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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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Purity: ≥98%
GSK-3 inhibitor 1 is a novel and potent GSK-3 (Glycogen synthase kinase-3) inhibitor. The serine/threonine protein kinase known as glycogen synthase kinase 3 mediates the addition of phosphate molecules to serine and threonine amino acid residues. GSK-3 was first discovered in 1980 as a Glycogen synthase regulatory kinase, but it has since been found to kine over forty different proteins in a variety of different pathways. In mammals, GSK-3 is encoded by two known genes, GSK-3 alpha (GSK3A) and GSK-3 beta (GSK3B). Numerous studies have recently concentrated on GSK-3, which has been linked to bipolar disorder, Type II diabetes, cancer, inflammation, and Type II diabetes (Diabetes mellitus type 2).
| Targets |
GSK-3
|
|---|---|
| ln Vitro |
GSK-3 inhibitor 1 can be used to induce, promote, or enhance the growth, proliferation, or regeneration of inner ear tissues like inner ear supporting cells or inner ear hair cells[2].
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| References |
| Molecular Formula |
C22H17CLFN5O2
|
|---|---|
| Molecular Weight |
437.8541
|
| Exact Mass |
337.10223
|
| CAS # |
603272-51-1
|
| Related CAS # |
603272-51-1
|
| PubChem CID |
78357782
|
| Appearance |
Yellow to orange solid
|
| LogP |
8.592
|
| Hydrogen Bond Donor Count |
3
|
| Hydrogen Bond Acceptor Count |
5
|
| Rotatable Bond Count |
2
|
| Heavy Atom Count |
31
|
| Complexity |
788
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
Cl[H].FC1=C([H])C2C([H])([H])N([H])C([H])([H])C([H])([H])N3C([H])=C(C4C(N([H])C(C=4C4=C([H])N=C5C([H])=C([H])C([H])=C([H])N45)=O)=O)C(=C1[H])C3=2
|
| InChi Key |
CXXAOCQHGIGIBJ-UHFFFAOYSA-N
|
| InChi Code |
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
|
| Chemical Name |
3-(6-fluoro-1,10-diazatricyclo[6.4.1.04,13]trideca-2,4,6,8(13)-tetraen-3-yl)-4-imidazo[1,2-a]pyridin-3-ylpyrrole-2,5-dione;hydrochloride
|
| Synonyms |
GSK-3 inhibitor 1
|
| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
DMSO: ~12.5 mg/mL (~28.55 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1.25 mg/mL (2.85 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 12.5 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. Solubility in Formulation 2: ≥ 1.25 mg/mL (2.85 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 12.5 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline 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 | 2.2839 mL | 11.4194 mL | 22.8389 mL | |
| 5 mM | 0.4568 mL | 2.2839 mL | 4.5678 mL | |
| 10 mM | 0.2284 mL | 1.1419 mL | 2.2839 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.
| NCT Number | Status | Interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT04239092 | Active Recruiting |
Drug: 9-ING-41 Drug: Irinotecan |
Refractory Cancer Cancer Pediatric |
Actuate Therapeutics Inc. | June 5, 2020 | Phase 1 |
| NCT05239182 | Active Recruiting |
Drug: 9-ING-41 Drug: Retifanlimab |
Pancreatic Adenocarcinoma | Anwaar Saeed | January 26, 2022 | Phase 2 |
| NCT03678883 | Recruiting | Drug: 9-ING-41 Drug: Doxorubicin |
Cancer Sarcoma |
Actuate Therapeutics Inc. | January 4, 2019 | Phase 2 |
| NCT05010629 | Recruiting | Drug: 9-ING-41 Drug: Carboplatin |
Metastatic Cancer Salivary Gland Cancer |
Glenn J. Hanna | September 14, 2021 | Phase 2 |
| NCT05077800 | Recruiting | Drug: 9-ING-41 Drug: Losartan |
Pancreatic Adenocarcinoma Pancreatic Adenocarcinoma Metastatic |
Colin D. Weekes, M.D. | March 21, 2022 | Phase 2 |
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