1. Cell Cycle/DNA Damage
  2. IRE1
  3. APY29

APY29, an ATP-competitive inhibitor, is an allosteric modulator of IRE1α which inhibits IRE1α autophosphorylation by binding to the ATP-binding pocket with IC50 of 280 nM. APY29 acts as a ligand that allosterically activates IRE1α adjacent RNase domain.

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APY29 Chemical Structure

APY29 Chemical Structure

CAS No. : 1216665-49-4

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Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
USD 82 In-stock
Solution
10 mM * 1 mL in DMSO USD 82 In-stock
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5 mg USD 75 In-stock
10 mg USD 125 In-stock
50 mg USD 385 In-stock
100 mg USD 690 In-stock
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Customer Review

Based on 16 publication(s) in Google Scholar

Top Publications Citing Use of Products

    APY29 purchased from MedChemExpress. Usage Cited in: FEBS J. 2019 Apr;286(7):1375-1392.  [Abstract]

    Western blot analysis shows the increase in expression of neuronal marker proteins NSE and NDRG1 with increased XBP1s levels in kaempferol and APY29 treated conditions.

    APY29 purchased from MedChemExpress. Usage Cited in: FEBS J. 2019 Apr;286(7):1375-1392.  [Abstract]

    STF083010 pretreatment reduces the number of neurite bearing cells in both kaempferol (KFL) and APY29 treated conditions further.

    APY29 purchased from MedChemExpress. Usage Cited in: FEBS J. 2019 Apr;286(7):1375-1392.  [Abstract]

    Immunocytochemistry for expression of β III tubulin showing reduces expression upon pretreatment of cells with STF083010 50 μM in the presence of kaempferol and APY29.

    APY29 purchased from MedChemExpress. Usage Cited in: FEBS J. 2019 Apr;286(7):1375-1392.  [Abstract]

    Immunocytochemistry for expression of β III tubulin showing reduces expression in IRE1α knockdown cells in the presence of kaempferol and APY29.

    APY29 purchased from MedChemExpress. Usage Cited in: Food Chem Toxicol. 2018 Apr;114:52-60.  [Abstract]

    (A) The p-IRE1a, IRE1a and XBP1s protein expression levels were determined in rat livers. (B, C, D) The expression of p-IRE1a, IRE1a, XBP1s, MTTP and p65 were detected in cells (n=3). A: APY-29; A+Q: APY-29+Quercetin; A+S: APY-29+STF-083010.

    APY29 purchased from MedChemExpress. Usage Cited in: Viruses. 2017 Aug 23;9(9). pii: E235.   [Abstract]

    Inhibition of IRE1 kinase activity has an inhibitory effect on HSV-1 replication in HEC-1-A cells. Cells are presence or absence of APY29 or STF-083010 or both of two drugs and then infected with HSV-1 (HF). Total cellular cells lysates are prepared at 24 h p.i. and subject to Western blot analysis against.

    APY29 purchased from MedChemExpress. Usage Cited in: Viruses. 2017 Aug 23;9(9). pii: E235.   [Abstract]

    IRE1 kinase activity inhibitor represses JNK activation induced by viral infection in HEC-1-A cells. HEC-1-A cells were pretreated or mock-pretreated with APY29, only or both APY29, and STF-083010 for 30 min and then infected or mock-infected with HSV-1.
    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    APY29, an ATP-competitive inhibitor, is an allosteric modulator of IRE1α which inhibits IRE1α autophosphorylation by binding to the ATP-binding pocket with IC50 of 280 nM. APY29 acts as a ligand that allosterically activates IRE1α adjacent RNase domain[1].

    IC50 & Target

    IC50: 280 nM (IRE1α)

    In Vitro

    APY29 divergently modulates the RNase activity and oligomerization state of IRE1α. APY29 is exerting their opposing effects on RNase activity through the same binding site. APY29 divergently affects IRE1α oligomerization. APY29 demonstrates opposing dose-dependent effects on ER stress-induced activation of the RNase of endogenous IRE1α[1].

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

    Molecular Weight

    332.36

    Formula

    C17H16N8

    CAS No.
    Appearance

    Solid

    Color

    White to yellow

    SMILES

    C1(NC2=CC=C3N=CNC3=C2)=NC=CC(NC4=NNC(C5CC5)=C4)=N1

    Shipping

    Room temperature in continental US; may vary elsewhere.

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

    DMSO : 50 mg/mL (150.44 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    H2O : 5 mg/mL (15.04 mM; ultrasonic and adjust pH to 3 with HCl)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 3.0088 mL 15.0439 mL 30.0879 mL
    5 mM 0.6018 mL 3.0088 mL 6.0176 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    * Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

    • Molarity Calculator

    • Dilution Calculator

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

    Mass
    =
    Concentration
    ×
    Volume
    ×
    Molecular Weight *

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

    ×
    Volume (start)

    V1

    =
    Concentration (final)

    C2

    ×
    Volume (final)

    V2

    In Vivo:

    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: ≥ 5 mg/mL (15.04 mM); Clear solution

      This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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.
    • Protocol 2

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: 5 mg/mL (15.04 mM); Clear solution; Need ultrasonic

      This protocol yields a clear solution of 5 mg/mL.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

      Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
    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.
    Purity & Documentation

    Purity: 99.90%

    References

    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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    H2O / DMSO 1 mM 3.0088 mL 15.0439 mL 30.0879 mL 75.2196 mL
    5 mM 0.6018 mL 3.0088 mL 6.0176 mL 15.0439 mL
    10 mM 0.3009 mL 1.5044 mL 3.0088 mL 7.5220 mL
    15 mM 0.2006 mL 1.0029 mL 2.0059 mL 5.0146 mL
    DMSO 20 mM 0.1504 mL 0.7522 mL 1.5044 mL 3.7610 mL
    25 mM 0.1204 mL 0.6018 mL 1.2035 mL 3.0088 mL
    30 mM 0.1003 mL 0.5015 mL 1.0029 mL 2.5073 mL
    40 mM 0.0752 mL 0.3761 mL 0.7522 mL 1.8805 mL
    50 mM 0.0602 mL 0.3009 mL 0.6018 mL 1.5044 mL
    60 mM 0.0501 mL 0.2507 mL 0.5015 mL 1.2537 mL
    80 mM 0.0376 mL 0.1880 mL 0.3761 mL 0.9402 mL
    100 mM 0.0301 mL 0.1504 mL 0.3009 mL 0.7522 mL

    * Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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    APY29 Related Classifications

    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.

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