LY-364947 #54678

LY-364947, also known as HTS-466284, is a potent and selective TGF-β type-I receptor (TGF-β RI, TGFR-I, TβR-I, ALK-5) inhibitor. This small molecule specifically targets TGF-β RI with an IC₅₀ value of 59 nM and is less effective on TGF-β RII and MLK-7K (IC₅₀ values of 400 nM and 1400 nM, respectively) (1). LY-364947 regulates MDA-MB-231 cell invasion by inhibiting autocrine TGF-β signaling (2). Patients in intensive care units (ICUs) that suffer from chronic sepsis can experience weakening of the diaphragm muscles caused by muscle wasting, requiring mechanical ventilation. Members of the TGF-β family can trigger the activation of protein breakdown. Inhibition of the TGF-β pathway can protect the diaphragm during chronic sepsis, making LY-364947 an interesting compound to study as it relates to effective ICU patient care (3).