HBX 19818
Based on 18 publication(s) in Google Scholar
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.
- Purity: 99.25%
- CAS No.: 1426944-49-1
- Formula: C25H28ClN3O
- Molecular Weight:421.96
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
Publications Citing Use of MedChemExpress (MCE) HBX 19818
More- Cell Metab. 2019 May 7;29(5):1166-1181.e6. [Abstract]
- Nat Commun. 2019 Jan 24;10(1):411. [Abstract]
- Cell Death Differ. 2023 Feb;30(2):527-543. [Abstract]
- Nat Chem Biol. 2017 Dec;13(12):1207-1215. [Abstract]
- Theranostics. 2020 Jul 23;10(20):9332-9347. [Abstract]
- Nat Struct Mol Biol. 2016 Apr;23(4):270-7. [Abstract]
- EMBO J. 2021 Jun 1;40(11):e99692. [Abstract]
- Cell Rep. 2025 Nov 25;44(11):116476. [Abstract]
- Cell Rep. 2024 Aug 5;43(8):114584. [Abstract]
- Cell Rep. 2023 Apr 3;42(4):112339. [Abstract]
- Br J Cancer. 2020 Sep;123(6):1012-1023. [Abstract]
- Br J Cancer. 2020 Apr;122(8):1175-1184. [Abstract]
- Int J Oncol. 2023 Aug;63(2):98. [Abstract]
- J Biol Chem. 2025 Sep 2;301(10):110675. [Abstract]
- Arch Pharm (Weinheim). 2023 Jul;356(7):e2200661. [Abstract]
- Anim Cells Syst. 2024 May 11;28(1):237-250. [Abstract]
- Mol Cell Biol. 2015 Apr 1;35(7):1157-68. [Abstract]
- Dev Growth Differ. 2019 Feb;61(2):176-185. [Abstract]
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WB
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WB
Biological Activity
IC50: 28.1 μM (USP7)[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HCT-116 | IC50 |
2 μM
Compound: HBX19818; Fig 10, Cpd 1
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Anticancer activity against human HCT-116 cells assessed as cell growth inhibition
Anticancer activity against human HCT-116 cells assessed as cell growth inhibition
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[PMID: 32092586] |
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 1426944-49-1
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Appearance Solid
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Molecular Weight 421.96
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Formula C25H28ClN3O
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Color Light yellow to yellow
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SMILES
CN(CCCNC(C1=CC=C(N=C(CCCC2)C2=C3Cl)C3=C1)=O)CC4=CC=CC=C4
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (18)
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Journal Impact Factor
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Most Recent
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Cell Metab
Deubiquitinases Maintain Protein Homeostasis and Survival of Cancer Cells upon Glutathione Depletion. [Abstract]2019 May 7;29(5):1166-1181.e6. PMID: 30799286 -
Nat Commun
Usp7 regulates Hippo pathway through deubiquitinating the transcriptional coactivator Yorkie. [Abstract]2019 Jan 24;10(1):411. PMID: 30679505 -
Cell Death Differ
Targeting USP10 induces degradation of oncogenic ANLN in esophageal squamous cell carcinoma. [Abstract]2023 Feb;30(2):527-543. PMID: 36526897 -
Nat Chem Biol
2017 Dec;13(12):1207-1215. PMID: 28967922
HBX 19818 purchased from MedChemExpress. Usage Cited in: Nat Chem Biol. 2017 Dec;13(12):1207-1215. [Abstract]
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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Theranostics
USP7 targeting modulates anti-tumor immune response by reprogramming Tumor-associated Macrophages in Lung Cancer. [Abstract]2020 Jul 23;10(20):9332-9347. PMID: 32802195 -
Nat Struct Mol Biol
2016 Apr;23(4):270-7. PMID: 26950370 -
EMBO J
2021 Jun 1;40(11):e99692. PMID: 33856059 -
Cell Rep
IGF2BP2 stabilized by USP7 promotes cancer-associated fibroblast activation and attenuates gemcitabine sensitivity in PDAC. [Abstract]2025 Nov 25;44(11):116476. PMID: 41201091 -
Cell Rep
Oxidative stress reprograms the transcriptional coactivator Yki to suppress cell proliferation. [Abstract]2024 Aug 5;43(8):114584. PMID: 39106181 -
Cell Rep
2023 Apr 3;42(4):112339. PMID: 37014752 -
Br J Cancer
WD repeat-containing protein 1 maintains β-Catenin activity to promote pancreatic cancer aggressiveness. [Abstract]2020 Sep;123(6):1012-1023. PMID: 32601462 -
Br J Cancer
2020 Apr;122(8):1175-1184. PMID: 32015510 -
Int J Oncol
circRPS19 affects HK2‑mediated aerobic glycolysis and cell viability via the miR‑125a‑5p/USP7 pathway in gastric cancer. [Abstract]2023 Aug;63(2):98. PMID: 37449524 -
J Biol Chem
Ubiquitin-specific protease 7 promotes the growth and oncogenic potential of acute myeloid leukemia cells through the deubiquitination and upregulation of LRRK2. [Abstract]2025 Sep 2;301(10):110675. PMID: 40907896 -
Arch Pharm (Weinheim)
2023 Jul;356(7):e2200661. PMID: 37196427 -
Anim Cells Syst
Blocking SLC7A11 attenuates the proliferation of esophageal squamous cell carcinoma cells. [Abstract]2024 May 11;28(1):237-250. PMID: 38741950 -
Mol Cell Biol
2015 Apr 1;35(7):1157-68. PMID: 25605328
HBX 19818 purchased from MedChemExpress. Usage Cited in: Mol Cell Biol. 2015 Apr 1;35(7):1157-68. [Abstract]
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.
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Dev Growth Differ
Ubiquitin-specific protease 7 (USP7) is essential for endometrial stromal cell decidualization in mice. [Abstract]2019 Feb;61(2):176-185. PMID: 30628051
Solvent & Solubility
1M HCl : 100 mg/mL (236.99 mM; ultrasonic and adjust pH to 1 with HCl)
DMSO : 20 mg/mL (47.40 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2 mg/mL (4.74 mM); Clear solution
This protocol yields a clear solution of ≥ 2 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocol
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
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Data Sheet (273 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO / 1M HCl | 1 mM | 2.3699 mL | 11.8495 mL | 23.6989 mL | 59.2473 mL |
| 5 mM | 0.4740 mL | 2.3699 mL | 4.7398 mL | 11.8495 mL | |
| 10 mM | 0.2370 mL | 1.1849 mL | 2.3699 mL | 5.9247 mL | |
| 15 mM | 0.1580 mL | 0.7900 mL | 1.5799 mL | 3.9498 mL | |
| 20 mM | 0.1185 mL | 0.5925 mL | 1.1849 mL | 2.9624 mL | |
| 25 mM | 0.0948 mL | 0.4740 mL | 0.9480 mL | 2.3699 mL | |
| 30 mM | 0.0790 mL | 0.3950 mL | 0.7900 mL | 1.9749 mL | |
| 40 mM | 0.0592 mL | 0.2962 mL | 0.5925 mL | 1.4812 mL | |
| 1M HCl | 50 mM | 0.0474 mL | 0.2370 mL | 0.4740 mL | 1.1849 mL |
| 60 mM | 0.0395 mL | 0.1975 mL | 0.3950 mL | 0.9875 mL | |
| 80 mM | 0.0296 mL | 0.1481 mL | 0.2962 mL | 0.7406 mL | |
| 100 mM | 0.0237 mL | 0.1185 mL | 0.2370 mL | 0.5925 mL |