ex 527

Selisistat R-enantiomer (EX-527 (R-enantiomer)) is a R-enantiomer of Selisistat (T6111) with much less activity than Selisistat (IC50 of SIRT1 > 100 μM).

Selisistat (EX-527) is a potent and specific inhibitor of the deacetylase SIRT1 (IC50 = 38 nM) and can be utilized in the study of neurological disorders such as Huntington's chorea.

Selisistat S-enantiomer (EX-527 S-enantiomer) is an effective and specific SIRT1 inhibitor (IC50 = 98 nM) and shows >200-fold selectivity against SIRT2/3.

PKSI-527 is a non-covalent, highly selective small molecule inhibitor of plasma kallikrein with an inhibition constant (Ki) of 0.81 µM for plasma kallikrein. PKSI-527 modulates the kallikrein-kinin system by inhibiting bradykinin generation, significantly reduces arthritis severity in a collagen-induced arthritis mouse model, and improves indicators of disseminated intravascular coagulation and organ damage in endotoxin-induced rat models.