Macozinone
Based on 5 publication(s) in Google Scholar
Macozinone (PBTZ169) is a bactericidal benzothiazinone and a potent DprE1 (decaprenylphosphoryl-β-d-ribose 2′-oxidase) inhibitor. Macozinone inhibits the essential flavoprotein DprE1 by forming a covalent bond with the active-site Cys387 residue. Macozinone has antituberculosis effect.
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- Pureza: 98.79%
- No. CAS: 1377239-83-2
- Fòrmula: C20H23F3N4O3S
- Peso molecular:456.48
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
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- Referencias
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Publications Citing Use of MedChemExpress (MCE) Macozinone
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Actividad biológica
DprE1[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | IC50 |
101.7 μM
Compound: PBTZ169
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Inhibition of human ERG transfected in HEK293 cells by whole-cell patch clamp method
Inhibition of human ERG transfected in HEK293 cells by whole-cell patch clamp method
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[PMID: 31408806] |
| HeLa | CC50 |
>1.1 x 102μM
Compound: 23
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Cytotoxicity against human HeLa cells assessed as cytolytic effect incubated for 72 hrs by methylene blue staining based colorimetric analysis
Cytotoxicity against human HeLa cells assessed as cytolytic effect incubated for 72 hrs by methylene blue staining based colorimetric analysis
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[PMID: 38071794] |
| HepG2 | IC50 |
18.98 μg/mL
Compound: 2; PBTZ169
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Cytotoxicity against human HepG2 cells assessed as reduction in cell viability after 48 hrs by MTT assay
Cytotoxicity against human HepG2 cells assessed as reduction in cell viability after 48 hrs by MTT assay
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[PMID: 30336450] |
| THP-1 | CC50 |
>64 μg/mL
Compound: PBTZ169
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Cytotoxicity against human THP-1 cells incubated for 48 hrs by MTS/PMS assay
Cytotoxicity against human THP-1 cells incubated for 48 hrs by MTS/PMS assay
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[PMID: 37300914] |
| Vero | CC50 |
>125 μM
Compound: PBTZ169
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Cytotoxicity against African green monkey Vero cells after 72 hrs by MTT assay
Cytotoxicity against African green monkey Vero cells after 72 hrs by MTT assay
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[PMID: 25754492] |
| Vero | CC50 |
>64 μg/mL
Compound: PBTZ169
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Cytotoxicity against African green monkey Vero cells incubated for 72 hrs by MTT assay
Cytotoxicity against African green monkey Vero cells incubated for 72 hrs by MTT assay
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[PMID: 33823392] |
| Vero | CC50 |
>64 μg/mL
Compound: PBTZ169
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Cytotoxicity against African green monkey Vero cells assessed as reduction in cell viability
Cytotoxicity against African green monkey Vero cells assessed as reduction in cell viability
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[PMID: 31408806] |
| Vero | CC50 |
>64 μg/mL
Compound: PBTZ169
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Cytotoxicity against African green monkey Vero cells
Cytotoxicity against African green monkey Vero cells
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[PMID: 32460114] |
| Vero | CC50 |
1402.82 μM
Compound: PBTZ169
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Cytotoxicity against African green monkey Vero cells assessed as cell viability after 72 hrs by MTT assay
Cytotoxicity against African green monkey Vero cells assessed as cell viability after 72 hrs by MTT assay
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[PMID: 28626525] |
| Vero | CC50 |
31 μg/mL
Compound: PBTZ169
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Cytotoxicity against African green monkey Vero cells assessed as reduction in cell viability after 72 hrs by MTT assay
Cytotoxicity against African green monkey Vero cells assessed as reduction in cell viability after 72 hrs by MTT assay
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[PMID: 30692025] |
| Vero | IC50 |
>64 μg/mL
Compound: 2; PBTZ169
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Cytotoxicity against African green monkey Vero cells assessed as reduction in cell viability after 48 hrs by MTT assay
Cytotoxicity against African green monkey Vero cells assessed as reduction in cell viability after 48 hrs by MTT assay
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[PMID: 30336450] |
Macozinone (PBTZ169) is highly potent against M. tuberculosis in vitro, ex vivo, and in vivo[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 1377239-83-2
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Appearance Solid
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Peso molecular 456.48
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Fòrmula C20H23F3N4O3S
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Color Light yellow to yellow
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SMILES
O=C1C2=CC(C(F)(F)F)=CC([N+]([O-])=O)=C2SC(N3CCN(CC4CCCCC4)CC3)=N1
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Synonyms
PBTZ169
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (5)
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Journal Impact Factor
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Most Recent
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J Med Chem
Discovery of N-(1-(6-Oxo-1,6-dihydropyrimidine)-pyrazole) Acetamide Derivatives as Novel Noncovalent DprE1 Inhibitors against Mycobacterium tuberculosis. [Abstract]2024 Feb 8;67(3):1914-1931. PMID: 38232131 -
Antimicrob Agents Chemother
Heterologous Expression of ethA and katG in Mycobacterium marinum Enables the Rapid Identification of New Prodrugs Active against Mycobacterium tuberculosis. [Abstract]2021 Mar 18;65(4):e01445-20. PMID: 33495223 -
Dis Model Mech
An anti-tuberculosis compound screen using a zebrafish infection model identifies an aspartyl-tRNA synthetase inhibitor. [Abstract]2021 Dec 1;14(12):dmm049145. PMID: 34643222 -
J Pharm Biomed Anal
Characterization of degradation products of Macozinone by LC-MS/MS and elucidation of their degradation pathway. [Abstract]2022 Sep 20:219:114865. PMID: 35716420 -
bioRxiv
Structural and functional analysis of the Mycobacterium tuberculosis MmpS5L5 efflux pump presages a pathway to increased bedaquiline resistance. [Abstract]2025 Jun 24:2025.06.24.661325. PMID: 40667120
Solvente y solubilidad
DMSO : 6.4 mg/mL (14.02 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Pureza y Documentación
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Ficha de datos (272 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instrucciones de manejo (2659 KB)
Referencias
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.1907 mL | 10.9534 mL | 21.9068 mL | 54.7669 mL |
| 5 mM | 0.4381 mL | 2.1907 mL | 4.3814 mL | 10.9534 mL | |
| 10 mM | 0.2191 mL | 1.0953 mL | 2.1907 mL | 5.4767 mL |
Macozinone Related Classifications
HY-12903 Related Classifications
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