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CGK733 {[allProObj[0].p_purity_real_show]}

货号：A140835 同义名： ATM/ATR Kinase Inhibitor

CGK 733 is an inhibitor of ATM and ATR with IC50 of ~200 nM, also induces cell death in prematurely senescent breast cancer cells.

CGK733 化学结构 CAS号：905973-89-9
CGK733 化学结构
CAS号：905973-89-9
CGK733 3D分子结构
CAS号：905973-89-9
CGK733 化学结构 CAS号：905973-89-9
CGK733 3D分子结构 CAS号：905973-89-9
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CGK733 纯度/质量文件 产品仅供科研

货号：A140835 标准纯度： {[allProObj[0].p_purity_real_show]}
批次查询： 批次纯度:

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产品名称 ATM ↓ ATR ↓ 其他靶点 纯度
Wortmannin ++

ATM, IC50: 150 nM

 		PI3K,DNA-PK,MLCK 99%+
CP-466722 +

ATM, IC50: 410 nM

 		99%+
Torin 2 ++

ATM, EC50: 28 nM

 		++

ATR, EC50: 35 nM

 		mTOR,DNA-PK 99%+
KU-55933 +++

ATM, IC50: 12.9 nM

 		96%
ETP-46464 +

ATM, IC50: 545 nM

 		+++

ATR, IC50: 14 nM

 		mTOR,DNA-PK 98%
CGK733 ++

ATM, IC50: 200 nM

 		++

ATR, IC50: 200 nM

 		99%+
AZD0156 ✔ 99%+
Dactolisib +++

ATR, IC50: 21 nM

 		98+%
Ceralasertib ++++

ATR, IC50: 1 nM

 		99%+
Berzosertib +++

ATR, IC50: 19 nM

 		99%+
VE-821 +++

ATR, Ki: 13 nM

 		99%+
AZ20 ++++

ATR, IC50: 5 nM

 		mTOR 99%+
Schizandrin B +

ATR, IC50: 7.25 μM

 		P-gp 98%
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。

CGK733 生物活性

靶点

  • ATM

    ATM, IC50:200 nM

  • ATR

    ATR, IC50:200 nM
描述 The ataxia telangiectasia mutated (ATM) and ATM-related (ATR) kinases facilitate the resistance of cancer cells to genotoxic agents. CGK733 is a thiourea-containing compound that inhibits both ATM and ATR with IC50 values of ~200nM. Treatment of MCF-7 breast cancer cells with 10μM CGK733 reduced the expression of cyclin D1 within 2h of exposure. CGK733 at 5-20μM induced a loss of cyclin D1 protein in T47D cells. In MCF-7 cells, treatment with CGK733 at 10μM for 24h reduced the expression of both phosphorylated and total retinoblastoma tumor suppressor protein. CGK733 at a dosage of 10μM inhibited the proliferation of MCF-7, T47D, HCT116, BALB/c3T3, MDA-MB436, and LnCap cancer cells.[3] In mice inoculated with D54-ATMR cells, treatment with CGK733 (25mg/kg) for 1, 4, and 8h induced an increase in ATM reporter activity with 2.4-fold, 3.1-fold, and 1.3-fold changes, respectively, over the control group.[4]
作用机制 CGK733 is a small-molecule inhibitor of both ATM and ATR.[3]

CGK733 参考文献

[1]Wang Y, Kuramitsu Y, et al. CGK733-induced LC3 II formation is positively associated with the expression of cyclin-dependent kinase inhibitor p21Waf1/Cip1 through modulation of the AMPK and PERK/CHOP signaling pathways. Oncotarget. 2015 Nov 24;6(37):39692-701.

[2]Crescenzi E, Palumbo G, et al. Ataxia telangiectasia mutated and p21CIP1 modulate cell survival of drug-induced senescent tumor cells: implications for chemotherapy. Clin Cancer Res. 2008 Mar 15;14(6):1877-87.

[3]Alao JP, Sunnerhagen P. The ATM and ATR inhibitors CGK733 and caffeine suppress cyclin D1 levels and inhibit cell proliferation. Radiat Oncol. 2009;4:51. Published 2009 Nov 10. doi:10.1186/1748-717X-4-51

[4]Williams TM, Nyati S, Ross BD, Rehemtulla A. Molecular imaging of the ATM kinase activity. Int J Radiat Oncol Biol Phys. 2013;86(5):969-977. doi:10.1016/j.ijrobp.2013.04.028

CGK733 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.80mL

0.36mL

0.18mL

9.00mL

1.80mL

0.90mL

17.99mL

3.60mL

1.80mL

CGK733 技术信息

CAS号905973-89-9
分子式C23H18Cl3FN4O3S
分子量 555.836
别名 ATM/ATR Kinase Inhibitor
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Sealed in dry,2-8°C
溶解度

DMSO: 105 mg/mL(188.9 mM)，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

Tags: CGK733 | 905973-89-9 | CGK 733 | CGK-733 | ATM/ATR Inhibitor | Cell Cycle/DNA Damage | PI3K/Akt/mTOR | ATM/ATR | 仅供科研使用 | AmBeed-信号通路专用抑制剂 | CGK733 纯度/质量文件 | CGK733 亚型比较 | CGK733 生物活性 | CGK733 参考文献 | CGK733 实验方案 | CGK733 技术信息

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