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
USD 70 In stock
USD 120 In stock
USD 370 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 MmnpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWXJR|UxRTNwMkezOVIh|ryP NGTzVmpUSU6JRWK=
HuO-3N1 M{HqUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGDIblhKSzVyPUSuNVcyPDJizszN Mo\2V2FPT0WU
LAMA-84 NGnOO3FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXPk[IdLUUN3ME20MlU5PDZ3IN88US=> MWDTRW5ITVJ?
CAL-72 M3vHTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NULUOGF{UUN3ME21MlQ5ODh2IN88US=> MX;TRW5ITVJ?
LoVo NEK2elhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnzQTWM2OD14LkmzNlM6KM7:TR?= NHS3dm5USU6JRWK=
HH NIXKW4NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGjOdG1KSzVyPUiuNlc3PzFizszN MXfTRW5ITVJ?
SK-MEL-3 NEfQOGpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV3wcndoUUN3ME24MlI5PTd3IN88US=> M{nVeXNCVkeHUh?=
KM12 MljtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUHJR|UxRTlwMkGxOFIh|ryP NIDkV3JUSU6JRWK=
NCI-H1437 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoHPTWM2OD17LkiwPVch|ryP MWHTRW5ITVJ?
NCI-H1838 MnTPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{LIbWlEPTB;MUGuNVg3PSEQvF2= MlrmV2FPT0WU
J-RT3-T3-5 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVvVZ5RjUUN3ME2xNU4zPDF5IN88US=> M1zYPXNCVkeHUh?=
GOTO NV;jdnFZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1KzZmlEPTB;MUGuOlk6PiEQvF2= M2ThU3NCVkeHUh?=
LB2241-RCC NGHsN4ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWPQe5ZFUUN3ME2xNU44OTh4IN88US=> M4PxWnNCVkeHUh?=
ES7 NH\MUoZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{S5U2lEPTB;MUGuO|g5KM7:TR?= NH\6blZUSU6JRWK=
KP-N-YS NEXBcpNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX7JR|UxRTF{Lk[zOVQh|ryP MWXTRW5ITVJ?
CAL-12T MoDlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWjJR|UxRTF|Lk[xO{DPxE1? MWXTRW5ITVJ?
COLO-684 MnjIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MonWTWM2OD1zND6xOVY6KM7:TR?= NEKwPZVUSU6JRWK=
DOK NF;FXXdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYTWbJByUUN3ME2xOU4{OzJ7IN88US=> MXvTRW5ITVJ?
Hs-578-T MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnrsTWM2OD1zNT60NVgzKM7:TR?= Ml;UV2FPT0WU
D-423MG M1G5Umdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXLJR|UxRTF3LkWyN|Yh|ryP M2jCW3NCVkeHUh?=
DBTRG-05MG M{LYPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHHzVG9KSzVyPUG1MlYyOTFizszN Mlq3V2FPT0WU
VM-CUB-1 M17RUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEO0c2tKSzVyPUG1Mlk5PDlizszN M3vGcXNCVkeHUh?=
KG-1 MnraS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGG5S|ZKSzVyPUG2MlA6QTZizszN MXfTRW5ITVJ?
8305C MlfhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXXJR|UxRTF4LkG4PFkh|ryP NHjqTnJUSU6JRWK=
HuH-7 NGXzOnZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkHGTWM2OD1zNj6yOlc1KM7:TR?= NEPOR5RUSU6JRWK=
LXF-289 M2\5Omdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYfJR|UxRTF4LkK3OFch|ryP NG[5[JlUSU6JRWK=
NCI-H1793 MmPLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEXLcZdKSzVyPUG2MlQ4OTJizszN NUDDXZpGW0GQR1XS
ChaGo-K-1 NEnD[JdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYTheJR3UUN3ME2xOk43PTZ6IN88US=> MYjTRW5ITVJ?
GCIY M2C3T2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIT1[nhKSzVyPUG2Mlc6ODVizszN MWTTRW5ITVJ?
SK-MEL-28 M2m5WWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{XrZ2lEPTB;MUeuNFQ4PSEQvF2= M4nYcXNCVkeHUh?=
NCI-SNU-1 MkTVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2noTmlEPTB;MUeuNVI3QSEQvF2= M1[zcnNCVkeHUh?=
CTB-1 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkDUTWM2OD1zNz6yNlU6KM7:TR?= NH:3TpJUSU6JRWK=
NCI-H82 M2TrZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUfPeY1MUUN3ME2xO{41PTd|IN88US=> MWjTRW5ITVJ?
