SB218078
- CAS号:135897-06-2
- 英文名:SB218078
- 中文名:SB218078
- CBNumber:CB51075435
- 分子式:C24H15N3O3
- 分子量:393.39
- MOL File:135897-06-2.mol
- 熔点 :>340 °C
- 密度 :1.80±0.1 g/cm3(Predicted)
- 储存条件 :Store at RT
- 溶解度 :≤5mg/ml in DMSO;5mg/ml in dimethyl formamide
- 形态 :crystalline solid
- 酸度系数(pKa) :9.75±0.20(Predicted)
- 颜色 :Light yellow to yellow
SB218078性质、用途与生产工艺
- 生物活性 SB-218078 是一种有效的,选择性,ATP 竞争性且细胞可渗透的检查点激酶 1 (Chk1) 抑制剂,可抑制 cdc25C 的 Chk1 磷酸化,IC50 为 15 nM。SB-218078 对 Cdc2 (IC50 为 250 nM) 和 PKC (IC50 为 1000 nM) 的抑制作用较弱。SB-218078 通过 DNA 损伤和细胞周期停滞诱导细胞凋亡。
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靶点
Chk1
15 nM (IC 50 )
Cdc2
250 nM (IC 50 )
PKC
1000 nM (IC 50 )
Apoptosis
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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 .Cell Cycle Analysis
Cell Line: HeLa cells Concentration: 2.5 μM, 5 μM Incubation Time: 18 hours Result: Abrogated G2 cell cycle arrest caused by γ-irradiation and topoisomerase I inhibition. Cell Cytotoxicity Assay
Cell Line: HeLa and HT-29 cells Concentration: 500 nM, 625 nM Incubation Time: 96 hours Result: Enhanced cytotoxicity of DNA damage. -
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.
- 公司名称:TOCRIS-US
- 联系电话:--
- 电子邮件:customerservice@tocris.co.uk
- 国家:英国
- 产品数:5729
- 优势度:77