mir-16

Cl-amidine hydrochloride is an orally available PAD inhibitor that blocks histone 3 deimination and neutrophil extracellular trap formation and improves survival in septic mice. It induces apoptosis in cancer cells and induces miR-16 to cause cell cycle arrest.

Cl-amidine TFA is an orally active PAD inhibitor with IC₅₀ values of 0.8 μM, 6.2 μM and 5.9 μM for PAD1, PAD3 and PAD4, respectively. This compound can induce cancer cell apoptosis, and also upregulate the expression of miR-16 (miRNA-16, microRNA-16), thereby triggering cell cycle arrest. In addition, Cl-amidine TFA can block the citrullination of histone 3 and the formation of neutrophil extracellular traps, effectively improving the survival rate of mice with sepsis.

Motixafortide TFA(664334-36-5,Free) (BKT140 TFA) is an antagonist of CXCR4 with IC50 of ～1 nM. It induces the apoptosis of AML blasts by down-regulating ERK, BCL-2, MCL-1 and cyclin-D1 via altered miR-15a/16-1 expression.