Brexpiprazole S-oxide D8 (DM-3411 D8) is a deuterium-labeled Brexpiprazole S-oxide, the primary metabolite of Brexpiprazole, which is a partial agonist of human 5-HT1A and dopamine receptors (Kis: 0.12 nM and 0.3 nM).
Brexpiprazole S-oxide (DM-3411), a primary metabolite of Brexpiprazole, acts as a partial agonist of human 5-HT1A and dopamine receptors with Ki values of 0.12 nM and 0.3 nM, respectively.
AZ5576 racemate is a racemic mixture of AZ5576 isomers. AZ5576 is a potent, highly selective, and orally bioavailable inhibitor of Cdk9 that inhibits Cdk9 enzyme activity with an IC50 <5nM and decreases phosphorlyation of Ser2-RNAPII in cells with an IC50 of 96nM. In the MLL-fusion containing acute myeloid leukemia (AML) line, MV411, short-term treatment with AZ5576 led to a rapid dose-dependent decrease in pSer2-RNAPII with concomitant loss of Mcl1 mRNA and protein, resulting in the cleavage and activation of caspase 3 and loss of cell viability.