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Tubacin

Cat. No. M1742
Tubacin Structure
Synonym:

Tubulin Acetylation Inducer

Size Price Availability Quantity
1mg USD 80 In stock
5mg USD 280 In stock
10mg USD 480 In stock
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Quality Control
Biological Activity

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.

Protocol
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; Sigma). 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 (Titertek Multiskan MCC Type 341). 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
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
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 resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 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 resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 721.86
Formula C41H43N3O7S
CAS Number 537049-40-4
Purity 100.00%
Solubility DMSO
Storage at -20°C
Customer Product Validations & Biological Datas
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).
Rating
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.
Rating
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.
Rating
Product Citations
References

Tubacin suppresses proliferation and induces apoptosis of acute lymphoblastic leukemia cells.
Aldana-Masangkay et al. Leuk Lymphoma. 2011 Aug;52(8):1544-55. PMID: 21699378.

Selective inhibition of histone deacetylase 6 (HDAC6) induces DNA damage and sensitizes transformed cells to anticancer agents.
Namdar M et al. Proc Natl Acad Sci USA. 2010 Nov 16;107(46):20003-8. PMID: 21037108.

Tubacin kills Epstein-Barr virus (EBV)-Burkitt lymphoma cells by inducing reactive oxygen species and EBV lymphoblastoid cells by inducing apoptosis.
Kawada et al. J Biol Chem. 2009 Jun 19;284(25):17102-9. PMID: 19386607.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: Tubacin, Tubulin Acetylation Inducer supplier, HDAC, inhibitors

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