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Art. -Nr.: HY-184599

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OICR-403184

OICR-403184 is a selective RNA-dependent protein kinase (PKR) inhibitor with limited brain penetration, with an IC₅₀ of 263 nM. OICR-403184 blocks the phosphorylation of eIF2α downstream of PKR. OICR-403184 is applicable to the research of inflammatory bowel disease.

Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.

Formel: C₂₄H₂₂F₃N₅O₂S₂
Molecular Weight:533.59

Speicherung:

Please store the product under the recommended conditions in the Certificate of Analysis.

OICR-403184 Chemical Structure

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

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

Biologische Aktivität

Beschreibung

IC₅₀ & Target^[1]

eIF2-α

In Vitro

OICR-403184 inhibits purified PKR with an IC₅₀ of 263 nM, while showing no detectable activity against BRAF WT and BRAF^V600E, and minimal activity against PERK, GCN2, and HRI in vitro^[1].
OICR-403184 (serial dilutions; 40 min) acts as an ATP-competitive inhibitor of purified PKR^[1].
OICR-403184 (0.005-1.1 μM; 4 h) does not induce paradoxical BRAF activation in HCT116 cells with wild-type BRAF and mutant KRAS, even at concentrations up to 1.1 μM^[1].
OICR-403184 (0.12-10 μM; 30 min-4 h pretreatment) shows no inhibitory activity against cellular PERK, HRI, or GCN2 in HEK293T cells at concentrations up to 10 μM^[1].
OICR-403184 (1 μM) exhibits high kinome selectivity, inhibiting only CaMKI by >50% at a concentration of 1 μM^[1].

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

Western Blot Analysis^[1]

Cell Line:

HCT116 cells (BRAF WT, KRAS G13D)
Concentration:

0.005-1.1 μM
Incubation Time:

4 h
Result:

Showed no paradoxical activation of RAF signaling at concentrations up to 1.1 μM, unlike dabrafenib which induced peak activation at ~40 nM.

Parmacokinetics

Species	Dose	Route	Plasma Concentration	Brain Concentration
Mice^[1]	10 mg/kg	p.o.	1887 (2 h) nM	25.9 (2 h) nM

In Vivo

OICR-403184 (10 mg/kg; p.o.; single dose) achieves adequate systemic plasma exposure but shows limited brain penetration in male NOD-SCID mice^[1].

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

Chemical Information

Molecular Weight 533.59
Formel C₂₄H₂₂F₃N₅O₂S₂
SMILES

CC1=NC(N)=NC(C(SC(C(C)(C)C)=N2)=C2C3=C(F)C(NS(C4=C(F)C=CC=C4F)(=O)=O)=CC=C3)=C1
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

Please store the product under the recommended conditions in the Certificate of Analysis.

Reinheit & Dokumentation

Handling Instructions (2659 KB)

Verweise

[1]. Yin J, et al. Structural Transformation of a BRAF Inhibitor into a Selective PKR Inhibitor. Journal of medicinal chemistry. 2026 Jun 22. [Content Brief]

Calculators

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)}

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.

Keywords

MOQ

Minimum order quantity

100 mg

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