HCC2998 NIj4cmtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYeydItQUUN3ME2xO{43PzN|IN88US=> NHzmZVJUSU6JRWK=
NCI-H2030 M2HwRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4DSXmlEPTB;MUiuNVk6PyEQvF2= MmixV2FPT0WU
HuP-T3 MlHrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoKyTWM2OD1zOD61PFg5KM7:TR?= MkLiV2FPT0WU
697 M3rsUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFHETlhKSzVyPUG5MlAzODFizszN NWe2OFFZW0GQR1XS
MLMA MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWXJR|UxRTF7LkC1OVch|ryP MnGyV2FPT0WU
HCC70 MoD5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX7JR|UxRTF7LkS4PUDPxE1? MlKwV2FPT0WU
A704 M1r1eWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlzLTWM2OD1zOT64N|A2KM7:TR?= M4TlVnNCVkeHUh?=
D-283MED MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlrxTWM2OD1{MD61N|M6KM7:TR?= M1rZR3NCVkeHUh?=
U031 MmjTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGXBPFZKSzVyPUKxMlE1QDlizszN MXrTRW5ITVJ?
HSC-3 M{X2emdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnjMTWM2OD1{MT6xPFM2KM7:TR?= NVnpbI9rW0GQR1XS
JVM-3 Mo\uS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX;3WlM1UUN3ME2yNk42ODZizszN MXrTRW5ITVJ?
Mewo Ml7lS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{foVWlEPTB;MkKuOVA4OyEQvF2= NYn2NldnW0GQR1XS
YH-13 MmHxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV2zeoppUUN3ME2yNk42OTJ|IN88US=> NGDHWlFUSU6JRWK=
LB1047-RCC MkDOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHXINGFKSzVyPUKyMlU5PzlizszN NY\MOIRSW0GQR1XS
HCC2157 NGT0PVFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmHTTWM2OD1{Mj64NFU1KM7:TR?= NWfQTldiW0GQR1XS
SNU-449 NInhOHpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MW\JR|UxRTJ{Lki3OFgh|ryP MXvTRW5ITVJ?
Ramos-2G6-4C10 NVXCU2R1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn7xTWM2OD1{Mj65OkDPxE1? MVfTRW5ITVJ?
CHL-1 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1jwZWlEPTB;MkOuO|I6OiEQvF2= NHznOodUSU6JRWK=
SK-MEL-30 M3TrfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1i1fGlEPTB;MkSuOFY3OiEQvF2= M3rTb3NCVkeHUh?=
PANC-08-13 Mlr3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFvRNWJKSzVyPUK1MlA6OzhizszN NULkbmRXW0GQR1XS
QIMR-WIL MmXxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mlq3TWM2OD1{NT6xPFU5KM7:TR?= Mm\pV2FPT0WU
BFTC-905 MnfrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXHJR|UxRTJ3LkW5OFQh|ryP MXnTRW5ITVJ?
GI-1 NX7acmxFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWHJR|UxRTJ3LkewOVUh|ryP M3PPUHNCVkeHUh?=
MDA-MB-415 NXfuOZF{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVSx[VZHUUN3ME2yOk42ODN|IN88US=> NXrUbZRVW0GQR1XS
GT3TKB M{\Kdmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmGxTWM2OD1{Nj61N|QzKM7:TR?= MlG2V2FPT0WU
DEL MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmTSTWM2OD1{Nj64N|U3KM7:TR?= NHLoc4lUSU6JRWK=
KOSC-2 NYrLfo1vT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIfkPHVKSzVyPUK2MlkxPzVizszN NXTrTpltW0GQR1XS
RVH-421 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1ztSmlEPTB;MkeuNlkzOSEQvF2= NFTJfW9USU6JRWK=
EW-13 NGfjNJpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1HkSWlEPTB;MkeuOFMxQCEQvF2= M1Gyd3NCVkeHUh?=
639-V MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXzqd29jUUN3ME2yO{42OTF7IN88US=> MmTzV2FPT0WU
A2780 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{CwXWlEPTB;MkeuOlQyKM7:TR?= NXG3NJBSW0GQR1XS
SW982 MoDaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmjITWM2OD1{Nz65NFUzKM7:TR?= M2r0SXNCVkeHUh?=
SW1710 NEX3ZWRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml\oTWM2OD1{OD6wPVgyKM7:TR?= NXLl[3NOW0GQR1XS
HCC1569 MlnWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3TWWGlEPTB;MkiuOFg6PyEQvF2= MorQV2FPT0WU
MV-4-11 M4fXZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGXaTZFKSzVyPUK4MlU4OzVizszN NUCwO5FiW0GQR1XS
BHT-101 NX\3[XNoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWrJR|UxRTJ6Lk[1O|Ih|ryP MWLTRW5ITVJ?
