1. Cell Cycle/DNA Damage
    Stem Cell/Wnt
  2. Casein Kinase
  3. PF-4800567

PF-4800567 

Cat. No.: HY-12470 Purity: 98.38%
Handling Instructions

PF-4800567 is a potent and selective inhibitor of casein kinase 1ϵ (CK1ϵ), with an IC50 of 32 nM, which is greater than 20-fold selectivity over CK1δ (IC50, 711 nM).

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

PF-4800567 Chemical Structure

PF-4800567 Chemical Structure

CAS No. : 1188296-52-7

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 88 In-stock
Estimated Time of Arrival: December 31
5 mg USD 80 In-stock
Estimated Time of Arrival: December 31
10 mg USD 140 In-stock
Estimated Time of Arrival: December 31
25 mg USD 290 In-stock
Estimated Time of Arrival: December 31
50 mg USD 490 In-stock
Estimated Time of Arrival: December 31
100 mg USD 850 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

PF-4800567 is a potent and selective inhibitor of casein kinase 1ϵ (CK1ϵ), with an IC50 of 32 nM, which is greater than 20-fold selectivity over CK1δ (IC50, 711 nM).

IC50 & Target[1]

CK1ϵ

32 nM (IC50)

CKIδ

711 nM (IC50)

In Vitro

PF-4800567 is a potent and selective inhibitor of casein kinase 1ϵ (CK1ϵ), with an IC50 of 32 nM, which is greater than 20-fold selectivity over CK1δ (IC50, 711 nM). PF-4800567 shows inhibitory activity against CK1ϵ and CK1δ in whole cells, with IC50s of 2.65 and 20.38 μM, respectively. PF-4800567 (0.01-10 μM) blocks CK1ϵ-mediated PER3 nuclear localization mediated by CK1ϵ and suppresses PER2 degradation at 1 μM. In addition, PF-4800567 has little effect on the circadian clock at 32 nM[1].

In Vivo

PF-4800567 (100 mg/kg, s.c.) is rapidly absorpted and distributed in plasma and brain of mice[1].

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 75 mg/mL (208.44 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.7792 mL 13.8962 mL 27.7924 mL
5 mM 0.5558 mL 2.7792 mL 5.5585 mL
10 mM 0.2779 mL 1.3896 mL 2.7792 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (6.95 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (6.95 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (6.95 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
Cell Assay
[1]

For drug treatment, 24 h after synchronization, individual dishes of cells under PMT recording are treated with CK1 inhibitors (PF-4800567 or PF-670462 at a range of doses) or DMSO (vehicle control). The compounds are left continuously with the samples thereafter, and the luminescence patterns are recorded for at least 6 days. Periods are analyzed by use of RAP software[1].

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

References
Molecular Weight

359.81

Formula

C₁₇H₁₈ClN₅O₂

CAS No.

1188296-52-7

SMILES

NC1=C2C(N(C3CCOCC3)N=C2COC4=CC=CC(Cl)=C4)=NC=N1

Shipping

Room temperature in continental US; may vary elsewhere

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The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2

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Product Name:
PF-4800567
Cat. No.:
HY-12470
Quantity:

PF-4800567

Cat. No.: HY-12470