产品
编 号:F611254
分子式:C12H15N3O4S
分子量:297.33
产品类型
结构图
CAS No: 787634-60-0
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产品详情
生物活性:
NBDHEX is a potent glutathione S-transferase P1-1 (GSTP1-1) inhibitor. NBDHEX induces apoptosis of tumor cells. NBDHEX acts as an anticancer agent by inhibiting GSTs catalytic activity, avoiding inconvenience of the inhibitor extrusion from the cell by specific pumps and disrupting the interaction between the GSTP1-1 and key signaling effectors. NBDHEX can also act as late-phase autophagy inhibitor.
体内研究:
NBDHEX (0.8 -80 mg/kg/天;口服给药;每天;持续 15 天;SCID 雌性小鼠) 处理导致具有统计学意义的肿瘤抑制 (约 70%)。Animal Model:SCID female mice (4-5 weeks) injected with Me501cells
Dosage:0.8 mg/kg/day, 8.0 mg/kg/day or 80 mg/kg/day
Administration:Oral administration; daily; for 15 days
Result:A statistically significant tumour inhibition (approximately 70%) was observed.
体外研究:
NBDHEX (0.05 -20 μM;48 hours;H69和H69AR cells) 对肺癌H69和H69AR细胞具有细胞毒性。 NBDHEX (0-5 μM;24 hours;H69AR 细胞) 处理导致 H69AR 细胞系发生剂量依赖性细胞凋亡。 NBDHEX (3 μM;1-12 小时;H69AR 细胞) 处理增加 JNK 的磷酸化/c-Jun 在 H69AR 细胞中呈时间依赖性。 NBDHEX 处理显示 p38MAPK 磷酸化显著增加,并且还增加H69 细胞中 GSSG 含量随时间变化。