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.

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In DMSO USD 112 In stock
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Cited by 41 Publications

5 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.

  • hTERT-RPE cells were synchronized in S-phase by single thymidine block and treated with HU +/- ATR (VE 821 (ATRi)) and ATM (KU-55933 (ATMi)) inhibitors alone (A) during the indicated time.

    Nucleic Acids Res, 2016, 44(10):4745-62. 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

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)
12.9 nM
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 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYToWGx1UUN3ME2zMlI4OzV{IN88US=> MkXGV2FPT0WU
HuO-3N1 M3\Bemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4\TXmlEPTB;ND6xO|E1OiEQvF2= Mn7GV2FPT0WU
LAMA-84 NW\2W4hTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXTJR|UxRTRwNUi0OlUh|ryP NVrJdGNyW0GQR1XS
CAL-72 Mk\GS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXvIVoxjUUN3ME21MlQ5ODh2IN88US=> Ml7PV2FPT0WU
LoVo MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3fKcGlEPTB;Nj65N|I{QSEQvF2= MoTaV2FPT0WU
HH NX7SWnFZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4DVTGlEPTB;OD6yO|Y4OSEQvF2= NXn4e5ZrW0GQR1XS
SK-MEL-3 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1\aOGlEPTB;OD6yPFU4PSEQvF2= NEfEfJBUSU6JRWK=
KM12 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV3JR|UxRTlwMkGxOFIh|ryP NIrCPI5USU6JRWK=
NCI-H1437 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVLJR|UxRTlwOEC5O{DPxE1? MXzTRW5ITVJ?
NCI-H1838 MonuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1fTTmlEPTB;MUGuNVg3PSEQvF2= NUTxU5pzW0GQR1XS
J-RT3-T3-5 M3jZeWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXfJR|UxRTFzLkK0NVch|ryP MUfTRW5ITVJ?
GOTO M{LVTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXnJR|UxRTFzLk[5PVYh|ryP NFixfVRUSU6JRWK=
LB2241-RCC MnHWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWTJR|UxRTFzLkexPFYh|ryP MXHTRW5ITVJ?
ES7 M2XwS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFTM[JNKSzVyPUGxMlc5QCEQvF2= NWHRS4VxW0GQR1XS
KP-N-YS M1nmT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVHVVlB6UUN3ME2xNk43OzV2IN88US=> M1v5V3NCVkeHUh?=
CAL-12T M4\uZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmLQTWM2OD1zMz62NVch|ryP NEDPfm5USU6JRWK=
COLO-684 NYe2b29YT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2L1R2lEPTB;MUSuNVU3QSEQvF2= M1y0UXNCVkeHUh?=
DOK NHrMU3FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1Hrd2lEPTB;MUWuN|MzQSEQvF2= M2PXfnNCVkeHUh?=
Hs-578-T M4Lhemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1;C[GlEPTB;MUWuOFE5OiEQvF2= MmHaV2FPT0WU
D-423MG MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYjJR|UxRTF3LkWyN|Yh|ryP NWeyUmJUW0GQR1XS
DBTRG-05MG NXqyNpo5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFzxOmdKSzVyPUG1MlYyOTFizszN NUfOcpVJW0GQR1XS
VM-CUB-1 MkfrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVnkbW9kUUN3ME2xOU46QDR7IN88US=> M3y2VHNCVkeHUh?=
KG-1 MnvPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2KxZmlEPTB;MU[uNFk6PiEQvF2= MYHTRW5ITVJ?
8305C MlywS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkTpTWM2OD1zNj6xPFg6KM7:TR?= Mm[1V2FPT0WU
HuH-7 NHLhNVVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWnJR|UxRTF4LkK2O|Qh|ryP NWD3do9FW0GQR1XS
LXF-289 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFnaN4tKSzVyPUG2MlI4PDdizszN NVjM[FFyW0GQR1XS
NCI-H1793 NGDDZWVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYPDd3dUUUN3ME2xOk41PzF{IN88US=> Mk\XV2FPT0WU
