1. Cell Cycle/DNA Damage
  2. Deubiquitinase
  3. HBX 19818

HBX 19818 

Cat. No.: HY-17540 Purity: 98.93%
Handling Instructions

HBX 19818 is a specific inhibitor of ubiquitin-specific protease 7 (USP7), with an IC50 of 28.1 μM.

For research use only. We do not sell to patients.

HBX 19818 Chemical Structure

HBX 19818 Chemical Structure

CAS No. : 1426944-49-1

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10 mM * 1 mL in DMSO USD 176 In-stock
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Customer Review

Based on 8 publication(s) in Google Scholar

Top Publications Citing Use of Products

    HBX 19818 purchased from MCE. Usage Cited in: Mol Cell Biol. 2015 Apr 1;35(7):1157-68.

    Western blot analysis of the chromatin fraction of HCT116 cells after treatment with the USP7 inhibitor HBX19818 for 4 or 8 h at 50 μM. Expression levels of USP7, RING1B, BMI1, and Ub-H2A are analyzed.

    HBX 19818 purchased from MCE. Usage Cited in: Nat Chem Biol. 2017 Dec;13(12):1207-1215.

    The effects of HBX19818 on FLT 3 expression in FLT 3-ITD-expressing Ba/F3 cells after 22 h of treatment. The effects of P22077 on FLT 3 levels in FLT 3-ITD-expressing Ba/F3 cells after 22 h of treatment.
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    Description

    HBX 19818 is a specific inhibitor of ubiquitin-specific protease 7 (USP7), with an IC50 of 28.1 μM.

    IC50 & Target

    IC50: 28.1 μM (USP7)[1]

    In Vitro

    HBX 19818 is an inhibitor of USP7, with an IC50 of 28.1 μM. HBX 19818 shows no effects on USP8, USP5, USP10, CYLD, UCH-L1, UCH-L3 or on SENP1, a SUMO protease, with IC50s of > 200 μM. HBX 19818 selectively inhibits USP7 with IC50 of ∼6 μM in in human cancer cells. In addition, HBX 19818 (1.5, 4, 12, 36, or 100 μM) inhibits USP7 deubiquitination of polyubiquitinated p53. HBX 19818 (30 μM) also causes significantly higher levels of Mdm2 polyubiquitinated forms in USP7-overproducing HEK293 cells than those in DMSO-treated control cells. HBX 19818 inhibits HCT116 proliferation in a dose-dependent manner, with an IC50 of ∼2 μM[1].

    Molecular Weight

    421.96

    Formula

    C₂₅H₂₈ClN₃O

    CAS No.

    1426944-49-1

    SMILES

    CN(CCCNC(C1=CC=C(N=C(CCCC2)C2=C3Cl)C3=C1)=O)CC4=CC=CC=C4

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : 3.5 mg/mL (8.29 mM; Need ultrasonic and warming)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.3699 mL 11.8495 mL 23.6989 mL
    5 mM 0.4740 mL 2.3699 mL 4.7398 mL
    10 mM --- --- ---
    *Please refer to the solubility information to select the appropriate solvent.
    References
    Kinase Assay
    [1]

    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].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Cell Assay
    [1]

    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].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    References
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