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KU-0060648 99%

货号:A571046 Ambeed 开学季,买赠积分,赢豪礼

KU-0060648 is a dual inhibitor of DNA-PK and PI3Kα, PI3Kβ, PI3Kδ with IC50 of 8.6 nM and 4 nM, 0.5 nM, 0.1 nM respectively, and with less inhibition of PI3Kγ with IC50 of 0.59 μM.

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KU-0060648 化学结构 CAS号:881375-00-4
KU-0060648 化学结构
CAS号:881375-00-4
KU-0060648 3D分子结构
CAS号:881375-00-4
KU-0060648 化学结构 CAS号:881375-00-4
KU-0060648 3D分子结构 CAS号:881375-00-4
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KU-0060648 纯度/质量文件 产品仅供科研

货号:A571046 标准纯度: 99%
批次查询: 批次纯度:

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产品名称 mTOR mTORC1 mTORC2 其他靶点 纯度
AZD-8055 ++++

mTOR (truncated), IC50: 0.13 nM

mTOR (full length), IC50: 0.8 nM

99%+
Gedatolisib ++++

mTOR, IC50: 1.6 nM

99%+
GSK1059615 ++

mTOR, IC50: 12 nM

98%
Vistusertib +++

mTOR, IC50: 2.8 nM

99%+
Torin 1 +++

mTOR, IC50: 4.32 nM

+++

mTORC1, IC50: 2 nM

++

mTORC2, IC50: 10 nM

DNA-PK 99%+
Dactolisib +++

mTOR (p70S6K), IC50: 6 nM

99%+
PI-103 +

mTOR, IC50: 30 nM

99%+
WAY-600 ++

mTOR, IC50: 9 nM

99%
Voxtalisib +

mTOR, IC50: 157 nM

99%+
PF-04691502 ++

mTOR, Ki: 16 nM

99%+
Onatasertib ++

mTOR, IC50: 16 nM

DNA-PK 99%+
Chrysophanol EGFR 98%
Samotolisib DNA-PK 99%+
Torkinib +++

mTOR, IC50: 8 nM

DNA-PK,PDGFR 99%+
Everolimus 99%+
WYE-354 +++

mTOR, IC50: 5 nM

99%+
Tacrolimus 98%
PP121 ++

mTOR, IC50: 13 nM

VEGFR,PDGFR 99%+
Torin 2 ++++

mTOR, IC50: 0.25 nM

DNA-PK 99%+
Rapamycin ++++

mTOR, IC50: ~0.1 nM

98%
GDC-0349 +++

mTOR, Ki: 3.8 nM

98%
XL388 ++

mTOR, IC50: 9.9 nM

+++

mTORC1, IC50: 8 nM

+

mTORC2, IC50: 166 nM

99%+
WYE-687 +++

mTOR, IC50: 7 nM

98+%
Apitolisib +

mTOR, Ki app: 17 nM

99%+
WYE-132 ++++

mTOR, IC50: 0.19 nM

99%+
Sapanisertib ++++

mTOR, Ki: 1.4 nM

99%+
BGT226 maleate 99%+
ETP-46464 ++++

mTOR, IC50: 0.6 nM

DNA-PK 99%+
PI3K-IN-1 +

mTOR, IC50: 157 nM

99%+
Zotarolimus +++

FKBP-12, IC50: 2.8 nM

99+%
OSI-027 +++

mTOR, IC50: 4 nM

+

mTORC1, IC50: 22 nM

+

mTORC2, IC50: 65 nM

99%+
Ridaforolimus ++++

mTOR, IC50: 0.2 nM

99%+
Temsirolimus +

mTOR, IC50: 1.76 μM

99%
CZ415 ++

mTOR, pIC50: 8.07

99%+
SF2523 +

mTOR, IC50: 280 nM

DNA-PK 99%+
KU-0063794 ++

mTORC1, IC50: ~10 nM

++

mTORC2, IC50: ~10 nM

99%+
Omipalisib ++++

mTORC1, Ki: 0.18 nM

++++

mTORC2, Ki: 0.3 nM

99%+
Palomid 529 99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。
产品名称 C2β p110α p110β p110γ p110δ PI3K Vps34 其他靶点 纯度
A66 +

