Name: 1-Azakenpaullone
Brand: Selleck Chemicals
SKU: S7193
Availability: InStock
Rating: 5 (18 reviews)

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Batch: S719301 DMSO]66 mg/mL]false]Water]Insoluble]false]Ethanol]Insoluble]false Purity: 99.66%

Cited in Nature Medicine for its top-tier quality
COA
NMR
SDS
Datasheet

99.66

Related Targets	PI3K Akt mTOR ATM/ATR DNA-PK AMPK PDPK1 PTEN PP2A PDK
Other GSK-3 Inhibitors	CHIR-99021 (Laduviglusib) Laduviglusib (CHIR-99021) Hydrochloride SB216763 TWS119 CHIR-98014 BIO LY2090314 Tideglusib SB415286 AR-A014418

Solubility

In vitro
Batch:

DMSO : 66 mg/mL (201.12 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	3.300mg/ml (10.06mM)	Taking the 1 mL working solution as an example, add 50 μL 66 mg/ml clarified DMSO stock solution to 400 μL PEG300, mix evenly to clarify it; add 50 μL Tween80 to the above system, mix evenly to clarify it; then continue to add 500 μL ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

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Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

%

% Tween 80

% ddH₂O

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Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight	328.16	Formula	C₁₅ H₁₀ Br N₃ O	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	676596-65-9	--		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	1-Akp			Smiles	C1C2=C(C3=C(C=CC=N3)NC1=O)NC4=C2C=C(C=C4)Br

Mechanism of Action

Targets/IC₅₀/Ki	GSK-3α GSK-3β (Cell-free assay) 18 nM
In vitro	1-Azakenpaullone inhibits the CDK1/cyclin B, CDK5/p25, and GSK-3β effectively, with IC50 of 0.018 μM, 4.2 μM, and 2.0 μM, respectively. In human islets, this compound (5 mM) in combination with glucose (8 mM) stimulates the β-cell proliferation. It effectively stimulates INS-1E cells replication and protects INS-1E cells against glucolipotoxicity-induced cell death.
Kinase Assay	Kinase preparations and assays
Kinase Assay	GSK-3β is assayed, following a 1/100 dilution in 1 mg BSA per mL 10 mM dithiothreitol, with 5 μL 40 μM GS-1 peptide as a substrate, in buffer A, in the presence of 15 μM [γ-³²P]ATP (3000 Ci·mmol^-1; 1 mCi·mL^-1 ) in a final volume of 30 μL. After 30 min incubation at 30℃, 25 μL aliquots of supernatant are spotted onto 2.5×3 cm pieces of Whatman P81 phosphocellulose paper, and 20 s later, the filters are washed five times in a solution of 10 mL phosphoric acid per L of water. The wet filters are counted in the presence of 1 mL ACS scintillation fluid. The kinase activity of CDK1/cyclin B is assayed in buffer C, with 1 mg/mL histone H1, in the presence of 15 μM [γ-32P]ATP (3000 Ci·mmol^-1; 1 mCi·mL^-1 ) in a final volume of 30 μL. After 10 min incubation at 30℃, 25 μL aliquots of supernatant are spotted onto P81 phosphocellulose papers and treated as described above. The activity of CDK5/p25 is assayed in buffer C as described for CDK1/cyclin B. (Buffer A: 10 mM MgCl2 , 1 mM EGTA, 1 mM dithiothreitol, 25 mM Tris/HCl pH 7.5. Buffer C: homogenization buffer but 5 mM EGTA, no NaF and no protease inhibitors.)
In vivo	Pretreatment with 1-Azakenpaullone (10 or 100 pmol, i.c.v.) attenuates the induced locomotor hyperactivity, disruption of PPI and cognitive deﬁcits, and improves the induced motor incoordination in rotarod test.
References	[1] https://pubmed.ncbi.nlm.nih.gov/14698171/ [2] https://pubmed.ncbi.nlm.nih.gov/19073772/ [3] https://pubmed.ncbi.nlm.nih.gov/18345612/ [4] https://pubmed.ncbi.nlm.nih.gov/17242403/ [5] https://pubmed.ncbi.nlm.nih.gov/22325078/ [6] https://pubmed.ncbi.nlm.nih.gov/10998059/

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1-Azakenpaullone GSK-3 inhibitor

Chemical Structure

Molecular Weight: 328.16