KU-55933 (ATM Kinase Inhibitor)

For research use only. Not for use in humans.

Catalog No.S1092

148 publications

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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Selleck's KU-55933 (ATM Kinase Inhibitor) has been cited by 148 publications

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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 MlT4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIPtZYdKSzVyPUOuNlc{PTJizszN NE[1Z|FUSU6JRWK=
HuO-3N1 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV3MSmRWUUN3ME20MlE4OTR{IN88US=> NFHUVoJUSU6JRWK=
LAMA-84 NI\ZT5ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NID4dHlKSzVyPUSuOVg1PjVizszN MXjTRW5ITVJ?
CAL-72 MoXQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoLRTWM2OD13LkS4NFg1KM7:TR?= M13weXNCVkeHUh?=
LoVo NGfQTYxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH2zfI1KSzVyPU[uPVMzOzlizszN MYPTRW5ITVJ?
HH M2fJZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NETQTo9KSzVyPUiuNlc3PzFizszN NWi5ZVkyW0GQR1XS
SK-MEL-3 NUfhPYZKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUnJR|UxRThwMki1O|Uh|ryP NH;zOXVUSU6JRWK=
KM12 NVvyWZRET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3P3d2lEPTB;OT6yNVE1OiEQvF2= M{G0bnNCVkeHUh?=
NCI-H1437 MkDxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXfJR|UxRTlwOEC5O{DPxE1? NXHyPI12W0GQR1XS
NCI-H1838 NFm5NppIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHjweJFKSzVyPUGxMlE5PjVizszN NHH1d2dUSU6JRWK=
J-RT3-T3-5 M4rIWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV7CN5RXUUN3ME2xNU4zPDF5IN88US=> MnjuV2FPT0WU
GOTO M4m0PWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1rq[2lEPTB;MUGuOlk6PiEQvF2= Mo\3V2FPT0WU
LB2241-RCC MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{nGXWlEPTB;MUGuO|E5PiEQvF2= MnvzV2FPT0WU
ES7 Ml;kS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV;FOXE4UUN3ME2xNU44QDhizszN NHH3NGJUSU6JRWK=
KP-N-YS MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlPYTWM2OD1zMj62N|U1KM7:TR?= M3TEVnNCVkeHUh?=
CAL-12T M1:4Nmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn7uTWM2OD1zMz62NVch|ryP NED5[4pUSU6JRWK=
COLO-684 NF:0e41Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYPJR|UxRTF2LkG1Olkh|ryP NGnhVIJUSU6JRWK=
DOK M3rDbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHzHdGtKSzVyPUG1MlM{OjlizszN NEG3VmhUSU6JRWK=
Hs-578-T NXXkOnNjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFznRmtKSzVyPUG1MlQyQDJizszN NIHUTmJUSU6JRWK=
D-423MG NX2wVHVoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFHmWIlKSzVyPUG1MlUzOzZizszN NWf4NYFjW0GQR1XS
DBTRG-05MG MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGHhS|hKSzVyPUG1MlYyOTFizszN M160XnNCVkeHUh?=
VM-CUB-1 NGfDNnlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFXUblVKSzVyPUG1Mlk5PDlizszN MVnTRW5ITVJ?
KG-1 NUTtXIhvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{DrZ2lEPTB;MU[uNFk6PiEQvF2= M{nR[HNCVkeHUh?=
8305C NUSyXXI3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF;XS3VKSzVyPUG2MlE5QDlizszN M1fLWHNCVkeHUh?=
HuH-7 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYPWTHVoUUN3ME2xOk4zPjd2IN88US=> NGPiPXRUSU6JRWK=
LXF-289 MlnjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnuxTWM2OD1zNj6yO|Q4KM7:TR?= MYXTRW5ITVJ?
NCI-H1793 M1;sZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXzzWZVSUUN3ME2xOk41PzF{IN88US=> MYXTRW5ITVJ?
