NSC116565
NSC116565 is an Antibacterial agent, Herbicide, and competitive Ketol-acid reductoisomerase inhibitor, with a Ki of 95.4 nM against Mycobacterium tuberculosis MtKARI. NSC116565 inhibits the growth of mycobacteria by disrupting the branched-chain amino acid biosynthesis pathway, and also inhibits the growth of weeds and brassicas. NSC116565 can be used in tuberculosis-related research.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- CAS. Nr.: 18903-23-6
- Formel: C6H5N3O3S
- Molecular Weight:199.19
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biologische Aktivität
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Chemical Information
- Protokoll
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
Biologische Aktivität
Beschreibung
In Vitro
NSC116565 (30 min) potently inhibits Mycobacterium tuberculosis KARI via a slow-binding kinetic mechanism, with an apparent inhibition constant of 0.36 μM[1].
NSC116565 (0.78-50 μM; 5 days) inhibits the growth of Mycobacterium tuberculosis strains H37Ra (MIC50 = 2.93 μM, MIC90 = 9.86 μM) and H37Rv (MIC50 = 6.06 μM, MIC90 = 20.42 μM) in defined minimal medium, and its activity decreases when branched-chain amino acids are added to the medium[2].
NSC116565 (30 min) inhibits Oryza sativa KARI with an apparent inhibition constant of 2.4 μM, and shows no time-dependent binding[1].
NSC116565 (100 μM) inhibits the growth of Mycobacterium tuberculosis H37Rv, with an MIC of 20.4 μM, and its target is the branched-chain amino acid biosynthetic pathway[1].
NSC116565 (10-100 mg/mL; 72 h) inhibits root growth of Brassica campestris by up to 95% at a concentration of 100 mg/mL and by 70% at 10 mg/mL[1].
NSC116565 (750-1500 g/ha) exhibits herbicidal activity against a variety of weeds, with the strongest post-emergence inhibitory effect on Amaranthus retroflexus (64.6% at 1500 g/ha)[1].
NSC116565 (1.6-200.0 μM; 24 h) exhibits no toxicity toward HEK293 and SW620 mammalian cell lines at the highest concentration of 200 μM[1].
NSC116565 is a potent, time-dependent competitive inhibitor of purified Mycobacterium tuberculosis ketol-acid reductoisomerase (MtKARI), with a Ki value of 95.4 nM[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
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Cell Line:HEK293, SW620
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Concentration:1.6-200.0 μM
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Incubation Time:24 h
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Result:Showed no inhibition of growth in either HEK293 or SW620 cells at concentrations up to 200 μM.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS. Nr. 18903-23-6
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Molecular Weight 199.19
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Formel C6H5N3O3S
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SMILES
O=C1NC2=C(C(N1O)=O)SC(C)=N2
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Protokoll
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Research Protocol for Infectious Diseases
Infectious-disease experiments test how pathogens interact with host barriers, innate immune receptors, inflammatory signaling, pathogen replication, and tissue injury; pattern-recognition receptors such as TLRs, RIG-I-like receptors, NOD-like receptors, and inflammasomes detect microbial molecules and activate NF-κB, interferon, and cytokine responses. The central hypothesis is that infection severity reflects the balance between pathogen burden and host response: protective inflammation restricts pathogen growth, whereas excessive or mislocalized inflammation contributes to tissue damage and disease phenotype. Unresolved questions include which host pathways are protective versus pathogenic, why some infection models fail to translate to human disease, and which combined readouts best predict clinically relevant infection outcomes.
Reinheit & Dokumentation
Verweise
[1]. Lin X, et al. A Ketol-Acid Reductoisomerase Inhibitor That Has Antituberculosis and Herbicidal Activity. Chemistry (Weinheim an der Bergstrasse, Germany). 2025 Jun 26;31(36):e202501158. [Content Brief]
[2]. Lin X, et al. Discovery of a Pyrimidinedione Derivative with Potent Inhibitory Activity against Mycobacterium tuberculosis Ketol-Acid Reductoisomerase. Chemistry (Weinheim an der Bergstrasse, Germany). 2021 Feb 10;27(9):3130-3141. [Content Brief]
[3]. Guida M, et al. Amino Acid Biosynthesis Inhibitors in Tuberculosis Drug Discovery. Pharmaceutics. 2024 May 28;16(6):725. [Content Brief]
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
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