transforming growth factor β 3

(E)-SIS3 (SIS3) is a Smad3 inhibitor (IC50=3 μM) and is selective. (E)-SIS3 inhibits the differentiation of fibroblasts into myofibroblasts via TGF-β1.

Luspatercept (ACE-536), a recombinant modified ActRIIB fusion protein, selectively binds to transforming growth factor β superfamily ligands, thereby enhancing erythrocyte production and advancing the maturation of erythroid precursors. Moreover, by binding with GDF11, it inhibits Smad2/3 signaling. This compound is instrumental in anemia research [1].

BMS-986260 is a selective, and orally bioavailable TGFβR1 inhibitor(IC50 = 1.6 nM).

sTGFBR3 antagonist 1 (Compound p24) is an antagonist of soluble transforming growth factor β receptor 3 (sTGFBR3) that activates the TGF-β signaling pathway while inhibiting the IκBα/NF-κB signaling pathway. It inhibits the release of NO induced by LPS in BV2 cells with an IC50 of 0.52 μM. sTGFBR3 antagonist 1 exhibits anti-inflammatory and neuroprotective activities and can enhance the permeability of the blood-brain barrier (BBB). This compound is applicable in research related to Alzheimers disease.

(Rac)-Hydnocarpin is a natural flavonolignan derived from the flowers of Pueraria lobata that demonstrates strong cytotoxic effects against multiple ovarian cancer cell lines while maintaining minimal toxicity toward normal ovarian surface epithelial cells. (Rac)-Hydnocarpin triggers intrinsic apoptotic signaling through activation of caspase-9 and caspase-3 with limited involvement of caspase-8, driven by reactive oxygen species generation as a dominant mediator of apoptosis. (Rac)-Hydnocarpin additionally reprograms tumor-associated immune cells by reducing M2 macrophage markers and pro-tumoral mediators including matrix metalloproteinase-2/9, C–C motif chemokine ligand 5, transforming growth factor-β, and vascular endothelial growth factor, while enhancing macrophage phagocytosis, reinforcing its role as a multifunctional anticancer agent.