PU 23
目录号 : GC50595
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。
Cas No.:817635-93-1
Sample solution is provided at 25 µL, 10mM.
;)
,-1-7$$$37316672.jpg');)
;)
;)
$$$36806353.jpg');)
;33(7)%EF%BC%9A546-561$$$37156877.jpg');)
;)
;)
;)
%201124-1138.$$$35908550.jpg');)
%20766-780.$$$37100057.jpg');)
%20418-432.$$$36893736.jpg');)
%EF%BC%9A-240-255.$$$35108512.jpg');)
533-545$$$36543525.jpg');)
%201-13.$$$36600053.jpg');)
;)
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
| 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. |
|
References: [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. |
|
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].
References:
[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.?
PU 23 是一种多药耐药蛋白 4 (MRP4/ABCC4) 抑制剂。 MRP4 是一种 ATP 结合盒 (ABC) 转运蛋白。它与多药耐药性 (MDR) 相关，这正成为癌症和感染治疗面临的越来越大的挑战[1]。
随后发现化合物 PU 23 可显着提高 HEK293/MRP4 细胞对 6-MP 的敏感性，低浓度 PU 23 (5 μM) 达到与 50 μM MK571 相当的效果。 6-MP 的积累是通过经过验证的高效液相色谱法确定的，用 50 μM MK571 或 PU 23 预处理 HEK293/MRP4 细胞导致 6-MP 的积累显着增加约 1.5 倍。与先前已知的 MRP4 抑制剂相比，该化合物首次被报道具有新型支架，是一种有望用于克服多药耐药性研究的分子工具[2]。
| Cas No. | 817635-93-1 | SDF | |
| Canonical SMILES | O=C(NC(=S)NC1=CC=C(C=C1)[S](=O)(=O)NCC1=CC=CC=C1)C1=CC=CC=C1 | ||
| 分子式 | C21H19N3O3S2 | 分子量 | 425.52 |
| 溶解度 | Soluble in DMSO | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
||
| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
 |
1 mg | 5 mg | 10 mg |
| 1 mM | 2.3501 mL | 11.7503 mL | 23.5007 mL |
| 5 mM | 0.47 mL | 2.3501 mL | 4.7001 mL |
| 10 mM | 0.235 mL | 1.175 mL | 2.3501 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。