产品
编 号:F137103
分子式:C24H15N3O3
分子量:393.39
产品类型
结构图
CAS No: 135897-06-2
联系客服
产品详情
生物活性:
SB-218078 is a potent, selective, ATP-competitive and cell-permeable checkpoint kinase 1 (Chk1) inhibitor that inhibits Chk1 phosphorylation of cdc25C with an IC50 of 15 nM. SB-218078 is less potently inhibits Cdc2 (IC50 of 250 nM) and PKC (IC50 of 1000 nM). SB-218078 causes apoptosis by DNA damage and cell cycle arrest.
体内研究:
SB-218078 (5 mg/kg; intraperitoneal injection; for 16 hours; C57/Bl6 mice) treatment could promote a strong increase of γ-H2AX and apoptosis throughout the lymphoma, while having no effect on a healthy spleen in Myc-induced lymphomas mouse model.Animal Model:C57/Bl6 mice injected with ARF-/- lymphomas
Dosage:5 mg/kg
Administration:Intraperitoneal injection; for 16 hours
Result:Promoted a strong increase of γ-H2AX and apoptosis throughout the lymphoma.
体外研究:
SB-218078 (2.5-5 μM; 18 hours; HeLa cells) treatment abrogates G2 cell cycle arrest caused by either γ-irradiation or a topoisomerase I Topotecan inhibition.SB-218078 (500-625 μM; 96 hours; HeLa and HT-29 cells) treatment significantly increases the cytotoxicity of DNA damage .