Art. -Nr.: HY-17537

APY29

11 Cited Publications

Kundenbewertung

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.

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Reinheit: 98.92%
CAS. Nr.: 1216665-49-4
Formel: C₁₇H₁₆N₈
Molecular Weight:332.36

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

APY29 Chemical Structure

CAS. Nr.: 1216665-49-4

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
Chemical Information
Publications (11)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

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.

Chemical Information

CAS. Nr. 1216665-49-4
Appearance Solid
Molecular Weight 332.36
Formel C₁₇H₁₆N₈
Color White to yellow
SMILES

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

Room temperature in continental US; may vary elsewhere.

Speicherung

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

Nat Commun

SEPTIN2 suppresses an IFN-γ-independent, proinflammatory macrophage activation pathway. [Abstract]

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
EMBO J

2019 Aug 1;38(15):e100999. PMID: 31196886
FEBS J

IRE1α is critical for Kaempferol-induced neuroblastoma differentiation. [Abstract]

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.
Viruses

Induction of the Unfolded Protein Response during Bovine Alphaherpesvirus 1 Infection. [Abstract]

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.
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.
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

Lösungsmittel & Löslichkeit

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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. 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.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

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

Stock Solution Working Solution

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.

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.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

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

This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (272 KB)
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)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Wang L, et al. Divergent allosteric control of the IRE1α endoribonuclease using kinase inhibitors. Nat Chem Biol. 2012 Dec;8(12):982-9. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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.

Keywords

APY29

11 Cited Publications

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APY29

Cell Cycle/DNA Damage Compound Library

Kinase Inhibitor Library

Anti-Cancer Compound Library

Anti-Aging Compound Library

Endoplasmic Reticulum Stress Compound Library

Allosteric Modulators (AMs) Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Protein Kinase Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Publications Citing Use of MedChemExpress (MCE) APY29

Biologische Aktivität

Chemical Information

Publications (11)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

APY29

Cell Cycle/DNA Damage Compound Library

Kinase Inhibitor Library

Anti-Cancer Compound Library

Anti-Aging Compound Library

Endoplasmic Reticulum Stress Compound Library

Allosteric Modulators (AMs) Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Protein Kinase Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Publications Citing Use of MedChemExpress (MCE) APY29

Biologische Aktivität

Chemical Information

Publications (11)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

APY29 Related Classifications

HY-17537 Related Classifications