Ca9-22 M2XGT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVXJR|UxRTJ6LkexOEDPxE1? M2\YcHNCVkeHUh?=
HAL-01 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVzJR|UxRTJ6Lke2NVUh|ryP NX7iTlNWW0GQR1XS
D-263MG M2rh[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYTJR|UxRTJ7LkO0OEDPxE1? NFPxWmtUSU6JRWK=
NEC8 M331[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVfDclRuUUN3ME2yPU42PTR6IN88US=> M2q3VXNCVkeHUh?=
EKVX M1PvdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mni2TWM2OD1|MT61PFQ4KM7:TR?= NUDBTnF2W0GQR1XS
EM-2 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MW\JR|UxRTNzLk[zNFQh|ryP NYXic41kW0GQR1XS
MFM-223 M4H5Nmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkLtTWM2OD1|MT64NFk5KM7:TR?= MY\TRW5ITVJ?
SK-PN-DW MkD2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIfOepdKSzVyPUOyMlE1ODZizszN MmjNV2FPT0WU
HuO9 NGfJbJVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{XuOWlEPTB;M{KuOVI5OiEQvF2= M{HzbHNCVkeHUh?=
MHH-PREB-1 NFK1RVlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYjJSHgzUUN3ME2zNk43OjN2IN88US=> MkjJV2FPT0WU
OVCAR-4 NXXRbWpDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkXCTWM2OD1|Mj64N|Y{KM7:TR?= MkPaV2FPT0WU
NCI-H1648 NXy4OottT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3rYXmlEPTB;M{KuPFY2OSEQvF2= NG\U[FZUSU6JRWK=
MKN1 NFzoUYpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH3NcVdKSzVyPUO0MlEyODFizszN NIDDUGdUSU6JRWK=
KYSE-450 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn;FTWM2OD1|ND62OFQ1KM7:TR?= MUPTRW5ITVJ?
ES8 MmDiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVfJR|UxRTN2Lki5O|Uh|ryP MXLTRW5ITVJ?
MS-1 MkLGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1Hr[mlEPTB;M{SuPVU2PCEQvF2= M3LFfnNCVkeHUh?=
HOP-92 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF\zT4NKSzVyPUO1MlkzPzdizszN MX;TRW5ITVJ?
SKG-IIIa NVnSc5dGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUOzW3E3UUN3ME2zOk4zPTZzIN88US=> NHPZNZhUSU6JRWK=
TE-11 NFmzR3lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFnwZ4ZKSzVyPUO2MlUzPDNizszN MnX3V2FPT0WU
SK-NEP-1 NUPUbWg5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWG4T5JqUUN3ME2zO{43PzR2IN88US=> M1\WOHNCVkeHUh?=
DB NGrq[GlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF2zZodKSzVyPUO3MlkyQDVizszN NGrlbY5USU6JRWK=
IA-LM MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVTJR|UxRTN6LkCyN|kh|ryP MnuzV2FPT0WU
COLO-829 MmnqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVLrXWp{UUN3ME2zPE41OTV7IN88US=> NEDTOoFUSU6JRWK=
TGBC11TKB MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVn0cIJMUUN3ME2zPU4yPDB6IN88US=> NYjqNYVsW0GQR1XS
CAL-51 NYTDTZhPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWDmOmU6UUN3ME20NE4xPjF{IN88US=> NH[3fXFUSU6JRWK=
NCI-H2228 Mn\hS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWK2bHFZUUN3ME20NE4{PjZ{IN88US=> Mn60V2FPT0WU
C32 NUPqcJZYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGr1TW5KSzVyPUSwMlQxOjRizszN MnnQV2FPT0WU
KU-19-19 NUTHZ4pHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3TaT2lEPTB;NECuO|Y5OyEQvF2= M3[xVXNCVkeHUh?=
KNS-62 M2fHbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEjtTXlKSzVyPUSwMlg{QDFizszN NWC0clZrW0GQR1XS
FADU NFnD[lhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWewNZlWUUN3ME20NU4zPTB{IN88US=> MYnTRW5ITVJ?
