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MedKoo Cat#: 563362 | Name: SJB2-043
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Description:

WARNING: This product is for research use only, not for human or veterinary use.

SJB2-043 is an inhibitor of USP1 target ID1 degradation in leukemic cells.

Chemical Structure

SJB2-043
CAS#63388-44-3

Theoretical Analysis

MedKoo Cat#: 563362

Name: SJB2-043

CAS#: 63388-44-3

Chemical Formula: C17H9NO3

Exact Mass: 275.0582

Molecular Weight: 275.26

Elemental Analysis: C, 74.18; H, 3.30; N, 5.09; O, 17.44

Price and Availability

Size Price Availability Quantity
5mg USD 90.00 Ready to ship
10mg USD 150.00 Ready to ship
25mg USD 320.00 Ready to ship
50mg USD 550.00 Ready to ship
100mg USD 925.00 Ready to ship
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Related CAS #
No Data
Synonym
SJB2-043; SJB2 043; SJB2043; SJB2043; SJB2043;
IUPAC/Chemical Name
2-Phenyl-naphth[2,3-d]oxazole-4,9-dione
InChi Key
CMYQQADDUUDCCA-UHFFFAOYSA-N
InChi Code
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
SMILES Code
O=C(C1=C2OC(C3=CC=CC=C3)=N1)C4=C(C=CC=C4)C2=O
Appearance
Solid powder
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO
Shelf Life
>3 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.03.00
More Info
Biological target:
SJB2-043 is a dual inhibitor of USP1 and the USP1-UAF1 complex (IC50 = 0.544 µM for deubiquitinase activity) and also targets the SARS-CoV-2 papain-like protease (PLpro). It demonstrates antiproliferative effects in K562 cells (EC50 = 1.07 µM), inducing concentration-dependent apoptosis. Additionally, SJB2-043 effectively inhibits SARS-CoV-2 PLpro, with IC50 values of 0.56 µM and 0.091 µM using the fluorogenic substrates Z-LRGG-AMC and ubiquitin-AMC (Ub-AMC), respectively.
In vitro activity:
SJB2-043 inhibits the DUB activity of native USP1 complexes isolated from human cells. After treating cells with SJB2-043 for 24 hours, the formation of the Ub-USP1 conjugate was suppressed. SJB2-043 also showed specificity by inhibiting the labeling of a limited number of endogenous DUB enzymes. Furthermore, SJB2-043 demonstrated a dose-dependent inhibition of the labeling of USP1 with Ub-VS. In summary, these findings establish SJB2-043 as an inhibitor of the native USP1/UAF1 complex. Reference: Mol Cancer Ther. 2013 Dec;12(12):2651-62. https://pubmed.ncbi.nlm.nih.gov/24130053/
In vivo activity:
To be determined
Solvent mg/mL mM comments
Solubility
DMSO 3.3 12.10
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 275.26 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
1. Cho CC, Li SG, Lalonde TJ, Yang KS, Yu G, Qiao Y, Xu S, Ray Liu W. Drug Repurposing for the SARS-CoV-2 Papain-Like Protease. ChemMedChem. 2022 Jan 5;17(1):e202100455. doi: 10.1002/cmdc.202100455. Epub 2021 Oct 12. Erratum in: ChemMedChem. 2022 Mar 4;17(5):e202200053. PMID: 34423563; PMCID: PMC8653067. 2. Mistry H, Hsieh G, Buhrlage SJ, Huang M, Park E, Cuny GD, Galinsky I, Stone RM, Gray NS, D'Andrea AD, Parmar K. Small-molecule inhibitors of USP1 target ID1 degradation in leukemic cells. Mol Cancer Ther. 2013 Dec;12(12):2651-62. doi: 10.1158/1535-7163.MCT-13-0103-T. Epub 2013 Oct 15. PMID: 24130053; PMCID: PMC4089878.
In vitro protocol:
1. Cho CC, Li SG, Lalonde TJ, Yang KS, Yu G, Qiao Y, Xu S, Ray Liu W. Drug Repurposing for the SARS-CoV-2 Papain-Like Protease. ChemMedChem. 2022 Jan 5;17(1):e202100455. doi: 10.1002/cmdc.202100455. Epub 2021 Oct 12. Erratum in: ChemMedChem. 2022 Mar 4;17(5):e202200053. PMID: 34423563; PMCID: PMC8653067. 2. Mistry H, Hsieh G, Buhrlage SJ, Huang M, Park E, Cuny GD, Galinsky I, Stone RM, Gray NS, D'Andrea AD, Parmar K. Small-molecule inhibitors of USP1 target ID1 degradation in leukemic cells. Mol Cancer Ther. 2013 Dec;12(12):2651-62. doi: 10.1158/1535-7163.MCT-13-0103-T. Epub 2013 Oct 15. PMID: 24130053; PMCID: PMC4089878.
In vivo protocol:
To be determined
1: Goncalves JM, Cordeiro MMR, Rivero ERC. The Role of the Complex USP1/WDR48 in Differentiation and Proliferation Processes in Cancer Stem Cells. Curr Stem Cell Res Ther. 2017;12(5):416-422. doi: 10.2174/1574888X12666170315104013. Review. PubMed PMID: 28302046.

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