Figure 10. Evaluation of substrate competition of ML309 with α-KG in IDH1 R132H.

Figure 10Evaluation of substrate competition of ML309 with α-KG in IDH1 R132H

A. Lineweaver-Burk plot demonstrating competitive mode of inhibition with respect to α-KG; inset shows untransformed data; the data point corresponding to the combination of 400 nM [ML309] and 125 μM [α-KG] did not provide signal above background, hence reaction rate could not be determined. B. Ki determination for ML309.

From: ML309: A potent inhibitor of R132H mutant IDH1 capable of reducing 2-hydroxyglutarate production in U87 MG glioblastoma cells

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