ChaGo-K-1 M4ezSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1W4WGlEPTB;MU[uOlU3QCEQvF2= M1\4OHNCVkeHUh?=
GCIY Mmq0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoTjTWM2OD1zNj63PVA2KM7:TR?= NVflU2RIW0GQR1XS
SK-MEL-28 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH;VdVhKSzVyPUG3MlA1PzVizszN MkLCV2FPT0WU
NCI-SNU-1 M1jYS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2PyeGlEPTB;MUeuNVI3QSEQvF2= NULkV2VyW0GQR1XS
CTB-1 MlP5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmS0TWM2OD1zNz6yNlU6KM7:TR?= NIjNPHFUSU6JRWK=
NCI-H82 NUjSfXBCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4rCSmlEPTB;MUeuOFU4OyEQvF2= M{XReHNCVkeHUh?=
HCC2998 NVTqOWk3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUDze4VpUUN3ME2xO{43PzN|IN88US=> MnnsV2FPT0WU
NCI-H2030 NXXifmNFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWWzUWpWUUN3ME2xPE4yQTl5IN88US=> M1T2RXNCVkeHUh?=
HuP-T3 NYLmbpBET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHHKOGtKSzVyPUG4MlU5QDhizszN NUDkS3c2W0GQR1XS
697 M3TEfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlTxTWM2OD1zOT6wNlAyKM7:TR?= NF3PRVRUSU6JRWK=
MLMA M1qzWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MljsTWM2OD1zOT6wOVU4KM7:TR?= NIK4SHpUSU6JRWK=
HCC70 NXPUPZY5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGjpZoNKSzVyPUG5MlQ5QSEQvF2= MXfTRW5ITVJ?
A704 NFjXPFhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHLIOVZKSzVyPUG5Mlg{ODVizszN MYnTRW5ITVJ?
D-283MED MkLFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYHMcpFGUUN3ME2yNE42OzN7IN88US=> NXTC[GhKW0GQR1XS
U031 M2j6T2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXrJR|UxRTJzLkG0PFkh|ryP M2jE[HNCVkeHUh?=
HSC-3 NIqzeYFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYTifY1uUUN3ME2yNU4yQDN3IN88US=> MYLTRW5ITVJ?
JVM-3 MnLyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFH3[WFKSzVyPUKyMlUxPiEQvF2= M1PQNHNCVkeHUh?=
Mewo MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVPw[WkyUUN3ME2yNk42ODd|IN88US=> NELOdJJUSU6JRWK=
YH-13 NEPlcVhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1q1XGlEPTB;MkKuOVEzOyEQvF2= NX3lOVgzW0GQR1XS
LB1047-RCC NFnyfo9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkjITWM2OD1{Mj61PFc6KM7:TR?= NHeweXNUSU6JRWK=
HCC2157 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlnlTWM2OD1{Mj64NFU1KM7:TR?= MV3TRW5ITVJ?
SNU-449 MnTzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NG\WWpNKSzVyPUKyMlg4PDhizszN NVnmWJd4W0GQR1XS
Ramos-2G6-4C10 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4\5bGlEPTB;MkKuPVYh|ryP MWLTRW5ITVJ?
CHL-1 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF3TRo1KSzVyPUKzMlczQTJizszN NWrjSY5OW0GQR1XS
SK-MEL-30 M3\4emdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYjJR|UxRTJ2LkS2OlIh|ryP NIjMSHZUSU6JRWK=
PANC-08-13 NGnlUlNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnvYTWM2OD1{NT6wPVM5KM7:TR?= MX;TRW5ITVJ?
QIMR-WIL NF3rb|RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF;zVVdKSzVyPUK1MlE5PThizszN NVHIXoxRW0GQR1XS
BFTC-905 M1r2R2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVPJR|UxRTJ3LkW5OFQh|ryP NFOwVGdUSU6JRWK=
GI-1 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{Tu[WlEPTB;MkWuO|A2PSEQvF2= M2K4dHNCVkeHUh?=
MDA-MB-415 M4DzW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmPBTWM2OD1{Nj61NFM{KM7:TR?= MXzTRW5ITVJ?
