Small molecules targeting histone demethylase genes (KDMs) inhibit growth of temozolomide-resistant glioblastoma cells.

After 48 hours the IC50 values of the resistant cells was approximately half of that of native cells although this difference did not reach statistical significance.

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Finally we studied the permeability of JIB 04 across the blood-brain barrier and found that this molecule reaches bioactive concentration in the brain; furthermore a pilot in vivo experiment in an orthotopic GB xenograft model showed a trend toward longer survival in treated mice with an Hazard Ratio of 0.5.

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However, after 24 hours the decrease of phosphorylation became much more evident and highly significant ( Supplementary Figure 2 , Panel 3D).

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