Art. -Nr.: HY-12661A

AMG PERK 44

12 Cited Publications

Kundenbewertung

Based on 12 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.

Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.

Reinheit: 99.67%
CAS. Nr.: 1883548-84-2
Formel: C₃₄H₂₉ClN₄O₂
Molecular Weight:561.07

Speicherung:

-20°C, sealed storage, away from moisture

* In solvent : -80°C, 1 year; -20°C, 6 months (sealed storage, away from moisture)

AMG PERK 44 Chemical Structure

CAS. Nr.: 1883548-84-2

Größe

Preis

Verfügbarkeit

Menge

Amount: USD 0.00

* Bitte wählen Sie Menge, bevor Sie Artikel hinzufügen.

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
- In Vivo
Chemical Information
Publications (12)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

IC50: 6 nM (PERK)^[1]

In Vitro

AMG PERK 44 has an IC₅₀ of 84 nM for cell pPERK^[1].

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

In Vivo

AMG PERK 44 (orally; 3-100 mg/kg) robustly inhibits PERK autophosphorylation in this assay (ED₅₀=3 mg/kg; ED₉₀=60 mg/kg at the 4 hours time point), and >50% target coverage is maintained for 24 h in a time course PD assay when dosed at 100 mg/kg po^[1].
AMG PERK 44 (iv; 1 mg/kg) has a CL of 1.6 L/h kg, a V_ss 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.

Animal Model:

Four- to six-week old naive athymic nude mice^[1]
Dosage:

3, 10, 30, 100 mg/kg
Administration:

Orally
Result:

Robustly inhibited PERK autophosphorylation in this assay (ED₅₀=3 mg/kg; ED₉₀=60 mg/kg at the 4 hours time point).

Animal Model:

Sprague-Dawley rats and male CD-1 mice^[1]
Dosage:

1 mg/kg (Pharmacokinetic Analysis)
Administration:

Iv
Result:

Had a CL of 1.6 L/h•kg, a V_ss of 3.6 L/kg and a MRT of 2.3 hours.

Chemical Information

CAS. Nr. 1883548-84-2
Appearance Solid
Molecular Weight 561.07
Formel C₃₄H₂₉ClN₄O₂
Color Light yellow to yellow
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
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

-20°C, sealed storage, away from moisture

* In solvent : -80°C, 1 year; -20°C, 6 months (sealed storage, away from moisture)

Publications (12)

All RT-PCRWBFlow Cytometry

Sort by:

Journal Impact Factor

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).
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
J Pharm Anal

2026 May 26.
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
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
Paris-Saclay University

2025.
bioRxiv

2024 Feb 19.
bioRxiv

2023 Jul 27

Lösungsmittel & Löslichkeit

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)

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

1.7823 mL

8.9115 mL

17.8231 mL

5 mM

0.3565 mL

1.7823 mL

3.5646 mL

10 mM

0.1782 mL

0.8912 mL

1.7823 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, 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.

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: ≥ 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.

Protocol 2

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.

Protocol 3

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

Solubility: ≥ 2.08 mg/mL (3.71 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 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 (20.8 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 (280 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]. 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]

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

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

Keywords

AMG PERK 44

12 Cited Publications

100 mg Angebot einholen

Subscribe to the

MedChemExpress

Newsletter

Produktname:
Art. -Nr.:
Menge:
MCE Japan Authorized Agent:

Produktname:
CAS. Nr.:
Species:
Reinheit:
Menge:

AMG PERK 44

Endoplasmic Reticulum Stress Compound Library

Targeted Diversity Library

Heterocyclic Compound Library

Highly Selective Inhibitors Library

Highly Selective Activators Library

Cell Death Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Anti-Aging Compound Library Mini

Cell Cycle/DNA Damage Compound Library

Kinase Inhibitor Library

Anti-Cancer Compound Library

Autophagy Compound Library

Anti-Aging Compound Library

Publications Citing Use of MedChemExpress (MCE) AMG PERK 44

Biologische Aktivität

Chemical Information

Publications (12)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

AMG PERK 44

Endoplasmic Reticulum Stress Compound Library

Targeted Diversity Library

Heterocyclic Compound Library

Highly Selective Inhibitors Library

Highly Selective Activators Library

Cell Death Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Anti-Aging Compound Library Mini

Cell Cycle/DNA Damage Compound Library

Kinase Inhibitor Library

Anti-Cancer Compound Library

Autophagy Compound Library

Anti-Aging Compound Library

Publications Citing Use of MedChemExpress (MCE) AMG PERK 44

Biologische Aktivität

Chemical Information

Publications (12)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

AMG PERK 44 Related Classifications

HY-12661A Related Classifications