GT3TKB MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHHQOI1KSzVyPUK2MlU{PDJizszN NWLmTmxPW0GQR1XS
DEL NX;rbXZzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3\HSmlEPTB;Mk[uPFM2PiEQvF2= MUHTRW5ITVJ?
KOSC-2 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NI\LXWZKSzVyPUK2MlkxPzVizszN MoDoV2FPT0WU
RVH-421 M3\ZNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4TU[2lEPTB;MkeuNlkzOSEQvF2= MnXmV2FPT0WU
EW-13 NUL3TnRQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYTJR|UxRTJ5LkSzNFgh|ryP NWX5[4xlW0GQR1XS
639-V Ml\YS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2Pj[2lEPTB;MkeuOVEyQSEQvF2= M4jzZ3NCVkeHUh?=
A2780 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnHxTWM2OD1{Nz62OFEh|ryP M33jZnNCVkeHUh?=
SW982 NGHzPGpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NInGXIdKSzVyPUK3MlkxPTJizszN Mn\OV2FPT0WU
SW1710 Mny1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVXJR|UxRTJ6LkC5PFEh|ryP M3\3cnNCVkeHUh?=
HCC1569 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYPJR|UxRTJ6LkS4PVch|ryP NIPFc|hUSU6JRWK=
MV-4-11 MknGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NY\QdphRUUN3ME2yPE42PzN3IN88US=> MXzTRW5ITVJ?
BHT-101 M3;RVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVjJR|UxRTJ6Lk[1O|Ih|ryP MnvSV2FPT0WU
Ca9-22 MmnwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUXJR|UxRTJ6LkexOEDPxE1? M4Ta[XNCVkeHUh?=
HAL-01 M4\DeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVrqSYhjUUN3ME2yPE44PjF3IN88US=> NITjPG5USU6JRWK=
D-263MG NWPRPGtTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX;JR|UxRTJ7LkO0OEDPxE1? MmHxV2FPT0WU
NEC8 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mmi3TWM2OD1{OT61OVQ5KM7:TR?= MlH6V2FPT0WU
EKVX NF\ONnhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{nkZ2lEPTB;M{GuOVg1PyEQvF2= NULtdYw5W0GQR1XS
EM-2 Mon6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYfSRWRpUUN3ME2zNU43OzB2IN88US=> Mk\GV2FPT0WU
MFM-223 MnfhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1\UcWlEPTB;M{GuPFA6QCEQvF2= NHHtc3VUSU6JRWK=
SK-PN-DW NVjwdGxDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NILLWGFKSzVyPUOyMlE1ODZizszN NVzsVlZZW0GQR1XS
HuO9 Mk\oS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M17CXGlEPTB;M{KuOVI5OiEQvF2= MX\TRW5ITVJ?
MHH-PREB-1 M1nPeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXvJR|UxRTN{Lk[yN|Qh|ryP NWLVT4JSW0GQR1XS
OVCAR-4 M{TYSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlXFTWM2OD1|Mj64N|Y{KM7:TR?= MlH2V2FPT0WU
NCI-H1648 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3zCTWlEPTB;M{KuPFY2OSEQvF2= M4nvd3NCVkeHUh?=
MKN1 M1zwUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn7zTWM2OD1|ND6xNVAyKM7:TR?= NFXLTHJUSU6JRWK=
KYSE-450 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml3TTWM2OD1|ND62OFQ1KM7:TR?= MWPTRW5ITVJ?
ES8 M2HBeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2TadGlEPTB;M{SuPFk4PSEQvF2= MVnTRW5ITVJ?
MS-1 NUC4WXBHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFXUWYRKSzVyPUO0Mlk2PTRizszN NI\1PGdUSU6JRWK=
HOP-92 MmDVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUPYfmZCUUN3ME2zOU46Ojd5IN88US=> M{Pwe3NCVkeHUh?=
SKG-IIIa MkPvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4rpcWlEPTB;M{[uNlU3OSEQvF2= NEXGPWRUSU6JRWK=
TE-11 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3jNSGlEPTB;M{[uOVI1OyEQvF2= MVLTRW5ITVJ?
SK-NEP-1 NFjYT3lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF7uenRKSzVyPUO3MlY4PDRizszN NIn4eVRUSU6JRWK=
