AMG PERK 44
Based on 13 publication(s) in Google Scholar
AMG PERK 44 is an orally active and highly selective PERK inhibitor with an IC50 of 6 nM. AMG PERK 44 has 1000-fold and 160-fold selectivity over GCN2 (IC50=7300 nM) and B-Raf (IC50 >1000 nM), respectively. AMG PERK 44 induces autophagy.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza : 99.67%
- No. CAS: 1883548-84-2
- Fòrmula: C34H29ClN4O2
- Peso molecular:561.07
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Almacenamiento:
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 1 year; -20°C, 6 months (sealed storage, away from moisture)
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
- Protocolo
- Pureza y Documentación
- Referencias
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) AMG PERK 44
More- Cell. 2024 Apr 25;187(9):2288-2304.e27. [Abstract]
- Cancer Commun (Lond). 2025 Nov 10. [Abstract]
- Cell Rep Med. 2026 May 19;7(5):102788. [Abstract]
- J Pharm Anal. 2026 May 26.
- Int J Biol Macromol. 2025 May;308(Pt 4):142265. [Abstract]
- Cancer Immunol Res. 2026 Jan 21:10.1158/2326-6066.CIR-25-0743. [Abstract]
- Int Immunopharmacol. 2026 Oct 1:186:117091.
- Cancer Res Commun. 2023 Dec 8;3(12):2497-2509. [Abstract]
- Vet Microbiol. 2025 Aug:307:110559. [Abstract]
- bioRxiv. 2026 Feb 1:2026.01.28.702376. [Abstract]
- Paris-Saclay University. 2025.
- bioRxiv. 2024 Feb 19.
- bioRxiv. 2023 Jul 27
Customer Validation & Images
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RT-PCR
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WB
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RT-PCR
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Flow Cytometry
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Flow Cytometry
Actividad biológica
Descripciòn
IC50 & Target
IC50: 6 nM (PERK)[1]
In Vitro
In Vivo
AMG PERK 44 (iv; 1 mg/kg) has a CL of 1.6 L/h kg, a Vss of 3.6 L/kg and MRT of 2.3 hours in Sprague-Dawley rats and male CD-1 mice[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Four- to six-week old naive athymic nude mice[1]
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Dosage:3, 10, 30, 100 mg/kg
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Administration:Orally
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Result:Robustly inhibited PERK autophosphorylation in this assay (ED50=3 mg/kg; ED90=60 mg/kg at the 4 hours time point).
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Animal Model:Sprague-Dawley rats and male CD-1 mice[1]
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Dosage:1 mg/kg (Pharmacokinetic Analysis)
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Administration:Iv
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Result:Had a CL of 1.6 L/h•kg, a Vss of 3.6 L/kg and a MRT of 2.3 hours.
Chemical Information
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No. CAS 1883548-84-2
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Appearance Solid
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Peso molecular 561.07
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Fòrmula C34H29ClN4O2
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Color Light yellow to yellow
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SMILES
O=C1N(C2=CC=CC=C2)N(C)C(C3=CC=CC=C3)=C1C(C4=CC=C(C)C(C5=CC=C6N=C(C)C=CC6=C5)=C4N)=O.[H]Cl
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 1 year; -20°C, 6 months (sealed storage, away from moisture)
Publications (13)
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Journal Impact Factor
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Most Recent
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Cell
Cancer SLC6A6-mediated taurine uptake transactivates immune checkpoint genes and induces exhaustion in CD8+ T cells. [Abstract]2024 Apr 25;187(9):2288-2304.e27. PMID: 38565142
AMG PERK 44 purchased from MedChemExpress. Usage Cited in: Cell. 2024 Apr 25;187(9):2288-2304.e27. [Abstract]
ATF4 levels in CD8+ T cells transfected with siSLC6A6 or cultured with MKN45 cell supernatant and AMG PERK 44 (AMG) (5 nM).
AMG PERK 44 purchased from MedChemExpress. Usage Cited in: Cell. 2024 Apr 25;187(9):2288-2304.e27. [Abstract]
AMG PERK 44 (AMG) (5 nM) abolished increases in p-JAK1 and p-STAT3 levels in CD8+ T cells induced by Thaps treatment.
AMG PERK 44 purchased from MedChemExpress. Usage Cited in: Cell. 2024 Apr 25;187(9):2288-2304.e27. [Abstract]
AMG PERK 44 (AMG) (5 nM) inhibited ATF4 mRNA expression in Thaps-treated CD8+ T cells.
