miransertib

Miransertib (ARQ-092) is an orally bioavailable, selective, and potent allosteric Akt inhibitor.

Miransertib mesylate is a selective AKT inhibitor that binds to and inhibits the activity of AKT in a non-ATP competitive manner, which may result in the inhibition of the PI3K/AKT signaling pathway. This may result in reduction in tumor cell proliferation and the induction of tumor cell apoptosis.

Miransertib hydrochloride (ARQ-092 hydrochloride) is a potent, orally bioavailable, selective, and allosteric inhibitor of Akt with an IC50 of 2.7 nM, 14 nM, and 8.1 nM against Akt1, Akt2, and Akt3, respectively. It also shows significant potency against the AKT1-E17K mutant protein and holds promise for research on PI3K/AKT-driven tumors and Proteus syndrome. Additionally, Miransertib hydrochloride exhibits efficacy against Leishmania [1, 2].

MeTC7 is a vitamin D receptor (VDR) antagonist with antitumor activity that inhibits PD-L1 and may inhibit the growth of xenografts and transgenic tumors in vivo.