P22077 | Selective USP7 inhibitor
NMR (Conforms)
Available Options
| Size: | Price | Quantity | |
|---|---|---|---|
| 10 mg | $65.00 | ||
| 50 mg | $250.00 |
P22077 (1247819-59-5) is a selective (tested against 23 other DUBs) inhibitor of USP7 (IC50 = 8 µM) and the closely related USP47.1,2 It destabilizes claspin, a scaffolding protein involved in regulating Chk1 kinase, a DNA damage response enzyme.2 P22077 inhibits neuroblastoma growth via induction of p53-mediated apoptosis.3 N-Myc was destabilized by P22077 inhibition of USP7 in human neuroblastoma cells.4 It was able to stabilize p53 levels in conjunction with an Mdm2 inhibitor (Nutlin-3, Cat# 10-1350) in HCT116 colorectal carcinoma cells.5
References/Citations:
1) Tian et al. (2011), Characterization of Selective Ubiquitin and Ubiquitin-like Protease Inhibitors Using a Fluorescence-Based Multiplex Assay Format; Assay Drug Dev. Technol. 9 165
2) Altun et al. (2011), Activity-based chemical proteomics accelerates inhibitor development for deubiquitinylating enzymes; Chem. Biol. 18 1401
3) Fan et al. (2013), USP7 inhibitor P22077 inhibits neuroblastoma growth via inducing p53-mediated apoptosis; Cell Death Dis. 4 e867
4) Tavana et al. (2016), HAUSP deubiquitinates and stabilizes M-Myc in neuroblastoma; Nat. Med. 22 1180
5) Tavana et al. (2018), Targeting HAUSP in both p53 wildtype and p53-mutant tumors; Cell Cycle 17 823
NMR (Conforms)
Safety Data Sheet:
Product Data Sheet:
Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications. Please note that we do not sell to individuals and that all orders placed by non-research organizations will incur a $20 restocking/refund fee
P22077 (1247819-59-5) is a selective (tested against 23 other DUBs) inhibitor of USP7 (IC50 = 8 µM) and the closely related USP47.1,2 It destabilizes claspin, a scaffolding protein involved in regulating Chk1 kinase, a DNA damage response enzyme.2 P22077 inhibits neuroblastoma growth via induction of p53-mediated apoptosis.3 N-Myc was destabilized by P22077 inhibition of USP7 in human neuroblastoma cells.4 It was able to stabilize p53 levels in conjunction with an Mdm2 inhibitor (Nutlin-3, Cat# 10-1350) in HCT116 colorectal carcinoma cells.5
References/Citations:
1) Tian et al. (2011), Characterization of Selective Ubiquitin and Ubiquitin-like Protease Inhibitors Using a Fluorescence-Based Multiplex Assay Format; Assay Drug Dev. Technol. 9 165
2) Altun et al. (2011), Activity-based chemical proteomics accelerates inhibitor development for deubiquitinylating enzymes; Chem. Biol. 18 1401
3) Fan et al. (2013), USP7 inhibitor P22077 inhibits neuroblastoma growth via inducing p53-mediated apoptosis; Cell Death Dis. 4 e867
4) Tavana et al. (2016), HAUSP deubiquitinates and stabilizes M-Myc in neuroblastoma; Nat. Med. 22 1180
5) Tavana et al. (2018), Targeting HAUSP in both p53 wildtype and p53-mutant tumors; Cell Cycle 17 823
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