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.
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- Fòrmula: C24H22F3N5O2S2
- Peso molecular:533.59
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
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Chemical Information
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Help & FAQs
Actividad biológica
Descripciòn
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 BRAFV600E, 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.
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Cell Line:HCT116 cells (BRAF WT, KRAS G13D)
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Concentration:0.005-1.1 μM
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Incubation Time:4 h
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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
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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Peso molecular 533.59
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Fòrmula C24H22F3N5O2S2
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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
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
OICR-403184 Related Classifications
HY-184599 Related Classifications
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