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Formula | C6H7N3O |
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Molecular Weight | 137.14 | CAS No. | 54-85-3 | |
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) | |||
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.) |
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. |
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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] |
Repurposing Tamoxifen as Potential Host-Directed Therapeutic for Tuberculosis [ mBio, 2022, e0302422.] | PubMed: 36475748 |
Pharmacological inhibition of fatty acid synthesis blocks SARS-CoV-2 replication [ Nat Metab, 2021, 10.1038/s42255-021-00479-4] | PubMed: 34580494 |
Pharmacological Poly (ADP-Ribose) Polymerase Inhibitors Decrease Mycobacterium tuberculosis Survival in Human Macrophages [ Front Immunol, 2021, 12:712021] | PubMed: 34899683 |
Pharmacological Poly (ADP-Ribose) Polymerase Inhibitors Decrease Mycobacterium tuberculosis Survival in Human Macrophages [ Front Immunol, 2021, 12:712021] | PubMed: 34899683 |
Repurposing diphenylbutylpiperidine-class antipsychotic drugs for host-directed therapy of Mycobacterium tuberculosis and Salmonella enterica infections [ Sci Rep, 2021, 11(1):19634] | PubMed: 34608194 |
Enniatin A1, A Natural Compound with Bactericidal Activity against Mycobacterium tuberculosis In Vitro. [ Molecules, 2019, 25(1)] | PubMed: 31861925 |
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SHIPPING AND STORAGE
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