Tubacin

Cat. No. M1742

Synonym:

Tubulin Acetylation Inducer

Size	Price	Availability
2mg	USD 150 USD150	In stock
5mg	USD 277 USD277	In stock
10mg	USD 500 USD500	In stock

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Quality Control & Documentation

Purity: >99%
COA
MSDS

Product Information

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.

Product Citations

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

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).

	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.

	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.

Protocol (for reference only)

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

Chemical Information

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

Conversion of different model animals based on BSA (PMID: 27057123)

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
K_m factor	3	6	12	8	5	20

Animal A (mg/kg) = Animal B (mg/kg) multiplied by	Animal B K_m
	Animal A K_m

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 K_m factor for a mouse and then divide by the K_m factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Aldana-Masangkay et al. Leuk Lymphoma. Tubacin suppresses proliferation and induces apoptosis of acute lymphoblastic leukemia cells.

[2] Namdar M et al. Proc Natl Acad Sci USA. Selective inhibition of histone deacetylase 6 (HDAC6) induces DNA damage and sensitizes transformed cells to anticancer agents.

[3] Kawada et al. J Biol Chem. Tubacin kills Epstein-Barr virus (EBV)-Burkitt lymphoma cells by inducing reactive oxygen species and EBV lymphoblastoid cells by inducing apoptosis.

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