Bioactivity | 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]. |
Target | G5K |
Invitro | Glutamate-5-kinase-IN-1 (compound 50) (40 µM) inhibits G5K activity with an I0.5 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 Kmapp for ATP at constant concentrations of L-Glu (150 mM, 300 mM and 600 mM) and ATP (10 mM)[1]. |
Name | Glutamate-5-kinase-IN-1 |
Formula | C20H18N2O |
Molar Mass | 302.37 |
Transport | Room temperature in continental US; may vary elsewhere. |
Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
Reference | [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. |