STK393606

Description

15-hydroxy prostaglandin dehydrogenase (15-hydroxy PGDH) is a key enzyme involved in the inactivation of PGs and related eiscosanoids. It functions by catalyzing the oxidation of primary PGs to their 15-keto metabolites. Two types of 15-hydroxy PGDH have been identified: type-I is NAD⁺-dependent primarily using eicosanoids as substrates, while type-II uses either NAD⁺ or NADP⁺ as cofactors and bears broader substrate specificity. STK393606 is a competitive inhibitor of NAD⁺-dependent type-I 15-hydroxy PGDH with an IC₅₀ value of 26.4 nM and a K_i value of 5 nM. It demonstrates selectivity for 15-hydroxy PGDH when profiled across a panel of related dehydrogenase or reductase enzymes.

Definition

ChEBI: 2-[[(6-bromo-1H-imidazo[4,5-b]pyridin-2-yl)thio]methyl]benzonitrile is an imidazopyridine.

target

nad+-dependent type-i 15-hydroxy pgdh

IC 50

26.4 nm

References

[1] niesen f h, schultz l, jadhav a, et al. high-affinity inhibitors of human nad + -dependent 15-hydroxyprostaglandin dehydrogenase: mechanisms of inhibition and structure-activity relationships[j]. plos one, 2010, 5(11).
[2] tai h, ensor c m, tong m, et al. prostaglandin catabolizing enzymes.[j]. prostaglandins & other lipid mediators, 2002: 483-493.
[3] lee s c, levine l. prostaglandin metabolism. ii. identification of two 15-hydroxyprostaglandin dehydrogenase types.[j]. journal of biological chemistry, 1975, 250(2): 548-552.