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].

Product Specifications

CAS Number

[1574354-24-7]

UNSPSC

12352005

Target

GSK-3; PKA

Related Pathways

PI3K/Akt/mTOR; Stem Cell/Wnt; TGF-beta/Smad

Applications

Cancer-Kinase/protease

Field of Research

Cancer; Neurological Disease

Smiles

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

Molecular Formula

C21H17N3O2

Molecular Weight

343.38

References & Citations

[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.