| Name | BML-277 |
| Synonyms | C 3742 BML277 BML-277 CS-1761 BML 277 BML-277 (C 3742) CHK2 INHIBITOR II BML-277,CHK2 INHIBITOR II 2-(4-(4-CHLOROPHENOXY)PHENYL)-1H-BENZO[D]IMIDAZOLE-5-CARBOXAMIDE |
| CAS | 516480-79-8 |
| Molecular Formula | C20H14ClN3O2 |
| Molar Mass | 363.8 |
| Density | 1.390±0.06 g/cm3(Predicted) |
| Boling Point | 637.1±63.0 °C(Predicted) |
| Solubility | DMSO: ≥ 55 mg/mL |
| Appearance | solid |
| Color | tan |
| pKa | 10.40±0.10(Predicted) |
| Storage Condition | 2-8°C |
| 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. |
| In vitro study | CHK2 Inhibitor II is 1000-fold more selective for Chk2 serine/threonine kinases than Cdk1/B and CK1 kinases and is a potent and selective small molecule Inhibitor, it has radioprotective effect on human T cells. Administration of a combination of CHK2 inhibitor II and an ERK inhibitor resulted in more apoptosis than administration alone. |
| In vivo study | The mice with transplanted tumor of SUDHL6 DLBCL were given intraperitoneal injection of vehicle, ERK inhibitor (5 mg/kg), CHK2 inhibitor II (1 mg/kg) or combination every other day, for 20 consecutive days, no fatal formation, significant weight loss, or overt abnormalities were noted. 5 mg/kg ERK inhibitor and 1 mg/kg CHK2 inhibitor II moderately inhibited tumor growth, but the effect of combined administration was more obvious. |
| WGK Germany | 3 |
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 2.749 ml | 13.744 ml | 27.488 ml |
| 5 mM | 0.55 ml | 2.749 ml | 5.498 ml |
| 10 mM | 0.275 ml | 1.374 ml | 2.749 ml |
| 5 mM | 0.055 ml | 0.275 ml | 0.55 ml |
| biological activity | Chk2 Inhibitor II (BML-277) is a ATP competitive inhibitor of Chk2. The IC50 is 15 nM. Its selectivity for Chk2 was more than 1000-fold higher than that for Chk1 and Cdk1/B kinases. Chk2 Inhibitor II (BML-277) dose-dependently protects human CD4 (+) and CD8 (+) T cells from apoptosis induced by ionizing radiation. |
| target | TargetValue Chk2 (Cell-free say) 15 nM |
| Target | Value |
| Chk2 (Cell-free assay) | 15 nM |
| in vitro study | CHK2 Inhibitor II The selectivity of Chk2 serine/threonine kinase is 1000 times higher than that of Cdk1/B and CK1 kinase, and it is an effective and selective small molecule inhibitor, radiation protection against human T cells. Administration of CHK2 inhibitor II and ERK inhibitors in combination caused more apoptosis than its administration alone. |
| in vivo study | SUDHL6 DLBCL transplanted tumor mice were intraperitoneally injected with vehicle, ERK inhibitor (5 mg/kg), CHK2 inhibitor II (1 mg/kg) or combination every other day for 20 consecutive days, no fatal formation, significant weight loss or significant abnormality was found. 5 mg/kg ERK inhibitor and 1 mg/kg CHK2 inhibitor II can moderately inhibit tumor growth, but the effect of combined administration is more obvious. |