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

APY29 

Cat. No.: HY-17537 Purity: 99.54%
Handling Instructions

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.

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

APY29 Chemical Structure

APY29 Chemical Structure

CAS No. : 1216665-49-4

Size Price Stock Quantity
10 mM * 1  mL in DMSO USD 198 In-stock
Estimated Time of Arrival: December 31
10 mg USD 180 In-stock
Estimated Time of Arrival: December 31
50 mg USD 780 In-stock
Estimated Time of Arrival: December 31
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200 mg   Get quote  

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Customer Review

Based on 15 publication(s) in Google Scholar

Top Publications Citing Use of Products

    APY29 purchased from MCE. Usage Cited in: Food Chem Toxicol. 2018 Feb 10;114:52-60.

    (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 MCE. Usage Cited in: Viruses. 2017 Aug 23;9(9). pii: E235. 

    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.

    APY29 purchased from MCE. Usage Cited in: Viruses. 2017 Aug 23;9(9). pii: E235. 

    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 MCE. Usage Cited in: FEBS J. 2019 Apr;286(7):1375-1392.

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

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

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

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

    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 MCE. Usage Cited in: FEBS J. 2019 Apr;286(7):1375-1392.

    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.
    • Biological Activity

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    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].

    Molecular Weight

    332.36

    Formula

    C₁₇H₁₆N₈

    CAS No.

    1216665-49-4

    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 6 months
      -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 100 mg/mL (300.88 mM)

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

    *"≥" means soluble, but saturation unknown.

    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
    10 mM 0.3009 mL 1.5044 mL 3.0088 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

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

      Solubility: ≥ 2.5 mg/mL (7.52 mM); Clear solution

    • 2.

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

      Solubility: ≥ 2.5 mg/mL (7.52 mM); Clear solution

    • 3.

      Add each solvent one by one:  10% DMSO    90% corn oil

      Solubility: ≥ 2.5 mg/mL (7.52 mM); Clear solution

    *All of the co-solvents are provided by MCE.
    References

    Purity: 99.54%

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    Keywords:

    APY29APY 29APY-29IRE1Inositol requiring enzyme 1Inhibitorinhibitorinhibit

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    Product Name:
    APY29
    Cat. No.:
    HY-17537
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