BI-5521
BI-5521 is an orally active GSK-3 inhibitor with an IC50 of 1.1 nM against GSK-3β. BI-5521 targets the two GSK-3 isoforms with similar potency and exhibits potent inhibitory activity against DYRK1A. By modulating GSK-3 activity, BI-5521 inhibits tumor proliferation and cancer cell growth, exerts cytotoxic effects, and reduces cancer cell viability. It shows consistent chemosensitivity across all subtypes of rhabdomyosarcoma, produces synergistic growth inhibitory effects when combined with SOS1 inhibitors, reduces oral glucose levels, regulates the myofibroblast differentiation pathway, decreases the nuclear localization of YAP/SMAD2/3, and lowers the positive rate of α-SMA in fibroblasts without affecting the apoptosis of CD4+ T cells. BI-5521 can be used in the research of non-small cell lung cancer, pleomorphic rhabdomyosarcoma, type 2 diabetes, pancreatic ductal adenocarcinoma, Alzheimer's disease, bipolar disorder, and metabolic dysfunction-associated steatotic liver disease.
For research use only. We do not sell to patients.
The BI-5521 was designed by Boehringer Ingelheim and could be obtained free of charge through the Boehringer Ingelheim open innovation portal opnMe.com, associated with its negative control.
- CAS No.: 864686-48-6
- Formula: C24H25N3O4
- Molecular Weight:419.47
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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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-3β 1.1 nM (IC50) |
hGSK-3α |
DYRK1A |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| NSCLC | IC50 |
0.8 μM
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Cytotoxicity against human BH1406 non-small cell lung cancer cells assessed as reduction in cell viability incubated for 4 days by modified MTT assay.
Cytotoxicity against human BH1406 non-small cell lung cancer cells assessed as reduction in cell viability incubated for 4 days by modified MTT assay.
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39670010 |
BI-5521 (0.0782-10 µM; 4 days) significantly inhibits the growth of 2D-cultured BH1406 NSCLC cells with an IC50 of 0.8 µM as a single agent, and exhibits synergistic growth inhibition when combined with BAY-293 (HY-114398)[1].
BI-5521 (4 days) potently inhibits the viability of BH1522, RD, and TE671 rhabdomyosarcoma cell lines with comparable IC50 values, demonstrating high chemosensitivity in all tested lines[2].
BI-5521 potently inhibits GSK-3β with an IC50 of 1.1 nM, targets both GSK-3 isoforms with similar potency, shows potent inhibition of DYRK1A, and maintains 100-1000-fold selectivity against all other tested kinases and non-kinase targets[3].
BI-5521 reveals the role of GSK-3 in activation pathways for myofibroblastic differentiation proteins in a PDAC 3D tumor microenvironment model[3].
BI-5521 has good permeability with a moderate efflux ratio in Caco2 cells and low clearance in rat hepatocytes[3].
BI-5521 (100 nM; Day 4 to day 8 of 3D culture) reduces nuclear localization of both YAP and SMAD2/3 in fibroblasts within heterotypic 3D PDAC tissues composed of Capan-2 cells and NHDFs, which correlates with diminished myofibroblastic differentiation marked by α-SMA expression[5].
BI-5521 (50 nM; 2 h pre-incubation, 48 h co-treatment with Oleic acid (HY-N1446)) significantly suppresses steatosis in insulin-resistant, dedifferentiated human HepG2 hepatoma cells treated with oleic acid[4].
BI-5521 (8 h) does not modulate cleaved caspase3-positive cell percentages in ex vivo cultured control or Creld1-deficient CD4+ T cells[6].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:2D-cultured BH1406 non-small cell lung cancer (NSCLC) cells
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Concentration:0.0782-10 µM
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Incubation Time:4 days
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Result:Inhibited BH1406 cell viability with an IC50 of 0.8 µM as a single agent.
Exhibited synergistic effects with BAY-293, resulting in a combined IC50 of 0.31 µM across concentrations from 0.0782 to 10 µM.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 864686-48-6
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Molecular Weight 419.47
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Formula C24H25N3O4
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SMILES
O=C(/C1=C(NC2CCN(C)CC2)/C3=CC(OCO4)=C4C=C3)NC5=C1C=C(C(C)=O)C=C5
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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
[1]. Hamilton G, et al. Characterization of the BH1406 non-small cell lung cancer (NSCLC) cell line carrying an activating SOS1 mutation. Translational lung cancer research. 2024 Nov 30;13(11):2987-2997. [Content Brief]
[2]. Stickler S, et al. Characterization of a pleomorphic rhabdomyosarcoma cell line. Scientific reports. 2025 Jan 23;15(1):2893. [Content Brief]
[3]. Gollner A, et al. Kinase Degraders, Activators, and Inhibitors: Highlights and Synthesis Routes to the Chemical Probes on opnMe.com, Part 1. ChemMedChem. 2023 May 16;18(10):e202300031. [Content Brief]
[4]. Ercin M, et al. Exploring the role of cellular plasticity in metabolic dysfunction-associated steatosis and related molecular mechanisms. Journal of translational medicine. 2025 Nov 13;23(1):1278. [Content Brief]
[5]. Tanaka HY, et al. Heterotypic 3D pancreatic cancer model with tunable proportion of fibrotic elements. Biomaterials. 2020 Aug;251:120077. [Content Brief]
[6]. Bonaguro L, et al. CRELD1 modulates homeostasis of the immune system in mice and humans. Nature immunology. 2020 Dec;21(12):1517-1527. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
BI-5521 Related Classifications
HY-171881 Related Classifications
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