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      P22077
      P22077

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      This product is for research use only, not for human use. We do not sell to patients.
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      InvivoChem Cat #: V1328
      CAS #: 1247819-59-5Purity ≥98%

      Description: P22077 (P-22077; P 22077) is a potent, cell-permeable and selective inhibitor of ubiquitin-specific protease USP7 (ubiquitin-specific protease 7) with potential antitumor activity. It inhibits USP7 with an EC50 of 8.6 μM, and also inhibits the closely related USP47. P22077 potently induces apoptosis in NB cells with an intact USP7-HDM2-p53 axis but not in NB cells with mutant p53 or without human homolog of MDM2 (HDM2) expression. P22077 also significantly augmented the cytotoxic effects of doxorubicin (Dox) and etoposide (VP-16) in NB cells with an intact USP7-HDM2-p53 axis. Moreover, P22077 was found to be able to sensitize chemoresistant LA-N-6 NB cells to chemotherapy.

      References: Assay Drug Dev Technol. 2011 Apr;9(2):165-73; Chem Biol. 2011 Nov 23;18(11):1401-12.

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      Molecular Weight (MW)315.32
      FormulaC12H7F2NO3S2
      CAS No.1247819-59-5
      Storage-20℃ for 3 years in powder form
      -80℃ for 2 years in solvent
      Solubility (In vitro)DMSO: 63 mg/mL (199.8 mM)
      Water:<1 mg/mL
      Ethanol: <1 mg/mL
      Other info

      Chemical Name: 1-(5-((2,4-difluorophenyl)thio)-4-nitrothiophen-2-yl)ethanone

      InChi Key: RMAMGGNACJHXHO-UHFFFAOYSA-N

      InChi Code: InChI=1S/C12H7F2NO3S2/c1-6(16)11-5-9(15(17)18)12(20-11)19-10-3-2-7(13)4-8(10)14/h2-5H,1H3

      SMILES Code: CC(C1=CC([N+]([O-])=O)=C(SC2=CC=C(F)C=C2F)S1)=O           

      Synonyms

      P22077; P-22077; P 22077


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      In Vitro

      In vitro activity: P22077 is an analog of the recently discovered USP7 inhibitor P5091. P22077 has negligible activity versus DEN1 and SENP2core over the concentration range tested, but inhibits USP7 with an IC50 of 8 μM. The inhibitory activities of P22077 in vitro against a panel of DUBs, cysteine proteases, and other families of proteolytic enzymes demonstrate that P22077 inhibits USP7 and the closely related DUB USP47. P22077 inhibits a smaller subset of DUBs at a concentration of 15–45 mM in cell lysates. P22077 induces (tumor) cell death with EC50 values in the low micromolar range. P22077 inhibition exhibited changes in ubiquitylated protein levels that are distinct from the broad specificity inhibitor. P22077 treatment of U2OS cells during release from G1/S arrest induces with hydroxyurea resulted in a dose-dependent loss of claspin protein and a concomitant decrease in phospho Serine 317 Chk1. Furthermore, quantitative MS suggestes the E3 ubiquitin ligase components RBX1, DCAF7, DCAF11, and the DNA damage binding protein 1 (DDB1) to be reduced upon cellular treatment with P22077.

      Kinase Assay: Recombinant full length USP7, USP2 core, USP5, JOSD2, DEN1, PLpro core, and SENP2 catalytic core are generated. Amino terminal His6 tagged USP4, USP8, USP28, UCH-L1, UCH-L3, UCH-L5, and MMP13 are expressed in Escherichia coli. N-terminal His6 tagged USP15, USP20, and USP47 are expressed in Sf9 cells. All the recombinant proteins are purified by chromatography. Amino terminal tagged His6 Ub-PLA2 (Ub-CHOP), SUMO3-PLA2 (SUMO3-CHOP), ISG15-PLA2 (ISG15-CHOP), NEDD8-PLA2 (NEDD8-CHOP), Ub-EKL (Ub-CHOP2), and free catalytically active PLA2 are prepared.

      Cell Assay: P022077 had negligible activity versus DEN1 and SENP2core over the concentration range tested, but inhibited USP7 with an IC50 of 8 μM. In another study Inhibiting, USP7 with the small-molecule inhibitor P22077 attenuates the p53-dependent apoptotic pathway by destabilizing Tip60. P22077, however, is still cytotoxic, and this is partly due to destabilization of Tip60.

      In VivoP 22077 (15 mg/kg, i.p. 21 days) shows potent antitumor activities in an xenograft mouse model bearing IMR-32-derived tumors; P 22077 also exhibits antitumor effects after treatment at 10 mg/kg for 14 days in mice bearing SH-SY5Y-derived tumors, and at 20 mg/kg for 12 days in mice bearing NGP-derived tumors.
      Animal modelMice
      Formulation & Dosage15 mg/kg, i.p. 
      References

      Assay Drug Dev Technol. 2011 Apr;9(2):165-73; Chem Biol. 2011 Nov 23;18(11):1401-12; Cell Death Dis. 2013 Oct 17;4:e867.

      These protocols are for reference only. InvivoChem does not independently validate these methods.

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