IHH0JHNmejR5M9Mg NWTGU3FiOjByNUO3PFE>
MDA-MB-453  NGjIXGpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX21MVQxKM7:TR?= MXO3NkBp NULvR4lkUUN3MDDv[kAyOCEQvF2= NIHyVpMzODB3M{e4NS=>
PC-3 NHfx[o5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYHhTVFVPS12MDFOwG0> NVXy[WdnPzJiaB?= NUHzdJdUUUN3MDDv[kAyOCEQvF2= MnPiNlAxPTN5OEG=

... 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
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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
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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