PF-5236216
PF-5236216 is a brain-penetrant CK1δ/CK1ε inhibitor with IC50 values of 8 and 36 nM. PF-5236216 inhibits CK1δ and CK1ε-mediated PER3 nuclear translocation. PF-5236216 forms an H-bond with the backbone NH of Leu85, hydrophobic stacking with Met82, and a water-mediated H-bond with Lys38 of CK1δ. PF-5236216 can be used as a tool ligand for CNS PET studies.
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- CAS. Nr.: 1383376-93-9
- Formel: C18H15FN4O
- Molecular Weight:322.34
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
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Chemical Information
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Biologische Aktivität
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CK1δ 8 nM (IC50) |
CK1ε 36 nM (IC50) |
PF-5236216 (Compound 9) (60 min) potently inhibits purified human CK1δ enzyme with an IC50 of 8 nM[1].
PF-5236216 (85 min) inhibits purified human CK1 enzyme with an IC50 of 36 nM[1].
PF-5236216 (overnight) inhibits human CK1δ-mediated PER3 nuclear translocation in COS-7 cells with an EC50 of 58 nM[1].
PF-5236216 (overnight) inhibits human CK1ε-mediated PER3 nuclear translocation in COS-7 cells with an EC50 of 318 nM[1].
PF-5236216 shows ≥70-fold selectivity for human CK1δ over 4 off-target kinases (CK1α, p38, ZC1, ZC3) in cell-free enzyme assays[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
PF-5236216 (56 mg/kg; s.c.; single dose) binds to CK1δ/ε in rat hypothalamus tissue with a Bmax of 250.2 fmol/mg and a Kd of 10.2 nM[1].
PF-5236216 (56 mg/kg; s.c.; single dose) binds to CK1δ/ε in monkey hypothalamus tissue with a Bmax of 135 fmol/mg and a Kd of 3.0 nM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6J (male, 9-12 weeks of age)[1]
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Dosage:56 mg/kg
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Administration:s.c.; single dose
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Result:Achieved a maximum free brain concentration (Cmax,b,u) of 8685 nM.
Determined a CK1δ/ε Bmax of 214.2 fmol/mg (10.7 nM) and a Kd of 10.4 nM, giving a Bmax/Kd ratio of 1.0.
Chemical Information
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CAS. Nr. 1383376-93-9
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Molecular Weight 322.34
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Formel C18H15FN4O
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SMILES
O=C1C2=C(C3=CN(C)N=C3C4=CC=C(F)C=C4)C=CN=C2CN1C
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
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Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
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