Tubacin

Catalog No.S2239

Tubacin is a highly potent and selective, reversible, cell-permeable HDAC6 inhibitor with an IC50 of 4 nM in a cell-free assay, approximately 350-fold selectivity over HDAC1.

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Tubacin Chemical Structure

Tubacin Chemical Structure
Molecular Weight: 721.86

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Product Description

Biological Activity

Description Tubacin is a highly potent and selective, reversible, cell-permeable HDAC6 inhibitor with an IC50 of 4 nM in a cell-free assay, approximately 350-fold selectivity over HDAC1.
Targets HDAC6 [1]
(Cell-free assay)
IC50 4 nM
In vitro Tubacin, without directly stabilizing microtubules, induces an increase in α-tubulin acetylation with EC50 of 2.5 μM in A549 cells. Tubacin inhibits HDAC6-mediated α-tubulin deacetylation, and inhibits the migration of both wild-type and HDAC6-overexpressing cells. [2] Tubacin, in combination with paclitaxel, synergistically enhances tubulin acetylation. [3] Tubacin significantly inhibits both drug-sensitive and drug–resistant MM cell growth with IC50 of 5–20 μM, and induces cell apoptosis by activation of caspases. [4]
In vivo In chick embryos, inhibition of HDAC6 activity by Tubacin reduces the formation of new blood vessels in matrigel/nylon mesh. In angioreactors implanted in mice, Tubacin also impairs the formation of new blood vessels. [5]
Features The first known selective inhibitor of α-tubulin deacetylation.

Protocol(Only for Reference)

Kinase Assay: [1]

Enzyme Inhibition Assay Enzyme inhibition assays are performed using the Reaction Biology HDAC Spectrum platform. The HDAC1, 2, 4, 5, 6, 7, 8, 9, 10, and 11 assays used isolated recombinant human protein; HDAC3/NcoR2 complex is used for the HDAC3 assay. Substrate for HDAC1, 2, 3, 6, 10, and 11 assays is a fluorogenic peptide from p53 residues 379-382 (RHKKAc); substrate for HDAC8 is fluorogenic diacyl peptide based on residues 379-382 of p53 (RHKAcKAc). Acetyl-Lys(trifluoroacetyl)-AMC substrate is used for HDAC4, 5, 7, and 9 assays. Compounds are dissolved in DMSO and tested in 10-dose IC50 mode with 3-fold serial dilution starting at 30 μM. Control Compound Trichostatin A (TSA) is tested in a 10-dose IC50 with 3-fold serial dilution starting at 5 μM. IC50 values are extracted by curve-fitting the dose/response slopes.

Cell Assay: [4]

Cell lines Drug-sensitive (MM.1S, U266, INA-6, and RPMI8226) and drug-resistant (RPMI-LR5 and RPMI-Dox40) MM cell lines
Concentrations ~20 μM
Incubation Time 72 hours
Method The inhibitory effect of bortezomib and/or tubacin on MM cell growth is assessed by measuring 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide (MTT) dye absorbance. All experiments are performed in quadruplicate.

Animal Study: [5]

Animal Models Athymic nude mice implanted with angioreactors
Formulation DMSO
Dosages
Administration Tubacin is filled in semiclosed angioreactors, and then implanted into the mice.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDog
Weight (kg)0.020.151.80.40.0810
Body Surface Area (m2)0.0070.0250.150.050.020.5
Km factor36128520
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.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

References

[1] Butler KV, et al. J Am Chem Soc. 2010, 132(31), 10842-0846.

[2] Haggarty SJ, et al. Proc Natl Acad Sci U S A. 2003, 100(8), 4389-4394.

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Chemical Information

Molecular Weight (MW) 721.86
Formula

C41H43N3O7S

CAS No. 537049-40-4
Storage 3 years -20℃powder
6 months-80℃in solvent
Synonyms N/A
Solubility (25°C) * In vitro DMSO 100 mg/mL (138.53 mM)
Water <1 mg/mL (<1 mM)
Ethanol <1 mg/mL (<1 mM)
In vivo 2% DMSO+30% PEG 300+5% Tween 80+ddH2O 10mg/mL
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
Chemical Name N1-(4-((2R,4R,6S)-4-((4,5-diphenyloxazol-2-ylthio)methyl)-6-(4-(hydroxymethyl)phenyl)-1,3-dioxan-2-yl)phenyl)-N8-hydroxyoctanediamide

Customer Product Validation(1)


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Source Nat Biotechnol, 2015, 33(4): 415-23 . Tubacin purchased from Selleck
Method Western Blot
Cell Lines MEF cells
Concentrations 10 µM
Incubation Time 16 h
Results HDAC6-regulated acetylation changes correlated with those caused by tubacin and bufexamac treatment.

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Tel: +1-832-582-8158 Ext:3

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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