SJB2-043
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.
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 275.26 |
| Cas No. | 63388-44-3 |
| Formula | C17H9NO3 |
| Solubility | insoluble in H2O; insoluble in EtOH; ≥4.62 mg/mL in DMSO |
| Chemical Name | 2-phenylbenzo[f][1,3]benzoxazole-4,9-dione |
| SDF | Download SDF |
| Canonical SMILES | O=C(c1c2[o]c(-c3ccccc3)n1)c(cccc1)c1C2=O |
| Shipping Condition | Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice. |
| General tips | We do not recommend long-term storage for the solution, please use it up soon. |
| Cell experiment [1]: | |
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Cell lines |
K562 cells |
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Preparation method |
This compound is soluble in DMSO. General tips for obtaining a higher concentration: Please warm the tube at 37℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months. |
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Reaction Conditions |
0, 0.5, 1, 1.5, 2, 5 and 10 μM; 24 hrs |
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Applications |
In K562 cells, SJB2-043 decreased USP1 levels in a dose-dependent way and caused degradation of the ID1 protein, which resulted from proteasomal degradation. |
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References: [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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Quality Control & MSDS
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Chemical structure
