KU-55933

別名：ATM Kinase Inhibitor

製品コード：S1092 純度：99.95%

KU-55933 is a potent and specific ATM inhibitor with IC50/K_i 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. KU‑55933 (ATM Kinase Inhibitor) inhibits the activation of autophagy‑initiating kinase ULK1 and results in a significant decrease of autophagy.

CAS No. 587871-26-9

サイズ	価格(税別)	在庫状況
10mM (1mL in DMSO)	JPY 29500	国内在庫あり
5mg	JPY 22000	国内在庫あり
10mg	JPY 37000	国内在庫あり
50mg	JPY 104500	国内在庫あり
200mg	JPY 190500	国内在庫あり
1g	JPY 418500	国内在庫なし(納期7~10日)

代表番号: 045-509-1970\|電子メール：[email protected] よく尋ねられる質問

文献中Selleckの製品使用例（375）

製品安全説明書

現在のバッチを見る：純度： 99.95%

99.95

KU-55933関連製品

関連ターゲット	ATM ATR	もっと見る
関連製品	VE-821 KU-60019 Berzosertib (VE-822) Ceralasertib (AZD6738) AZ20 AZD0156 Mirin AZD1390 CP-466722 Elimusertib (BAY-1895344) hydrochloride ETP-46464 Elimusertib (BAY-1895344) CGK 733 VX-803 (M4344) AZ31 AZ32 HAMNO	もっと見る
関連化合物ライブラリー	FDA-approved Drug Library Natural Product Library Apoptosis Compound Library DNA Damage/DNA Repair compound Library Cell Cycle compound library	もっと見る

