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Table 1 Representing the IC50 values of ENO1-deleted cells treated with POMHEX in pyruvate free DMEM or DMEM exogenously supplemented with different anaplerotic substrates at the indicated concentrations. IC50 values in italic indicate metabolites that confer partial or complete rescue to POMHEX toxicity. Human plasma metabolite concentrations are indicated where relevant, based on human metabolome database (HMD). Pyruvic acid (HMDB0000243), lactic acid (HMDB0000190), acetate, (HMDB0000042) alanine, (HMDB0000161), aspartate (HMDB0000191), and oxovalerate (HMDB0001865)

From: Impaired anaplerosis is a major contributor to glycolysis inhibitor toxicity in glioma

Anaplerotic substrates

D423

N

Concentrations

ENO1 deleted

in Human Blood (μM)

Pyruvate Free

22

12

 

100 μM Pyruvate

28

6

35

1 mM Pyruvate

51

6

35

5 mM Pyruvate

49

6

35

2.5 mM Methyl Pyruvate

133

4

N/A

5 mM dimethyl 2-oxoglutarate

189

2

N/A

5 mM Lactate

19

4

1,118-1,860

5 mM Acetate

19

2

27-64

5 mM Alanine

11

2

427

2.5 mM Aspartate

29

2

8-20

1X B27

36

2

N/A

1X Fatty Acid

39

2

N/A

2.5 mM Oxaloacetate

87

4

N/A

2.5 mM Oxovalerate

60

4

13

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Cancer & Metabolism

ISSN: 2049-3002