CAL-33 NGDyemZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGXa[lVKSzVyPUSyMlY4PDlizszN MUTTRW5ITVJ?
CHP-134 M13sV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFjoTHJKSzVyPUSyMlg1QTZizszN MXjTRW5ITVJ?
HDLM-2 NXfKTWY1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH:5WoRKSzVyPUSyMlkxQDRizszN MlKzV2FPT0WU
NBsusSR MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFGzb4RKSzVyPUSzMlA4OjVizszN NFTTW2lUSU6JRWK=
SW954 MonGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEfDSHVKSzVyPUSzMlExPTNizszN MmfKV2FPT0WU
HCC1806 M2G1NGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4i2[WlEPTB;NEOuOFEyKM7:TR?= NF20Uo5USU6JRWK=
VMRC-RCZ M4TIT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFnFclNKSzVyPUSzMlQ2QDZizszN M{\sdXNCVkeHUh?=
A549 NXzpR|NNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4X1RWlEPTB;NEOuPVMyKM7:TR?= NGDpN4FUSU6JRWK=
NKM-1 Mmn2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF\VcZFKSzVyPUSzMlk2PThizszN NHr6eFhUSU6JRWK=
DMS-273 MofBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2L3bGlEPTB;NESuO|U3PyEQvF2= M{XZe3NCVkeHUh?=
TYK-nu MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFT5UIZKSzVyPUS1MlEzOzRizszN MUPTRW5ITVJ?
KALS-1 MonxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFPhe3ZKSzVyPUS1MlE1PiEQvF2= NFvPZ2xUSU6JRWK=
A101D MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXyxbm1NUUN3ME20OU41PDV4IN88US=> NX;yW4J5W0GQR1XS
G-361 NEjTV25Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFTqdHJKSzVyPUS2MlIyOzhizszN MVHTRW5ITVJ?
KARPAS-299 MnjIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml[1TWM2OD12Nj6zOVE3KM7:TR?= MkHOV2FPT0WU
RS4-11 NX3DXpBoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHPkeFdKSzVyPUS2MlU1OiEQvF2= NGG2WnBUSU6JRWK=
HT-1376 M1zFfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUL5S2NNUUN3ME20Ok44PDJ4IN88US=> M1zpRXNCVkeHUh?=
SK-N-AS NFzkUZZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoXkTWM2OD12Nj63PFIzKM7:TR?= M3nXV3NCVkeHUh?=
MG-63 NVy1UnV4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF6xPIhKSzVyPUS2MlkxOzZizszN NYjlfoRlW0GQR1XS
EPLC-272H NYDUdXNTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWnJR|UxRTR4Lkm1NFMh|ryP MoHPV2FPT0WU
BALL-1 NV74eolyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmLBTWM2OD12Nz64N|Ih|ryP NWPMVnVRW0GQR1XS
LCLC-97TM1 MoHGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3z2NWlEPTB;NEiuNlAzKM7:TR?= NXLN[XNyW0GQR1XS
HO-1-N-1 MojSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3\5UGlEPTB;NEiuPVY4PiEQvF2= MVjTRW5ITVJ?
MFE-280 M{nKSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGiyUppKSzVyPUS5MlQ3OTdizszN M4CyOnNCVkeHUh?=
NCI-H526 MnS3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1r3WWlEPTB;NEmuPFE3OyEQvF2= M1S5cnNCVkeHUh?=
D-566MG NIjjT2xIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWLXbHZSUUN3ME20PU46ODl4IN88US=> NFnOVZdUSU6JRWK=
BB30-HNC M4PsZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoHXTWM2OD12OT65OFk5KM7:TR?= MlrBV2FPT0WU
SK-N-DZ NXfsOYRoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXHYcXZuUUN3ME21NE4xPDhzIN88US=> MXLTRW5ITVJ?
