Art. -Nr.: HY-148238

GNE-2256

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GNE-2256 (molecule 19), a chemical probe, is an orally active IRAK4 (Interleukin 1 receptor associated kinase 4) inhibitor (IRAK4 K_i=1.4 nM; IL-6 IC₅₀=190 nM).

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Reinheit: 99.14%
CAS. Nr.: 2102170-43-2
Formel: C₂₄H₂₇FN₆O₄
Molecular Weight:482.51

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

GNE-2256 Chemical Structure

CAS. Nr.: 2102170-43-2

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

Biologische Aktivität

Beschreibung

GNE-2256 (molecule 19), a chemical probe, is an orally active IRAK4 (Interleukin 1 receptor associated kinase 4) inhibitor (IRAK4 K_i=1.4 nM; IL-6 IC₅₀=190 nM)^[1].

IC₅₀ & Target^[1]

IRAK4

1.4 nM (Ki)

Alle IRAK Isoform-spezifische Produkte anzeigen :

In Vivo

GNE-2256 (3 mg/kg) shows inhibition of IL-6, TNFα, and IFNα secretion in R848-induced mouse PD model^[1].

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

Chemical Information

CAS. Nr. 2102170-43-2
Appearance Solid
Molecular Weight 482.51
Formel C₂₄H₂₇FN₆O₄
Color off-white
SMILES

O=C(C1=C2N(C=CC=N2)N=C1)NC3=C(N4CCOCC4)C=C5C(CN(C5=O)C[C@@H](F)C(C)(O)C)=C3
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 50 mg/mL (103.62 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

2.0725 mL

10.3625 mL

20.7250 mL

5 mM

0.4145 mL

2.0725 mL

4.1450 mL

10 mM

0.2072 mL

1.0362 mL

2.0725 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.5 mg/mL (5.18 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 2

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

Solubility: ≥ 2.5 mg/mL (5.18 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 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 (25.0 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 (277 KB)
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 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]. Rajapaksa NS, et al. Discovery of Potent Benzolactam IRAK4 Inhibitors with Robust in Vivo Activity. ACS Med Chem Lett. 2019 Nov 11;11(3):327-333. [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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.0725 mL	10.3625 mL	20.7250 mL	51.8124 mL
	5 mM	0.4145 mL	2.0725 mL	4.1450 mL	10.3625 mL
	10 mM	0.2072 mL	1.0362 mL	2.0725 mL	5.1812 mL
	15 mM	0.1382 mL	0.6908 mL	1.3817 mL	3.4542 mL
	20 mM	0.1036 mL	0.5181 mL	1.0362 mL	2.5906 mL
	25 mM	0.0829 mL	0.4145 mL	0.8290 mL	2.0725 mL
	30 mM	0.0691 mL	0.3454 mL	0.6908 mL	1.7271 mL
	40 mM	0.0518 mL	0.2591 mL	0.5181 mL	1.2953 mL
	50 mM	0.0414 mL	0.2072 mL	0.4145 mL	1.0362 mL
	60 mM	0.0345 mL	0.1727 mL	0.3454 mL	0.8635 mL
	80 mM	0.0259 mL	0.1295 mL	0.2591 mL	0.6477 mL
	100 mM	0.0207 mL	0.1036 mL	0.2072 mL	0.5181 mL

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GNE-2256

Immunology/Inflammation Compound Library

Kinase Inhibitor Library

Orally Active Compound Library

Antidepressant Compound Library

Anti-Prostate Cancer Compound Library

Pain-Related Compound Library

Highly Selective Inhibitors Library

Serine/Threonine Kinase Inhibitor Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Protein Kinase Compound Library

High-Throughput Bioactive Compound Library

Anti-Rheumatic Arthritis Compound Library

Alle IRAK Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

GNE-2256

Immunology/Inflammation Compound Library

Kinase Inhibitor Library

Orally Active Compound Library

Antidepressant Compound Library

Anti-Prostate Cancer Compound Library

Pain-Related Compound Library

Highly Selective Inhibitors Library

Serine/Threonine Kinase Inhibitor Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Protein Kinase Compound Library

High-Throughput Bioactive Compound Library

Anti-Rheumatic Arthritis Compound Library

Alle IRAK Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

GNE-2256 Related Classifications

HY-148238 Related Classifications