AMG PERK 44 purchased from MedChemExpress. Usage Cited in: Cell. 2024 Apr 25;187(9):2288-2304.e27. [Abstract]
Flow cytometric analysis of Annexin V- or IFNg/TNFa-positive CD8+ T cells cultured with MKN45 cell supernatant and treated with AMG PERK 44 (AMG) (5 nM).
AMG PERK 44 purchased from MedChemExpress. Usage Cited in: Cell. 2024 Apr 25;187(9):2288-2304.e27. [Abstract]
Flow cytometric analysis of Annexin V- or IFNg/TNFa-positive CD8+ T cells transfected with siSLC6A6 and treated with AMG PERK 44 (AMG) (5 nM).
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Cancer Commun (Lond)
Unfolded protein response kinase PERK supports survival and metastasis of circulating tumor cell clusters via SAM synthesis and H3K4me3-dependent PDGFB signaling. [Abstract]2025 Nov 10. PMID: 41212905 -
Cell Rep Med
Taxane chemotherapy promotes response to TIM-3 checkpoint blockade via STING-mediated ER stress and HMGB1 secretion. [Abstract]2026 May 19;7(5):102788. PMID: 42097146 -
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Int J Biol Macromol
Preparation of cellulose microfibrils from Gelidium amansii relieving ocular endoplasmic reticulum stress and inflammatory responses in human retinal pigmented epithelial cells. [Abstract]2025 May;308(Pt 4):142265. PMID: 40120910 -
Cancer Immunol Res
Ex Vivo Immuno-Oncology Platform Reveals Spatial T Cell Infiltration Patterns Linked to ATR Inhibition Responses in High-Grade Serous Ovarian Cancer. [Abstract]2026 Jan 21:10.1158/2326-6066.CIR-25-0743. PMID: 41563843 -
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Cancer Res Commun
Statin-induced mitochondrial priming sensitizes multiple myeloma cells to BCL2 and MCL1 inhibitors. [Abstract]2023 Dec 8;3(12):2497-2509. PMID: 37956312 -
Vet Microbiol
PERK-mediated eIF2α phosphorylation suppresses porcine epidemic diarrhea virus replication by attenuating global protein synthesis and inducing IFN-Ⅰ production. [Abstract]2025 Aug:307:110559. PMID: 40494050 -
bioRxiv
The active secretion of a subunit of IL-12 by tissue cells is regulated by Valosin-Containing Protein and intracellular calcium redistribution. [Abstract]2026 Feb 1:2026.01.28.702376. PMID: 41659431 -
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Solvente y solubilidad
In Vitro:
DMSO : 25 mg/mL (44.56 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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, 1 year; -20°C, 6 months (sealed storage, away from moisture). When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
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, 1 year; -20°C, 6 months (sealed storage, away from moisture). When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (3.71 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: ≥ 2.08 mg/mL (3.71 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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:
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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. * In solvent : -80°C, 1 year; -20°C, 6 months (sealed storage, away from moisture)
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 (280 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
[1]. Smith AL, et al. Discovery of 1H-pyrazol-3(2H)-ones as potent and selective inhibitors of protein kinase R-like endoplasmic reticulum kinase (PERK). J Med Chem. 2015 Feb 12;58(3):1426-41. [Content Brief]
[2]. Roest G, et al. The ER Stress Inducer l-Azetidine-2-Carboxylic Acid Elevates the Levels of Phospho-eIF2α and of LC3-II in a Ca2+-Dependent Manner. Cells. 2018 Nov 30;7(12). pii: E239. [Content Brief]
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, 1 year; -20°C, 6 months (sealed storage, away from moisture). When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.7823 mL | 8.9115 mL | 17.8231 mL | 44.5577 mL |
| 5 mM | 0.3565 mL | 1.7823 mL | 3.5646 mL | 8.9115 mL | |
| 10 mM | 0.1782 mL | 0.8912 mL | 1.7823 mL | 4.4558 mL | |
| 15 mM | 0.1188 mL | 0.5941 mL | 1.1882 mL | 2.9705 mL | |
| 20 mM | 0.0891 mL | 0.4456 mL | 0.8912 mL | 2.2279 mL | |
| 25 mM | 0.0713 mL | 0.3565 mL | 0.7129 mL | 1.7823 mL | |
| 30 mM | 0.0594 mL | 0.2971 mL | 0.5941 mL | 1.4853 mL | |
| 40 mM | 0.0446 mL | 0.2228 mL | 0.4456 mL | 1.1139 mL |
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