| Name | Isoniazid |
| Description | Isoniazid (Isonicotinic hydrazide) is an antibacterial agent used primarily as a tuberculostatic. |
| 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] |
| Storage | Keep away from direct sunlight | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | DMSO : 60.63 mg/mL (442.1 mM), Sonication is recommended.
10% DMSO+40% PEG300+5% Tween-80+45% Saline : 2 mg/mL (14.58 mM), Sonication is recommended.
H2O : 25 mg/mL (182.3 mM), Sonication is recommended.
Ethanol : 26 mg/mL (189.59 mM), Sonication is recommended.
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| Keywords | tuberculostatic | NAPDH | mycobacteria | Mitophagy | Mitochondrial Autophagy | KatG | Isoniazid | Inhibitor | inhibit | CAT | Bacterial | Autophagy |
| Inhibitors Related | Neomycin sulfate | Aceglutamide | Hemin | D(+)-Raffinose pentahydrate | Guanidine hydrochloride | Sulfamethoxazole sodium | Terbinafine hydrochloride | Hydroxychloroquine | Hyaluronic acid sodium (MW 20 kDa) | Dimethyl sulfoxide | Sodium diacetate | Sodium bicarbonate |
| Related Compound Libraries | Failed Clinical Trials Compound Library | Featured Novel Bioactive Compound Library | Pediatric Drug Library | Drug-induced Liver Injury (DILI) Compound Library | Drug Repurposing Compound Library | Drug-Fragment Library | Mitochondria-Targeted Compound Library | Anti-Bacterial Compound Library | FDA-Approved Drug Library | Anti-Cancer Approved Drug Library | Anti-Aging Compound Library | Anti-Cancer Drug Library |
United States
