1. Metabolic Enzyme/Protease
  2. E1/E2/E3 Enzyme

PYR-41 

Cat. No.: HY-13296 Purity: >98.0%
Handling Instructions

PYR-41 is a specific and cell permeable inhibitor of ubiquitin-activating enzyme E1 with an IC50 of < 10 μM, with no or little activity at E2.

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

PYR-41 Chemical Structure

PYR-41 Chemical Structure

CAS No. : 418805-02-4

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 66 In-stock
Stock in the United States
Estimated Time of Arrival: December 31
5 mg USD 60 In-stock
Stock in the United States
Estimated Time of Arrival: December 31
10 mg USD 90 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
50 mg USD 360 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
100 mg USD 560 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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    PYR-41 purchased from MCE. Usage Cited in: Mol Cell Biol. 2018 May 14. pii: MCB.00024-18.

    Western blotting assays demonstrate that treatment of 20 μM PYR-41 or 20 μM PYZD-4409 inhibits ubiquitination and CD133 secretion. Hsp90 and β-actin are used as loading controls.
    • Biological Activity

    • Protocol

    • Technical Information

    • Purity & Documentation

    • References

    Description

    PYR-41 is a specific and cell permeable inhibitor of ubiquitin-activating enzyme E1 with an IC50 of < 10 μM, with no or little activity at E2.

    IC50 & Target

    IC50: < 10 μM (E1)

    In Vitro

    PYR-41 increases total sumoylation in cells in addition to blocking ubiquitylation. PYR-41 attenuates cytokine-mediated nuclear factor-κB activation. PYR-41 also prevents the downstream ubiquitylation and proteasomal degradation of IκBα. Furthermore, PYR-41 inhibits degradation of p53 and activates the transcriptional activity of this tumor suppressor[1]. PYR-41 (50 μM) promotes accumulation of ubiquitinated proteins. PYR-41 causes a concentration-dependent (10-50 μM) decline in DUB activity in Z138 cells after 4 h. PYR-41 potently inhibits USP5 DUB activity, even at the lowest concentration (10 μM). PYR-41 potently (10-50 μM) inhibits the activity of various DUBs, determined to represent USP9x, USP5, USP14, UCH37 and UCH-L3. Co-treatment of Z138 cells with DTT and PYR-41 completely abolishes the accumulation of ubiquitinated proteins[2].

    References
    Preparing Stock Solutions
    Concentration Volume Mass 1 mg 5 mg 10 mg
    1 mM 2.6932 mL 13.4662 mL 26.9324 mL
    5 mM 0.5386 mL 2.6932 mL 5.3865 mL
    10 mM 0.2693 mL 1.3466 mL 2.6932 mL
    Please refer to the solubility information to select the appropriate solvent.
    Kinase Assay
    [1]

    Rabbit or mouse E1 (apper 250 ng) is incubated with 32P-ubiquitin in 1× reaction buffer [50 mM Tris (pH 7.4), 0.2 mM ATP, 0.5 mM MgCl2] at room temperature for 15 min. In some experiments, the His-tagged mouse E1 is bound to TALON cobalt affinity resin before carrying out incubations and reactions. Mouse E1 and 32P-ubiquitin are added to the beads in 1× reaction buffer and incubated as for E1 reactions. Samples are heated in nonreducing SDS-PAGE sample buffer and resolved by SDS-PAGE. Thioesters with ubiquitin are visualized by Storm PhosphoImager. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    References
    Molecular Weight

    371.3

    Formula

    C₁₇H₁₃N₃O₇

    CAS No.

    418805-02-4

    SMILES

    O=C(N1)/C(C(N1C2=CC=C(C=C2)C(OCC)=O)=O)=C/C3=CC=C([N+]([O-])=O)O3

    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Shipping

    Room temperature in continental US; may vary elsewhere

    Solvent & Solubility

    DMSO: ≥ 46 mg/mL

    * "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

    Purity: >98.0%

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    Product Name:
    PYR-41
    Cat. No.:
    HY-13296
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