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^[1].

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 (t_1/2 is 101 min) and lower intrinsic clearance profile (CL_int 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.

343.38

C₂₁H₁₇N₃O₂

1574354-24-7

OC1=CC=C(C2=NC(NN=C3)=C3C(C4=CC=C(C(C)C)C=C4)=C2O5)C5=C1

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Emmerich TD, et al. Structure-Based Discovery Targeting GSK-3α Reveals Potent Nanomolar Selective 4-Phenyl-1H-benzofuro[3,2-b]pyrazolo[4,3-e]pyridine Inhibitor with Promising Glioblastoma and CNS-Active Potential in Cellular Models. J Med Chem. 2025 Apr 24;68(8):8679-8693.  [Content Brief]