C2β, IC50: 462 nM

++

p110α, IC50: 32 nM

99%+
Taselisib +

C2β, IC50: 292 nM

++++

PI3Kα, Ki: 0.29 nM

+++

PI3Kβ, Ki: 9.1 nM

++++

PI3Kγ, Ki: 0.97 nM

++++

PI3Kδ, Ki: 0.12 nM

+

hVps34, IC50: 374 nM

99%+
Gedatolisib ++++

PI3Kα, IC50: 0.4 nM

+++

PI3Kγ, IC50: 5.4 nM

mTOR 99%+
HS-173 ++++

PI3Kα , IC50: 0.8 nM

99%+
Serabelisib +++

PI3Kα, IC50: 21 nM

99%+
GNE-477 ++++

PI3Kα, IC50: 4 nM

mTOR 99%+
YM-201636 +

p110α, IC50: 3.3 μM

PIKfyve 99%+
AS-252424 +

PI3Kα, IC50: 935 nM

++

PI3Kγ, IC50: 33 nM

99%
Alpelisib +++

PI3Kα, IC50: 5 nM

99%+
AS-604850 +

PI3Kα, IC50: 4.5 μM

+

PI3Kγ, IC50: 0.25 μM

99%+
SF2523 ++

PI3Kα, IC50: 34 nM

++

PI3Kγ, IC50: 158 nM

DNA-PK,mTOR 99%+
Inavolisib ++++

PI3K alpha, IC50: 0.038 nM

99%+
Bimiralisib ++++

PI3Kα, Kd: 1.5 nM

+++

PI3Kβ, Kd: 11 nM

++

PI3Kγ, Kd: 25 nM

++

PI3Kδ, Kd: 25 nM

mTOR 99%+
GSK1059615 ++++

PI3Kα, IC50: 0.4 nM

++++

PI3Kβ, IC50: 0.6 nM

+++

PI3Kγ, IC50: 5 nM

++++

PI3Kδ, IC50: 2 nM

mTOR 98%
GSK2636771 99%+
Fimepinostat +++

PI3Kα, IC50: 19 nM

++

PI3Kβ, IC50: 54 nM

++

PI3Kδ, IC50: 39 nM

99%+
VS-5584 ++++

PI3Kα, IC50: 2.6 nM

+++

PI3Kβ, IC50: 21 nM

++++

PI3Kγ, IC50: 3.0 nM

++++

PI3Kδ, IC50: 2.7 nM

mTOR 99%
Dactolisib ++++

p110α1, IC50: 4 nM

++

p110β, IC50: 75 nM

+++

p110γ, IC50: 5 nM

+++

p110δ, IC50: 7 nM

99%+
PI-103 ++++

p110α, IC50: 2 nM

++++

p110β, IC50: 3 nM

+++

p110γ, IC50: 15 nM

++++

p110δ, IC50: 3 nM

DNA-PK,mTOR 99%+
PI-3065 +

p110β, IC50: 1078 nM

+++

p110δ, IC50: 15 nM

99%+
Voxtalisib ++

PI3Kα, IC50: 39 nM

++

PI3Kβ, IC50: 113 nM

+++

PI3Kγ, IC50: 9 nM

++

PI3Kδ, IC50: 43 nM

DNA-PK,mTOR 99%+
AZD-8835 +++

PI3Kα, IC50: 6.2 nM

+

PI3Kβ, IC50: 431 nM

++

PI3Kγ, IC50: 90 nM

+++

PI3Kδ, IC50: 5.7 nM

99%+
Pilaralisib analogue ++

PI3Kα, IC50: 39 nM

++

PI3Kβ, IC50: 36 nM

+++

PI3Kγ, IC50: 23 nM

++

PI3Kδ, IC50: 36 nM

99%+
ZSTK474 +++

PI3Kα, IC50: 16 nM

++

PI3Kβ, IC50: 44 nM

++

PI3Kγ, IC50: 49 nM

+++

PI3Kδ, IC50: 4.6 nM

++

PI3K, IC50: 37 nM

99%+
AS-605240 ++

PI3Kα, IC50: 60 nM

+

PI3Kβ, IC50: 270 nM

+++