ChaGo-K-1 M{PLOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1LyeWlEPTB;MU[uOlU3QCEQvF2= MYXTRW5ITVJ?
GCIY Mn;sS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M13ydmlEPTB;MU[uO|kxPSEQvF2= MmLCV2FPT0WU
SK-MEL-28 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUTUXW43UUN3ME2xO{4xPDd3IN88US=> MXrTRW5ITVJ?
NCI-SNU-1 M3rjSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnrZTWM2OD1zNz6xNlY6KM7:TR?= NGO1XYNUSU6JRWK=
CTB-1 NYK0e4FpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4fVU2lEPTB;MUeuNlI2QSEQvF2= MnzUV2FPT0WU
NCI-H82 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVTJR|UxRTF5LkS1O|Mh|ryP NEnE[pdUSU6JRWK=
HCC2998 M4rzWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1\V[2lEPTB;MUeuOlc{OyEQvF2= NXHvUJE1W0GQR1XS
NCI-H2030 NUXSXYhFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUfKeHFxUUN3ME2xPE4yQTl5IN88US=> NUfDS5ZLW0GQR1XS
HuP-T3 NViyXnV2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoPmTWM2OD1zOD61PFg5KM7:TR?= NUP5e2MxW0GQR1XS
697 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnXaTWM2OD1zOT6wNlAyKM7:TR?= NWTESIM2W0GQR1XS
MLMA NH\abFZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYLJR|UxRTF7LkC1OVch|ryP NUPmdWJ7W0GQR1XS
HCC70 M{OzNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVXUcJF3UUN3ME2xPU41QDlizszN MljBV2FPT0WU
A704 NUDYbIZyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2DpUmlEPTB;MUmuPFMxPSEQvF2= NIPHb2tUSU6JRWK=
D-283MED NF3ZfWlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWfJR|UxRTJyLkWzN|kh|ryP NXvySmRRW0GQR1XS
U031 M2fzbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoDUTWM2OD1{MT6xOFg6KM7:TR?= NITTeGhUSU6JRWK=
HSC-3 NIjDOGhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3nsbGlEPTB;MkGuNVg{PSEQvF2= M13lZnNCVkeHUh?=
JVM-3 NX;5eVBiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUDucVBEUUN3ME2yNk42ODZizszN NWX5dldwW0GQR1XS
Mewo NVLD[pdTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn7OTWM2OD1{Mj61NFc{KM7:TR?= MlrIV2FPT0WU
YH-13 MkT6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2Dne2lEPTB;MkKuOVEzOyEQvF2= NHOwXlFUSU6JRWK=
LB1047-RCC M4HiTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX7IRZFKUUN3ME2yNk42QDd7IN88US=> NEjQNHRUSU6JRWK=
HCC2157 M4TlOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV\ueFFHUUN3ME2yNk45ODV2IN88US=> MXPTRW5ITVJ?
SNU-449 NFG5T5VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUnWTJRtUUN3ME2yNk45PzR6IN88US=> MVfTRW5ITVJ?
Ramos-2G6-4C10 NUH2TFV{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWrJR|UxRTJ{Lkm2JO69VQ>? NHrOWG1USU6JRWK=
CHL-1 M2P5O2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUjJR|UxRTJ|LkeyPVIh|ryP NX;nUZFCW0GQR1XS
SK-MEL-30 NX[2Unk3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGnjcJdKSzVyPUK0MlQ3PjJizszN M1PSU3NCVkeHUh?=
PANC-08-13 NGXHflRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVXJR|UxRTJ3LkC5N|gh|ryP M2LXSnNCVkeHUh?=
QIMR-WIL MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4T1d2lEPTB;MkWuNVg2QCEQvF2= M37xWHNCVkeHUh?=
BFTC-905 NEXCNlRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXTTfWpWUUN3ME2yOU42QTR2IN88US=> NITtVmZUSU6JRWK=
GI-1 NXnQSo13T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVmwWIptUUN3ME2yOU44ODV3IN88US=> NWTIPGNPW0GQR1XS
MDA-MB-415 NETqSI9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWXYTllCUUN3ME2yOk42ODN|IN88US=> Mn7mV2FPT0WU
GT3TKB NGPxOYxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX2wfYxNUUN3ME2yOk42OzR{IN88US=> NFK0dHBUSU6JRWK=
DEL NFTLZnFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnXaTWM2OD1{Nj64N|U3KM7:TR?= MV;TRW5ITVJ?
