Name | SB218078 |
Synonyms | SB218078 SB218078 ?SB-218078 |
CAS | 135897-06-2 |
Molecular Formula | C24H15N3O3 |
Molar Mass | 393.39 |
Storage Condition | Store at RT |
biological activity | SB-218078 is a potent, selective, an ATP-competitive and cell-permeable checkpoint kinase 1 (Chk1) inhibitor inhibits Chk1 phosphorylation of cdc25C with an IC50 of 15 nM. The inhibitory effect of SB-218078 on Cdc2 (IC50 250 nM) and PKC (IC50 1000 nM) was weak. SB-218078 induction of apoptosis by DNA damage and cell cycle arrest. |
Cell Line: | HeLa cells HeLa and HT-29 cells |
Concentration: | 2.5 μM, 5 μM 500 nM, 625 nM |
Incubation Time: | 18 hours 96 hours |
Result: | Abrogated G2 cell cycle arrest caused by γ-irradiation and topoisomerase I inhibition. Enhanced cytotoxicity of DNA damage. Promoted a strong increase of γ-H2AX and apoptosis throughout the lymphoma. |
Animal Model: | C57/Bl6 mice injected with ARF -/- lymphomas |
Dosage: | 5 mg/kg |
Administration: | Intraperitoneal injection; for 16 hours |