シグナル伝達経路

ATM/ATRシグナル伝達経路

ATM/ATR阻害剤の選択性比較

Cell Data

Cell Lines	Assay Type	Concentration	Incubation Time	活性情報	PMID
HepG2	Growth Inhibition Assay	10 μM	24 h	blocks SC-III3-induced S phase arrest	25527123
HepG2	Function Assay	10 μM	24 h	suppresses the phosphorylations of ATM on Ser1981, Chk1 on Ser345, Chk2 on Thr68, and Cdk2 on Tyr15 induced by SC-III3	25527123
MCF10A	Growth Inhibition Assay	10 μM	24 h	potentiates the cytotoxicity of GA	24150595
HL-60	Function Assay	10 μM	0.5 h	reduces phosphorylation of Chk2	23934411
MCF-7	Growth Inhibition Assay	1-100μM	24 h	inhibits the cell proliferation	23185347
HeLa	Growth Inhibition Assay	1-100μM	24 h	inhibits the cell proliferation	23185347
SH-SY5Y	Function Assay	10 μM	24 h	inhibits clioquinol-induced phosphorylation of p53	22627294
IMR-32	Function Assay	10 μM	24 h	inhibits clioquinol-induced phosphorylation of p53	22627294
A549	Function Assay	10 μM	1 h	suppresses Nano-Co-induced p53 accumulation	22559321
T47D	Function Assay	20 mM	24 h	prevents IR-induced degradation of IκBα	21144805
A29 MEF	Function Assay	10 μM	1h	blocks the phosphorylation of Akt at Ser473	20053781
MDA-MB-453	Growth Inhibition Assay	5-40 μM	72 h	IC50 of 10 μM	20053781
PC-3	Growth Inhibition Assay	5-40 μM	72 h	IC50 of 10 μM	20053781
BJ	Function assay	10 uM	10 days	Suppression of senescence in human BJ cells assessed as increase in cell number at 10 uM after 10 days by senescence reversal assay	16767085
BJ	Function assay	10 uM	10 days	Inhibition of ataxia telangiectasia-mutated in human BJ cells assessed as increase in cell number at 10 uM after 10 days by senescence reversal assay	16767085
MCF7	Function assay	10 uM	10 mins	Sensitization of infrared-induced DNA damage in human MCF7 cells assessed as reduction in colony formation at 10 uM pretreated for 10 mins followed by irradiation for 4 hrs measured after 10 days by crystal violet staining analysis	26632965
KATO III	Growth Inhibition Assay	2.5/5/7.5 μM		enhances the toxicity of olaparib	24841718
hTCEpi	Growth Inhibition Assay	10 μM		prevents the cytopathic effect of HSV-1	24370835
MCF7	Function assay		1 hr	Inhibition of ATM kinase in human MCF7 cells after 1 hr by immunofluorescence assay, IC50 = 0.3 μM.	26632965
KOSC-2	Growth Inhibition Assay			IC50=26.9075 μM	SANGER
DEL	Growth Inhibition Assay			IC50=26.8356 μM	SANGER
GT3TKB	Growth Inhibition Assay			IC50=26.5342 μM	SANGER
MDA-MB-415	Growth Inhibition Assay			IC50=26.5033 μM	SANGER
GI-1	Growth Inhibition Assay			IC50=25.7055 μM	SANGER
BFTC-905	Growth Inhibition Assay			IC50=25.5944 μM	SANGER
QIMR-WIL	Growth Inhibition Assay			IC50=25.1858 μM	SANGER
PANC-08-13	Growth Inhibition Assay			IC50=25.0938 μM	SANGER
SK-MEL-30	Growth Inhibition Assay			IC50=24.4662 μM	SANGER
CHL-1	Growth Inhibition Assay			IC50=23.7292 μM	SANGER
Ramos-2G6-4C10	Growth Inhibition Assay			IC50=22.96 μM	SANGER
SNU-449	Growth Inhibition Assay			IC50=22.8748 μM	SANGER
HCC2157	Growth Inhibition Assay			IC50=22.8054 μM	SANGER
LB1047-RCC	Growth Inhibition Assay			IC50=22.5879 μM	SANGER
YH-13	Growth Inhibition Assay			IC50=22.5123 μM	SANGER
Mewo	Growth Inhibition Assay			IC50=22.5073 μM	SANGER
JVM-3	Growth Inhibition Assay			IC50=22.506 μM	SANGER
HSC-3	Growth Inhibition Assay			IC50=21.1835 μM	SANGER
