GSK-3 inhibitor 1CAS# 603272-51-1 |
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Quality Control & MSDS
3D structure
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| Cas No. | 603272-51-1 | SDF | Download SDF |
| PubChem ID | 78357782 | Appearance | Powder |
| Formula | C22H17ClFN5O2 | M.Wt | 437.85 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Solubility | Soluble in DMSO | ||
| SMILES | C1CN2C=C(C3=CC(=CC(=C32)CN1)F)C4=C(C(=O)NC4=O)C5=CN=C6N5C=CC=C6.Cl | ||
| Standard InChIKey | CXXAOCQHGIGIBJ-UHFFFAOYSA-N | ||
| Standard InChI | InChI=1S/C22H16FN5O2.ClH/c23-13-7-12-9-24-4-6-27-11-15(14(8-13)20(12)27)18-19(22(30)26-21(18)29)16-10-25-17-3-1-2-5-28(16)17;/h1-3,5,7-8,10-11,24H,4,6,9H2,(H,26,29,30);1H | ||
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
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| About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
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| Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. | ||
| Description | GSK-3 inhibitor 1 is an inhibitor of GSK-3. References: | |||||
GSK-3 inhibitor 1 Dilution Calculator
GSK-3 inhibitor 1 Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 2.2839 mL | 11.4194 mL | 22.8389 mL | 45.6777 mL | 57.0972 mL |
| 5 mM | 0.4568 mL | 2.2839 mL | 4.5678 mL | 9.1355 mL | 11.4194 mL |
| 10 mM | 0.2284 mL | 1.1419 mL | 2.2839 mL | 4.5678 mL | 5.7097 mL |
| 50 mM | 0.0457 mL | 0.2284 mL | 0.4568 mL | 0.9136 mL | 1.1419 mL |
| 100 mM | 0.0228 mL | 0.1142 mL | 0.2284 mL | 0.4568 mL | 0.571 mL |
| * Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations. | |||||
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GSK-3 inhibitor 1 is a potent GSK-3 inhibitor.
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Efficacy of a novel, orally active GSK-3 inhibitor 6-Methyl-N-[3-[[3-(1-methylethoxy)propyl]carbamoyl]-1H-pyrazol-4-yl]pyridine-3-ca rboxamide in tau transgenic mice.[Pubmed:19698704]
Brain Res. 2009 Nov 3;1296:148-63.
Neurofibrillary tangles (NFTs) composed of hyperphosphorylated and aggregated tau are common pathological characteristics in Alzheimer's disease (AD) and other tauopathies. Aberrant tau phosphorylation is an early and pivotal event in the pathogenesis of tauopathies, and since GSK-3 is a key factor implicated in aberrant tau phosphorylation, GSK-3 inhibition is expected to suppress tauopathy disease progression. In the present study, we report the efficacy of a newly discovered small molecule GSK-3 inhibitor, 6-methyl-N-[3-[[3-(1-methylethoxy)propyl]carbamoyl]-1H-pyrazol-4-yl]pyridine-3-ca rboxamide (compound A), to inhibit tau phosphorylation and to reduce the amount of pathological aggregated tau in JNPL3 mice that overexpress a mutant form of human tau. Compound A is a highly potent and selective inhibitor of GSK-3 with an IC(50) of 2 nM, with at least 230-fold lower potency against 27 other kinases. Oral administration of compound A resulted in a significant reduction of tau phosphorylation at several GSK-3 directed sites. Furthermore, chronic oral administration of compound A markedly reduced aggregated tau in old JNPL3 mice. These results suggest that a novel, orally active GSK-3 inhibitor, compound A, has potency in the prevention of tau pathology.
9-cyano-1-azapaullone (cazpaullone), a glycogen synthase kinase-3 (GSK-3) inhibitor activating pancreatic beta cell protection and replication.[Pubmed:18345612]
J Med Chem. 2008 Apr 10;51(7):2196-207.
Recently, the serine/threonine kinase glycogen synthase kinase-3 (GSK-3) emerged as a regulator of pancreatic beta cell growth and survival. On the basis of the previous observation that GSK-3 inhibitors like 1-azakenpaullone promote beta cell protection and replication, paullone derivatives were synthesized including 1-aza-, 2-aza-, and 12-oxapaullone scaffolds. In enzymatic assays distinct 1-azapaullones were found to exhibit selective GSK-3 inhibitory activity. Within the series of 1-azapaullones, three derivatives stimulated INS-1E beta cell replication and protected INS-1E cells against glucolipotoxicity induced cell death. Cazpaullone (9-cyano-1-azapaullone), the most active compound in the protection assays, also stimulated the replication of primary beta cells in isolated rat islets. Furthermore, cazpaullone showed a pronounced transient stimulation of the mRNA expression of the beta cell transcription factor Pax4, an important regulator of beta cell development and growth. These features distinguish cazpaullone as a unique starting point for the development of beta cell regenerative agents which might be useful in the treatment of diabetes.
