APY29
Based on 11 publication(s) in Google Scholar
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.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 98.92%
- No. CAS: 1216665-49-4
- Fòrmula: C17H16N8
- Peso molecular:332.36
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
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Endoplasmic Reticulum Stress Compound Library
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Publications Citing Use of MedChemExpress (MCE) APY29
More- Nat Commun. 2023 Nov 17;14(1):7441. [Abstract]
- Sci Transl Med. 2019 Feb 6;11(478):eaau5266. [Abstract]
- Sci Adv. 2019 Apr 10;5(4):eaaw0025. [Abstract]
- EMBO J. 2019 Aug 1;38(15):e100999.
- FEBS J. 2019 Apr;286(7):1375-1392. [Abstract]
- Viruses. 2020 Sep 2;12(9):974. [Abstract]
- Viruses. 2017 Aug 23;9(9):235. [Abstract]
- Food Chem Toxicol. 2018 Apr:114:52-60. [Abstract]
- Vet Microbiol. 2026 May:316:110968. [Abstract]
- Vet Microbiol. 2020 May:244:108648. [Abstract]
- FASEB Bioadv. 2025 Jul 9;7(7):e70031. [Abstract]
Customer Validation & Images
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IHC
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Cell Proliferation/Viability Assay
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IHC
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WB
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WB
Actividad biológica
IC50: 280 nM (IRE1α)
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.
Chemical Information
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No. CAS 1216665-49-4
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Appearance Solid
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Peso molecular 332.36
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Fòrmula C17H16N8
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Color White to yellow
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SMILES
C1(NC2=CC=C3N=CNC3=C2)=NC=CC(NC4=NNC(C5CC5)=C4)=N1
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (11)
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Journal Impact Factor
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Most Recent
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Nat Commun
2023 Nov 17;14(1):7441. PMID: 37978190 -
Sci Transl Med
Modulation of the sigma-1 receptor-IRE1 pathway is beneficial in preclinical models of inflammation and sepsis. [Abstract]2019 Feb 6;11(478):eaau5266. PMID: 30728287 -
Sci Adv
Transient activation of the UPRER is an essential step in the acquisition of pluripotency during reprogramming. [Abstract]2019 Apr 10;5(4):eaaw0025. PMID: 30989118 -
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FEBS J
2019 Apr;286(7):1375-1392. PMID: 30719816
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: 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]
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.
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Viruses
2020 Sep 2;12(9):974. PMID: 32887282 -
Viruses
Opposite Roles of RNase and Kinase Activities of Inositol-Requiring Enzyme 1 (IRE1) on HSV-1 Replication. [Abstract]2017 Aug 23;9(9):235. PMID: 28832521
APY29 purchased from MedChemExpress. Usage Cited in: Viruses. 2017 Aug 23;9(9):235. [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.
APY29 purchased from MedChemExpress. Usage Cited in: Viruses. 2017 Aug 23;9(9):235. [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.
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Food Chem Toxicol
Quercetin ameliorates HFD-induced NAFLD by promoting hepatic VLDL assembly and lipophagy via the IRE1a/XBP1s pathway. [Abstract]2018 Apr:114:52-60. PMID: 29438776
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.
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Vet Microbiol
The PERK-eIF2α branch activates the NLRP3 inflammasome through the NF-κB signaling pathway to suppress NDV replication. [Abstract]2026 May:316:110968. PMID: 41793984 -
Vet Microbiol
A rough Brucella mutant induced macrophage death depends on secretion activity of T4SS, but not on cellular Txnip- and Caspase-2-mediated signaling pathway. [Abstract]2020 May:244:108648. PMID: 32402333 -
FASEB Bioadv
Endoplasmic Reticulum Stress and Unfolded Protein Response Sensor ERN1 Regulates Organic Dust Induction of Lung Inflammation. [Abstract]2025 Jul 9;7(7):e70031. PMID: 40641847
Solvente y solubilidad
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
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.
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.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
Pureza y Documentación
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Ficha de datos (272 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Instrucciones de manejo (2659 KB)
Referencias
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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