516480-79-8 Usage
Uses
Used in Pharmaceutical Industry:
CHK2 Inhibitor II is used as a research tool for studying the role of CHK2 in various cellular processes, particularly in the context of DNA damage response and apoptosis. It can be employed to investigate the potential therapeutic applications of CHK2 inhibition in cancer treatment and other conditions related to DNA damage and cell cycle regulation.
Used in Cancer Research:
CHK2 Inhibitor II is used as a selective inhibitor for CHK2 in cancer research, aiming to understand its role in tumor development and progression. By inhibiting CHK2, researchers can explore the effects on cell cycle arrest, DNA repair mechanisms, and apoptosis, which may lead to the development of novel cancer therapeutics.
Used in Drug Development:
CHK2 Inhibitor II serves as a lead compound in the development of new drugs targeting the CHK2 pathway. Its selective inhibition of CHK2 can be leveraged to design more potent and specific drugs with improved pharmacological properties, potentially leading to more effective treatments for cancer and other diseases associated with DNA damage response dysregulation.
Used in Radioprotection Studies:
CHK2 Inhibitor II is used as a radioprotective agent in studies involving ionizing radiation. By preventing apoptosis in human T-cells exposed to radiation, it can help researchers understand the mechanisms of radiation-induced cell death and develop strategies to mitigate the harmful effects of radiation exposure.
Biochem/physiol Actions
Chk2 Inhibitor II is a checkpoint kinase 2 inhibitor, which controls the p53 response to DNA breaks induced by radiation, leading to apoptosis. Protection of T-cells from apoptosis implies use as an adjuvant for radiation therapy in cancer. IC50 = 15 nM; Ki = 37 nM. Chk2 Inhibitor II shows 1000-fold greater selectivity for the Chk2 serine/threonine kinase than for the Cdk1/B and CK1 kinases (for which IC50 = 12 μM and 17 μM, respectively). Chk2 Inhibitor II weakly inhibits a panel of 31 other kinases (<25% inhibition at a concentration of 10 μM and prevents apoptosis of human CD4+ and CD8+ T-cells subjected to ionizing radiation (EC50 = 3 μM and 7.6 μM, respectively).
References
1) Arienti et al. (2005), Checkpoint kinases inhibitors: SAR and radioprotective properties of a series of 2-arylbenzimidazoles; J. Med. Chem., 48 1873
2) Pereg et al. (2006), Differential roles of ATM- and Chk2-mediated phosphorylations of Hdmx in response to DNA damage; Mol. Cell. Biol., 26 6819
Check Digit Verification of cas no
The CAS Registry Mumber 516480-79-8 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 5,1,6,4,8 and 0 respectively; the second part has 2 digits, 7 and 9 respectively.
Calculate Digit Verification of CAS Registry Number 516480-79:
(8*5)+(7*1)+(6*6)+(5*4)+(4*8)+(3*0)+(2*7)+(1*9)=158
158 % 10 = 8
So 516480-79-8 is a valid CAS Registry Number.
InChI:InChI=1/C20H14ClN3O2/c21-14-4-8-16(9-5-14)26-15-6-1-12(2-7-15)20-23-17-10-3-13(19(22)25)11-18(17)24-20/h1-11H,(H2,22,25)(H,23,24)
