Isoniazid

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

Isoniazid Chemical Structure

CAS: 54-85-3

Selleck's Isoniazid has been cited by 5 publications

Purity & Quality Control

Batch: Purity: 99.9%
99.9

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
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
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]
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05655702 Recruiting Tuberculosis ANRS Emerging Infectious Diseases|Haiphong University of Medicine and Pharmacy|Expertise France|Université Montpellier|New York University|CENTER FOR SUPPORTING COMMUNITY DEVELOPMENT INITIATIVES October 2 2023 Not Applicable
NCT06054334 Recruiting Tuberculosis Centre Hospitalier Universitaire Amiens January 4 2023 --

Chemical lnformation & Solubility

Molecular Weight 137.14 Formula

C6H7N3O

CAS No. 54-85-3 SDF Download Isoniazid SDF
Smiles C1=CN=CC=C1C(=O)NN
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 27 mg/mL ( (196.87 mM); Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : 27 mg/mL

Ethanol : 27 mg/mL


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In vivo
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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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