1. Apoptosis
  2. RIP kinase
  3. GSK2983559 free acid

GSK2983559 free acid (compound 3) is an orally active and potent receptor interacting protein 2 (RIP2) kinase inhibitor. GSK2983559 free acid can block many proinflammatory cytokine responses in vivo and in human inflammatory bowel disease explant samples.

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

GSK2983559 free acid Chemical Structure

GSK2983559 free acid Chemical Structure

CAS No. : 1579965-12-0

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Based on 1 publication(s) in Google Scholar

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Description

GSK2983559 free acid (compound 3) is an orally active and potent receptor interacting protein 2 (RIP2) kinase inhibitor. GSK2983559 free acid can block many proinflammatory cytokine responses in vivo and in human inflammatory bowel disease explant samples[1].

IC50 & Target[1]

RIPK2

 

Cellular Effect
Cell Line Type Value Description References
THP-1 IC50
1.34 nM
Compound: 5; GSK2983559
Antiinflammatory activity in MDP-stimulated IL-8 production in human THP-1 cells pretreated for 2 hrs followed by MDP stimulation for 6 hrs
Antiinflammatory activity in MDP-stimulated IL-8 production in human THP-1 cells pretreated for 2 hrs followed by MDP stimulation for 6 hrs
[PMID: 36058467]
In Vitro

GSK2983559 (1-1024 nM; 2 h) blocks MDP-induced IL-8 in THP-1 cells[2].

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

Cell Viability Assay[2]

Cell Line: THP-1 cells
Concentration: 1-1024 nM
Incubation Time: 2 hours
Result: Inhibited IL-8 production with an IC50 of 1.34 nM.
In Vivo

GSK2983559 (oral gavage; 3 and 10 mg/kg; once) inhibits effectively MDP-induced IL-6 in mouse[2].

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

Animal Model: C57BL/6 mice (female) injected with MDP (100 μg)[2]
Dosage: 3 and 10 mg/kg
Administration: Oral gavage; 3 and 10 mg/kg; once
Result: Suppressed serum IL-6 levels in a dose-dependent manner.
Clinical Trial
Molecular Weight

538.53

Formula

C21H23N4O7PS2

CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

CC(C)(C)S(C(C(OCCOP(O)(O)=O)=CC1=NC=N2)=CC1=C2NC3=CC(N=CS4)=C4C=C3)(=O)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 5 mg/mL (9.28 mM; ultrasonic and warming and heat to 80°C; 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 1.8569 mL 9.2845 mL 18.5691 mL
5 mM 0.3714 mL 1.8569 mL 3.7138 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, 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.

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

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

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation

Purity: 99.90%

References

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, 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
DMSO 1 mM 1.8569 mL 9.2845 mL 18.5691 mL 46.4227 mL
5 mM 0.3714 mL 1.8569 mL 3.7138 mL 9.2845 mL
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GSK2983559 free acid 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.

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GSK2983559 free acid
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