Thiophene-2 (TP2) is a targeted inhibitor of polyketide synthase 13 (Pks13), specifically designed to disrupt mycolic acid biosynthesis. By doing so, it effectively induces rapid cell death in mycobacteria. Thiophene-2 demonstrates notable anti-tuberculosis activity and exhibits a minimum inhibitory concentration (MIC) value of 1 μM against Mycobacterium tuberculosis.
ITP-2 is a selective activator of hERG channels. ITP-2 causes large depolarizing shifts in the midpoint of voltage-dependent inactivation and hyperpolarizing shifts in the voltage-dependence of activation.
TP-238 hydrochloride is a highly potent and selective dual CECR2 BPTF probe, demonstrating IC50 values of 30 nM and 350 nM, respectively. It additionally exerts inhibitory effects on BRD9, with a pIC50 value of 5.9, while displaying lower activity against 338 other kinases.
Prostaglandin H2 (PGH2), initially isolated from the incubation of arachidonic acid with ovine seminal vesicle microsomes, acts as a potent vasoconstrictor. It serves as the precursor for all 2-series prostaglandins (PGs) and thromboxanes (TXs). Moreover, as a TP receptor agonist, PGH2 irreversibly aggregates human platelets at concentrations of 50-100 ng ml.