USP7-IN-9

• CAT Number: I043826
• CAS Number: 2444374-01-8
• Molecular Formula: C32H33ClF6N6O8
• Molecular Weight: 779.08
• Purity: ≥95%
• Synonyms: [4-[6-[[1-[(2-chloro-4-methoxycarbonylphenyl)methyl]-4-hydroxypiperidin-1-ium-4-yl]methyl]-2-methyl-7-oxopyrazolo[4,3-d]pyrimidin-3-yl]phenyl]methylazanium;2,2,2-trifluoroacetate
• InChI: InChI=1S/C28H31ClN6O4.2C2HF3O2/c1-33-25(19-5-3-18(14-30)4-6-19)23-24(32-33)26(36)35(17-31-23)16-28(38)9-11-34(12-10-28)15-21-8-7-20(13-22(21)29)27(37)39-2;2*3-2(4,5)1(6)7/h3-8,13,17,38H,9-12,14-16,30H2,1-2H3;2*(H,6,7)
• InChIKey: WZRJDCAJOKOZRD-UHFFFAOYSA-N
• SMILES: CN1C(=C2C(=N1)C(=O)N(C=N2)CC3(CC[NH+](CC3)CC4=C(C=C(C=C4)C(=O)OC)Cl)O)C5=CC=C(C=C5)C[NH3+].C(=O)(C(F)(F)F)[O-].C(=O)(C(F)(F)F)[O-]

USP7-IN-9 is a highly potent ubiquitin-specific protease 7 (USP7) inhibitor with an IC50 value of 40.8 nM. USP7-IN-9 can induce apoptosis and arrest cell progression at G0/G1 and S phases in RS4; 11 cells. USP7-IN-9 reduces the protein levels of oncoproteins MDM2 and DNMT1 and increases the protein levels of tumor suppressors p53 and p21[1].
USP7-IN-9 (compound L55) (0-50 μM; 3 or 6 days) exhibits inhibitory activity against cancer cells[1].
USP7-IN-9 (1 μM; 0-72 hours) reduces the proportions of G2/M cells, and does not change the proportions of G0/G1 and S cells[1].
USP7-IN-9 (0.1-1 μM; 24 hours) reduces the protein levels of MDM2 and DNMT1 in a dose-dependent manner, and increases the protein levels of p53 and p21[1].

Reference

[1]. Li M, Liu S, Chen H, et al. N-benzylpiperidinol derivatives as novel USP7 inhibitors: Structure-activity relationships and X-ray crystallographic studies. Eur J Med Chem. 2020;199:112279.
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