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With BI-0314 the first allosteric activator of tyrosine phosphatases is described. We hope to spark the design of selective allosteric ligands of phosphatases with the disclosure of the X-ray structure, and the elucidation of the mode of action of BI-0314 on STEP.
Chymase plays an important and diverse role in the homeostasis for a number of cardiovascular processes and has been linked to heart failure.
BI-5521 is a potent and selective ATP-competitive small molecule inhibitor of glycogen synthase kinase 3 (GSK-3) with demonstrated in vivo activity. The N-alkylated derivative BI-4481 is also available as negative control.
BI-4659 inhibits ALK5 with an IC50 value of 19 nM and blocks the cellular phosphorylation of SMAD2/SMAD3 with an EC50 of 185 nM. BI-4659 is a suitable tool for testing biological hypotheses in vitro.
BI-167107 was used to support crystallization of active state β2AR complexes and can be employed as a tool for the crystallization of other beta receptors.