SJB2-043USP1 inhibitor CAS# 63388-44-3 |
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Quality Control & MSDS
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| Cas No. | 63388-44-3 | SDF | Download SDF |
| PubChem ID | 509070 | Appearance | Powder |
| Formula | C17H9NO3 | M.Wt | 275.26 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Solubility | DMSO : 3.33 mg/mL (12.10 mM; Need ultrasonic) H2O : < 0.1 mg/mL (insoluble) | ||
| Chemical Name | 2-phenylbenzo[f][1,3]benzoxazole-4,9-dione | ||
| SMILES | C1=CC=C(C=C1)C2=NC3=C(O2)C(=O)C4=CC=CC=C4C3=O | ||
| Standard InChIKey | CMYQQADDUUDCCA-UHFFFAOYSA-N | ||
| Standard InChI | InChI=1S/C17H9NO3/c19-14-11-8-4-5-9-12(11)15(20)16-13(14)18-17(21-16)10-6-2-1-3-7-10/h1-9H | ||
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
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| About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
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| Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. | ||
| Description | SJB2-043 is an inhibitor of the native USP1/UAF1 complex with IC50 of 544 nM.In Vitro: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]. References: | |||||
SJB2-043 Dilution Calculator
SJB2-043 Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 3.6329 mL | 18.1646 mL | 36.3293 mL | 72.6586 mL | 90.8232 mL |
| 5 mM | 0.7266 mL | 3.6329 mL | 7.2659 mL | 14.5317 mL | 18.1646 mL |
| 10 mM | 0.3633 mL | 1.8165 mL | 3.6329 mL | 7.2659 mL | 9.0823 mL |
| 50 mM | 0.0727 mL | 0.3633 mL | 0.7266 mL | 1.4532 mL | 1.8165 mL |
| 100 mM | 0.0363 mL | 0.1816 mL | 0.3633 mL | 0.7266 mL | 0.9082 mL |
| * Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations. | |||||
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SJB2-043 is a novel and potent inhibitor of USP1 with IC50 value of 0.544 μM [1].
Ubiquitin-specific protease 1 (USP1) is a deubiquitinating enzyme (DUB) and is a member of the ubiquitin-specific processing (UBP) family of proteases. It deubiquitinates a protein in the DNA repair pathway of the Fanconi anemia (FA) [1].
In the K562 cell line, SJB2-043 decreased USP1 levels in a dose-dependent way and caused degradation of the ID1 protein, which resulted from proteasomal degradation. Also, SJB2-043 decreased the levels of ID2 and ID3 proteins. Importantly, knockdown of USP1 inhibited cell growth and increased apoptosis. In primary AML cells, SJB2-043 inactivated USP1 and promoted ID 1 degradation. In primary human cord blood CD34+ cells, SJB2-043 in low micromolar levels inhibited cell growth. In HeLa cells, SJB2-043 increased the levels of Ub-FANCD2 and Ub-PCNA. And deubiquitination of FANCD2 is an important step in the BRCA/Fanconi anemia (FA) DNA repair pathway [1].
Reference:
[1]. Helena Mistry, Grace Hsieh, Sara S, et al. Buhrlage, et al. Small molecule inhibitors of USP1 target ID1 degradation in leukemic cells. Mol Cancer Ther, 2013, 12(12): 2651-2662.
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The Role of the Complex USP1/WDR48 in Differentiation and Proliferation Processes in Cancer Stem Cells.[Pubmed:28302046]
Curr Stem Cell Res Ther. 2017;12(5):416-422.
BACKGROUND: Recently, some studies identified the Basic-Helix-Loop-Helix (bHLH) transcription factor as a significant regulator for the evolution of neoplasms. The binding between bHLH proteins and DNA is restricted by heterodimerization with Inhibitors of DNA binding (ID). IDs prevent cellular differentiation, promote growth and sustain tumor development. The wide presence of stem cells in cancers suggests that genes ID are essential to cancer stem cells (CSC) progress. The enzyme Ubiquitin-specific protease 1 (USP1) is reported to deubiquitinate and stabilize IDs. Considering the action of the proteins ID, USP1 contributes to prevent differentiation mediated by bHLH and, consequently, keep CSC original characteristics. USP1 has its activity potentiated when bound to protein WD repeat-containing protein (WDR48). OBJECTIVE: To identify the influence of the complex USP1/WDR48 during the CSC tumorigenesis process, and whether this complex is a possible therapeutic target. METHODS: A literature search regarding the role of the complex USP1/WDR48 in inhibiting differentiation and increasing proliferation of CSC was performed, and possible selective molecule inhibitors of these deubiquitinase proteins were investigated. RESULTS: There is evidence that USP1/WDR48 complex promotes stem cell conservation and regulation of DNA damage repair. For this reason, inhibitors as Pimozide, GW7647, C527, SJB2-043, ML323 have been studied to inhibit USPs in cases of treatment intervention. CONCLUSION: It is consolidated in the literature the role of USP1/WDR48 during tumorigenesis. However, these studies are not enough to completely clarify the process; but certainly, the researchers are converging towards a promising direction to provide a new treatment option for cancer.
