MPT0G211

MPT0G211 is an inhibitor of histone deacetylase 6 (HDAC6, IC50 = 0. nM). It is selective for HDAC6 over HDAC1-5 (IC50s = 9. 12. 7. 4. and 3. µM, respectively), HDAC7-11 (IC50s = 0. 1. 1. 9. and 0. µM, respectively), and sirtuin 1 (SIRT1, IC50 = > 20 µM), as well as a panel of 97 kinases at 1 µM. MPT0G211 inhibits the growth of RPMI-8226, U266, and NCI H929 multiple myeloma cells (GI50s = 7. 40. and 9. µM, respectively) and does not inhibit the growth of HS-5 normal bone marrow cells (GI50 = >100 µM). In vivo, MPT0G211 (30 mg/kg) reduces tumor volume in an RPMI-8226 mouse xenograft model. It also decreases cognitive deficits and tau phosphorylation in the 3xTg mouse model of Alzheimer's disease. InChI: InChI=1S/C17H15N3O2/c21-17(20-22)14-8-6-12(7-9-14)11-19-15-5-1-3-13-4-2-10-18-16(13)15/h1-10,19,22H,11H2,(H,20,21), InChIKey: BPDQUKCPNSRTTR-UHFFFAOYSA-N, SMILES: O=C(C1=CC=C(CNC2=CC=CC3=CC=CN=C32)C=C1)NO