Topoisomerase I inhibitor 5 is an efficient inhibitor of topoisomerase I, with an IC50 value. It effectively disrupts DNA and inhibits the activity of topoisomerase I. Moreover, it can induce apoptosis in MCF-7 cells and arrest the cell cycle at the G1 phase. Topoisomerase I inhibitor 5 also exhibits potency in reversing P-gp-mediated resistance to Adriamycin [1].
IRAK inhibitor 4 is a compound that functions as an inhibitor of interleukin-1 receptor-associated kinase 4 (IRAK4). It specifically targets and inhibits the activity of IRAK4. The (trans) form of IRAK inhibitor 4 refers to its specific molecular configuration.
5(S),6(R)-11-trans DiHETE is a C-11 double bond isomer of 5(S),6(R)-DiHETE that is formed by the enzymatic isomerization of 5(S),6(R)-DiHETE by a membrane bound factor. 5(S),6(R)-11-trans DiHETE has been found in rat kidney homogenates and is potentially formed by the epoxide hydrolase pathway in this tissue. The isomerase activity responsible for the conversion of leukotriene B4 (LTB4) to 6-trans LTB4 in rat kidney homogenates has also been implicated in its formation. 5(S),6(R)-11-trans DiHETE is not a substrate for soybean lipoxygenase. The biological activity of 5(S),6(R)-11-trans DiHETE has not been reported.
5-trans-Prostaglandin E2 accelerates fibrinolysis by enhancing plasminogen activation mediated by tissue-type plasminogen activator. It also inhibits platelet aggregation in human PRP.
Cloprostenol is a synthetic derivative of prostaglandin F2α that is used in veterinary medicine as a luteolytic agent for the induction of estrus and in the treatment of reproductive disorders in cattle, swine, and horses. (+)-5-trans Cloprostenol is a minor impurity produced in the synthesis of (+)-cloprostenol. The (+)-5-trans isomer is 20-fold less active than the 5-cis form in terminating pregnancy in the hamster.
Microtubule inhibitor 5 (compound 17f) is a highly potent cytotoxic agent that inhibits microtubule function. It exhibits a substantial cytotoxic effect on NCI-H460 cells, with an IC50 value of 154.5 nM. Moreover, this compound demonstrates excellent cell permeability [1].
PKI PKA Inhibitor (5-24) is a synthetic peptide inhibitor of PKA (cAMP-dependent protein kinase) (Ki= 2.3 nM) derived from the active site of the skeletal muscle inhibitor protein.1It mimics the protein substrate by binding to the catalytic site through the arginine-cluster basic subsite.1The prominent enzyme-substrate interaction site occurs where PKA catalytic subunit residues Tyr235and Phe239form a sandwich-like structure with residue Phe10of PKI (5-24).2
5-trans-17-phenyl trinor Prostaglandin F2α (5-trans-17-phenyl trinor PGF2α) represents the 5-trans isomer and the free acid variant of 17-phenyl trinor PGF2α, distinct from its ethyl amide and dimethyl amide derivatives. This compound serves as a potential impurity in 17-phenyl trinor PGF2α formulations. It is utilized as an analytical standard for the detection and quantification of itself in 17-phenyl trinor PGF2α preparations.
ITK inhibitor 5 (compound 27) is a highly potent and selectively targeted inhibitor of ITK. It exhibits IC50 values of 5.6 nM and 25 nM for ITK and BTK respectively [1].