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.
For research use only. We do not sell to patients.
- CAS No.: 794552-29-7
- Formula: C21H17NO4
- Molecular Weight:347.36
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
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.
Chemical Information
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CAS No. 794552-29-7
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Molecular Weight 347.36
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Formula C21H17NO4
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SMILES
O=C(C1=C2C=C(C)C=CN2C(C(C3=C4C=CC=C3)=O)=C1C4=O)OC(C)C
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)