KOSC-2 NFHEZZlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVPOVGRGUUN3ME2yOk46ODd3IN88US=> MlnRV2FPT0WU
RVH-421 NF;T[ZpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYHJR|UxRTJ5LkK5NlEh|ryP M3XYWnNCVkeHUh?=
EW-13 M1:ybWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWq5dJlRUUN3ME2yO{41OzB6IN88US=> NW\uW2xwW0GQR1XS
639-V MmPKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVeyVlNxUUN3ME2yO{42OTF7IN88US=> M4Dab3NCVkeHUh?=
A2780 NWHmTpd1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV;JR|UxRTJ5Lk[0NUDPxE1? M4PxTXNCVkeHUh?=
SW982 NV;LO|BiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYHJR|UxRTJ5LkmwOVIh|ryP NF7zVYxUSU6JRWK=
SW1710 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFnPOmNKSzVyPUK4MlA6QDFizszN MXPTRW5ITVJ?
HCC1569 NV;DVWFVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MonITWM2OD1{OD60PFk4KM7:TR?= MlTHV2FPT0WU
MV-4-11 MoTUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlrrTWM2OD1{OD61O|M2KM7:TR?= MlOyV2FPT0WU
BHT-101 MlHxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHy3R4dKSzVyPUK4MlY2PzJizszN M4PPbnNCVkeHUh?=
Ca9-22 NHvZRo9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoLNTWM2OD1{OD63NVQh|ryP M37sVnNCVkeHUh?=
HAL-01 NYq1SHM1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{HYV2lEPTB;MkiuO|YyPSEQvF2= MVfTRW5ITVJ?
D-263MG MmDuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3TxcmlEPTB;MkmuN|Q1KM7:TR?= M4LXdXNCVkeHUh?=
NEC8 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUPJR|UxRTJ7LkW1OFgh|ryP MmDPV2FPT0WU
EKVX NHnqZ4JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFLjWXBKSzVyPUOxMlU5PDdizszN MnvMV2FPT0WU
EM-2 NVXZ[o92T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MljwTWM2OD1|MT62N|A1KM7:TR?= MnTzV2FPT0WU
MFM-223 MlHxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2O3e2lEPTB;M{GuPFA6QCEQvF2= MXrTRW5ITVJ?
SK-PN-DW MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVTJR|UxRTN{LkG0NFYh|ryP M2fXbXNCVkeHUh?=
HuO9 NVXKU24zT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIDzTFdKSzVyPUOyMlUzQDJizszN M{DGe3NCVkeHUh?=
MHH-PREB-1 NHTaTItIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXHLT2IyUUN3ME2zNk43OjN2IN88US=> MmP4V2FPT0WU
OVCAR-4 M3LNUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGLRcnZKSzVyPUOyMlg{PjNizszN M3TtRnNCVkeHUh?=
NCI-H1648 M2\1ZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFPX[41KSzVyPUOyMlg3PTFizszN NVPKNlJ3W0GQR1XS
MKN1 NYnyTFJuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV\U[41FUUN3ME2zOE4yOTBzIN88US=> NV3XOodJW0GQR1XS
KYSE-450 NUPZXo5mT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV\JR|UxRTN2Lk[0OFQh|ryP NXvtOW85W0GQR1XS
ES8 NVfnTZpTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlnMTWM2OD1|ND64PVc2KM7:TR?= M4P6eHNCVkeHUh?=
MS-1 NFTNWYJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlvGTWM2OD1|ND65OVU1KM7:TR?= MUDTRW5ITVJ?
HOP-92 NUDoN3RxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVfJR|UxRTN3LkmyO|ch|ryP MlfhV2FPT0WU
SKG-IIIa NYCxRXZlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmjZTWM2OD1|Nj6yOVYyKM7:TR?= M4jyS3NCVkeHUh?=
TE-11 M4\tbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXrJR|UxRTN4LkWyOFMh|ryP NXrBU5M6W0GQR1XS
SK-NEP-1 NXWxNHprT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mo\DTWM2OD1|Nz62O|Q1KM7:TR?= MkLGV2FPT0WU
DB Mk\3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFHVOmJKSzVyPUO3MlkyQDVizszN M{O1NHNCVkeHUh?=
IA-LM NFvmSFdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVnJR|UxRTN6LkCyN|kh|ryP NGTqVXBUSU6JRWK=
COLO-829 M{fXXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVjJR|UxRTN6LkSxOVkh|ryP MmDQV2FPT0WU
