DC-U4106

• CAT Number: I043338
• CAS Number: 2410534-62-0
• Molecular Formula: C29H27N5O5
• Molecular Weight: 525.56
• Purity: ≥95%
• Synonyms: 8-[(3,5-dimethyl-1H-pyrazol-4-yl)oxy]-5,7-dihydroxy-2-[4-(4-pyridin-2-ylpiperazin-1-yl)phenyl]chromen-4-one
• InChI: InChI=1S/C29H27N5O5/c1-17-27(18(2)32-31-17)39-28-23(37)15-21(35)26-22(36)16-24(38-29(26)28)19-6-8-20(9-7-19)33-11-13-34(14-12-33)25-5-3-4-10-30-25/h3-10,15-16,35,37H,11-14H2,1-2H3,(H,31,32)
• InChIKey: VNWOJNLRTJFWRQ-UHFFFAOYSA-N
• SMILES: CC1=C(C(=NN1)C)OC2=C(C=C(C3=C2OC(=CC3=O)C4=CC=C(C=C4)N5CCN(CC5)C6=CC=CC=N6)O)O

DC-U4106 is a USP8 targeting inhibitor with the Kdvalue of 4.7 μM and the IC50 value of 1.2 μM. DC-U4106 can target the ubiquitin pathway and facilitate the degradation of Erα. DC-U4106 inhibits tumor growth with minimal toxicity and has the potential for the research of breast cancer[1].
DC-U4106 (1.2-45.2 μM) inhibits USP8 and USP2 with the IC50 values of 1.2 μM and 58.4 μM, respectively, and no activity in USP7[1].
DC-U4106 (0-7 μM, 24 hours) reduces mRNA levels of ERα and PR[1].
DC-U4106 (0-5 μM, 24 hours) can regulate the RTK pathway related proteins and the expression of ERα and PR proteins[1].
DC-U4106 (0-5 μM, 12 hours) can induce apoptosis and inhibit cell proliferation[1].
DC-U4106 (intraperitoneal injection, 5 mg/kg or 20 mg/kg, every 2 days, 14 days) inhibits the proliferation of tumors and no significantly effects on body weight, organ morphology and structure in BALB/c nude mice[1].

Reference

[1]. Yucheng Tian, et al. Discovery of Potent Small-Molecule USP8 Inhibitors for the Treatment of Breast Cancer through Regulating ERα Expression. J Med Chem. 2022 Jul 5.
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