Tanzisertib HCl (CC-930)

Tanzisertib HCl (CC-930, JNK-930, JNKI-1) is kinetically competitive with ATP in the JNK-dependent phosphorylation of the protein substrate c-Jun and potent against all isoforms of JNK (Ki (JNK1) = 44 ± 3 nM, IC50 (JNK1) = 61 nM, Ki (JNK2) = 6.2 ± 0.6 nM, IC50 (JNK2) = 5 nM, IC50 (JNK3) = 5 nM) and selective against MAP kinases ERK1 and p38a with IC50 of 0.48 and 3.4 μM respectively.