PI3Kγ, IC50: 8 nM

+

PI3Kδ, IC50: 300 nM

99%+
TGX-221 +++

p110β, IC50: 5 nM

++

p110δ, IC50: 0.1 μM

99%+
PF-04691502 ++++

PI3Kα, Ki: 1.8 nM

++++

PI3Kβ, Ki: 2.1 nM

++++

PI3Kγ, Ki: 1.9 nM

++++

PI3Kδ, Ki: 1.6 nM

mTOR 99%+
GDC-0084 ++++

PI3Kα, Ki app: 2 nM

++

PI3Kβ, Ki app: 46 nM

+++

PI3Kγ, Ki app: 10 nM

++++

PI3Kδ, Ki app: 3 nM

mTOR 99%+
Buparlisib ++

p110α, IC50: 52 nM

+

p110β, IC50: 166 nM

+

p110γ, IC50: 262 nM

++

p110δ, IC50: 116 nM

+

Vps34, IC50: 2.4 μM

mTOR 98%
LY294002 +

p110α, IC50: 0.5 μM

+

p110β, IC50: 0.97 μM

+

p110δ, IC50: 0.57 μM

DNA-PK 99%+
AZD 6482 +

PI3Kα, IC50: 870 nM

+++

PI3Kβ, IC50: 10 nM

++

PI3Kδ, IC50: 80 nM

DNA-PK 99%+
Pictilisib ++++

p110α, IC50: 3 nM

++

p110β, IC50: 33 nM

++

p110γ, IC50: 75 nM

++++

p110δ, IC50: 3 nM

mTOR 99%+
PKI-402 ++++

PI3Kα, IC50: 2 nM

+++

PI3Kβ, IC50: 7 nM

+++

PI3Kγ, IC50: 16 nM

+++

PI3Kδ, IC50: 14 nM

mTOR 99+%
Copanlisib ++++

PI3Kα, IC50: 0.5 nM

++++

PI3Kβ, IC50: 3.7 nM

+++

PI3Kγ, IC50: 6.4 nM

++++

PI3Kδ, IC50: 0.7 nM

99%+
Omipalisib ++++

p110α, Ki: 0.019 nM

++++

p110β, Ki: 0.13 nM

++++

p110γ, Ki: 0.06 nM

++++

p110δ, Ki: 0.024 nM

99%+
Izorlisib +++

PI3Kα, IC50: 14 nM

++

PI3Kβ, IC50: 0.12 μM

++

PI3Kγ, IC50: 36 nM

+

PI3Kδ, IC50: 0.50 μM

99%+
AZD8186 ++

PI3Kα, IC50: 35 nM

++++

PI3Kβ, IC50: 4 nM

+++

PI3Kδ, IC50: 12 nM

99%+
KU-0060648 ++++

PI3Kα, IC50: 4 nM

++++

PI3Kβ, IC50: 0.5 nM

+

PI3Kγ, IC50: 0.59 μM

++++

PI3Kδ, IC50: 0.1 nM

DNA-PK 99%
Apitolisib +++

p110α, IC50: 5 nM

++

p110β, IC50: 27 nM

+++

p110γ, IC50: 14 nM

+++

p110δ, IC50: 7 nM

mTOR 99%+
CZC24832 +

PI3Kβ, IC50: 1.1 μM

++

PI3Kγ, IC50: 27 nM

99%+
BGT226 maleate ++++

PI3Kα, IC50: 4 nM

++

PI3Kβ, IC50: 63 nM

++

PI3Kγ, IC50: 38 nM

mTOR 99%+
TG 100713 ++

PI3Kα, IC50: 165 nM

+

PI3Kβ, IC50: 215 nM

++

PI3Kγ, IC50: 50 nM

+++

PI3Kδ, IC50: 24 nM

99%+
PI3K-IN-1 ++

PI3Kα, IC50: 39 nM

++

PI3Kβ, IC50: 113 nM

+++

PI3Kγ, IC50: 9 nM

++

PI3Kδ, IC50: 43 nM

DNA-PK,mTOR 99%+
TG100-115 +

PI3Kα, IC50: 1.3 μM

+

PI3Kβ, IC50: 1.2 μM

++

