Niltubacin, as an inactive derivative of Tubacinis, is a highly potent and selective, reversible cell-permeable inhibitor of HDAC6. Histone deacetylase 6 (HDAC6) is structurally and functionally unique among the 11 human zinc-dependent histone deacetylases. HDAC6-selective inhibitor tubacin significantly enhances cell death induced by the topoisomerase II inhibitors etoposide and doxorubicin and the pan-HDAC inhibitor SAHA (vorinostat) in transformed cells (LNCaP, MCF-7), an effect not observed in normal cells. The inactive analogue of tubacin, nil-tubacin, does not sensitize transformed cells to these anticancer agents.
EMBO J. 2019 Jan 15;38(2).
Prominin-1 controls stem cell activation by orchestrating ciliary dynamics.
Niltubacin purchased from AbMole
J Cell Biochem. 2017 Apr 27.
The HDAC6 Inhibitor Tubacin Induces Release of CD133þ Extracellular Vesicles From Cancer Cells
Niltubacin purchased from AbMole
Mol Cell Biol. 2016 Oct 28;36(22):2838-2854.
Activated Transcription Factor 3 in Association with Histone Deacetylase 6 Negatively Regulates MicroRNA 199a2 Transcription by Chromatin Remodeling and Reduces Endothelin-1 Expression.
Niltubacin purchased from AbMole
Cell Experiment | |
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Cell lines | Raji cells |
Preparation method | Cell adhesion assay Prior to SDF-1α (100 ng/ml) stimulation, Raji cells were treated with DMSO, NaB (1 μM), or tubacin (1 μM) for 3 hours. Then cells were plated into a 96-well plate which were precoated with Fibronectin (50 ng/ml) to allow cell adherence for 30 minutes. Subsequently cells were washed with PBS three times to remove the non-adherent cells, and adherent cells were measured by CellTiter-Glo luminescent cell viability assay kit. |
Concentrations | 1μM |
Incubation time | 3h |
Animal Experiment | |
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Animal models | PLD animal model 3-week-old PCK rats |
Formulation | saline |
Dosages | 30 mg/kg body |
Administration | intraperitoneally |
Molecular Weight | 706.85 |
Formula | C41H42N2O7S |
Solubility (25°C) | DMSO ≥5 mg/mL |
Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
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