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

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.

연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.

1-Azakenpaullone

1-Azakenpaullone 화학구조

CAS No. : 676596-65-9

사이즈 가격 재고 수량
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
해외재고보유
Solution
10 mM * 1 mL in DMSO 해외재고보유
Solid
2 mg 해외재고보유
5 mg 해외재고보유
10 mg 해외재고보유
25 mg 해외재고보유
50 mg 해외재고보유
100 mg 해외재고보유
200 mg   견적 받기  
500 mg   견적 받기  

* 장바구니에 담기 전 물품의 수량을 선택해 주십시오.

This product is a controlled substance and not for sale in your territory.

고객리뷰

Based on 3 publication(s) in Google Scholar

Top Publications Citing Use of Products

View All GSK-3 Isoform Specific Products:

  • Biological Activity

  • 순도&문서

  • References

  • 고객리뷰

제품 설명

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.

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.

분자량

328.16

화학식

C15H10BrN3O

CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

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

선적

Room temperature in continental US; may vary elsewhere.

보관
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 1 year
-20°C 6 months
용액&용해도
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.

  • 몰농도 계산기

  • 농도 희석 계산기

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.
순도&문서

Purity: 99.61%

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
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.
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.

최근 본 상품:

온라인 문의

Your information is safe with us. * Required Fields.

상품명

 

Requested Quantity *

고객명 *

 

호칭

메일주소 *

 

전화번호 *

Department

 

회사명 *

City

Country or Region *

     

비고

대량구매 문의

Inquiry Information

상품명:
1-Azakenpaullone
Cat. No.:
HY-59090
수량:
MCE Japan Authorized Agent: