| Identification | Back Directory | [Name]
SJB2-043 | [CAS]
63388-44-3 | [Synonyms]
SJB2-043
2-Phenylnaphth[2,3-d]oxazole-4,9-dione
Naphth[2,3-d]oxazole-4,9-dione, 2-phenyl-
2-phenylbenzo[f][1,3]benzoxazole-4,9-dione | [Molecular Formula]
C17H9NO3 | [MDL Number]
MFCD26960957 | [MOL File]
63388-44-3.mol | [Molecular Weight]
275.26 |
| Chemical Properties | Back Directory | [Melting point ]
>290℃ | [Boiling point ]
495.0±48.0 °C(Predicted) | [density ]
1.373±0.06 g/cm3(Predicted) | [storage temp. ]
Sealed in dry,Room Temperature | [solubility ]
insoluble in H2O; insoluble in EtOH; ≥4.62 mg/mL in DMSO | [form ]
solid | [pka]
-3.87±0.20(Predicted) |
| Hazard Information | Back Directory | [Biological Activity]
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]. | [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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| Company Name: |
SPIRO PHARMA
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| Tel: |
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| Website: |
www.spiropharma.com.cn |
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