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| CHK2 INHIBITOR II Basic information |
| Product Name: | CHK2 INHIBITOR II | | Synonyms: | 2-(4-(4-CHLOROPHENOXY)PHENYL)-1H-BENZO[D]IMIDAZOLE-5-CARBOXAMIDE, >98%;BML-277, >98%;BML-277 (C 3742);CS-1761;BML-277,CHK2 INHIBITOR II;CHK2 INHIBITOR II; C 3742; BML277; BML 277;Chk2 Inhibitor II - CAS 516480-79-8 - Calbiochem;InSolution Chk2 Inhibitor II - CAS 516480-79-8 - Calbiochem | | CAS: | 516480-79-8 | | MF: | C20H14ClN3O2 | | MW: | 363.8 | | EINECS: | | Product Categories: | Inhibitors;API | | Mol File: | 516480-79-8.mol |
| CHK2 INHIBITOR II Chemical Properties |
| Boiling point | 637.1±63.0 °C(Predicted) | | density | 1.390±0.06 g/cm3(Predicted) | | storage temp. | 2-8°C | | solubility | DMSO: 18 mg/mL | | form | solid | | pka | 10.40±0.10(Predicted) | | color | tan | | Stability: | Stable for 1 year from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20°C for up to 3 months. |
| CHK2 INHIBITOR II Usage And Synthesis |
| Description | Chk2 inhibitor II is a selective, ATP-competitive inhibitor of the DNA damage control kinase, checkpoint kinase 2 (IC50 = 15 nM). It has been shown to prevent apoptosis in human T-cells exposed to ionizing radiation (EC50 = 3-7.6 μM). This compound has been used to target the role of Chk2 in cellular signaling in response to DNA damage. | | Uses | Chk2 Inhibitor II is a selective APT-competitive inhibitors of the DNA damage response signaling enzyme checkpoint kinase 2 (CHK2). | | 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 |
| CHK2 INHIBITOR II Preparation Products And Raw materials |
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