U031	Growth Inhibition Assay			IC50=21.1489 μM	SANGER
D-283MED	Growth Inhibition Assay			IC50=20.5339 μM	SANGER
A704	Growth Inhibition Assay			IC50=19.8305 μM	SANGER
HCC70	Growth Inhibition Assay			IC50=19.489 μM	SANGER
MLMA	Growth Inhibition Assay			IC50=19.0557 μM	SANGER
697	Growth Inhibition Assay			IC50=19.0201 μM	SANGER
HuP-T3	Growth Inhibition Assay			IC50=18.5888 μM	SANGER
NCI-H2030	Growth Inhibition Assay			IC50=18.1997 μM	SANGER
HCC2998	Growth Inhibition Assay			IC50=17.6733 μM	SANGER
NCI-H82	Growth Inhibition Assay			IC50=17.4573 μM	SANGER
CTB-1	Growth Inhibition Assay			IC50=17.2259 μM	SANGER
NCI-SNU-1	Growth Inhibition Assay			IC50=17.1269 μM	SANGER
SK-MEL-28	Growth Inhibition Assay			IC50=17.0475 μM	SANGER
GCIY	Growth Inhibition Assay			IC50=16.7905 μM	SANGER
ChaGo-K-1	Growth Inhibition Assay			IC50=16.6568 μM	SANGER
NCI-H1793	Growth Inhibition Assay			IC50=16.4712 μM	SANGER
LXF-289	Growth Inhibition Assay			IC50=16.2747 μM	SANGER
HuH-7	Growth Inhibition Assay			IC50=16.2674 μM	SANGER
8305C	Growth Inhibition Assay			IC50=16.1889 μM	SANGER
KG-1	Growth Inhibition Assay			IC50=16.0996 μM	SANGER
VM-CUB-1	Growth Inhibition Assay			IC50=15.9849 μM	SANGER
DBTRG-05MG	Growth Inhibition Assay			IC50=15.6111 μM	SANGER
D-423MG	Growth Inhibition Assay			IC50=15.5236 μM	SANGER
Hs-578-T	Growth Inhibition Assay			IC50=15.4182 μM	SANGER
DOK	Growth Inhibition Assay			IC50=15.3329 μM	SANGER
COLO-684	Growth Inhibition Assay			IC50=14.1569 μM	SANGER
CAL-12T	Growth Inhibition Assay			IC50=13.617 μM	SANGER
KP-N-YS	Growth Inhibition Assay			IC50=12.6354 μM	SANGER
ES7	Growth Inhibition Assay			IC50=11.788 μM	SANGER
LB2241-RCC	Growth Inhibition Assay			IC50=11.7186 μM	SANGER
GOTO	Growth Inhibition Assay			IC50=11.6996 μM	SANGER
J-RT3-T3-5	Growth Inhibition Assay			IC50=11.2417 μM	SANGER
NCI-H1838	Growth Inhibition Assay			IC50=11.1865 μM	SANGER
NCI-H1437	Growth Inhibition Assay			IC50=9.8097 μM	SANGER
KM12	Growth Inhibition Assay			IC50=9.21142 μM	SANGER
SK-MEL-3	Growth Inhibition Assay			IC50=8.28575 μM	SANGER
HH	Growth Inhibition Assay			IC50=8.27671 μM	SANGER
LoVo	Growth Inhibition Assay			IC50=6.93239 μM	SANGER
CAL-72	Growth Inhibition Assay			IC50=5.48084 μM	SANGER
LAMA-84	Growth Inhibition Assay			IC50=4.58465 μM	SANGER
HuO-3N1	Growth Inhibition Assay			IC50=4.17142 μM	SANGER
DU-145	Growth Inhibition Assay			IC50=3.27352 μM	SANGER
RVH-421	Growth Inhibition Assay			IC50=27.2921 μM	SANGER
EW-13	Growth Inhibition Assay			IC50=27.4308 μM	SANGER
639-V	Growth Inhibition Assay			IC50=27.5119 μM	SANGER
A2780	Growth Inhibition Assay			IC50=27.641 μM	SANGER
SW982	Growth Inhibition Assay			IC50=27.9052 μM	SANGER
SW1710	Growth Inhibition Assay			IC50=28.0981 μM	SANGER
HCC1569	Growth Inhibition Assay			IC50=28.4897 μM	SANGER
MV-4-11	Growth Inhibition Assay			IC50=28.5735 μM	SANGER
BHT-101	Growth Inhibition Assay			IC50=28.6572 μM	SANGER
Ca9-22	Growth Inhibition Assay			IC50=28.714 μM	SANGER
HAL-01	Growth Inhibition Assay			IC50=28.7615 μM	SANGER
D-263MG	Growth Inhibition Assay			IC50=29.344 μM	SANGER
NEC8	Growth Inhibition Assay			IC50=29.5548 μM	SANGER
EKVX	Growth Inhibition Assay			IC50=31.5847 μM	SANGER
EM-2	Growth Inhibition Assay			IC50=31.6304 μM	SANGER