PI3Kγ, IC50: 83 nM

+

PI3Kδ, IC50: 235 nM

99%+
PIK-90 +++

PI3Kα, IC50: 11 nM

+

PI3Kβ, IC50: 350 nM

+++

PI3Kγ, IC50: 18 nM

++

PI3Kδ, IC50: 58 nM

99%+
PIK-294 +

p110β, IC50: 490 nM

++

p110γ, IC50: 160 nM

+++

p110δ, IC50: 10 nM

99%+
Duvelisib ++++

PI3Kβ, Ki: 1564 pM

++

PI3Kγ, Ki: 243 pM

++++

PI3Kδ, Ki: 23 pM

99%+
GDC-0326 ++++

PI3Kα, Ki: 0.2 nM

++

PI3Kβ, Ki: 26.6 nM

+++

PI3Kγ, Ki: 10.2 nM

++++

PI3Kδ, Ki: 4 nM

98%
Quercetin Dihydrate +

PI3Kβ, IC50: 5.4 μM

+

PI3Kγ, IC50: 2.4 μM

+

PI3Kδ, IC50: 3.0 μM

98%+
Quercetin +

PI3Kβ, IC50: 5.4 μM

+

PI3Kγ, IC50: 2.4 μM

+

PI3Kδ, IC50: 3.0 μM

Src,Sirtuin,PKC 97%
Leniolisib +

PI3Kα, IC50: 0.244 μM

+

PI3Kβ, IC50: 0.424 μM

+

PI3Kγ, IC50: 2.23 μM

+++

PI3Kδ, IC50: 0.011 μM

DNA-PK 99%+
PIK-108 99%+
Eganelisib +++

PI3Kγ, IC50: 16 nM

99%+
CAY10505 99%+
IPI-3063 ++++

p110δ, IC50: 2.5 nM

99%
Nemiralisib ++++

PI3Kδ, pKi: 9.9

99%+
PF-4989216 ++++

p110α, IC50: 2 nM

++

p110γ, IC50: 65 nM

++++

p110δ, IC50: 1 nM

99%+
PIK-75 HCl +++

p110α, IC50: 5.8 nM

++

p110γ, IC50: 76 nM

+

p110δ, IC50: 0.51 μM

DNA-PK 99%+
Tenalisib ++

PI3Kγ, IC50: 33.2 nM

++

PI3Kδ, IC50: 24.5 nM

98%+
Acalisib +++

p110δ, IC50: 14 nM

99%+
Umbralisib +++

PI3Kδ, IC50: 22.2 nM

99%+
AMG319 +

PI3Kγ, IC50: 850 nM

+++

PI3Kδ, IC50: 18 nM

99%
IC-87114 +

PI3Kγ, IC50: 29 μM

+

PI3Kδ, IC50: 0.5 μM

99%+
Idelalisib ++

p110γ, IC50: 89 nM

++++

p110δ, IC50: 2.5 nM

98%
PIK-293 +

p110γ, IC50: 10 μM

+

p110δ, IC50: 0.24 μM

99%+
Vps34-PIK-III +

PI3Kδ, IC50: 1.2μM

+++

Vps34, IC50: 0.018μM

99%+
GSK2292767 99+%
Seletalisib +

PI3Kγ, IC50: 282 nM

+++

PI3Kδ, IC50: 12 nM

99%+
P110δ-IN-1 ++++

P110δ, IC50: 0.6 nM

99%+
PI3Kδ-IN-5 ++++

PI3Kδ, IC50: 0.9 nM

99%+
SRX3207 +

PI3K alpha, IC50: 244 nM

+

PI3K gamma, IC50: 9790 nM

+

PI3K delta, IC50: 388 nM

Syk 98%
Parsaclisib HCl ++++

PI3Kδ, IC50: 1 nM

98%
IHMT-PI3Kδ-372 +++

PI3Kδ, IC50: 14 nM

98%
Trigonelline Akt 99%+
Wortmannin ++++

PI3K, IC50: 3 nM

MLCK,DNA-PK 99%+
Samotolisib DNA-PK 99%+
GNE-317 99%+
Oroxin B Akt,PTEN 99%+
NU 7026 +

