All AbMole products are for research use only, cannot be used for human consumption.
Tubacin (Tubulin Acetylation Inducer) is a highly potent and selective, reversible cell-permeable inhibitor of HDAC6 with IC50 of 0.004µM. The IC50 for the other HDACs are 1000-fold higher, making tubacin both more selective and more potent than Tubastatin A, which also inhibits HDAC8. Concentration in cell culture experiments typically ranges from 2-50µM.
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.
Tubacin purchased from AbMole
. figure 9..jpg) |
Source | Mol. Cell. Biol. (2016). Figure 9. Tubacin and Niltubacin for animal studies were obtained from AbMole Bioscience Inc. (Houston, TX) |
| Method | BK-SS mice | |
| Cell Lines | ||
| Concentrations | 0.5mg/kg i.p. | |
| Incubation Time | 5 or 10 or 30 days | |
| Results | These drug regimens showed a time dependent reduction of PlGF (Fig. 9C) and ET-1 (Fig. 9D) in plasma, compared to Niltubacin. The 30 day drug treatment effectively reduced plasma levels of PlGF by ~60% (p <0.001, Fig. 9C) and plasma levels of ET-1 by ~60% (p<0.001, Fig. 9D). |
. figure 7..jpg) |
Source | Mol. Cell. Biol. (2016). Figure 7. Tubacin and Niltubacin for animal studies were obtained from AbMole Bioscience Inc. (Houston, TX) |
| Method | FAIRE-qPCR | |
| Cell Lines | HMEC-1 cells | |
| Concentrations | 5 µM | |
| Incubation Time | 30 min | |
| Results | Taken together, these data showed PlGF induced chromatin condensation to repress DNM3os transcription, while Tubacin prevented the repressive effect following PlGF signaling. |
. figure 6..jpg) |
Source | Mol. Cell. Biol. (2016). Figure 6. Tubacin and Niltubacin for animal studies were obtained from AbMole Bioscience Inc. (Houston, TX) |
| Method | qRT-PCR and reporter luciferase activity | |
| Cell Lines | HMEC-1 cells | |
| Concentrations | 5 µM | |
| Incubation Time | 30 min | |
| Results | We concluded that HDAC6 required functional ATF3 binding sites in the DNM3os promoter and any antagonism of PlGF effects by Tubacin was not due to a general effect on transcription of the endogenous DNM3os gene or the wt DNM3os reporter construct. |
| Cell Experiment | |
|---|---|
| Cell lines | ALL cells and normal T lymphocytes |
| Preparation method | Growth inhibition assay The inhibitory effect of tubacin on ALL cells and normal T lymphocytes was assessed by colorimetric assay, 3-(4,5-dimethylthiazol-e-yl)- 2,5-diphenyl tetrazolium bromide (MTT; AbMole). Only active mitochondria dehydrogenase enzymes can perform cleavage of a tetrazolium ring, and therefore the amount of purple formazan generated by cells with a drug was compared with the amount of formazan produced from non-treated cells. Absorbance readings at a wavelength of 550 nm were taken on a spectrophotometer. Cells from 72 h cultures were incubated with 10 μL of 5 mg/mL MTT for 2 h, followed by 100 μL isopropanol that contained 0.1 N HCl. Normal T lymphocytes were incubated with MTT for 30–37 min. All experiments were performed in triplicate. |
| Concentrations | 0, 0.5, 1, 1.5, 2, 2.5µM |
| Incubation time | 72 h |
| Animal Experiment | |
|---|---|
| Animal models | Xenograft system of primary leukemia samples |
| Formulation | saline |
| Dosages | 50 mg/kg/day |
| Administration | intraperitoneally |
| Molecular Weight | 721.86 |
| Formula | C41H43N3O7S |
| CAS Number | 537049-40-4 |
| Solubility (25°C) | DMSO 90 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
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| Givinostat hydrochloride monohydrate
ITF2357 (Givinostat, Gavinostat) is a histone deacetylase inhibitor. The IC50 values for maize HDAC preparations HD2, HD-1B and HD-1A are 10, 7.5 and 16 nM respectively. |
| Niltubacin
Niltubacin, as an inactive derivative of Tubacin, is a highly potent and selective, reversible cell-permeable inhibitor of HDAC6. |
All AbMole products are for research use only, cannot be used for human consumption or veterinary use. We do not provide products or services to individuals. Please comply with the intended use and do not use AbMole products for any other purpose.
Products are for research use only. Not for human use. We do not sell to patients.
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