MFM-223	Growth Inhibition Assay			IC50=31.8098 μM	SANGER
SK-PN-DW	Growth Inhibition Assay			IC50=32.1406 μM	SANGER
HuO9	Growth Inhibition Assay			IC50=32.5282 μM	SANGER
MHH-PREB-1	Growth Inhibition Assay			IC50=32.6234 μM	SANGER
OVCAR-4	Growth Inhibition Assay			IC50=32.8363 μM	SANGER
NCI-H1648	Growth Inhibition Assay			IC50=32.8651 μM	SANGER
MKN1	Growth Inhibition Assay			IC50=34.1101 μM	SANGER
KYSE-450	Growth Inhibition Assay			IC50=34.6444 μM	SANGER
ES8	Growth Inhibition Assay			IC50=34.8975 μM	SANGER
MS-1	Growth Inhibition Assay			IC50=34.9554 μM	SANGER
HOP-92	Growth Inhibition Assay			IC50=35.9277 μM	SANGER
SKG-IIIa	Growth Inhibition Assay			IC50=36.2561 μM	SANGER
TE-11	Growth Inhibition Assay			IC50=36.5243 μM	SANGER
SK-NEP-1	Growth Inhibition Assay			IC50=37.6744 μM	SANGER
DB	Growth Inhibition Assay			IC50=37.9185 μM	SANGER
IA-LM	Growth Inhibition Assay			IC50=38.0239 μM	SANGER
COLO-829	Growth Inhibition Assay			IC50=38.4159 μM	SANGER
TGBC11TKB	Growth Inhibition Assay			IC50=39.1408 μM	SANGER
CAL-51	Growth Inhibition Assay			IC50=40.0612 μM	SANGER
NCI-H2228	Growth Inhibition Assay			IC50=40.3662 μM	SANGER
C32	Growth Inhibition Assay			IC50=40.4024 μM	SANGER
KU-19-19	Growth Inhibition Assay			IC50=40.7683 μM	SANGER
KNS-62	Growth Inhibition Assay			IC50=40.8381 μM	SANGER
FADU	Growth Inhibition Assay			IC50=41.2502 μM	SANGER
CAL-33	Growth Inhibition Assay			IC50=42.6749 μM	SANGER
CHP-134	Growth Inhibition Assay			IC50=42.8496 μM	SANGER
HDLM-2	Growth Inhibition Assay			IC50=42.9084 μM	SANGER
NBsusSR	Growth Inhibition Assay			IC50=43.0725 μM	SANGER
SW954	Growth Inhibition Assay			IC50=43.1053 μM	SANGER
HCC1806	Growth Inhibition Assay			IC50=43.411 μM	SANGER
VMRC-RCZ	Growth Inhibition Assay			IC50=43.4586 μM	SANGER
A549	Growth Inhibition Assay			IC50=43.931 μM	SANGER
NKM-1	Growth Inhibition Assay			IC50=43.9558 μM	SANGER
DMS-273	Growth Inhibition Assay			IC50=44.7567 μM	SANGER
TYK-nu	Growth Inhibition Assay			IC50=45.1234 μM	SANGER
KALS-1	Growth Inhibition Assay			IC50=45.146 μM	SANGER
A101D	Growth Inhibition Assay			IC50=45.4456 μM	SANGER
G-361	Growth Inhibition Assay			IC50=46.2138 μM	SANGER
KARPAS-299	Growth Inhibition Assay			IC50=46.3516 μM	SANGER
RS4-11	Growth Inhibition Assay			IC50=46.542 μM	SANGER
HT-1376	Growth Inhibition Assay			IC50=46.7426 μM	SANGER
SK-N-AS	Growth Inhibition Assay			IC50=46.7822 μM	SANGER
MG-63	Growth Inhibition Assay			IC50=46.9036 μM	SANGER
EPLC-272H	Growth Inhibition Assay			IC50=46.9503 μM	SANGER
BALL-1	Growth Inhibition Assay			IC50=47.832 μM	SANGER
LCLC-97TM1	Growth Inhibition Assay			IC50=48.202 μM	SANGER
HO-1-N-1	Growth Inhibition Assay			IC50=48.9676 μM	SANGER
MFE-280	Growth Inhibition Assay			IC50=49.4617 μM	SANGER
NCI-H526	Growth Inhibition Assay			IC50=49.8163 μM	SANGER
D-566MG	Growth Inhibition Assay			IC50=49.9096 μM	SANGER
BB30-HNC	Growth Inhibition Assay			IC50=49.9498 μM	SANGER
SK-N-DZ	Growth Inhibition Assay			IC50=50.0481 μM	SANGER
U2OS	Function assay			Inhibition of ATM in human U2OS cells assessed as inhibition of p53 phosphorylation at Ser15 residue, IC50 = 0.25 μM.	26632965
SK-N-MC	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells	29435139
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生物活性