PI3K, IC50: 13 μM

DNA-PK 99%+
Deguelin Akt 99%+
Ailanthone CDK,Akt,ATM/ATR 98%
Resibufogenin ROS 98%
KU-57788 +

PI3K, IC50: 5 μM

DNA-PK,mTOR 99%+
Cinobufagine Akt 98%
α-Linolenic acid 97% GC
MTX-211 EGFR 99%+
PI3K/mTOR Inhibitor-2 ++++

PI3K, IC50: 3.4 nM

mTOR 99%+
SPP-86 99%+
(E)-Akt inhibitor-IV 98%
Vps34-IN-1 ++

Vps34, IC50: 25 nM

98%
SAR405 ++++

Vps34, IC50: 1.2 nM

99%+
3-Methyladenine +

PI3Kγ, IC50: 60 μM

+

Vps34, IC50: 25 μM

Autophagy 98%
Vps34-IN-4 +++

VPS34, IC50: 15 nM

99%+
Autophinib +++

Vps34, IC50: 19 nM

Autophagy 99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。
产品名称 DNA-PK 其他靶点 纯度
PI-103 ++

DNA-PK, IC50: 23 nM

99%+
CC-115 +++

DNA-PK, IC50: 0.013 μM

mTOR 99%+
Samotolisib 99%+
NU 7026 +

DNA-PK, IC50: 0.23 μM

PI3K 99%+
PIK-75 HCl ++++

DNA-PK, IC50: 2 nM

99%+
PP121 +

DNA-PK, IC50: 60 nM

VEGFR,PDGFR 99%+
KU-0060648 ++++

DNA-PK, IC50: 5 nM

99%
KU-57788 +++

DNA-PK, IC50: 14 nM

99%+
LTURM34 ++

DNA-PK, IC50: 0.034 μM

99%+
SF2523 +++

DNA-PK, IC50: 9 nM

99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。

KU-0060648 生物活性

靶点
  • p110γ

    PI3Kγ, IC50:0.59 μM

  • p110β

    PI3Kβ, IC50:0.5 nM

  • p110α

    PI3Kα, IC50:4 nM

  • p110δ

    PI3Kδ, IC50:0.1 nM

  • DNA-PK

    DNA-PK, IC50:5 nM

描述 KU-0060648 is a dual inhibitor of DNA-PK and PI3Kα, PI3Kβ, PI3Kδ with IC50 of 8.6 nM and 4 nM, 0.5 nM, 0.1 nM respectively, and with less inhibition of PI3Kγ with IC50 of 0.59 μM.

KU-0060648 细胞研究

细胞系 浓度 检测类型 检测时间 活动说明 数据源
human HeLa cells Function assay Inhibition of DNA-PK autophosphorylation at S2056 in human HeLa cells, EC50=0.136 μM 23855836
MO59J-Fus1 cells 1 μM Function assay Inhibition of human DNA-PK autophosphorylation at S2056 in MO59J-Fus1 cells at 1 uM 23855836

KU-0060648 参考文献

[1]Mao M, Liu Y, et al. Feedback autophagy activation as a key resistance factor of Ku-0060648 in colorectal cancer cells. Biochem Biophys Res Commun. 2017 Sep 2;490(4):1244-1249.

[2]Chen MB, Zhou ZT, et al. KU-0060648 inhibits hepatocellular carcinoma cells through DNA-PKcs-dependent and DNA-PKcs-independent mechanisms. Oncotarget. 2016 Mar 29;7(13):17047-59.

KU-0060648 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.72mL

0.34mL

0.17mL

8.58mL

1.72mL

0.86mL

17.16mL

3.43mL

1.72mL

KU-0060648 技术信息

CAS号881375-00-4
分子式C33H34N4O4S
分子量 582.712
别名
运输蓝冰
存储条件

粉末 Keep in dark place,Inert atmosphere,2-8°C

液体 -20°C:3-6个月-80°C:12个月

溶解度

DMSO: 2 mg/mL(3.43 mM),配合低频超声,并水浴加热至45℃助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

动物实验配方
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