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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研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 98.79%
- CAS 番号: 1377239-83-2
- 分子式: C20H23F3N4O3S
- 分子量:456.48
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
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MedChemExpress（MCE）の使用を引用している文献 Macozinone
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生物活性
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 |
化学情報
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CAS 番号 1377239-83-2
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性状 Solid
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分子量 456.48
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分子式 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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別名
PBTZ169
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
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
溶剤 & 溶解度
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.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
純度とドキュメンテーション
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データシート (272 KB)
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SDS (393 KB)
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- 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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取扱説明書 (2659 KB)
参考文献
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 関連分類
HY-12903 関連分類
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