- CP-466722
- VE-821
- ETP-46464
- KU-60019
- KU 55933
- AZ20
| CGK733ATM/ATR inhibitor,potent and selective |
Sample solution is provided at 25 µL, 10mM.
Nature.2017 Jan 19;541(7637):417-420.
Nature.2018 Nov;563(7731):407-411.Nature.2018 Jun 13.Nature.2018 Jun 27.Nature.2018 Mar 29;555(7698):673-677.Nature.2017 Sep 7;549(7670):96-100.Nature.2016 Apr 21;532(7599):398-401.
Science.2016 Aug 5;353(6299)594-8Nat Nanotechnol.2017 Dec;12(12):1190-1198.Nature Biotechnology.2017 Jun;35(6):569-576Nat Med.2018 Sep 17.Cell.2018 Dec 21. pii: S0092-8674(18)31561-7.Cell.Available online 25 October 2018.Cell.2018 Sep 27. pii: S0092-8674(18)31183-8.Cell.2018 Jun 28;174(1):172-186.e21.Cell.2018 Feb 22;172(5):1007-1021.e17.Cell.2017 Nov 30;171(6):1284-1300.e21.Cell.2017 Aug 17. pii: S0092-8674(17)30869-3.Cell.2017 Jul 13;170(2):312-323Nat Med.2018 Jan 29.Nat Med.2017 Nov;23(11):1342-1351.Cell.2017 Apr 6;169(2):286-300.Cell.2015 Aug 27;162(5):987-1002.Cell.2015 Feb 12;160(4):729-44.Nature Medicine.2017 Apr;23(4):493-500.Cancer Cell.2018 May 14;33(5):905-921.e5.Cancer Cell.2018 Apr 9;33(4):752-769.e8.Cancer Cell.2018 Mar 12;33(3):401-416.e8.Cancer Cell.2017 Aug 14;32(2):253-267.e5.Nat Methods.2018 Jul;15(7):523-526.Cell Stem Cell.2018 May 3;22(5):769-778.e4.Cell Stem Cell.2017 Nov 20. pii: S1934-5909(17)30375-2.Quality Control & MSDS
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- Purity = 99.56%
- COA (Certificate Of Analysis)
- HPLC
- NMR (Nuclear Magnetic Resonance)
- MSDS (Material Safety Data Sheet)
- Datasheet
Chemical structure
| Description | CGK 733 is a potent and selective inhibitor of ATM/ATR with an IC50 value of ~200 nM. | |||||
| Targets | ATM | ATR | ||||
| IC50 | 200 nM | 200 nM | ||||
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| Cas No. | 905973-89-9 | SDF | Download SDF |
| Synonyms | N/A | ||
| Chemical Name | 2,2-diphenyl-N-[2,2,2-trichloro-1-[(4-fluoro-3-nitrophenyl)carbamothioylamino]ethyl]acetamide | ||
| 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-] | ||
| Formula | C23H18Cl3FN4O3S | M.Wt | 555.84 |
| Solubility | ≥27.8mg/mL in DMSO, <2.76mg l="" in="" h2o,="" ≥5.55mg/ml="" in="" etoh="" with="" ultrasonic="" and="" warming=""> | Storage | Store at -20°C |
| Physical Appearance | A solid | Shipping Condition | Evaluation sample solution : ship with blue ice.All other available size:ship with RT , or blue ice upon request |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. | ||
CGK733 is an inhibitor of kinase ATM and ATR with IC50 value of ~200 nM [1].Ataxia telangiectasia mutated (ATM) is a serine/threonine kinase which plays pivotal role in DNA repair and cell cycle checkpoints. And when in hypoxia circumstance, loss of ATM-related (ATR) kinase induces the decreasing of HIF-1 DNA binding, which consequently affects GLUT-1 and CAIX expression in the protein level. The components of ATM and ATR regulated signaling pathways which enhances cellular sensitivity to chemo- and radiotherapy thus provide attractive pharmacological targets [2, 3]. CGK733 selectively inhibited ATM and ATR kinase activities and blocked their checkpoint signaling pathways. Treated HEK-293 cells with GSK733 would increase the sensitivity of cells to radiotherapy [1]. When tested with HBV-positive HCC cell line HepG2.2.15, CGK733 treatment significantly increased the cells sensitivity to taxol via inducing the formation of multinucleated cells [2]. Treated with CGK733, senescent breast, lung, and colon carcinoma cells were induced to undergo cell death [4]. CGK733 treated tumor cells could enhance the sensitivity to radio therapy via inhibiting DNA repair and cell cycle checkpoints of tumor cells [5]. In MCF-7 breast cancer cells, CGK733 treatment induced detectable decline levels of cyclin D1 protein and reduced phosphorylated and total retinoblastoma protein (RB) which inhibited cell proliferation [3]. References: [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.
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上海好多的供应商的，具体还是看你选择了，其实试剂盒产品都差不多，什么远慕生物，古朵生物...好多的额
用双氧水去除过氧化物酶时，我是自己配的3%双氧水滴到片上而非将片浸入双氧水，这样可否？
用博士德的DAB染色，配制方法为：1mlH20中加入DAB、H2O2、TBS各一滴，我配制的时候发现将DAB加入H20时很容易沉淀，要震荡才能混匀，且将配好的DAB滴到玻片上时，DAB会结为很小块的微颗粒悬浮在液体中但并不染色，是否DAB有问题？
现在打算换中衫的试剂盒，代理商说中衫的试剂盒包括了二抗和DAB，想请教一下该试剂盒的具体内容有些什么？
万分感谢！