HepG2  NF;EUWpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{LITVExyqEQvF2= Ml;oNlQhcA>? MYXicI9kc3NiU1OtTWlKOy2rbnT1Z4VlKFNicHjhd4Uh[XK{ZYP0 MkS5NlU2OjdzMkO=
HepG2  MUjGeY5kfGmxbjDBd5NigQ>? NEXYN|EyOMLizszN MYWyOEBp NVPTN2RFe3WycILld5NmeyC2aHWgdIhwe3Cqb4L5cIF1cW:wczDv[kBCXE1ib36gV4VzOTl6MTygR4hsOSCxbjDT[ZI{PDVuIFPob|Ihd25iVHjyOlgtKGGwZDDD[IszKG:wIGT5dlE2KGmwZIXj[YQh[nliU1OtTWlKOw>? MViyOVUzPzF{Mx?=
KATO III  NFzIbFlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml[5Nk42NzVxNz61JO69VQ>? NY\pbHZbTE2VTx?= MmnG[Y5p[W6lZYOgeIhmKHSxeHnjbZR6KG:oIH;sZZBiemmk NU\HWnk3OjR6NEG3NVg>
hTCEpi NXi3UZJJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVWxNEDPxE1? M1zZOGROW09? MorldJJmfmWwdIOgeIhmKGO7dH;wZZRpcWNiZX\m[YN1KG:oIFjTWk0y NFX3[GozPDN5MEizOS=>
MCF10A M2f1dWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIjtZVYyOCEQvF2= M13nZ|I1KGh? NUjXe3UzTE2VTx?= MWLwc5RmdnSrYYTld{B1cGViY4n0c5RwgGmlaYT5JI9nKEeD NUSzbVBsOjRzNUC1PVU>
HL-60  NEPaT45HfW6ldHnvckBCe3OjeR?= Mm\GNVAh|ryP NX[4cphJOC53IHi= MniwSG1UVw>? MVjy[YR2[2W|IIDoc5NxcG:{eXzheIlwdiCxZjDDbIszyqB? MYSyN|k{PDRzMR?=
MCF-7 MlHqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M370eFEuOTByzszN MWeyOEBp NVnpd4d6TkKV M2rlTYlvcGmkaYTzJJRp\SClZXzsJJBzd2yrZnXyZZRqd25? MUeyN|E5PTN2Nx?=
HeLa  MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MknCNU0yODEQvF2= NX;6OG9KOjRiaB?= MU\GRnM> NVLuO5l5cW6qaXLpeJMhfGinIHPlcIwheHKxbHnm[ZJifGmxbh?= M{HJW|I{OTh3M{S3
SH-SY5Y MVLGeY5kfGmxbjDBd5NigQ>? M2j3Z|ExyqEQvF5CpC=> NIO4UY4zPCCq NY\4UnUzcW6qaXLpeJMh[2yrb4H1bY5wdC2rbnT1Z4VlKHCqb4PwbI9zgWyjdHnvckBw\iCyNUO= NWixNIhJOjJ4MkeyPVQ>
IMR-32 M3;UUGZ2dmO2aX;uJGF{e2G7 MV6xNOKh|ryPwrC= Mn\sNlQhcA>? NU\vUnhlcW6qaXLpeJMh[2yrb4H1bY5wdC2rbnT1Z4VlKHCqb4PwbI9zgWyjdHnvckBw\iCyNUO= MmfWNlI3Ojd{OUS=
A549 MV3GeY5kfGmxbjDBd5NigQ>? NGXRW|QyOMLizszNxsA> NVHGOFFVOSCq MUTzeZBxemW|c3XzJG5idm9vQ3:tbY5lfWOnZDDwOVMh[WOldX31cIF1cW:w MWKyNlU2QTN{MR?=
T47D  NEPDc5lHfW6ldHnvckBCe3OjeR?= MWiyNOKhdU1? NIeyeIkzPCCq M{\3WmROW09? M4\LTpBz\X[nboTzJGlTNWmwZIXj[YQh\GWpcnHkZZRqd25ib3[gTe67Ss7z NV;Xbo1yOjFzNES4NFU>
A29 MEF Mnn6SpVv[3Srb36gRZN{[Xl? MYWxNOKh|ryPwrC= M1ntd|Fp NXLhWlNG[myxY3vzxsB1cGVicHjvd5Bpd3K7bHH0bY9vKG:oIFHreEBifCCVZYK0O|PDqA>? MWqyNFA2Ozd6MR?=
MDA-MB-453  NHPR[HJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3TGT|UuPDBizszN MXS3NkBp NY\Fd2hLUUN3MDDv[kAyOCEQvF2= NEnqRVQzODB3M{e4NS=>
PC-3 M4X4emdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVS1MVQxKM7:TR?= NXLHbnVjPzJiaB?= M3fhUWlEPTBib3[gNVAh|ryP NIDFXmwzODB3M{e4NS=>

... 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)
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

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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