GlpBio

Rpn11-IN-1

目录号: GC32407纯度: >98%同义词: Capzimin intermediate
COASDSData Sheet
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。
Rpn11-IN-1
Cas No.: 2084867-65-0
规格价格库存数量操作
250mg询价现货
1
500mg询价现货
1
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文献被引

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    183(7):1867-1883 (2020)
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产品描述 Description

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.

实验参考方法 Experimental Reference Method

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.

产品文档 Product Documents

Purity:>98%
COASDSData Sheet

化学性质Chemical Properties

CAS 号
2084867-65-0
同义词
Capzimin intermediate
SMILES
SC1=CC=CC2=C1N=CC(C(NCCC3=NC=CS3)=O)=C2
分子式
C15H13N3OS2
分子量
315.41 g/mol
溶解性
Soluble in DMSO
保存条件
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°C，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。

计算工具摩尔浓度 / 稀释 / 分子量 / 单位换算 / 体内配方 / 溶解度

g/mol