2. Cell Cycle/DNA Damage Stem Cell/Wnt
  3. Casein Kinase
  4. 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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PF-5236216

PF-5236216 Chemical Structure

CAS No. : 1383376-93-9

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PF-5236216 Related Antibodies

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Description

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[1].

IC50 & Target[1]

CK1δ

8 nM (IC50)

CK1ε

36 nM (IC50)

In Vitro

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 Related Antibodies
In Vivo

PF-5236216 (Compound 9) (56 mg/kg; s.c.; single dose) achieves high free brain exposure in male C57BL/6J mice and binds to CK1δ/ε in mouse hypothalamus tissue with a Bmax of 214.2 fmol/mg and a Kd of 10.4 nM[1].
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.

Animal Model: C57BL/6J (male, 9-12 weeks of age)[1]
Dosage: 56 mg/kg
Administration: s.c.; single dose
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.
Molecular Weight

322.34

Formula

C18H15FN4O
CAS No.
SMILES

O=C1C2=C(C3=CN(C)N=C3C4=CC=C(F)C=C4)C=CN=C2CN1C
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Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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PF-5236216 Related Classifications

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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.

Keywords:

PF-52362161383376-93-9PF5236216PF 5236216Casein KinaseCK1εCK1δLys38C57BL/6J miceMet82human CK1δCOS-7 cellshuman CK1εLeu85hypothalamus tissueInhibitorinhibitorinhibit

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