NBDHEX 是一种谷胱甘肽 S-转移酶 P1-1 抑制剂,也是晚期自噬抑制剂。它诱导肿瘤细胞凋亡,通过抑制GST的催化活性,避免抑制剂被特异性泵从细胞中排出,以及破坏GSTP1-1和关键信号传导因子之间的相互作用,从而起到抗癌的作用。
产品描述
NBDHEX is a potent inhibitor of glutathione S-transferase P1-1 (GSTP1-1).
体外活性
NBDHEX not only is cytotoxic toward the parental small cell lung cancer H69 cell line (LC(50) of 2.3 +/- 0.6 micromol/L) but also overcomes the multidrug resistance of its variant, H69AR, which overexpresses the ATP-binding cassette transporter multidrug resistance-associated protein 1 (MRP1;?LC(50) of 4.5 +/- 0.9 micromol/L).?Drug efflux experiments, done in the presence of a specific inhibitor of MRP1, confirmed that NBDHEX is not a substrate for this export pump [1].
体内活性
NBDHEX, In female mice, treatment results in a statistically significant tumour inhibition (approximately 70%) [1].
Cas No.
787634-60-0
分子式
C12H15N3O4S
分子量
297.33
储存和溶解度
DMSO:125 mg/mL (420.41 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years