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Purity: ≥98%
1-Azakenpaullone (1-Akp), an analog of kenpaullone, is a novel, ATP-competitive and selective inhibitor of GSK-3β (glycogen synthase kinase 3β) with potential antidiabetic and neuroprotective activities. It exhibits >100-fold selectivity for GSK-3β over CDK1/cyclin B and CDK5/p25 and inhibits GSK-3β with an IC50 of 18 nM.
| Targets |
GSK-3β (IC50 = 18 nM); CDK1/cyclin B (IC50 = 2 μM); CDK5/p25 (IC50 = 4.2 μM)
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|---|---|
| ln Vitro |
1-Azakenpaullone has an effective IC50 of 0.018 μM, 4.2 μM, and 2.0 μM for inhibiting CDK1/cyclin B, CDK5/p25, and GSK-3β, respectively. [1] When combined with glucose (8 mM), 1-Azakenpaullone (5 mM) stimulates the proliferation of β-cell in human islets. [2] 1-Azakenpaullone efficiently promotes INS-1E cell replication and guards against glucolipotoxicity-induced cell death in INS-1E cells. [3] [4]
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| ln Vivo |
Pretreatment with 1-Azakenpaullone (10 or 100 pmol, i.c.v.) reduces the rotarod test-induced ketamine-induced motor incoordination and reduces the ketamine-induced disruption of PPI and cognitive deficits.[5]
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| Enzyme 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.
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| Cell Assay |
Cell replication is determined by BrdUrd incorporation after treatment with 1-Azakenpaullone for 24 h. After receiving 1-azakenpaullone treatment for 4 days, the relative cell number is calculated using the CyQuant cell proliferation assay. Results are displayed as fold changes in comparison to the control.
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| Animal Protocol |
Male NMRI mice
~500 pmol i.c.v. |
| References |
| Molecular Formula |
C15H10N3OBR
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|---|---|
| Molecular Weight |
328.1634
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| Exact Mass |
327.0007
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| Elemental Analysis |
C, 54.90; H, 3.07; Br, 24.35; N, 12.80; O, 4.88
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| CAS # |
676596-65-9
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| Related CAS # |
676596-65-9
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| Appearance |
Solid powder
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| SMILES |
C1C2=C(C3=C(C=CC=N3)NC1=O)NC4=C2C=C(C=C4)Br
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| InChi Key |
NTSBZVCEIVPKBJ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C15H10BrN3O/c16-8-3-4-11-9(6-8)10-7-13(20)18-12-2-1-5-17-15(12)14(10)19-11/h1-6,19H,7H2,(H,18,20)
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| Chemical Name |
14-bromo-3,8,18-triazatetracyclo[9.7.0.02,7.012,17]octadeca-1(11),2(7),3,5,12(17),13,15-heptaen-9-one
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| Synonyms |
1-Azakenpaullone
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| HS Tariff Code |
2934.99.03.00
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: 66~125 mM(201.1~380.9 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: 1.67 mg/mL (5.09 mM) in 10% DMSO + 40% PEG300 +5% Tween-80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 16.7 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 + to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 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 | |
| 10 mM | 0.3047 mL | 1.5236 mL | 3.0473 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
Optimization of isoquinolinone PI3K inhibitors led to the discovery of a potent inhibitor of PI3K-γ (26or IPI-549) with >100-fold selectivity over other lipid and protein kinases.ACS Med Chem Lett.2016 Jul 22;7(9):862-7. |
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Effect of compound26on migration of bone marrow derived macrophages (BMDM) in vitro.ACS Med Chem Lett.2016 Jul 22;7(9):862-7. |
(a) Effect of compound26on neutrophil migration in the mouse air pouch model.ACS Med Chem Lett.2016 Jul 22;7(9):862-7. |
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