1. Cell Cycle/DNA Damage
  2. Deubiquitinase
  3. NSC632839

NSC632839 

Cat. No.: HY-100708 Purity: 98.43%
Handling Instructions

NSC632839 is a nonselective isopeptidase inhibitor, which inhibits USP2, USP7, and SENP2 with EC50s of 45±4 μM, 37±1 μM, and 9.8±1.8 μM, respectively.

For research use only. We do not sell to patients.

NSC632839 Chemical Structure

NSC632839 Chemical Structure

CAS No. : 157654-67-6

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10 mM * 1 mL in DMSO USD 66 In-stock
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100 mg USD 552 In-stock
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Customer Review

Based on 3 publication(s) in Google Scholar

Top Publications Citing Use of Products

Publications Citing Use of MCE NSC632839

    NSC632839 purchased from MCE. Usage Cited in: Biochem Biophys Res Commun. 2018 Mar 4;497(2):726-733.

    Drug screen of UCHL1 and the function of inhibitors in autophagy. Both LDN and NSC could inhibit UCHL1 hydrolase activity. mRFP-GFP-LC3 stable cell line is treated with 5 μM LDN or 10 μM NSC in the condition of DMSO or Torin1 respectively for 6 h. The number of LC3 puncta remarkably is raised both in LDN and NSC treatment cells compared to the control.

    NSC632839 purchased from MCE. Usage Cited in: Biochem Biophys Res Commun. 2018 Mar 4;497(2):726-733.

    Drug screen of UCHL1 and the function of inhibitors in autophagy. Both LDN and NSC could inhibit UCHL1 hydrolase activity. Each cell lysate is analyzed by immunoblotting with anti p62 and LC3 antibodies.
    • Biological Activity

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    Description

    NSC632839 is a nonselective isopeptidase inhibitor, which inhibits USP2, USP7, and SENP2 with EC50s of 45±4 μM, 37±1 μM, and 9.8±1.8 μM, respectively.

    IC50 & Target

    EC50: 45±4 μM (USP2), 37±1 μM (USP7), 9.8±1.8 μM (SENP2)[1]

    In Vitro

    NSC 632839 inhibits ubiquitin isopeptidases as illustrated by its ability to inhibit z-LRGG-AMC cleavage by crude lysates in the mid-micromolar range. To further characterize NSC 632839 against purified enzymes, its inhibitory potential is determined against purified USP2, USP7, and SENP2 and demonstrated that NSC 632839 is not only a DUB inhibitor, but also a deSUMOylase inhibitor. Specifically, NSC 632839 inhibits USP2, USP7, and SENP2 with EC50 values of 45±4 μM, 37±1 μM, and 9.8±1.8 μM, respectively. Importantly, NSC 632839 does not inhibit the reporter enzyme PLA2 over the concentration range tested (1.2-150 μM), indicating that the reported inhibition is selective for isopeptidases. Moreover, the isopeptidase inhibitory activity of NSC 632839 is confirmed by the observation that it does not inhibit free PLA2 over the concentration range tested[1].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Molecular Weight

    339.86

    Formula

    C₂₁H₂₂ClNO

    CAS No.

    157654-67-6

    SMILES

    O=C1/C(CNC/C1=C\C2=CC=C(C)C=C2)=C/C3=CC=C(C)C=C3.[H]Cl

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 6 months
    -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : 6.2 mg/mL (18.24 mM; Need warming)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.9424 mL 14.7119 mL 29.4239 mL
    5 mM 0.5885 mL 2.9424 mL 5.8848 mL
    10 mM 0.2942 mL 1.4712 mL 2.9424 mL
    *Please refer to the solubility information to select the appropriate solvent.
    References
    Kinase Assay
    [1]

    In a 96-well-plate, 40 nM USP2, 40 nM USP7, or 20 nM SENP2 is preincubated with a concentration range of NSC 632839 (NCI/NIH developmental therapeutics program) or control for 30 min before supplementation with an equal volume of 60 nM Ub-PLA2/40 μM NBD C6-HPC (USP2 or 7) or 20 nM SUMO3-PLA2/40 μM NBD C6-HPC (SENP2). Relative activity of the enzymes is determined by measuring the RFU values at single time points within the initial linear range (USP, 50 min; USP7, 50 min; and SENP2, 30 min). The RFU values within the initial linear range are normalized such that isopeptidase+vehicle=0% inhibition and isopeptidase+NEM=100% inhibition. The EC50 values are determined as above. The inhibitory activity of the test compound against the reporter enzyme PLA2 is performed as described above except there is no preincubation step and the data are normalized such that free PLA2+vehicle=0% inhibition and free PLA2+EDTA=100% inhibition. PLA2 activity is determined 8 min after the addition of the reagents[1].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    References

    Purity: 98.43%

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    Keywords:

    NSC632839NSC 632839NSC-632839DeubiquitinaseDUBsInhibitorinhibitorinhibit

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