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

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
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 88 In-stock
Solution
10 mM * 1 mL in DMSO USD 88 In-stock
Solid
1 mg USD 41 In-stock
5 mg USD 80 In-stock
10 mg USD 130 In-stock
25 mg USD 280 In-stock
50 mg USD 410 In-stock
100 mg USD 590 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 2 publication(s) in Google Scholar

Other Forms of PF-4800567:

PF-4800567 Related Antibodies

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CK1 CK2

  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

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]

CKIδ

711 nM (IC50)

In Vitro

PF-4800567 is a potent and selective inhibitor of casein kinase 1? (CK1?), with an IC50 of 32 nM, which is greater than 20-fold selectivity over CK1δ (IC50, 711 nM). PF-4800567 shows inhibitory activity against CK1? and CK1δ in whole cells, with IC50s of 2.65 and 20.38 μM, respectively. PF-4800567 (0.01-10 μM) blocks CK1?-mediated PER3 nuclear localization mediated by CK1? and suppresses PER2 degradation at 1 μM. In addition, PF-4800567 has little effect on the circadian clock at 32 nM[1].

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

PF-4800567 Related Antibodies
In Vivo

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

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

359.81

Formula

C17H18ClN5O2
CAS No.
Appearance

Solid

Color

Off-white to light yellow

SMILES

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

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 40 mg/mL (111.17 mM; ultrasonic and adjust pH to 3 with 1 M HCL; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    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

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    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

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.69%

COA (255 KB) HNMR (264 KB) LCMS (91 KB)

Handling Instructions (2659 KB)
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

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.7792 mL 13.8962 mL 27.7924 mL 69.4811 mL
5 mM 0.5558 mL 2.7792 mL 5.5585 mL 13.8962 mL
10 mM 0.2779 mL 1.3896 mL 2.7792 mL 6.9481 mL
15 mM 0.1853 mL 0.9264 mL 1.8528 mL 4.6321 mL
20 mM 0.1390 mL 0.6948 mL 1.3896 mL 3.4741 mL
25 mM 0.1112 mL 0.5558 mL 1.1117 mL 2.7792 mL
30 mM 0.0926 mL 0.4632 mL 0.9264 mL 2.3160 mL
40 mM 0.0695 mL 0.3474 mL 0.6948 mL 1.7370 mL
50 mM 0.0556 mL 0.2779 mL 0.5558 mL 1.3896 mL
60 mM 0.0463 mL 0.2316 mL 0.4632 mL 1.1580 mL
80 mM 0.0347 mL 0.1737 mL 0.3474 mL 0.8685 mL
100 mM 0.0278 mL 0.1390 mL 0.2779 mL 0.6948 mL
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PF-4800567 Related Classifications

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-48005671188296-52-7PF4800567PF 4800567Casein KinaseInhibitorinhibitorinhibit

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