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OATD-02 is an orally active, competitive, reversible, noncovalent dual inhibitor of Arginase1 and 2. OATD-02 is a slow offset inhibitor, blocking intracellular arginases with IC50s of 20 nM (hARG1), 39 nM (hARG2), 39 nM (mARG1), and 28 nM (rARG1), respectively. OATD-02 abolishes tumor immunosuppression induced by both arginases. OATD-02 can be used for melanoma study.
AZD0011 (AZD-0011) a novel peptidic boronic acid prodrug of AZD0011-PL, highly potent and orally available Arginase (ARG) inhibitor with IC50 of 404/308 nM for ARG1/2, respectively.