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SB 431542: Potent ALK5 Inhibitor

SB 431542 is a highly selective and potent inhibitor of ALK5, offering exceptional specificity over other kinases like p38 MAPK. This remarkable specificity is evident in its IC50 value of 94 nM, which is 100-fold more selective for ALK5. This unique characteristic makes SB 431542 an invaluable tool in research involving ALK5 signaling pathways.

• High Selectivity: 100-fold more selective for ALK5 than p38 MAPK and other kinases.
• Low IC50: IC50 of 94 nM for ALK5 inhibition.

Targeted Inhibition of Activin and Nodal Receptors

SB 431542 effectively inhibits the activin type I receptor ALK4 and the nodal type I receptor ALK7, which are pivotal in the phosphorylation of Smad2. This inhibition has minimal impact on ALK1, ALK2, ALK3, and ALK6, which phosphorylate Smad1. Furthermore, SB 431542 selectively inhibits endogenous activin without affecting BMP signaling. This targeted inhibition offers a valuable advantage in research and therapeutic applications.

• Targeted Inhibition: Inhibits ALK4 and ALK7 without affecting ALK1, ALK2, ALK3, and ALK6.
• Activin Specificity: Selectively inhibits endogenous activin without affecting BMP signaling.

Multi-Targeted Effects and Cell Cycle Regulation

SB 431542 demonstrates a wide range of effects, including the inhibition of TGF-β1-induced collagen lα1 and PAI-1 mRNA production, as well as the suppression of TGF-β-mediated growth factors like PDGF-A, FGF-2, and HB-EGF. This inhibitor also plays a crucial role in cell cycle regulation, significantly suppressing TGF-β-induced G1 arrest and promoting cell proliferation. Additionally, SB 431542 inhibits TGF-β-induced EMT and elevates the expression of CD86 and CD83, highlighting its potential in modulating immune responses.

• Multi-Targeted: Inhibits TGF-β1-induced collagen lα1 and PAI-1 mRNA production.
• Cell Cycle Regulation: Suppresses TGF-β-induced G1 arrest and promotes cell proliferation.