BI-4659 is a selective inhibitor of ALK5 (activin receptor-like kinase 5), also known as TGF-β receptor type I (TGFBR1), which plays a central role in TGF-β signaling. BI-4659 exhibits potent in vitro inhibition of ALK5 with an IC₅₀ in the low nanomolar range (typically reported between 1–10 nM, depending on the assay). It effectively blocks TGF-β–induced phosphorylation of SMAD2/3 and downstream transcriptional activity in cellular models. In preclinical studies, BI-4659 has demonstrated antifibrotic effects in vitro and in vivo, particularly in models of organ fibrosis where aberrant TGF-β signaling is a driver of pathology. The compound is under investigation as a potential therapeutic for fibrotic diseases and certain cancers associated with dysregulated TGF-β signaling.
MedKoo Cat#: 466195
Name: BI-4659
CAS#: 894784-05-5
Chemical Formula: C27H28N4O2
Exact Mass: 440.2212
Molecular Weight: 440.55
Elemental Analysis: C, 73.61; H, 6.41; N, 12.72; O, 7.26
The following data is based on the product molecular weight 440.55 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
