KHS-101

KHS-101 is an inhibitor of heat shock protein 60 (Hsp60), also known as HSPD1, and an inducer of neuronal differentiation.^1,2 It inhibits the refolding activity of the complex of Hsp60 with the co-chaperone Hsp10, also known as HSPE1, in a cell-free assay (IC₅₀ = 14.4 µM) and induces autophagy in GBM1 glioblastoma cells.¹ KHS-101 induces differentiation of primary rat hippocampal neural progenitor cells (NPCs) into neurons (EC₅₀ = ^~1 µM) and inhibits BMP4-induced differentiation induced of primary rat hippocampal NPCs into astrocytes when used at a concentration of 5 µM.² It increases nuclear localization of the transforming acidic coiled-coil containing protein 3 (Tacc3) target aryl hydrocarbon receptor nuclear translocator 2 (Arnt2) in HEK293T cells expressing the rat proteins when used at a concentration of 5 µM. KHS-101 reduces tumor burden and increases survival in a patient-derived xenograft (PDX) mouse model of giant cell glioblastoma.¹

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1. Polson, E.S., Kuchler, V.B., Abbosh, C., et al. KHS101 disrupts energy metabolism in human glioblastoma cells and reduces tumor growth in mice. Sci. Transl. Med. 10(454), eaar2718 (2018).

2. Wurdak, H., Zhu, S., Min, K.H., et al. A small molecule accelerates neuronal differentiation in the adult rat. Proc. Natl. Acad. Sci. USA 107(38), 16542-16547 (2010).