DB MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX\JR|UxRTN5LkmxPFUh|ryP MnLZV2FPT0WU
IA-LM MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NY\GXpZFUUN3ME2zPE4xOjN7IN88US=> NWjKZWk4W0GQR1XS
COLO-829 NXf1NnFMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUTMTYxiUUN3ME2zPE41OTV7IN88US=> NUn1b|k5W0GQR1XS
TGBC11TKB MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnnvTWM2OD1|OT6xOFA5KM7:TR?= MmK0V2FPT0WU
CAL-51 M3zWbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHH3VnhKSzVyPUSwMlA3OTJizszN M1r0OnNCVkeHUh?=
NCI-H2228 MofRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX3JR|UxRTRyLkO2OlIh|ryP MkHnV2FPT0WU
C32 MnLvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV;1UmFXUUN3ME20NE41ODJ2IN88US=> MmOyV2FPT0WU
KU-19-19 M4fpNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M325UmlEPTB;NECuO|Y5OyEQvF2= NHnkO25USU6JRWK=
KNS-62 NUjKWmlnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUTJR|UxRTRyLkizPFEh|ryP MojmV2FPT0WU
FADU MnvwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVzoZ4F{UUN3ME20NU4zPTB{IN88US=> MYjTRW5ITVJ?
CAL-33 MlLsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVTseVh5UUN3ME20Nk43PzR7IN88US=> Mn\5V2FPT0WU
CHP-134 NFPq[HFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mmr5TWM2OD12Mj64OFk3KM7:TR?= NWmwSHp2W0GQR1XS
HDLM-2 NVjmfoRxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH:zPG9KSzVyPUSyMlkxQDRizszN M1vxR3NCVkeHUh?=
NBsusSR NWqwWpNsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXXJR|UxRTR|LkC3NlUh|ryP NVXSRoZDW0GQR1XS
SW954 NYrYV5BuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2j1d2lEPTB;NEOuNVA2OyEQvF2= MlrRV2FPT0WU
HCC1806 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHm3N4NKSzVyPUSzMlQyOSEQvF2= M4LBdHNCVkeHUh?=
VMRC-RCZ Mlq4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoHhTWM2OD12Mz60OVg3KM7:TR?= Mlv4V2FPT0WU
A549 M2fSOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmLkTWM2OD12Mz65N|Eh|ryP M3jEfXNCVkeHUh?=
NKM-1 NYjPbZJ3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2rzfGlEPTB;NEOuPVU2QCEQvF2= NIPYUpRUSU6JRWK=
DMS-273 NEPBclFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NY\RU41MUUN3ME20OE44PTZ5IN88US=> M1\rbnNCVkeHUh?=
TYK-nu NXWyUnJNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M37XbmlEPTB;NEWuNVI{PCEQvF2= MX3TRW5ITVJ?
KALS-1 M4e1WGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEm0TWpKSzVyPUS1MlE1PiEQvF2= M1jwZXNCVkeHUh?=
A101D NYLtUmZWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFzzWXNKSzVyPUS1MlQ1PTZizszN M3i4ZnNCVkeHUh?=
G-361 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mmm2TWM2OD12Nj6yNVM5KM7:TR?= NILlS4pUSU6JRWK=
KARPAS-299 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoCzTWM2OD12Nj6zOVE3KM7:TR?= NYnzVI5[W0GQR1XS
RS4-11 M1vUdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHf2Z3pKSzVyPUS2MlU1OiEQvF2= NWDLNottW0GQR1XS
HT-1376 NGSzdVVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWTkT|VbUUN3ME20Ok44PDJ4IN88US=> M3nDXHNCVkeHUh?=
SK-N-AS MnOwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXHJR|UxRTR4Lke4NlIh|ryP NHLUTIVUSU6JRWK=
MG-63 M{DjUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWP4S25oUUN3ME20Ok46ODN4IN88US=> NGK0dGdUSU6JRWK=
EPLC-272H MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3iyR2lEPTB;NE[uPVUxOyEQvF2= NYHr[FdNW0GQR1XS
