2. Metabolic Enzyme/Protease Apoptosis
  3. E1/E2/E3 Enzyme Apoptosis
  4. PYR-41

PYR-41 is a selective and cell permeable inhibitor of ubiquitin-activating enzyme E1 with an IC50 of < 10 μM, with little activity at E2 and E3.

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CAS 番号 : 418805-02-4

容量 価格（税別） 在庫状況 数量
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 72 在庫あり
Solution
10 mM * 1 mL in DMSO USD 72 在庫あり
Solid
5 mg $66 在庫あり
10 mg $99 在庫あり
25 mg $218 在庫あり
50 mg $396 在庫あり
100 mg $616 在庫あり
200 mg $820 在庫あり
500 mg $1296 在庫あり
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カスタマーレビュー

Based on 25 publication(s) in Google Scholar

PYR-41 関連抗体

Top Publications Citing Use of Products

    PYR-41 purchased from MedChemExpress. Usage Cited in: Cell Host Microbe. 2024 Jun 27:S1931-3128(24)00198-7.  [Abstract]

    The treatment of PYR-41 (50 μM; 24 h), an E1 inhibitor, reduced PUB44-mediated CRCK3 ubiquitylation in N. benthamiana.

    PYR-41 purchased from MedChemExpress. Usage Cited in: Cell Host Microbe. 2024 Jun 27:S1931-3128(24)00198-7.  [Abstract]

    The PYR-41 (50 μM; 10 h) treatment reduced CRCK3 internalization of p35S::gCRCK3-GFP/WT transgenic plants.

    PYR-41 purchased from MedChemExpress. Usage Cited in: Nat Neurosci. 2023 May;26(5):751-764.  [Abstract]

    PYR-41 (10 μg/0.5 μL, each side) significantly reversed the downregulated KCC2 in the VPM of anesthetized mice.

    PYR-41 purchased from MedChemExpress. Usage Cited in: Nat Neurosci. 2023 May;26(5):751-764.  [Abstract]

    PYR-41 (10 μg/0.5 μL, each side) treatment enhanced the effect of anesthesia, manifested as increased duration and depth of LORR and MRS in mice.

    PYR-41 purchased from MedChemExpress. Usage Cited in: Nat Neurosci. 2023 May;26(5):751-764.  [Abstract]

    PYR-41 (10 μg/0.5 μL, each side) treatment prolonged time from the MRS to the RRR in C57BL/6J mice.

    PYR-41 purchased from MedChemExpress. Usage Cited in: Int Immunopharmacol. 2020 Oct;87:106763.  [Abstract]

    293 T cells are pretreated with DMSO or PYR41 for 3 h, and then PYR41 inhibitor is added followed by stimulation with IFNα and VSV. After 24 h, VSVG protein expression level is determined by Western blotting analyses.

    PYR-41 purchased from MedChemExpress. Usage Cited in: Mol Cell Biol. 2018 Jul 16;38(15). pii: e00024-18.  [Abstract]

    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.

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    製品説明

    PYR-41 is a selective and cell permeable inhibitor of ubiquitin-activating enzyme E1 with an IC50 of < 10 μM, with little activity at E2 and E3.

    IC50 & Target

    IC50: < 10 μM (E1)
    Cellular Effect
    Cell Line Type Value Description References
    HEK293 IC50
    22 μM
    Compound: PYR-41
    Cytotoxicity against human HEK293 cells assessed as cell viability measured by Cell titre glo assay
    Cytotoxicity against human HEK293 cells assessed as cell viability measured by Cell titre glo assay
    		[PMID: 34246753]
    体外実験

    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].

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

    PYR-41 関連抗体
    分子量

    371.30

    分子式

    C17H13N3O7
    CAS 番号
    Appearance

    Solid

    Color

    Brown to reddish brown

    SMILES

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

    Room temperature in continental US; may vary elsewhere.
    保管条件
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    溶剤 & 溶解度
    体外: 

    DMSO : 50 mg/mL (134.66 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    Preparing
    Stock Solutions
    Concentration Solvent 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
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    • Molarity Calculator

    • Dilution Calculator

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    Mass
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    Volume
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    Molecular Weight *

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    一般には略語で表示されます：C1V1 = C2V2

    濃度 （開始）

    C1

    ×
    体積 （開始）

    V1

    =
    濃度 （終了）

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    体積 （終了）

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    体内:

    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.5 mg/mL (6.73 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    純度とドキュメンテーション

    純度: 98.84%

    COA (253 KB) HNMR (462 KB) RP-HPLC (280 KB) LCMS (98 KB)

    取扱説明書 (2659 KB)
    参考文献
    キナーゼ実験
    [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.

    MedChemExpress (MCE) はこれらの方法の精度を確認していません。 こちらは参照専用です。
    参考文献

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.6932 mL 13.4662 mL 26.9324 mL 67.3310 mL
    5 mM 0.5386 mL 2.6932 mL 5.3865 mL 13.4662 mL
    10 mM 0.2693 mL 1.3466 mL 2.6932 mL 6.7331 mL
    15 mM 0.1795 mL 0.8977 mL 1.7955 mL 4.4887 mL
    20 mM 0.1347 mL 0.6733 mL 1.3466 mL 3.3666 mL
    25 mM 0.1077 mL 0.5386 mL 1.0773 mL 2.6932 mL
    30 mM 0.0898 mL 0.4489 mL 0.8977 mL 2.2444 mL
    40 mM 0.0673 mL 0.3367 mL 0.6733 mL 1.6833 mL
    50 mM 0.0539 mL 0.2693 mL 0.5386 mL 1.3466 mL
    60 mM 0.0449 mL 0.2244 mL 0.4489 mL 1.1222 mL
    80 mM 0.0337 mL 0.1683 mL 0.3367 mL 0.8416 mL
    100 mM 0.0269 mL 0.1347 mL 0.2693 mL 0.6733 mL
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    PYR-41 Related Classifications

    • Molarity Calculator

    • Dilution Calculator

    The molarity calculator equation

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    質量   濃度   体積   分子量 *
    = × ×

    The dilution calculator equation

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    一般には略語で表示されます：C1V1 = C2V2

    濃度 （開始） × 体積 （開始） = 濃度 （終了） × 体積 （終了）
    × = ×
    C1   V1   C2   V2
    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Keywords:

    PYR-41418805-02-4PYR41PYR 41E1/E2/E3 EnzymeApoptosisE1 activating enzymeE2 conjugating enzymeE3 ligating enzymeUbiquitin activating enzymeUbiquitin conjugating enzymeUbiquitin ligaseInhibitorinhibitorinhibit

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    製品名:
    PYR-41
    製品番号:
    HY-13296
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