Rpn11-IN-1
(Synonyms: Capzimin intermediate) 目录号 : GC32407
Rpn11-IN-1是一种有效的选择性蛋白酶体亚基Rpn11抑制剂，IC50为390nM。
Cas No.:2084867-65-0
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Cell experiment: | 293T, A549 and HCT 116 cell lines are cultured in DMEM with 10% FBS in white, clear-bottom tissue culture-treated 96-well plates. Cells are treated with different concentrations of inhibitor compounds (e.g., Rpn11-IN-1; 0.01, 0.1, 1, 10, and 100 μM) in triplicates for 72 h at 37°C with 5% CO2 in air. CellTiter-Glo reagent is added to the 96 well plates to measure cell viability. Luminescence values are measured in PHERAstar microplate reader. Collected data is normalized to DMSO control and fit to a dose-response equation to determine IC50 values[1]. |
References: [1]. Perez C, et al. Discovery of an Inhibitor of the Proteasome Subunit Rpn11. J Med Chem. 2017 Feb 23;60(4):1343-1361. | |
Rpn11-IN-1 is a potent and selective inhibitor of proteasome subunit Rpn11 with an IC50 of 390 nM.
Rpn11 is a Zn2+-dependent metalloisopeptidase that hydrolyzes ubiquitin from tagged proteins that are trafficked to the proteasome for degradation. When inhibition of Rpn11-IN-1 (Compound 35) against Rpn11 is measured in the presence of Zn(cyclen)2+ (100 μM), a significant loss in activity against Rpn11 is observed (IC50=77.4 μM vs. 0.39 μM). The observed IC50 value shift is attributed to the ability of Zn(cyclen)2+ to compete/titrate Rpn11-IN-1 away from Rpn11. Rpn11-IN-1 blocks proliferation of tumor cells in culture. Rpn11-IN-1 has an IC50 of 2.1 μM and 3.8 μM against 293T and A549 cells, respectively[1].
[1]. Perez C, et al. Discovery of an Inhibitor of the Proteasome Subunit Rpn11. J Med Chem. 2017 Feb 23;60(4):1343-1361.
| Cas No. | 2084867-65-0 | SDF | |
| 别名 | Capzimin intermediate | ||
| Canonical SMILES | SC1=CC=CC2=C1N=CC(C(NCCC3=NC=CS3)=O)=C2 | ||
| 分子式 | C15H13N3OS2 | 分子量 | 315.41 |
| 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。 |
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| 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 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.1705 mL | 15.8524 mL | 31.7048 mL |
| 5 mM | 0.6341 mL | 3.1705 mL | 6.341 mL |
| 10 mM | 0.317 mL | 1.5852 mL | 3.1705 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。