Isoniazid

Catalog No.S1937

For research use only.

Isoniazid is a prodrug that blocks the action of fatty acid synthase by interacting with KatG , used for the prevention and treatment of tuberculosis.

Isoniazid Chemical Structure

CAS No. 54-85-3

Selleck's Isoniazid has been cited by 3 Publications

Purity & Quality Control

Choose Selective Fatty Acid Synthase Inhibitors

Biological Activity

Description Isoniazid is a prodrug that blocks the action of fatty acid synthase by interacting with KatG , used for the prevention and treatment of tuberculosis.
In vitro

Isoniazid is a prodrug that requires activation by the mycobacterial catalase-peroxidase enzyme (KatG) to an active form that then exerts a lethal effect on an intracellular target or targets. [1] Isoniazid upregulates the expression of an operon containing five FAS II components, including kasA and acpM. Isoniazid results in the accumulation of ACP-bound lipid precursors to mycolic acids that are 26 carbons long and fully saturated. [2] Isoniazid enters the mycobacterial cell by passive diffusion. Isoniazid itself is not toxic to the bacterial cell, but acts as a prodrug and is activated by the mycobacterial enzyme KatG, a multifunctional catalase-peroxidase that has other activities, including peroxynitritase and NADH oxidase. Isoniazid inhibits cell wall lipid synthesis, coupled with the findings that inhibitory INH adducts of NAD+/NADP+ are formed from the isonicotinoyl radical, leading the field away from this area. [3] Isoniazid induces a concentration-dependent (0-40 mM) cytotoxic effect in day-1 treated HepG2 cells and not significantly affected by decreases in intracellular GSH concentrations. [4]

In vivo Isoniazid increases CYP2E1 protein, and the 6-hydroxychlorzoxazone formation rate is increased by 2.7 and 2.2-fold in liver and kidney, respectively. Isoniazid decreases liver and kidney 20-HETE content to 34% and 15.6% of control, respectively, without significantly altering tissue 19-HETE concentration. [5]

Protocol (from reference)

Solubility (25°C)

In vitro

DMSO 27 mg/mL
(196.87 mM)
Water 27 mg/mL
(196.87 mM)
Ethanol 27 mg/mL
(196.87 mM)

Chemical Information

Molecular Weight 137.14
Formula

C6H7N3O

CAS No. 54-85-3
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles C1=CN=CC=C1C(=O)NN

In vivo Formulation Calculator (Clear solution)

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Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT05117788 Not yet recruiting -- Tuberculosis Multidrug-Resistant Foundation for Innovative New Diagnostics Switzerland|V. N. Karazin Kharkiv National University|Kenya Medical Research Institute|Universidad Peruana Cayetano Heredia|Bioneer Corporation January 2022 --
NCT05124678 Not yet recruiting Drug: Isoniazid Tablets Tuberculosis Makerere University November 18 2021 Phase 2
NCT05073926 Recruiting Other: No intervention is part of the study protocol Latent Tuberculosis|Staphylococcus Aureus Region Skane September 30 2021 --
NCT04972903 Not yet recruiting -- Tuberculosis|Pulmonary Institut National de la Santé Et de la Recherche Médicale France|National Agency for Research on AIDS and Viral Hepatitis (ANRS) August 2021 --

(data from https://clinicaltrials.gov, updated on 2022-01-17)

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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