GSK-3α/β-IN-1
GSK-3α/β-IN-1 is GSK-3α/β inhibitor with IC50 s of 0.265 μM and 0.255 μM for GSK-3α and GSK-3β, respectively. GSK-3α/β-IN-1 also inhibits PKA with an IC50 of 0.188 μM. GSK-3α/β-IN-1 potently inhibits cell viability of three Glioblastoma (GBM) cell lines (IC50 : 3-6 μM, 72 h) with no toxicity to human astrocytes and good metabolic stability. GSK-3α/β-IN-1 has potential CNS activity in all-human blood-brain barrier (BBB) model of GBM.
For research use only. We do not sell to patients.
- CAS No.: 1574354-24-7
- Formula: C21H17N3O2
- Molecular Weight:343.38
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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GSK-3α 0.265 μM (IC50) |
GSK-3β 0.255 μM (IC50) |
PKA 0.188 μM (IC50) |
GSK-3α/β-IN-1 (Compound 1) shows kinase selectivity for GSK-3α/β and PKA over other homologous kinases (CDK2, CDK5, CDK9, ERK1, ERK2, PKBα, PKBβ, PKCα, and PKCγ)[1].
GSK-3α/β-IN-1 shows (0.3-300 μM, 24-72 h) potent cytotoxicity against the three GBM cell lines (U87-MG, T98G, and U251-MG) with a dose- and time-dependent effects[1].
GSK-3α/β-IN-1 (3.3-6.2 μM, 72 h) shows a significant decrease in the cell distribution in G1 phase and a increase in the S phase for all three cell lines (U87-MG, U251-MG and T98G)[1].
GSK-3α/β-IN-1 (6.2 μM, 72 h) is nontoxic to the BBB cells and the BBB remains intact in a BBB model of GBM[1].
GSK-3α/β-IN-1 has a >4-fold higher half-life (t1/2 is 101 min) and lower intrinsic clearance profile (CLint is 5.6 mL/min/mg protein) than Verapamil (HY-14275)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:GBM cells (U87-MG, U251-MG, and T98G)
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Concentration:0.3, 1, 3, 10, 30, 100, and 300 μM
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Incubation Time:24, 48, and 72 h
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Result:Significantly reduced the cell viability of U87-MG with IC50 15 μM (24h), 4.7 μM (48h) and 3.3 μM (48h).
Significantly reduced the cell viability of U251-MG with IC50 15.1 μM (24h), 8.3 μM (48h) and 6.1 μM (48h).
Significantly reduced the cell viability of T98G with IC50 12 μM (24h), 8.1 μM (48h) and 6.2 μM (48h).
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Cell Line:GBM cells
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Concentration:U87-MG : 3.3μM, U251-MG : 6.1 μM, T98G : 6.2 μM
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Incubation Time:72 h
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Result:Significantly decreased in the cell distribution in G1 phase for all three cell lines at 45.5% (U87-MG), 61.6% (U251-MG), and 65.8% (T98G) and increased in the S phase at 27.8%, 15.9%, and 22.3% respectively.
Chemical Information
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CAS No. 1574354-24-7
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Molecular Weight 343.38
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Formula C21H17N3O2
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SMILES
OC1=CC=C(C2=NC(NN=C3)=C3C(C4=CC=C(C(C)C)C=C4)=C2O5)C5=C1
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
GSK-3α/β-IN-1 Related Classifications
HY-172586 Related Classifications
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