SJB2-043
Based on 4 publication(s) in Google Scholar
SJB2-043 is an inhibitor of the native USP1/UAF1 complex with IC50 of 544 nM.
For research use only. We do not sell to patients.
- Purity: 99.52%
- CAS No.: 63388-44-3
- Formula: C17H9NO3
- Molecular Weight:275.26
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocol
- Purity & Documentation
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) SJB2-043
More
Biological Activity
IC50: 544 nM (USP1/UAF1)[1]
SJB2-043 causes a dose-dependent decrease in ubiquitin-specific protease 1 (USP1) levels and a concomitant degradation of inhibitor of DNA-binding-1 (ID1) protein in the K562 cells at a micromolar drug concentration. SJB2-043 also causes a decrease in the levels of other ID proteins, namely ID2 and ID3 in K562 cells. SJB2-043 causes a dose-dependent decrease in the number of viable K562 cells, with an EC50 of approximately 1.07 μM. Moreover, SJB2-043 induces apoptosis of K562 cells in a dose-dependent manner[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. 63388-44-3
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Appearance Solid
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Molecular Weight 275.26
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Formula C17H9NO3
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Color Green to dark green
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SMILES
O=C1C2=C(N=C(C3=CC=CC=C3)O2)C(C4=CC=CC=C41)=O
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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 (4)
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Journal Impact Factor
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Most Recent
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Trends Pharmacol Sci
Toward understanding ubiquitin-modifying enzymes: from pharmacological targeting to proteomics. [Abstract]2014 Apr;35(4):187-207. PMID: 24717260 -
J Med Chem
Discovery of Potent OTUB1/USP8 Dual Inhibitors Targeting Proteostasis in Non-Small-Cell Lung Cancer. [Abstract]2022 Oct 27;65(20):13645-13659. PMID: 36221183 -
FASEB J
2021 Aug;35(8):e21800. PMID: 34324733 -
Curr Issues Mol Biol
SJB2-043, a USP1 Inhibitor, Suppresses A549 Cell Proliferation, Migration, and EMT via Modulation of PI3K/AKT/mTOR, MAPK, and Wnt Signaling Pathways. [Abstract]2025 Feb 27;47(3):155. PMID: 40136409
Solvent & Solubility
DMSO : 3.33 mg/mL (12.10 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)
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.
Working solution concentration: 0.22 mg/mL
Protocol
The in vitro enzymatic assays are performed using ubiquitin-AMC (Ub-7-amido-4methylcoumarin) as a substrate in a reaction buffer containing 20 mM HEPES-KOH (pH 7.8), 20 mM NaCl, 0.1 mg/mL ovalbumin, 0.5 mM EDTA and 10 mM dithiothreitol. The fluorescence is measured by FluoStar Galaxy Fluorometer. For the Ub-vinylsulfone (VS) assay, the proteins are incubated with Ub-VS at 0.5 μM final concentration for 45 min at 30°C, followed by the immunoblotting analysis[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Leukemic cell lines are grown in RPMI 1640 medium supplemented with 10% fetal bovine serum and penicillin/streptomycin. Hela cells and U2OS cells are grown in DMEM supplemented with 10% fetal bovine serum and penicillin/streptomycin. USP1 inhibitor C527 and its derivatives (e.g., SJB2-043) are synthesized and the purity is validated by high-performance liquid chromatography. Primary human AML patient samples are collected from DFCI leukemia program under the approval of appropriate protocols. Cells are treated with DMSO or USP1 inhibitors (e.g., SJB2-043) in appropriate medium for 24-72 hrs. The viable cell counts are determined using Trypan blue staining, Cell TiterGlo reagent or MTT assay. The apoptotic cells are detected using AnnexinV and 7AAD staining using flow cytometry. For Benzidine staining, the cells are washed twice with PBS and resuspended in 45 μL of PBS + 5 μL of Benzidine stain solution (0.2% in 0.5 M glacial acetic acid, 3% H2O2). After 45 min incubation at room temperature, the Benzidine positive cells are detected by light microscopy[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 (276 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)
- 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 | 1 mM | 3.6329 mL | 18.1646 mL | 36.3293 mL | 90.8232 mL |
| 5 mM | 0.7266 mL | 3.6329 mL | 7.2659 mL | 18.1646 mL | |
| 10 mM | 0.3633 mL | 1.8165 mL | 3.6329 mL | 9.0823 mL |
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