IMP-1710
目录号 : GC48614
A clickable UCH-L1 inhibitor
Cas No.:2383117-96-0
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
IMP-1710 is an inhibitor of ubiquitin C-terminal hydrolase L1 (UCH-L1; IC50 = 38 nM in a fluorescence polarization assay) that contains an alkyne moiety for use in click chemistry reactions.1 It is selective for UCH-L1 over a panel of 20 deubiquitinating enzymes at 1 µM. IMP-1710 inhibits TGF-β1-induced fibroblast-to-myofibroblast transition (FMT) in primary lung fibroblasts isolated from patients with idiopathic pulmonary fibrosis (IC50 = 740 nM). It has been used for labeling UCH-L1 in cell-based assays, followed by click reactions with azide-modified TAMRA and biotin capture reagents.
1.Panyain, N., Godinat, A., Lanyon-Hogg, T., et al.Discovery of a potent and selective covalent inhibitor and activity-based probe for the deubiquitylating enzyme UCHL1, with antifibrotic activityJ. Am. Chem. Soc.142(28)12020-12026(2020)
| Cas No. | 2383117-96-0 | SDF | |
| Canonical SMILES | O=C([C@H]1N(C#N)CCC1)N2C3=CC=CC(C(C4=C5)=CNC4=NC=C5C#C)=C3CC2 | ||
| 分子式 | C23H19N5O | 分子量 | 381.4 |
| 溶解度 | Chloroform: 10 mg/ml,Ethanol: 5 mg/ml | 储存条件 | -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 | 2.6219 mL | 13.1096 mL | 26.2192 mL |
| 5 mM | 0.5244 mL | 2.6219 mL | 5.2438 mL |
| 10 mM | 0.2622 mL | 1.311 mL | 2.6219 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。
Discovery of a Potent and Selective Covalent Inhibitor and Activity-Based Probe for the Deubiquitylating Enzyme UCHL1, with Antifibrotic Activity
J Am Chem Soc 2020 Jul 15;142(28):12020-12026.PMID:32579346DOI:PMC7366380
Ubiquitin carboxy-terminal hydrolase L1 (UCHL1) is a deubiquitylating enzyme that is proposed as a potential therapeutic target in neurodegeneration, cancer, and liver and lung fibrosis. Herein we report the discovery of the most potent and selective UCHL1 probe (IMP-1710) to date based on a covalent inhibitor scaffold and apply this probe to identify and quantify target proteins in intact human cells. IMP-1710 stereoselectively labels the catalytic cysteine of UCHL1 at low nanomolar concentration in cells. We further demonstrate that potent and selective UCHL1 inhibitors block pro-fibrotic responses in a cellular model of idiopathic pulmonary fibrosis, supporting the potential of UCHL1 as a potential therapeutic target in fibrotic diseases.