Naph-Se-TMZ
Naph-Se-TMZ is a PROTAC-like HDAC1 degrader. Naph-Se-TMZ induces ROS-dependent reduction in HDAC1 protein expression and total HDAC activity, and decreases cell viability in a dose-dependent manner. Naph-Se-TMZ exhibits activity in both TMZ-sensitive and TMZ-resistant glioma cells, and its cytotoxicity is reversed by the ROS scavenger N-acetylcysteine (HY-B0215). Naph-Se-TMZ can be used in studies related to glioblastoma.
Naph-Se-TMZ consists of a target protein ligand (red segment): Temozolomide (HY-17364), a DNA intercalator (blue segment): Nitro-Naphthalimide-C2-acylamide (HY-169437), and a molecular linker (black segment). Meanwhile, the activity control for the target protein ligand is Temozolomide-amino hydrochloride (HY-169439), and the DNA intercalator+linker is NNISC-2 (HY-169438).
(Pink: HDAC and HDAC1 ligand (HY-17364); Blue: DNA Alkylator/Crosslinker ligand (HY-169437); Black: linker).
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Formel: C21H16N10O6Se
- Molecular Weight:583.38
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
Beschreibung
Naph-Se-TMZ consists of a target protein ligand (red segment): Temozolomide (HY-17364), a DNA intercalator (blue segment): Nitro-Naphthalimide-C2-acylamide (HY-169437), and a molecular linker (black segment). Meanwhile, the activity control for the target protein ligand is Temozolomide-amino hydrochloride (HY-169439), and the DNA intercalator+linker is NNISC-2 (HY-169438). (Pink: HDAC and HDAC1 ligand (HY-17364); Blue: DNA Alkylator/Crosslinker ligand (HY-169437); Black: linker).
IC50 & Target
[1]|
HDAC1 |
In Vitro
Naph-Se-TMZ exhibits stronger binding affinity for human HDAC1 protein than TMZ or Vorinostat, and its interaction targets key residues in the catalytic channel of HDAC1[1].
Naph-Se-TMZ (96 h) reduces the HDAC1 protein level in TMZ-sensitive human glioma A172 cells, and this effect is reversed by the ROS scavenger NAC[1].
Naph-Se-TMZ (96 h) inhibits the total activity of class I/II HDACs in human TMZ-sensitive glioma A172 cells, and this effect is mediated in a ROS-dependent manner[1].
Naph-Se-TMZ (75-300 μM; 96 h) dose-dependently increases intracellular ROS levels in TMZ-sensitive human glioma A172 cells, and this effect can be partially reversed by the ROS scavenger NAC[1].
Naph-Se-TMZ (75-300 μM; 96 h) reduces the viability of human temozolomide (TMZ)-sensitive glioma A172 cells and human TMZ-resistant glioma LN18 cells in a dose-dependent manner, and this cytotoxic effect is mediated in a ROS-dependent manner[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:human TMZ-sensitive glioma A172 cells, human TMZ-resistant glioma LN18 cells
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Concentration:75 μM; 150 μM; 300 μM
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Incubation Time:96 h
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Result:Reduced cell viability by 20%, 40%, and 70% respectively at 75 μM, 150 μM, and 300 μM in A172 cells compared to control.
Reduced cell viability in a dose-dependent manner in LN18 cells compared to control.
Co-treatment with NAC significantly reversed the reduced cell viability induced by Naph-Se-TMZ alone in both cell lines.
- RNA extraction experimental
- Western Blot
- Cell Cytotoxicity Assay
- Mammalian live/dead viability and cytotoxicity staining
- ROS/oxidative-stress fluorescent staining
- CCK-8/WST-8 Cell Proliferation Assay
- MTT Cell Proliferation Assay
- Protocol For Protein Expression And Purification
- Cell Viability Determination by MTT Colorimetric Assay
Chemical Information
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Molecular Weight 583.38
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Formel C21H16N10O6Se
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SMILES
[Se]=C(NNC(C1=C2N(C(N(C)N=N2)=O)C=N1)=O)NCCN(C(C3=C4C(C=C(C=C54)[N+]([O-])=O)=CC=C3)=O)C5=O
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Naph-Se-TMZ Related Classifications
HY-169433 Related Classifications
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