TGBC11TKB Mk\GS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmrOTWM2OD1|OT6xOFA5KM7:TR?= NEnobFdUSU6JRWK=
CAL-51 NILC[3pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NE[2dVhKSzVyPUSwMlA3OTJizszN MV;TRW5ITVJ?
NCI-H2228 NGLtXJpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFjSRlNKSzVyPUSwMlM3PjJizszN NYXvSpFxW0GQR1XS
C32 NGW2VIVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUjtb5FuUUN3ME20NE41ODJ2IN88US=> M{LacHNCVkeHUh?=
KU-19-19 MmK0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MY\JR|UxRTRyLke2PFMh|ryP NEfUPHhUSU6JRWK=
KNS-62 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXnp[HFMUUN3ME20NE45OzhzIN88US=> MnTVV2FPT0WU
FADU NXvSdo0{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYn3fJpvUUN3ME20NU4zPTB{IN88US=> MWfTRW5ITVJ?
CAL-33 NEH0bnRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEDXNm9KSzVyPUSyMlY4PDlizszN M1\BS3NCVkeHUh?=
CHP-134 MlHxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWfVVVhoUUN3ME20Nk45PDl4IN88US=> NUTqfoRPW0GQR1XS
HDLM-2 NFn1WoJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NY\KZpJQUUN3ME20Nk46ODh2IN88US=> NYG0SXB[W0GQR1XS
NBsusSR MoDvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWPJR|UxRTR|LkC3NlUh|ryP NH;1T5dUSU6JRWK=
SW954 M1rk[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH;UZmpKSzVyPUSzMlExPTNizszN MYfTRW5ITVJ?
HCC1806 M36xOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml\sTWM2OD12Mz60NVEh|ryP MWPTRW5ITVJ?
VMRC-RCZ NIjNSItIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWDJR|UxRTR|LkS1PFYh|ryP MXHTRW5ITVJ?
A549 M1nPT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVPJR|UxRTR|LkmzNUDPxE1? MULTRW5ITVJ?
NKM-1 NYK3PYl2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{[xcmlEPTB;NEOuPVU2QCEQvF2= MkTQV2FPT0WU
DMS-273 M2fRO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NETuXlBKSzVyPUS0Mlc2PjdizszN Mmf0V2FPT0WU
TYK-nu NYiyXopRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVjJR|UxRTR3LkGyN|Qh|ryP M1Hpc3NCVkeHUh?=
KALS-1 NIfJNFJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkjHTWM2OD12NT6xOFYh|ryP NHLHcnNUSU6JRWK=
A101D NVrmVmxIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3rkT2lEPTB;NEWuOFQ2PiEQvF2= Ml;SV2FPT0WU
G-361 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWnJR|UxRTR4LkKxN|gh|ryP NVrRemJDW0GQR1XS
KARPAS-299 M{m4c2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4HC[GlEPTB;NE[uN|UyPiEQvF2= NWTGdHZGW0GQR1XS
RS4-11 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHTpWlFKSzVyPUS2MlU1OiEQvF2= NVvPblRzW0GQR1XS
HT-1376 NYPUbIFCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mmr4TWM2OD12Nj63OFI3KM7:TR?= MkPQV2FPT0WU
SK-N-AS MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnnTTWM2OD12Nj63PFIzKM7:TR?= MXfTRW5ITVJ?
MG-63 MljuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn\OTWM2OD12Nj65NFM3KM7:TR?= M3nyd3NCVkeHUh?=
EPLC-272H MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXvJR|UxRTR4Lkm1NFMh|ryP MnzTV2FPT0WU
BALL-1 NGPTOY9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVfJR|UxRTR5LkizNkDPxE1? M4[4WHNCVkeHUh?=
LCLC-97TM1 MoXhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWDJR|UxRTR6LkKwNkDPxE1? NWfYSJhFW0GQR1XS
HO-1-N-1 NEjZS2tIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3TlcGlEPTB;NEiuPVY4PiEQvF2= MWDTRW5ITVJ?
MFE-280 NU\BeY9IT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFK5fG5KSzVyPUS5MlQ3OTdizszN NWToVY5LW0GQR1XS
NCI-H526 M{jIT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF7IeIhKSzVyPUS5MlgyPjNizszN MlLiV2FPT0WU
D-566MG NVTC[GpmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYXJR|UxRTR7LkmwPVYh|ryP MnG2V2FPT0WU
