315702-40-0
中文名称
化合物CEEFOURIN 1
英文名称
Ceefourin 1
CAS
315702-40-0
分子式
C11H10N4S3
分子量
294.42
MOL 文件
315702-40-0.mol
315702-40-0 结构式
基本信息
中文别名
化合物CEEFOURIN 1 英文别名
Ceefourin 15-[(2-Benzothiazolylthio)methyl]-2,4-dihydro-4-methyl-3H-1,2,4-triazole-3-thione
P-glycoprotein,chemosensitizers,inhibit,efflux,protein,resistance,Ceefourin 1,Ceefourin1,MRP4,HEK293,D-luciferin,ABC,ABCG2,P-gp,multidrug,MRP1,Inhibitor,neuroblastoma,Ceefourin-1,ABCC1,BCRP
常见问题列表
生物活性
Ceefourin 1 是一种有效且高度选择性的多药抗性蛋白 4 (MRP4) 抑制剂。Ceefourin 1 抑制多种 MRP4 底物的转运，但对其他 ABC 转运蛋白没有选择性。Ceefourin 1 是一种苯并噻唑，主要用作高危神经母细胞瘤的化学增敏剂。靶点
MRP4
体外研究
Ceefourin 1 are highly selective for MRP4 over other ABC transporters, including P-glycoprotein (P-gp), ABCG2 (Breast Cancer Resistance Protein; BCRP) and MRP1 (ABCC1). Ceefourin 1 has limited off-target effects and high stability.
Ceefourin 1 (100 nM-100 μM) has low cellular toxicity (IC
50
>50) in two normal (HSF, MRC5), seven neuroblastoma (BE(2)-C, IMR-32, LAN-1, IMR-32, SK-N-SH, NBL-WN, SHEP) and four other human cancer cell lines (HEPG2, LNCap, SJ-G2, MCF7).
Ceefourin 1 has an IC
50
of 2.5 μM in HEK293 cell. Ceefourin 1 blocks D-luciferin efflux with an IC
50
of 1.5 μM.