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).
연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.
- 화학식: C21H16N10O6Se
- 분자량:583.38
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보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- 순도&문서
- References
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Biological Activity
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).
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HDAC1 |
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.
Chemical Information
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분자량 583.38
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화학식 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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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Naph-Se-TMZ Related Classifications
HY-169433 Related Classifications
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