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| Product Name: | SJB2-043 | | Synonyms: | SJB2-043;2-Phenylnaphth[2,3-d]oxazole-4,9-dione;2-phenylbenzo[f][1,3]benzoxazole-4,9-dione;Naphth[2,3-d]oxazole-4,9-dione, 2-phenyl-;2-Phenylnaphtho[2,3-d]oxazole-4,9-dione;SJB2-043,inhibit,DUBs,SJB2043,SJB-2-043,SJB2 043,Deubiquitinase,Inhibitor | | CAS: | 63388-44-3 | | MF: | C17H9NO3 | | MW: | 275.26 | | EINECS: | | | Product Categories: | | | Mol File: | 63388-44-3.mol |  |
| | SJB2-043 Chemical Properties |
| 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) |
| | SJB2-043 Usage And Synthesis |
| Description | SJB2-043 is a potent USP1 inhibitor that inhibits the activity of native USP1/UAF1 with IC50 of 544 nM. | | 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. |
| | SJB2-043 Preparation Products And Raw materials |
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