research use only
Cat.No.S1937
| Related Targets | Dehydrogenase HSP Transferase P450 (e.g. CYP17) PDE phosphatase PPAR Vitamin Carbohydrate Metabolism Mitochondrial Metabolism |
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| Other Fatty Acid Synthase Inhibitors | Denifanstat (TVB-2640) Fatostatin TVB-3664 C75 Betulin FT113 C75 trans Desoxyrhaponticin Sodium palmitate Praeruptorin B |
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In vitro |
DMSO
: 27 mg/mL
(196.87 mM)
Water : 27 mg/mL Ethanol : 27 mg/mL |
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In vivo |
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| Molecular Weight | 137.14 | Formula | C6H7N3O |
Storage (From the date of receipt) | |
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| CAS No. | 54-85-3 | Download SDF | Storage of Stock Solutions |
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| Synonyms | N/A | Smiles | C1=CN=CC=C1C(=O)NN | ||
| 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. This compound upregulates the expression of an operon containing five FAS II components, including kasA and acpM. It results in the accumulation of ACP-bound lipid precursors to mycolic acids that are 26 carbons long and fully saturated. This chemical enters the mycobacterial cell by passive diffusion. It 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. The agent 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. It 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.
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| 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. This compound decreases liver and kidney 20-HETE content to 34% and 15.6% of control, respectively, without significantly altering tissue 19-HETE concentration.
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References |
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(data from https://clinicaltrials.gov, updated on 2024-05-22)
| 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 |
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