BB30-HNC NUnDNo5FT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkK5TWM2OD12OT65OFk5KM7:TR?= MUjTRW5ITVJ?
SK-N-DZ NV\EbZRmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYjJR|UxRTVyLkC0PFEh|ryP MU\TRW5ITVJ?
HepG2  M37VVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUjrbmdYOTEEoN88US=> MWCyOEBp MkHEZoxw[2u|IGPDMWlKUTNvaX7keYNm\CCVIIDoZZNmKGG{cnXzeC=> MmTVNlU2OjdzMkO=
HepG2  NF7hWZJHfW6ldHnvckBCe3OjeR?= M1vU[VExyqEQvF2= M3O1elI1KGh? MV3zeZBxemW|c3XzJJRp\SCyaH;zdIhwenmuYYTpc45{KG:oIFHUUUBwdiCVZYKxPVgyNCCFaHuxJI9vKFOnckO0OUwhS2itMjDvckBVcHJ4ODygZY5lKEOma{Kgc44hXHm{MUWgbY5lfWOnZDDifUBUSy2LSVmz NEPYNlkzPTV{N{GyNy=>
KATO III  NHnWUpNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX[yMlUwPS95LkWg{txO NHrpRotFVVOR M3TFbIVvcGGwY3XzJJRp\SC2b4jpZ4l1gSCxZjDvcIFx[XKrYh?= MlzCNlQ5PDF5MUi=
hTCEpi NGTpNVlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGq4dFMyOCEQvF2= NFrGbVJFVVOR MmfndJJmfmWwdIOgeIhmKGO7dH;wZZRpcWNiZX\m[YN1KG:oIFjTWk0y M3Sxb|I1OzdyOEO1
MCF10A MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWOxNEDPxE1? NFfRS4gzPCCq MXfEUXNQ NHPiRpFxd3SnboTpZZRmeyC2aHWgZ5l1d3SxeHnjbZR6KG:oIFfB MkHzNlQyPTB3OUW=
HL-60  MnnySpVv[3Srb36gRZN{[Xl? M17jflExKM7:TR?= Ml\qNE42KGh? NFzOe|FFVVOR NIDzTmlz\WS3Y3XzJJBpd3OyaH;yfYxifGmxbjDv[kBEcGt{wrC= Ml\WNlM6OzR2MUG=
MCF-7 M3HnVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFPQW44yNTFyMN88US=> NVv0fYE4OjRiaB?= MX;GRnM> Mn\SbY5pcWKrdIOgeIhmKGOnbHygdJJwdGmoZYLheIlwdg>? NHvOZlAzOzF6NUO0Oy=>
HeLa  MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmTLNU0yODEQvF2= MoCyNlQhcA>? M3TTZmZDWw>? Mon6bY5pcWKrdIOgeIhmKGOnbHygdJJwdGmoZYLheIlwdg>? M4\hNFI{OTh3M{S3
SH-SY5Y NFXPSnlHfW6ldHnvckBCe3OjeR?= NVHTOVdwOTEEoN88UeKh NGP5W|EzPCCq M3vGSolvcGmkaYTzJINtcW:zdXnuc4wucW6mdXPl[EBxcG:|cHjvdplt[XSrb36gc4YheDV| NYPSZXRkOjJ4MkeyPVQ>
IMR-32 MU\GeY5kfGmxbjDBd5NigQ>? NXPD[ohOOTEEoN88UeKh M4L3c|I1KGh? NEPHeXNqdmirYnn0d{BkdGmxcYXpco9tNWmwZIXj[YQheGixc4Doc5J6dGG2aX;uJI9nKHB3Mx?= M3LtSlIzPjJ5Mkm0
A549 M1\ESmZ2dmO2aX;uJGF{e2G7 NEXEUpIyOMLizszNxsA> MmXqNUBp MUDzeZBxemW|c3XzJG5idm9vQ3:tbY5lfWOnZDDwOVMh[WOldX31cIF1cW:w MnO0NlI2PTl|MkG=
T47D  NEjmb3dHfW6ldHnvckBCe3OjeR?= M3fvTVIxyqCvTR?= MoGyNlQhcA>? MYDEUXNQ NYe1Zo83eHKndnXueJMhUVJvaX7keYNm\CCmZXfyZYRifGmxbjDv[kBK|rqEzsG= NYnR[GdWOjFzNES4NFU>
A29 MEF NEnVOlZHfW6ldHnvckBCe3OjeR?= MVWxNOKh|ryPwrC= MVyxbC=> NFz3WW1jdG:la4RCpJRp\SCyaH;zdIhwenmuYYTpc44hd2ZiQXv0JIF1KFOnckS3N:Kh M13hUVIxODV|N{ix
MDA-MB-453  MmnNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M37nfVUuPDBizszN NYTmOpNZPzJiaB?= MXHJR|UxKG:oIEGwJO69VQ>? MV2yNFA2Ozd6MR?=
PC-3 NYPqd5ZQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYC1MVQxKM7:TR?= NFnmcIM4OiCq NWjJ[pN3UUN3MDDv[kAyOCEQvF2= MkPCNlAxPTN5OEG=

... 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]

+ Expand
  • 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)
Animal Research:

[3]

+ Expand
  • Animal Models: BALB/c nu/nu nude mice bearing LU1205 cells
  • Formulation: --
  • Dosages: 10 μM
  • Administration: --
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 33 mg/mL (83.44 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
5% DMSO and 47.5% PEG300
For best results, use promptly after mixing.
10 mg/mL

* 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

Bio Calculators

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Tech Support

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.

Handling Instructions

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ATM/ATR Signaling Pathway Map

ATM/ATR Inhibitors with Unique Features

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID