| ln Vitro |
GSK-3α/β-IN-1 (compound 1) exhibits kinase selectivity for GSK-3α/β and PKA, but poor selectivity for other homologous kinases (CDK2, CDK5, CDK9, ERK1, ERK2, PKBα, PKBβ, PKCα, and PKCγ) [1]. GSK-3α/β-IN-1 (0.3-300 μM, 24-72 h) showed potent cytotoxicity against three glioblastoma (GBM) cell lines (U87-MG, T98G, and U251-MG) in a dose- and time-dependent manner [1]. GSK-3α/β-IN-1 (3.3-6.2 μM, 72 h) significantly reduced the proportion of G1 phase cells and increased the proportion of S phase cells in the three cell lines (U87-MG, U251-MG, and T98G) [1]. GSK-3α/β-IN-1 (6.2 μM, 72 hours) was non-toxic to blood-brain barrier cells and the blood-brain barrier remained intact in the GBM blood-brain barrier model [1]. The half-life of GSK-3α/β-IN-1 (t1/2 of 101 min) was more than 4 times that of verapamil, and its intrinsic clearance (CLint of 5.6 mL/min/mg protein) was lower than that of verapamil [1].
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| Cell Assay |
Cell viability assay [1]
Cell Types: GBM cells (U87-MG, U251-MG and T98G) Tested Concentrations: 0.3, 1, 3, 10, 30, 100 and 300 μM Incubation Duration: 24, 48 and 72 hours Experimental Results: Significantly reduced the viability of U87-MG cells, with IC50 values of 15 μM (24 hours), 4.7 μM (48 hours) and 3.3 μM (48 hours), respectively. Significantly reduced the viability of U251-MG cells, with IC50 values of 15.1 μM (24 hours), 8.3 μM (48 hours) and 6.1 μM (48 hours), respectively. It significantly reduced the viability of T98G cells, with IC50 values of 12 μM (24 h), 8.1 μM (48 h), and 6.2 μM (48 h), respectively. Cell cycle analysis [1] Cell Types: GBM cells Tested Concentrations: U87-MG: 3.3 μM, U251-MG: 6.1 μM, T98G: 6.2 μM Incubation Duration: 72 hours Experimental Results: The proportion of G1 phase cells in all three cell lines was significantly reduced, at 45.5% (U87-MG), 61.6% (U251-MG) and 65.8% (T98G), respectively, while the proportion of S phase cells increased to 27.8%, 15.9% and 22.3%, respectively. |
| References |
| CAS # |
1574354-24-7
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| Appearance |
Typically exists as solids at room temperature
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| 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 |
| 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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
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.
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