CGK733
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
CGK 733是ATM / ATR激酶的选择性抑制剂,IC50值约为200 nM[1]。
ATM是一种丝氨酸/苏氨酸激酶,在DNA修复和细胞周期检查点中发挥关键作用。在缺氧的情况下,ATM相关激酶(ATR)损失减弱了HIF-1的DNA结合,随后影响GLUT-1和CAIX的蛋白表达水平。ATM和ATR组分调节信号转导途径,增强细胞对化疗和放疗的敏感性,是一种有吸引力的药理学靶标[2,3]。
CGK733选择性抑制ATM和ATR激酶的活性,并阻止他们的检查点信号通路。使用GSK733处理HEK-293细胞,增加细胞对放疗的敏感度[1]。在HBV阳性肝癌细胞系HepG2.2.15中,CGK733显著诱导多核细胞的形成,增加细胞对紫杉醇的敏感性[2]。CGK733引起衰老乳腺癌、肺癌和结肠癌细胞死亡[4]。使用CGK733处理肿瘤细胞,其可通过抑制肿瘤细胞的DNA修复和细胞周期检查点提高细胞对放疗的敏感性[5]。在MCF-7乳腺癌细胞中,CGK733治疗诱导细胞周期蛋白D1的含量下降,并减少磷酸化的和总的视网膜母细胞瘤(RB)蛋白,最终抑制细胞增殖[3]。
参考文献:
[1]. Williams, T.M., et al., Molecular imaging of the ATM kinase activity. Int J Radiat Oncol Biol Phys, 2013. 86(5): p. 969-77.
[2]. Wang, H., et al., CGK733 enhances multinucleated cell formation and cytotoxicity induced by taxol in Chk1-deficient HBV-positive hepatocellular carcinoma cells. Biochem Biophys Res Commun, 2012. 422(1): p. 103-8.
[3]. Alao, J.P. and P. Sunnerhagen, The ATM and ATR inhibitors CGK733 and caffeine suppress cyclin D1 levels and inhibit cell proliferation. Radiat Oncol, 2009. 4(51): p. 4-51.
[4]. Crescenzi, E., et al., Ataxia telangiectasia mutated and p21CIP1 modulate cell survival of drug-induced senescent tumor cells: implications for chemotherapy. Clin Cancer Res, 2008. 14(6): p. 1877-87.
[5]. Kuroda, S., Y. Urata, and T. Fujiwara, Ataxia-telangiectasia mutated and the Mre11-Rad50-NBS1 complex: promising targets for radiosensitization. Acta Med Okayama, 2012. 66(2): p. 83-92.
Physical Appearance | A solid |
Storage | Store at -20°C |
M.Wt | 555.84 |
Cas No. | 905973-89-9 |
Formula | C23H18Cl3FN4O3S |
Solubility | ≥27.8 mg/mL in DMSO; insoluble in H2O; ≥5.55 mg/mL in EtOH with gentle warming and ultrasonic |
Chemical Name | 2,2-diphenyl-N-[2,2,2-trichloro-1-[(4-fluoro-3-nitrophenyl)carbamothioylamino]ethyl]acetamide |
SDF | Download SDF |
Canonical SMILES | C1=CC=C(C=C1)C(C2=CC=CC=C2)C(=O)NC(C(Cl)(Cl)Cl)NC(=S)NC3=CC(=C(C=C3)F)[N+](=O)[O-] |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。 |
Description | CGK 733是ATM / ATR的有效选择性抑制剂,IC50值约为200 nM。 | |||||
靶点 | ATM | ATR | ||||
IC50 | 200 nM | 200 nM |
质量控制和MSDS
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