BALL-1 NVjZNnQxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXPGN49iUUN3ME20O{45OzJizszN NGrnNVhUSU6JRWK=
LCLC-97TM1 M2iyPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoHZTWM2OD12OD6yNFIh|ryP NFrvZm1USU6JRWK=
HO-1-N-1 MmXMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYTJR|UxRTR6Lkm2O|Yh|ryP NEL0eW9USU6JRWK=
MFE-280 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NInncFlKSzVyPUS5MlQ3OTdizszN MW\TRW5ITVJ?
NCI-H526 MlzrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVnSZmdMUUN3ME20PU45OTZ|IN88US=> MXfTRW5ITVJ?
D-566MG Mly4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGrZ[o9KSzVyPUS5MlkxQTZizszN MXPTRW5ITVJ?
BB30-HNC NEfPfG9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MofLTWM2OD12OT65OFk5KM7:TR?= NYfTO2dxW0GQR1XS
SK-N-DZ MnnUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFLiO21KSzVyPUWwMlA1QDFizszN NYHRSoY5W0GQR1XS
HepG2  Mn3vS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVvDWHh4OTEEoN88US=> M3q1NlI1KGh? NITXdGVjdG:la4OgV2MuUUmLMz3pcoR2[2WmIGOgdIhie2ViYYLy[ZN1 M1nTPVI2PTJ5MUKz
HepG2  MlzySpVv[3Srb36gRZN{[Xl? Mn;3NVDDqM7:TR?= MlKwNlQhcA>? NYLpTZB6e3WycILld5NmeyC2aHWgdIhwe3Cqb4L5cIF1cW:wczDv[kBCXE1ib36gV4VzOTl6MTygR4hsOSCxbjDT[ZI{PDVuIFPob|Ihd25iVHjyOlgtKGGwZDDD[IszKG:wIGT5dlE2KGmwZIXj[YQh[nliU1OtTWlKOw>? NUK4bnRwOjV3MkexNlM>
KATO III  NVHDXWVvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVzx[FVTOi53L{WvO{42KM7:TR?= M13wfmROW09? MlS0[Y5p[W6lZYOgeIhmKHSxeHnjbZR6KG:oIH;sZZBiemmk NGTId2gzPDh2MUexPC=>
hTCEpi NXHaUmZ4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoXlNVAh|ryP NF7wb2hFVVOR M2[zRpBz\X[nboTzJJRp\SCleYTvdIF1cGmlIHXm[oVkfCCxZjDIV3YuOQ>? M3\S[FI1OzdyOEO1
MCF10A M4C0e2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYjWeXlnOTBizszN MlXaNlQhcA>? NYS4ZXcyTE2VTx?= MlnmdI91\W62aXH0[ZMhfGinIHP5eI91d3irY3n0fUBw\iCJQR?= MU[yOFE2ODV7NR?=
HL-60  M3fSOmZ2dmO2aX;uJGF{e2G7 M2\k[lExKM7:TR?= NHmxN3IxNjViaB?= NVnNUIRrTE2VTx?= MYry[YR2[2W|IIDoc5NxcG:{eXzheIlwdiCxZjDDbIszyqB? MofGNlM6OzR2MUG=
MCF-7 NGLWfYhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXOxMVExOM7:TR?= NFXURYEzPCCq NFmyOIlHSlN? M4PJO4lvcGmkaYTzJJRp\SClZXzsJJBzd2yrZnXyZZRqd25? M{K2VFI{OTh3M{S3
HeLa  NVvv[VlYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIPsTYcyNTFyMN88US=> NEHu[oczPCCq NFLUZZVHSlN? NHfrcWxqdmirYnn0d{B1cGViY3XscEBxem:uaX\ldoF1cW:w MYOyN|E5PTN2Nx?=
SH-SY5Y MVzGeY5kfGmxbjDBd5NigQ>? NXPqSph2OTEEoN88UeKh MVmyOEBp Mlm1bY5pcWKrdIOgZ4xqd3G3aX7vcE1qdmS3Y3XkJJBpd3OyaH;yfYxifGmxbjDv[kBxPTN? NXzrbY9qOjJ4MkeyPVQ>
IMR-32 M3HIS2Z2dmO2aX;uJGF{e2G7 Mn;BNVDDqM7:TdMg NUnCcmdCOjRiaB?= M3LhfolvcGmkaYTzJINtcW:zdXnuc4wucW6mdXPl[EBxcG:|cHjvdplt[XSrb36gc4YheDV| NXqxNFNDOjJ4MkeyPVQ>
A549 NEfLNJFHfW6ldHnvckBCe3OjeR?= NFXNb5UyOMLizszNxsA> NYDkXIVnOSCq MlXzd5VxeHKnc4Pld{BP[W6xLVPvMYlv\HWlZXSgdFU{KGGlY4XteYxifGmxbh?= MXGyNlU2QTN{MR?=
T47D  NFHpTo5HfW6ldHnvckBCe3OjeR?= NHzXVIQzOMLibV2= MXyyOEBp Moi1SG1UVw>? Ml\hdJJmfmWwdIOgTXIucW6mdXPl[EBl\We{YXTheIlwdiCxZjDJ{tpD|rF? NWr5ZWdVOjFzNES4NFU>
A29 MEF NXPYT405TnWwY4Tpc44hSXO|YYm= MX6xNOKh|ryPwrC= MVmxbC=> NYnHSFVW[myxY3vzxsB1cGVicHjvd5Bpd3K7bHH0bY9vKG:oIFHreEBifCCVZYK0O|PDqA>? MoLxNlAxPTN5OEG=
MDA-MB-453  MoHjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUG1MVQxKM7:TR?= MnjYO|IhcA>? NHrkdohKSzVyIH;mJFExKM7:TR?= MXuyNFA2Ozd6MR?=
PC-3 NHHWdodIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NE\hOlE2NTRyIN88US=> MmHZO|IhcA>? MVPJR|UxKG:oIEGwJO69VQ>? NWfWcWNVOjByNUO3PFE>

