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HBX 19818 Sale

(Synonyms: 9-氯-5,6,7,8-四氢-N-[3-[甲基(苄基)氨基]丙基]-2-吖啶甲酰胺) 目录号 : GC36211

HBX19818 is a specific inhibitor of USP7 with an IC 50 of 28.1 μM.

HBX 19818 Chemical Structure

Cas No.:1426944-49-1

规格 价格 库存 购买数量
10mM (in 1mL DMSO)
¥2,005.00
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2mg
¥1,080.00
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5mg
¥2,160.00
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10mg
¥3,555.00
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50mg
¥9,900.00
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Sample solution is provided at 25 µL, 10mM.

产品文档

Quality Control & SDS

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实验参考方法

Kinase experiment:

The ability of HBX 19818 and HBX 28,258 to inhibit a panel of deubiquitinating enzymes, including UCH-L3 (13 pM), USP7 (100 pM), USP8 (1.36 nM), UCH-L1 (2.5 nM), USP5 (10 nM), USP20 (10 nM), and USP2 (500 pM), is tested using the UbAMC substrate (300 nM). The potential effects of HBX 19818 and HBX 28,258 are also tested on the enzymatic activities of SENP1 (80 pM), cathepsin-B (100 pM), and caspase-3 (100 pM) using the SUMO1-AMC (750 nM), ZRR-AMC (3 μM), and DEVD-AMC (250 nM) substrates, respectively. All enzymes are tested in USP7 reaction buffer (50 mM Tris-HCl [pH 7.6], 0.5 mM EDTA, 5 mM DTT, 0.01% Triton X-100, and 0.05 mg/mL serum albumin), except for two enzymes, USP8 (same buffer but pH 8.8) and caspase-3 (100 mM HEPES [pH 7.5], 10% sucrose, and 0.1% CHAPS). All enzymes are pre-incubated with DMSO or compounds (including HBX 19818) for 30 min at room temperature, and the enzymatic reaction is initiated by adding the substrate of interest. The reaction mixture is incubated at room temperature for 1 hr, and the reaction is stopped by adding acetic acid (100 mM). The reactions are monitored using the PHERAstar[1].

Cell experiment:

HCT116 cell proliferation is evaluated by incubating HCT116 cells for 30 min in culture medium containing 10 µM 5- bromo-2-deoxyuridine (BrdU), which is incorporated into the DNA of proliferating cells. Cells are then harvested by trypsin treatment, collected by centrifugation, and the pellet is resuspended and incubated in 70% ethanol for 30 min at 4°C. After centrifugation and supernatant removal, DNA is denaturated by incubating it in 2 N HCl for 30 min at room temperature. The percentage of BrdU-containing cells is then determined by flow cytometry, making it possible to quantify proliferating cells. Cell cycle is evaluated after treatment with HBX 19818 for 24 hr, followed by fixing detached cells and trypsinized cells in 70% ethanol for 30 minutes at 4°C. Cells are then incubated in PBS supplemented with 1% BSA, 0.5% Tween 20, 50 µg/mL RNase A and 50 µg/mL propidiumiodide for 30 minutes at 37°C. Samples are analyzed on a FACSort fluorocytometer. The percentage of cells in the different phases of the cell cycle is calculated using Multicycle software[1].

References:

[1]. Reverdy C, et al. Discovery of specific inhibitors of human USP7/HAUSP deubiquitinating enzyme. Chem Biol. 2012 Apr 20;19(4):467-77.

产品描述

HBX19818 is a specific inhibitor of USP7 with an IC 50 of 28.1 μM.

[1] Céline Reverdy, et al. Chem Biol. 2012 Apr 20;19(4):467-77.

Chemical Properties

Cas No. 1426944-49-1 SDF
别名 9-氯-5,6,7,8-四氢-N-[3-[甲基(苄基)氨基]丙基]-2-吖啶甲酰胺
Canonical SMILES CN(CCCNC(C1=CC=C(N=C(CCCC2)C2=C3Cl)C3=C1)=O)CC4=CC=CC=C4
分子式 C25H28ClN3O 分子量 421.96
溶解度 DMSO: 20 mg/mL (47.40 mM) 储存条件 Store at -20°C
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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。
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1 mg 5 mg 10 mg
1 mM 2.3699 mL 11.8495 mL 23.6989 mL
5 mM 0.474 mL 2.3699 mL 4.7398 mL
10 mM 0.237 mL 1.1849 mL 2.3699 mL
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