An OTUB1 and USP8 inhibitor and a derivative of SJB2-043
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SJB2-043 analog (trifluoroacetate salt)

Item No. 38497

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
(R)-2-(2-chloro-6-fluoro-3-((1-methylpyrrolidin-3-yl)oxy)phenyl)naphtho[2,3-d]oxazole-4,9-dione, trifluoroacetate salt
Synonyms
  • OTUB1/Ubiquitin-specific Protease 8-IN-1
  • OTUB1/Ubiquitin-specific Protease 8 Inhibitor 1
  • OTUB1/USP8-IN-1
  • OTUB1/USP8 Inhibitor i
Molecular Formula
C22H16ClFN2O4 • XCF3COOH
Formula Weight
426.8
Purity
≥95%
Formulation
A solid
Solubility(Learn about Variance in Solubility)
Acetonitrile: Slightly soluble: 0.1-1 mg/mlDMSO: Sparingly soluble: 1-10 mg/ml
SMILES
O=C1C2=C(C(C3=C1C=CC=C3)=O)N=C(C4=C(F)C=CC(O[C@H]5CN(C)CC5)=C4Cl)O2.FC(F)(C(O)=O)F
InChi Code
InChI=1S/C22H16ClFN2O4.C2HF3O2/c1-26-9-8-11(10-26)29-15-7-6-14(24)16(17(15)23)22-25-18-19(27)12-4-2-3-5-13(12)20(28)21(18)30-22;3-2(4,5)1(6)7/h2-7,11H,8-10H2,1H3;(H,6,7)/t11-;/m1./s1
InChi Key
ZTOLAWIMKYRBAF-RFVHGSKJSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Wet ice in continental US; may vary elsewhere
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    500 µg

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    1 mg

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    5 mg

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    Product Description

    SJB2-043 analog is an inhibitor of OTUB1 and ubiquitin-specific protease 8 (USP8; IC50s = 0.17 and 0.28 nM, respectively) and a derivative of the USP1/UAF1 complex and SARS-CoV-2 PLPro inhibitor SJB2-043 (Item No. 36605).1 It is selective for OTUB1 and USP8 over USP1, USP2, USP7, USP36, and ataxin-3 (IC50s = 1,370, 3,800, >10,000, 8,400, and >10,000 nM, respectively). SJB2-043 analog reduces viability in H1975, EBC-1, NCI H1703, H23, and A549 non-small cell lung cancer (NSCLC) cells (IC50s = 118, 172, 145, 431, and 1,004 nM, respectively). In vivo, SJB2-043 analog (5 mg/kg twice daily) decreases tumor volume in an H1975 mouse xenograft model.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Tan, L., Shan, H., Han, C., et al. Discovery of potent OTUB1/USP8 dual inhibitors targeting proteostasis in non-small-cell lung cancer. J. Med. Chem. 65(20), 13645-13659 (2022).