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TGase 2 inhibitor GK921 abrogates RCC growth in xenograft tumor models
and efficacious inhibitor of NPM-ALK
InChi: InChI=1S/C14H15N5S/c1-19(2)14(20)18-17-13(11-7-3-5-9-15-11)12-8-4-6-10-16-12/h3-10H
LDN-214117 shows a high degree of selectivity for ALK2 and low cytotoxicity that could provide a template for preclinical development
BAY 61-3606 dihydrochloride ntel TGase 2 inhibitor GK921 abrogatesBAY 61 3606 is a potent (Ki = 7. 5 nM) and selective inhibitor of Syk kinase. BAY 61 3606 inhibited not only degranulation (IC50 values between 5 and 46 nM) but also lipid mediator and cytokine synthesis in mast cells. BAY 61 3606 was highly efficacious in basophils obtained from healthy human subjects (IC50 = 10 nM) and seems to be at least as potent in basophils obtained from atopic (high serum IgE) subjects (IC50 = 8. 1 nM). B cell receptor
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