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| | SJB2-043 analog (trifluoroacetate salt) Basic information |
| | SJB2-043 analog (trifluoroacetate salt) Chemical Properties |
| solubility | Acetonitrile: Slightly soluble: 0.1-1 mg/ml
DMSO: Sparingly soluble: 1-10 mg/ml |
| | SJB2-043 analog (trifluoroacetate salt) Usage And Synthesis |
| 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 | [1] LINGLI TAN, LI TAN* Discovery of Potent OTUB1/USP8 Dual Inhibitors Targeting Proteostasis in Non-Small-Cell Lung Cancer[J]. Journal of Medicinal Chemistry, 2022, 65 20: 13645-13659. DOI: 10.1021/acs.jmedchem.2c00408 |
| | SJB2-043 analog (trifluoroacetate salt) Preparation Products And Raw materials |
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