PU 23 是一种非羧基多药耐药蛋白 4 (MRP4) 抑制剂，作为降低抗癌剂 6-Mercaptopurine 耐药性的活性剂。
货号:ajcx27864
CAS:817635-93-1
分子式:C21H19N3O3S2
分子量：425.52
溶解度:Soluble in DMSO
纯度：98%
存储：Store at -20°C
库存：现货

Background:

PU 23 is a Multidrug resistance protein 4 (MRP4/ABCC4) inhibitor. MRP4 is an ATP-binding cassette (ABC) transporter. It is associated with multidrug resistance (MDR), which is becoming a growing challenge to the treatment of cancer and infections^[1].

Then compound?PU 23?was discovered to improve HEK293/MRP4 cell sensibility to 6-MP dramatically, and low concentration?PU 23?(5 μM) achieved the equivalent effect of 50 μM MK571. The accumulation of 6-MP was determined by validated high-performance liquid chromatography methods, and pretreatment of the HEK293/MRP4 cells with 50 μM MK571 or?PU 23?resulted in significantly increased accumulation of 6-MP by approximately 1.5 times. This compound was first reported with a novel scaffold compared with previously known MRP4 inhibitors, which is a hopeful molecular tool that can be used for overcoming multidrug resistance research^[2].

参考文献:
[1]: Chen Y, Yuan X, et al. Discovery of novel multidrug resistance protein 4 (MRP4) inhibitors as active agents reducing resistance to anticancer drug 6-Mercaptopurine (6-MP) by structure and ligand-based virtual screening. PLoS One. 2018 Oct 15;13(10):e0205175.?

Protocol:

Cell experiment [1]:
Cell lines	HEK293/MRP4 cell line
Preparation Method	MRP4 was overexpressed in the HEK293/MRP4 cell line. The PU 23 compounds in the presence of 6-MP(15 μM), using MK571 as the positive control.?Cell viability was assessed using sulforhodamine B (SRB)
Reaction Conditions	10 μM PU 23 for 72h.
Applications	PU 23?showed the highest activity with an inhibition rate of 81.71% at the concentration of 10 μM with 6-MP and only 15.26% without 6-MP.?It increased cell sensitivity to 6-MP, but not toxic on its own.
参考文献: [1]. Chen Y, Yuan X, et al. Discovery of novel multidrug resistance protein 4 (MRP4) inhibitors as active agents reducing resistance to anticancer drug 6-Mercaptopurine (6-MP) by structure and ligand-based virtual screening. PLoS One. 2018 Oct 15;13(10):e0205175.?