| Identification | Back Directory | [Name]
CHK2 INHIBITOR II | [CAS]
516480-79-8 | [Synonyms]
C 3742
BML-277
CS-1761
BML-277, >98%
BML-277 (C 3742)
C 3742 BML-277
Chk2 Inhibitor II hydrate
BML-277,CHK2 INHIBITOR II
Chk2 Inhibitor II (BML-277)
InSolution? 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
2-[4-(4-chlorophenoxy)phenyl]-3H-benzimidazole-5-carboxamide
2-[4-(4-chlorophenoxy)phenyl]-1H-benzimidazole-6-carboxamide
1H-Benzimidazole-6-carboxamide, 2-[4-(4-chlorophenoxy)phenyl]-
2-(4-(4-CHLOROPHENOXY)PHENYL)-1H-BENZO[D]IMIDAZOLE-5-CARBOXAMIDE
2-(4-(4-Chlorophenoxy)phenyl)-1H-benzimidazole-5-carboxamide hydrate
2-[4-(4-Chlorophenoxy)phenyl]-1H-benzimidazole-5-carboxylic acid amide
2-(4-(4-CHLOROPHENOXY)PHENYL)-1H-BENZO[D]IMIDAZOLE-5-CARBOXAMIDE, >98% | [Molecular Formula]
C20H14ClN3O2 | [MDL Number]
MFCD08276917 | [MOL File]
516480-79-8.mol | [Molecular Weight]
363.8 |
| Chemical Properties | Back Directory | [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. |
| Hazard Information | Back Directory | [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 |
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