MPT0G211

MPT0G211 is an inhibitor of histone deacetylase 6 (HDAC6; IC₅₀ = 0.291 nM).¹ It is selective for HDAC6 over HDAC1-5 (IC₅₀s = 9.55, 12.5, 7.75, 4.438, and 3.112 µM, respectively), HDAC7-11 (IC₅₀s = 0.709, 1.19, 1.53, 9.791, and 0.376 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 = 7.49, 40.61, and 9.14 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.²

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1. Lee, H.-Y., Nepali, K., Huang, F.-I., et al. (N-Hydroxycarbonylbenylamino)quinolines as selective histone deacetylase 6 inhibitors suppress growth of multiple myeloma in vitro and in vivo. J. Med. Chem. 61(3), 905-917 (2018).

2. Fan, S.-J., Huang, F.-I., Liou, J.-P., et al. The novel histone de acetylase 6 inhibitor, MPT0G211, ameliorates tau phosphorylation and cognitive deficits in an Alzheimer’s disease model. Cell Death Dis. 9(6), 655 (2018).