Glutamate-5-kinase-IN-1 

Glutamate-5-kinase-IN-1 (compound 50) is a potent glutamate-5-kinase (G5K) inhibitor with an MIC (minimum inhibitory concentration) of 4.1 µM. Glutamate-5-kinase-IN-1 shows G5K inhibition by alters the ATP binding site architecture for enzyme recognition. Glutamate-5-kinase-IN-1 has the potential for the research of anti-TB agents^[1].

G5K^[1]

Glutamate-5-kinase-IN-1 (compound 50) (40 µM) inhibits G5K activity with an I_0.5 of 22.1 µM at 10 mM concentration of L-Glu and ATP^[1].
Glutamate-5-kinase-IN-1 (5, 10, 20 µM) shows no relevant cytotoxicity in HepG2 cells^[1].
Glutamate-5-kinase-IN-1 (120 µM) causes a substantial increase in the Km^app for ATP at constant concentrations of L-Glu (150 mM, 300 mM and 600 mM) and ATP (10 mM)^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

302.37

C₂₀H₁₈N₂O

COC1=CC=C2C3=C(NC=C3)C(CCC4=CC=CC=C4)=NC2=C1

Room temperature in continental US; may vary elsewhere.

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• [1]. Panciera M, et al. Discovery of 3H-pyrrolo[2,3-c]quinolines with activity against Mycobacterium tuberculosis by allosteric inhibition of the glutamate-5-kinase enzyme. Eur J Med Chem. 2022 Mar 15;232:114206.  [Content Brief]