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Cat. No. Product Name CAS No. Information
PC-35263

MF-094

2241025-68-1

MF-094 (MF094) is a potent, highly selective inhibitor of ubiquitin specific protease 30 (USP30) with IC50 of 0.12 uM, demonstrates <30% inhibitory activity for a panel of 22 USPs assays at 10 uM; increases protein ubiquitination and accelerates mitophagy.

PC-62189

Spautin-1

1262888-28-7

Spautin-1 is a potent, small molecule inhibitor of autophagy with IC50 of 0.74 uM, inhibits USP10 and USP13 with IC50 of 0.6-0.7 uM, but not USP14; promotes cell death under starvation condition and inhibits autophagic cell death, selectively promotes the degradation of Vps34 complexes, reduces the levels of PtdIns3P in cells, but is not a direct inhibitor of class III PI3 kinase activity; promotes the degradation of p53 via inhibition of USP10, which can be inhibited in the presence of MG132; sensitizes ovarian cancer cells to cisplatin and PARP inhibitor (olaparib).

PC-61935

USP7i-1

1381291-36-6

USP7i-1 is a potent, selective USP7 inhibitor.

PC-60494

XL 188

XL188 (XL-188) is a potent, selective, non-covalent active-site inhibitor of USP7 with IC50 of 90 nM and 193 nM for USP7 full length enzyme and catalytic domain, respectively; exhibits little to no inhibition against a panel of 41 DUBs; promotes USP7-dependent loss of HDM2 and increases p53 and p21, significantly blocks labeling of USP7 by HA-Ub-Vs with an IC50 of 0.9 uM; a probe suitable for in vivo studies, highly valuable for pharmacological validation of USP7 in animal disease models.

PC-60089

GNE-6776

2009273-71-4

GNE-6776 is a novel potent, specific, non-covalent, orally bioavailable USP7 inhibitor with IC50 of 1.34 uM ; dislpalys selectivity over USP47 and USP5 (>200 uM); promotes endogenous MDM2 ubiquitination, stabilized p53 and upregulated p21, induces tumour cell death and enhances cytotoxicity with chemotherapeutic agents; promotes on-target pathway modulation in human xenografts.

PC-60088

FT-671

1959551-26-8

FT-671 is a novel potent, specific, non-covalent USP7 inhibitor with Kd of 65 nM (USP7 catalytic domain); inhibits USP7 with IC50 values of 52 nM (USP7 CD) and 69 nM (USP7C-term), display good USP7 selectivity in a panel of 38 deubiquitinases (DUBs); destabilizes USP7 substrates including MDM2, increases levels of p53, and results in the transcription of p53 target genes and induces tumour suppressor p21; blocks the proliferation of MM.1S cells (IC50=33 nM), suppresses tumour growth in mice; orally available.

PC-60026

USP25 and 28 inhibitor AZ-2

2165322-95-0

USP25 and 28 inhibitor AZ-2 is a potent, selective, dual USP25/28 inhibitor with IC50 of 0.9/0.9 uM, respectively; shows a high degree of selectivity over other deubiquitinases (USP4,7 etc.); demonstrates target engagement against both USP25 and USP28 in cells, elicits modulation of both the total levels and the half-life of the c-Myc oncoprotein in cells, and also induces apoptosis and inhibits cell viability in a range of cancer cell lines.

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