63388-44-3

Basic information

• Product Name: SJB2-043
• Synonyms: SJB2-043;2-Phenylnaphth[2,3-d]oxazole-4,9-dione
• CAS NO: 63388-44-3
• Molecular Formula: C₁₇H₉NO₃
• Molecular Weight: 275.25826
• Mol File: 63388-44-3.mol
• Article Data: 4

Chemical Properties

• Melting Point: >290℃
• Boiling Point: 495.0±48.0 °C(Predicted)
• Appearance: /
• 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
• PKA: -3.87±0.20(Predicted)
• CAS DataBase Reference: SJB2-043(CAS DataBase Reference)
• NIST Chemistry Reference: SJB2-043(63388-44-3)
• EPA Substance Registry System: SJB2-043(63388-44-3)

Safety Data

• Hazardous Substances Data: 63388-44-3(Hazardous Substances Data)

Usage

Description

SJB2-043 is a potent USP1 inhibitor, characterized by its ability to inhibit the activity of native USP1/UAF1 with an IC50 of 544 nM. SJB2-043 holds potential in various applications due to its inhibitory properties.

Uses

Used in Pharmaceutical Industry:
SJB2-043 is used as a pharmaceutical agent for its ability to inhibit USP1, a deubiquitinating enzyme that plays a crucial role in the DNA damage response and cell cycle regulation. By targeting USP1, SJB2-043 may have potential applications in the development of therapeutic strategies for cancer and other diseases where the USP1 pathway is implicated.
Used in Research and Development:
SJB2-043 is used as a research tool for studying the role of USP1 in cellular processes and its potential as a therapeutic target. Its potent inhibition of USP1/UAF1 makes it a valuable compound for investigating the underlying mechanisms of diseases and the development of novel treatment approaches.
Used in Drug Discovery:
SJB2-043 is used as a lead compound in drug discovery efforts, particularly for the development of new therapeutics targeting the USP1 pathway. Its potent inhibition of USP1/UAF1 activity can serve as a starting point for the design and optimization of more effective and selective USP1 inhibitors for various applications.

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.

Upstream product

• 54808-30-9 2-hydroxy-3-nitronaphthalene-1,4-dione 
• 7208-14-2 2-amino-3-bromo-1,4-naphthoquinone 
• 98-88-4 benzoyl chloride 
• 117-80-6 2,3-Dichloro-1,4-naphthoquinone 
• 354156-08-4 2-hydroxy-3-nitroso-1,4-naphthoquinone 
• 83-72-7 2-hydroxynaphtho-1,4-quinone 
• 474433-66-4 2-benzoyl-3-amino-1,4-naphthoquinone 
• 474433-65-3 2-benzoyl-3-nitroso-1,4-naphthoquinone 
• 22158-41-4 2-amino-3-hydroxy-1,4-naphthoquinone 
• 707-07-3 orthobenzoic acid trimethyl ester 
• 63351-45-1 N-(3-chloro-1,4-dioxo-1,4-dihydronaphthalen-2-yl)benzamide 

Relevant articles and documents

Compounds and methods for treating cancer

Provided are small molecule inhibitors of ubiquitin specific protease 2, 8 and 12 (USP2 and USP8 and USP12) activity and methods for their use in treating cancers. The small molecule inhibitors of the invention are particularly useful in the treatment of non-small cell lung cancers that are resistant to tyrosine kinase inhibitors and in the treatment of prostate cancer that is resistant to AR inhibitor therapy.

Synthesis and antimicrobial evaluation of oxazole-1,4-naphthquinones

Several routes for preparing oxazole nucleus fused to 1,4-naphthoquinone moiety were studied. Three new oxazole-1,4-naphthoquinone derivatives (4a-c) were prepared and evaluated against phatogenic bacteria. The use of ortho-ester methodology was found to be the best synthetic method for preparing these oxazoles, which showed very low antibacterial activity. The intermediate 2 showed a broad spectrum of activity comparable with oxacillin and vancomycin.