Biologically Active Small Molecules

A DYRK1B inhibitor (IC₅₀ = 17 nM) that demonstrates 5-fold and 110-fold selectivity against the related family members DYRK1A and DYRK2, respectively used as a probe to elucidate the mechanism of DYRK1B regulation of cell cycle

A selective, irreversible inhibitor of cytochrome P450 (CYP) 3A isoforms (IC₅₀ values range from 26 to 240 nM for CYP3A4 and CYP3A4/5 from different sources) potently blocks the hydroxylation of testosterone and midazolam by CYP3A4.

A selective, irreversible inhibitor of cytochrome P450 (CYP) 3A isoforms (IC₅₀ values range from 26 to 240 nM for CYP3A4 and CYP3A4/5 from different sources) potently blocks the hydroxylation of testosterone and midazolam by CYP3A4.

A selective, irreversible inhibitor of cytochrome P450 (CYP) 3A isoforms (IC₅₀ values range from 26 to 240 nM for CYP3A4 and CYP3A4/5 from different sources) potently blocks the hydroxylation of testosterone and midazolam by CYP3A4.

A tumor-inhibiting antibiotic that inhibits the glutamine-dependent amidotransferases involved in nucleotide biosynthesis, N-formylglycineamidine ribotide synthetase and glucosamine-6-phosphate isomerase also inhibits the hexosamine biosynthetic

A tumor-inhibiting antibiotic that inhibits the glutamine-dependent amidotransferases involved in nucleotide biosynthesis, N-formylglycineamidine ribotide synthetase and glucosamine-6-phosphate isomerase also inhibits the hexosamine biosynthetic

A tumor-inhibiting antibiotic that inhibits the glutamine-dependent amidotransferases involved in nucleotide biosynthesis, N-formylglycineamidine ribotide synthetase and glucosamine-6-phosphate isomerase also inhibits the hexosamine biosynthetic

A tumor-inhibiting antibiotic that inhibits the glutamine-dependent amidotransferases involved in nucleotide biosynthesis, N-formylglycineamidine ribotide synthetase and glucosamine-6-phosphate isomerase also inhibits the hexosamine biosynthetic

A purine analog with immunosuppressive effects serves as a prodrug for 6-mercaptopurine, which alters purine processing and DNA synthesis, interfering with lymphocyte proliferation used to benefit IBD, as well as additional diseases with

A purine analog with immunosuppressive effects serves as a prodrug for 6-mercaptopurine, which alters purine processing and DNA synthesis, interfering with lymphocyte proliferation used to benefit IBD, as well as additional diseases with

A potent, selective, brain permeable inhibitor of GSK3&alpha and GSK3&beta (Kis = 6.9 and 31 nM, respectively) shows good bioavailability after oral administration in vivo, inhibiting hippocampal tau phosphorylation and reversing cognitive

A potent, selective, brain permeable inhibitor of GSK3&alpha and GSK3&beta (Kis = 6.9 and 31 nM, respectively) shows good bioavailability after oral administration in vivo, inhibiting hippocampal tau phosphorylation and reversing cognitive