TGF-β / Smad Signaling
The TGF-β family is generally classified into two sub-families, TGF-β ligands, and bone morphogenic protein (BMP) ligands. In canonical signaling, receptor activation lead to phosphorylation of a group of transcription factors called Smads. TGF-β ligands bind to type II receptors (TGF-β II) which recruit and phosphorylate type I receptor (TGF-β I) on serine/threonine residues. The TGF-β I then recruits and phosphorylates a receptor regulated Smad (R-Smad). The R-Smad binds to the common Smad (Co-Smad) and forms a heterodimeric complex. This complex then translocates into the cell nucleus where it binds with nuclear co-factors to regulate the transcription of various target genes. Dysregulation of TGF-β/Smad signaling pathway is associated with a number of pathological conditions including fibrosis, cancer, immunodeficiency, diabetes and cardiovascular diseases etc.
- B4964 (-)-epicatechinSummary: inducer of pancreatic β-cell regeneration
- B4965 (-)-epicatechin gallateSummary: major catechin in green tea
- B5858 ITD 1Summary: The first selective TGFβ inhibitor
- B5946 EW-71971 CitationTarget: BMP and Other Activin ReceptorsSummary: Selective inhibitor of TGF-β type I receptor kinase
- B5965 Tamoxifen1 CitationTarget: PKCSummary: TGF-β modulatory and PKC inhibitory effects
- A8232 Nilotinib(AMN-107)1 CitationTarget: Bcr-AblSummary: Bcr-Abl kinase inhibitor,selective
- A8249 SB 4315422 CitationSummary: ALK inhibitor
- A2149 Bosutinib (SKI-606)1 CitationTarget: Bcr-Abl|SrcSummary: Potent Abl/Src kinases
- A1670 Enzastaurin (LY317615)2 CitationTarget: PKCSummary: PKC beta inhibitor,potent and selective
- A1805 Imatinib Mesylate (STI571)Target: PDGFR|c-Kit|Bcr-AblSummary: Abl/c-kit/PDGFR inhibitor