F1414-1444 

F1414-1444 is a DBPI skeleton derivative and a potent inhibitor of IspQ (Rv0338c)-targeting Mycobacterium tuberculosis. F1414-1444 binds to the membrane-bound iron-sulfur oxidoreductase IspQ, induces oxidative stress and thiol stress in bacterial cells, upregulates the expression of stress-related genes such as the SigK regulon, thereby inhibiting bacterial proliferation and exerting bactericidal activity. F1414-1444 only inhibits the Mycobacterium tuberculosis complex and Mycobacterium marinum. F1414-1444 can be used in studies related to Mycobacterium tuberculosis^[1].

F1414-1444 (0.5X-16X MIC; 7-14 d) exhibits bactericidal activity against Mycobacterium tuberculosis Erdman with an MBC₉₉ of 1.56 μM, and its cidal effect is time-dependent^[1].
F1414-1444 (23.6 μM) inhibits growth of non-replicating Mycobacterium tuberculosis SS18b by 54%^[1].
F1414-1444 inhibits 99% of growth of all tested drug-susceptible, drug-resistant, and multidrug-resistant Mycobacterium tuberculosis clinical isolates and laboratory mutants with MIC₉₉ values ranging from 0.7 μM to 7.2 μM, indicating activity against strains resistant to frontline and other TB drugs^[1].
F1414-1444 enables the isolation of drug-resistant Mycobacterium tuberculosis Erdman mutants harboring mutated rv0338c (ispQ). Complementation of these resistant mutants with wild-type rv0338c restores compound susceptibility, genetically verifying IspQ as the functional target of F1414-1444^[1].
F1414-1444 (0.1-10 μM；0-12.5 ng/mL ATc) works in combination to reduce IspQ expression via anhydrotetracycline-induced knockdown and sensitizes Mycobacterium tuberculosis H37Rv toward this compound, further validating IspQ as its primary target^[1].
F1414-1444 (10-30 μM; 6 h) upregulates genes associated with redox homeostasis, oxidative/thiol stress, and drug efflux, and downregulates a small cluster of oxidoreductase and regulatory genes when Mycobacterium tuberculosis H37Rv is exposed to it^[1].

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

347.36

C₂₁H₁₇NO₄

794552-29-7

O=C(C1=C2C=C(C)C=CN2C(C(C3=C4C=CC=C3)=O)=C1C4=O)OC(C)C

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Székely R, et al. 6,11-Dioxobenzo[f]pyrido[1,2-a]indoles Kill Mycobacterium tuberculosis by Targeting Iron-Sulfur Protein Rv0338c (IspQ), A Putative Redox Sensor. ACS Infect Dis. 2020 Nov 13;6(11):3015-3025.