2. PI3K/Akt/mTOR Stem Cell/Wnt
  3. GSK-3
  4. PF-04802367

PF-04802367  (Synonyms: PF-367)

Cat. No.: HY-122026 Purity: 98.84%
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PF-04802367 (PF-367) is a highly selective GSK-3 inhibitor with an IC50 of 2.1 nM based on a recombinant human GSK-3β enzyme assay and 1.1 nM based on ADP-Glo assay. PF-04802367 shows desirable central nervous system (CNS) properties and potency. PF-04802367 is equally effective at inhibition of the two known GSK-3 isoforms (GSK-3α and GSK-3β) with IC50 values of 10.0 and 9.0 nM in mobility shift assays, respectively.

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

PF-04802367 Chemical Structure

PF-04802367 Chemical Structure

CAS No. : 1962178-27-3

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 286 In-stock
Solution
10 mM * 1 mL in DMSO USD 286 In-stock
Solid
5 mg USD 260 In-stock
10 mg USD 420 In-stock
25 mg USD 840 In-stock
50 mg USD 1340 In-stock
100 mg USD 2100 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Based on 1 publication(s) in Google Scholar

PF-04802367 Related Antibodies

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GSK-3 GSK-3α GSK-3β

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Description

PF-04802367 (PF-367) is a highly selective GSK-3 inhibitor with an IC50 of 2.1 nM based on a recombinant human GSK-3β enzyme assay and 1.1 nM based on ADP-Glo assay. PF-04802367 shows desirable central nervous system (CNS) properties and potency. PF-04802367 is equally effective at inhibition of the two known GSK-3 isoforms (GSK-3α and GSK-3β) with IC50 values of 10.0 and 9.0 nM in mobility shift assays, respectively[1].

IC50 & Target[1]

GSK-3α

10 nM (IC50)

GSK-3β

9 nM (IC50)

In Vitro

PF-04802367 (PF-367) is efficient at inhibiting GSK-3β enzymatic activity in vitro with ligand and lipophilic efficiency scores of 0.46 and 7.0, respectively[1].
PF-367 has reasonable in vitro stability in human hepatic microsomes (t1/2=78.7 min), has excellent passive permeability[1].
In a stable inducible CHO cell line over-expressing GSK-3β and its substrate tau, PF-367 inhibited phosphorylation of tau with an IC50 of 466 nM[1].
PF-367 has good cell viability (IC50 of 117 μM in THLE cytotoxicity assays) and an IC50 >100 μM in a hERG screening assay[1].
PF-367 shows significant right shifts against β-catenin translocation in HeLa cells with EC50 of 6.2 μM, gene transcription in U20S cells with EC50 of 20.6 μM, and cell proliferation in HeLa cells as evaluated by Ki-67 incorporation with EC50 of 9.0 μM[1].

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

PF-04802367 Related Antibodies
In Vivo

PF-04802367 (PF-367) a potent GSK-3 inhibitor with exceptional kinome selectivity that modulates phosphorylated tau levels in vivo. Inhibition of phosphorylation of tau in brain by PF-367 (A single subcutaneous of 1, 3.2, 10, 32 or 50 mg/kg) is dose-dependent[1].
PF-04802367 (PF-367), a potent type-I dual GSK-3α/β inhibitor, showing promising absorption; distribution, metabolism and elimination (ADME) properties combined with robust CNS/peripheral p-Tau and muscle phosphorylated glycogen synthase (pGS) inhibition in vivo[2].

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

Animal Model: Sprague-Dawley rats[1]
Dosage: 1, 3.2, 10, 32 or 50 mg/kg
Administration: A single subcutaneous
Result: Inhibition of phosphorylation of tau in brain is dose-dependent.
Molecular Weight

361.78

Formula

C16H16ClN5O3
CAS No.
Appearance

Solid

Color

White to light yellow

SMILES

O=C(C1=C(C2=CC=C(OC)C(Cl)=C2)OC=N1)NCCCN3N=CN=C3
Shipping

Room temperature in continental US; may vary elsewhere.
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 : 100 mg/mL (276.41 mM; Need ultrasonic; 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 2.7641 mL 13.8206 mL 27.6411 mL
5 mM 0.5528 mL 2.7641 mL 5.5282 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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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 (6.91 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 (6.91 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
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.7641 mL 13.8206 mL 27.6411 mL 69.1028 mL
5 mM 0.5528 mL 2.7641 mL 5.5282 mL 13.8206 mL
10 mM 0.2764 mL 1.3821 mL 2.7641 mL 6.9103 mL
15 mM 0.1843 mL 0.9214 mL 1.8427 mL 4.6069 mL
20 mM 0.1382 mL 0.6910 mL 1.3821 mL 3.4551 mL
25 mM 0.1106 mL 0.5528 mL 1.1056 mL 2.7641 mL
30 mM 0.0921 mL 0.4607 mL 0.9214 mL 2.3034 mL
40 mM 0.0691 mL 0.3455 mL 0.6910 mL 1.7276 mL
50 mM 0.0553 mL 0.2764 mL 0.5528 mL 1.3821 mL
60 mM 0.0461 mL 0.2303 mL 0.4607 mL 1.1517 mL
80 mM 0.0346 mL 0.1728 mL 0.3455 mL 0.8638 mL
100 mM 0.0276 mL 0.1382 mL 0.2764 mL 0.6910 mL
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PF-04802367 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-048023671962178-27-3PF-367PF04802367PF 04802367PF367PF 367GSK-3Glycogen synthase kinase-3Glycogen synthase kinase 3Glycogensynthasekinase-3phosphorylationtauproteinAlzheimerdiseaseneurologyneurodegenerativeInhibitorinhibitorinhibit

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