製品説明

Targets

ATM ^[1]
(Cell-free assay)

12.9 nM

In Vitro
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]
Kinase Assay	Purified enzyme assays
Kinase Assay	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.
細胞実験	細胞株	U2OS cells
	濃度	10 μM
	反応時間	2 hours
	実験の流れ	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.
実験結果図	Methods	Biomarkers	結果図	PMID
	Western blot	p-AKT(Ser473) / p-AKT(Thr308) PARP / Cleaved PARP / Caspase-3 / Cleaved caspase-3 ATM-S1981 / ATM / p-p53(S15) / p53 p21 / p27 / p53		22739265
	Immunofluorescence	p-S824 KAP1 / ZEBRA		28249048

In Vivo
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]
動物実験	動物モデル	BALB/c nu/nu nude mice bearing LU1205 cells
	投与量	10 μM
	投与経路	--

参考
[1] Hickson I, et al. Cancer Res. 2004, 64(24), 9152-9159. [2] Soleimani R, et al. Aging. 2011, 3(8), 782-793. [3] Ivanov VN, et al. Cancer Res. 2009, 69(8), 3510-3519.

参考

化学情報

分子量	395.49	化学式	C₂₁H₁₇NO₃S₂
CAS No.	587871-26-9	SDF	Download KU-55933 SDFをダウンロードする
Smiles	C1COCCN1C2=CC(=O)C=C(O2)C3=C4C(=CC=C3)SC5=CC=CC=C5S4
保管	3年-20°C粉	溶液の保管冷凍と解凍の繰り返しを避けるため小分けにしてください	1年-80°Cin solvent
保管	3年-20°C粉	溶液の保管冷凍と解凍の繰り返しを避けるため小分けにしてください	１ケ月-20°Cin solvent

In vitro
Batch:

DMSO : 39 mg/mL ( (98.61 mM)；吸湿したDMSOは溶解度を減少させます。新しいDMSOをご使用ください。)

Water : Insoluble

Ethanol : Insoluble

モル濃度計算器

in vivo
Batch:

Add solvents to the product individually and in order.

投与溶液組成計算機

実験計算

モル濃度計算器

質量	濃度	体積	分子量
=	×	×

希釈計算器分子量計算器

投与溶液組成計算機(クリア溶液)

ステップ１：実験データを入力してください。（実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します）

投与量 mg/kg 動物平均体重 g 投与体積（動物毎）μL 動物数匹

ステップ２：投与溶媒の組成を入力してください。（ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください）

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

計算結果：

投与溶媒濃度： mg/ml;

DMSOストック溶液調製方法： mg 試薬を μL DMSOに溶解する（濃度 mg/mL, 注：濃度が当該ロットのDMSO溶解度を超える場合はご連絡ください。 )

投与溶媒調製方法：Take μL DMSOストック溶液に μL PEG300，を加え、完全溶解後μL Tween 80，を加えて完全溶解させた後 μL ddH₂O，を加え完全に溶解させます。

投与溶媒調製方法：μL DMSOストック溶液に μL Corn oil，を加え、完全溶解。

注意：１.ストック溶液に沈殿、混濁などがないことをご確認ください；
２.順番通りに溶剤を加えてください。次のステップに進む前に溶液に沈殿、混濁などがないことを確認してから加えてください。ボルテックス、ソニケーション、水浴加熱など物理的な方法で溶解を早めることは可能です。

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C1=C0/X	C1:	LOG(C1):
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C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
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