AMG PERK 44

Name: AMG PERK 44
Brand: MedChemExpress
SKU: HY-12661A
Rating: 5.0 (10 reviews)

Cat. No.: HY-12661A Purity: 99.67%: Data Sheet
COA

SDS
Handling Instructions
FAQs
Technical Support

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.

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

CAS No. : 1883548-84-2

Size	Stock	Quantity

Free Sample (0.1 - 0.2 mg)	Apply Now
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
25 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	In-stock	Estimated Time of Arrival: December 31
100 mg	In-stock	Estimated Time of Arrival: December 31
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Customer Review

Based on 10 publication(s) in Google Scholar

10 Publications Citing Use of MCE AMG PERK 44

RT-PCR

Flow Cytometry

: 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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Description

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.

Molecular Weight

561.07

Formula

C₃₄H₂₉ClN₄O₂

CAS No.

1883548-84-2

Appearance

Solid

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

-20°C, sealed storage, away from moisture

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

Solvent & Solubility

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)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

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

View the 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.

Molarity Calculator
Dilution Calculator

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

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

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.

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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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.
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.
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

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

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

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

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

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).

Calculation results:

Working solution concentration: 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)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

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.

Purity & Documentation

Purity: 99.67%

Select Batch:

Data Sheet (280 KB) SDS (252 KB)

COA (256 KB) LCMS (95 KB)

Handling Instructions (2659 KB)

References

[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

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

AMG PERK 44 Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

AMG PERK 441883548-84-2AMG PERK44AMG PERK-44PERKAutophagyProtein kinase R-like endoplasmic reticulum kinasePKR-like endoplasmic reticulum kinaseorallyGCN2B-RafInhibitorinhibitorinhibit

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AMG PERK 44

Customer Review

AMG PERK 44 Related Antibodies

10 Publications Citing Use of MCE AMG PERK 44

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Purity & Documentation

References

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AMG PERK 44 Related Antibodies

Molarity Calculator

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Complete Stock Solution Preparation Table

AMG PERK 44 Related Classifications

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