BI-4659
Based on 1 Customer Validation
BI-4659 is a TGFβRI and PDGFRα inhibitor with IC50 values of 19 nM and 99 nM, respectively. BI-4659 inhibits the kinase activities of TGFβRI and PDGFRα, blocks the downstream TGFβRI signaling pathway, and reduces the phosphorylation level of Smad2/3 without altering the expression of TGF-β1. BI-4659 is applicable to research related to pulmonary fibrosis, cancer, and renal ischemia-reperfusion injury.
For research use only. We do not sell to patients.
The BI-4659 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.
- Purity: 99.78%
- CAS No.: 894784-05-5
- Formula: C27H28N4O2
- Molecular Weight:440.54
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
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TGFBR1 19 nM (IC50) |
PDGFRα 99 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HaCaT | EC50 |
185 nM
Compound: 47i
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Inhibition of TGFbeta receptor in human HaCaT cells assessed as Smad phosphorylation by ELISA
Inhibition of TGFbeta receptor in human HaCaT cells assessed as Smad phosphorylation by ELISA
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[PMID: 20919678] |
| HaCaT | IC50 |
>1 μM
Compound: 47i
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Cytotoxicity against human HaCaT cells
Cytotoxicity against human HaCaT cells
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[PMID: 20919678] |
BI-4659 (75 min) inhibits TGFβRI-mediated phosphorylation of Smad2/3 in HaCaT cells with an EC50 of 185 nM[1].
BI-4659 (up to 1 μM; 24 h) shows no significant cytotoxicity in HaCaT cells at concentrations as high as 1 μM following a 24 h incubation[1].
BI-4659 (1 μM; 24 h) inhibits the TGF-β-Smad2/3 pathway in mouse bone marrow-derived neutrophils, thereby blocking sFgl2-MSC-induced transformation of neutrophils into an anti-inflammatory N2-like phenotype, inhibition of neutrophil extracellular trap formation, and regulation of inflammatory cytokine secretion[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HaCaT cells
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Concentration:up to 1 μM
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Incubation Time:24 h
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Result:Exhibited no significant cytotoxicity (IC50 > 1 μM).
Chemical Information
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CAS No. 894784-05-5
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Appearance Solid
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Molecular Weight 440.54
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Formula C27H28N4O2
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Color Off-white to yellow
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SMILES
CN(C)CC(C=C1)=CC=C1N/C(C2=CC=CC=C2)=C3C4=CC=C(C(NCC)=O)C=C4NC/3=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMSO : 5 mg/mL (11.35 mM; Need warming; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
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Data Sheet (278 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
[1]. Roth GJ, et al. Design, synthesis, and evaluation of indolinones as inhibitors of the transforming growth factor β receptor I (TGFβRI). J Med Chem. 2010;53(20):7287-7295. [Content Brief]
[2]. Chen GS, et al. Overexpression of Soluble Fibrinogen-like Protein 2 in MSCs Ameliorates Renal Ischemia-Reperfusion Injury in Mice by Modulating Neutrophils. Balkan Med J. 2026;43(3):136-150. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.2699 mL | 11.3497 mL | 22.6994 mL | 56.7485 mL |
| 5 mM | 0.4540 mL | 2.2699 mL | 4.5399 mL | 11.3497 mL | |
| 10 mM | 0.2270 mL | 1.1350 mL | 2.2699 mL | 5.6749 mL |
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