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 No. 54-85-3

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Isoniazid Related Products

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
NCT06281834 Not yet recruiting
Pediatric HIV Infection|Latent Tuberculosis
Brigham and Women''s Hospital|APIN Public Health Initiatives|University of Cape Town
May 2024 Phase 1
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

Chemical Information & 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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