2. PI3K/Akt/mTOR Stem Cell/Wnt
  3. GSK-3
  4. 1-Azakenpaullone

1-Azakenpaullone  (Synonyms: 1-Akp)

Cat. No.: HY-59090 Purity: 99.61%
COA Handling Instructions

Molarity Calculator

1-Azakenpaullone (1-Akp) is a highly selective and ATP-competitive inhibitor of glycogen synthase kinase-3 β (GSK-3β), with an IC50 value of 18 nM.

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

1-Azakenpaullone Chemical Structure

1-Azakenpaullone Chemical Structure

CAS No. : 676596-65-9

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 239 In-stock
Solution
10 mM * 1 mL in DMSO USD 239 In-stock
Solid
2 mg USD 132 In-stock
5 mg USD 200 In-stock
10 mg USD 320 In-stock
25 mg USD 590 In-stock
50 mg USD 850 In-stock
100 mg USD 1200 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 3 publication(s) in Google Scholar

1-Azakenpaullone Related Antibodies

Top Publications Citing Use of Products

View All GSK-3 Isoform Specific Products:

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GSK-3 GSK-3α GSK-3β

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

1-Azakenpaullone (1-Akp) is a highly selective and ATP-competitive inhibitor of glycogen synthase kinase-3 β (GSK-3β), with an IC50 value of 18 nM[1].

IC50 & Target[1]

GSK-3β

18 nM (IC50)

CDK1/cyclin B

2 μM (IC50)

CDK5/p25

4.2 μM (IC50)

In Vitro

1-Azakenpaullone (2.5 μM, 48 h) stimulates proliferation in irradiated zebrafish lateral line neuromasts[2].
1-Azakenpaullone (3 μM, 48 h) induces the osteoblastic differentiation and mineralization of human human mesenchymal stem cells (MSCs), by activating Wnt signaling[3].
1-Azakenpaullone (30 μM, 24 h) reduces S6K1 phosphorylation in HCC1806 cells[5].

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

1-Azakenpaullone Related Antibodies

Real Time qPCR[3]

Cell Line: human MSCs
Concentration: 3 µM
Incubation Time: 48 h
Result: Increased gene expression of osteoblast-specific marker genes (ALP, OC, ON, COL1A1, and OPN).
In Vivo

1-Azakenpaullone (10 or 100 pmol, i.c.v.) reverses Ketamine (20 mg/kg, i.p.)-induced locomotor hyperactivity and behavioral aberrations in Male NMRI mice[4].

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

328.16

Formula

C15H10BrN3O
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C(NC1=CC=CN=C12)CC3=C2NC4=C3C=C(Br)C=C4
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 1 year
-20°C 6 months
Solvent & Solubility
In Vitro: 

DMSO : 200 mg/mL (609.46 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 3.0473 mL 15.2365 mL 30.4729 mL
5 mM 0.6095 mL 3.0473 mL 6.0946 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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

  • 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: 1.67 mg/mL (5.09 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 1.67 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (16.7 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.
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: 99.61%

COA (257 KB) HNMR (471 KB) LCMS (93 KB)

Handling Instructions (2659 KB)
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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.0473 mL 15.2365 mL 30.4729 mL 76.1823 mL
5 mM 0.6095 mL 3.0473 mL 6.0946 mL 15.2365 mL
10 mM 0.3047 mL 1.5236 mL 3.0473 mL 7.6182 mL
15 mM 0.2032 mL 1.0158 mL 2.0315 mL 5.0788 mL
20 mM 0.1524 mL 0.7618 mL 1.5236 mL 3.8091 mL
25 mM 0.1219 mL 0.6095 mL 1.2189 mL 3.0473 mL
30 mM 0.1016 mL 0.5079 mL 1.0158 mL 2.5394 mL
40 mM 0.0762 mL 0.3809 mL 0.7618 mL 1.9046 mL
50 mM 0.0609 mL 0.3047 mL 0.6095 mL 1.5236 mL
60 mM 0.0508 mL 0.2539 mL 0.5079 mL 1.2697 mL
80 mM 0.0381 mL 0.1905 mL 0.3809 mL 0.9523 mL
100 mM 0.0305 mL 0.1524 mL 0.3047 mL 0.7618 mL
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1-Azakenpaullone 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:

1-Azakenpaullone676596-65-91-AkpGSK-3Glycogen synthase kinase-3Glycogen synthase kinase 3Inhibitorinhibitorinhibit

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