... Click to View More Cell Line Experimental Data
Assay
Methods Test Index PMID
Western blot
p-AKT(Ser473) / p-AKT(Thr308); 

PubMed: 22739265     


Cells were serum-starved for 6 h and treated with KU-55933 (10 µmol/L) for 1 h before treatment with insulin (100 nmol/L) for 45 min. Cells were lysed, and cell lysates were subjected to SDS-PAGE and Western blotting for the detection of phospho-Akt at Se䲧疝Ỵ疞㧀疜膉痘 瘿�෋ᾰƌ෋à 㺣痖

PARP / Cleaved PARP / Caspase-3 / Cleaved caspase-3 ; 

PubMed: 22739265     


ATM inhibition by KU-55933 induces apoptosis in differentiated but not undifferentiated SH-SY5Y cells. Cells were starved for 6 h in serum-free medium. KU-55933 (10 µmol/L) was added 1 h before insulin (100 nmol/L) treatment. After 3 h of insulin stimulat䲧疝Ỵ疞㧀疜膉痘 瘿�෋ᾰƌ෋à 㺣痖帉痖Ѐ瑖堘𢡄빢᎒෋à鑸᎒彿堙奋堙巫堙᎒ﻺ᎒彿堙ﻮ᎒塚堙ﻺ᎒ꍈ堞빢᎒學堙漸堞圔堙빢᎒圞堙圭堙𢡄玚Wᾰƌ ᾰƌ戤

ATM-S1981 / ATM / p-p53(S15) / p53 ; 

PubMed: 20639198     


Antioxidant and ATM inhibitors blocked phosphorylation of ATM-S1981, Akt-S473, and p53-S15 as stimulated by H2O2 exposure. Cells were treated with 100 μm H2O2 for 30 min in the absence or presence of KU-55933. Whole cell lysates were subjected to Western 䲧疝Ỵ疞㧀疜膉痘 瘿뾠ՂᾰƌՂĀ 㺣痖

p21 / p27 / p53 ; 

PubMed: 20177072     


HMGE cells were incubated for the indicated times with 1 μm KU-55933 or DMSO. Total protein extracts were analyzed by Western blotting for p21WAF1/CIP1, p27KIP1, p53, or β-actin.

22739265 20639198 20177072
Immunofluorescence
p-S824 KAP1 / ZEBRA ; 

PubMed: 28249048     


HH514-16 cells were treated with NaB (upper panel) or NaB plus KU-55933 (1μM; middle panel) or NaB plus Torin1 (0.5μM; lower panel) for 24 hours and stained with anti-phospho KAP1 (S824) plus anti-ZEBRA antibodies and visualized at 1000X magnification.

28249048
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]
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  • 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+40%PEG300+5%Tween80+50%ddH2O
For best results, use promptly after mixing. 		3.95 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
Smiles O=C1C=C(OC(=C1)C2=CC=CC3=C2SC4=CC=CC=C4S3)N5CCOCC5

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ATM/ATR Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID