Tubacin

Catalog No.S2239 Batch:S223901

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Technical Data

Formula

C41H43N3O7S
Molecular Weight 721.86 CAS No. 537049-40-4
Solubility (25°C)* In vitro DMSO 100 mg/mL (138.53 mM)
Water Insoluble
Ethanol Insoluble
* <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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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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. Tubacin reduces the replication of the Japanese Encephalitis Virus via the decrease of viral RNA synthesis.
Targets
HDAC6 [1]
(Cell-free assay)
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 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 (from 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 on MM cell growth is assessed by measuring the MTT dye absorbance. All experiments are performed in quadruplicate.
Animal Study:

[5]
  • Animal Models

    Athymic nude mice implanted with angioreactors

  • Dosages

    --

  • Administration

    Tubacin is filled in semiclosed angioreactors, and then implanted into the mice.

Customer Product Validation

Data from [Data independently produced by , , Nat Biotechnol, 2015, 33(4): 415-23 ]

Data from [Data independently produced by , , Oncogene, 2016, 35(18):2333-44]

Data from [Data independently produced by , , J Biol Chem, 2016, 291(10):5396-405]

Selleck's Tubacin has been cited by 35 publications

Inhibition of HDAC activity directly reprograms murine embryonic stem cells to trophoblast stem cells [ Dev Cell, 2024, S1534-5807(24)00326-5] PubMed: 38823394
Selective inhibition of HDAC6 promotes bladder cancer radiosensitization and mitigates the radiation-induced CXCL1 signalling [ Br J Cancer, 2023, 10.1038/s41416-023-02195-0] PubMed: 36810912
Selectivity of Hydroxamate- and Difluoromethyloxadiazole-Based Inhibitors of Histone Deacetylase 6 In Vitro and in Cells [ Int J Mol Sci, 2023, 24(5)4720] PubMed: 36902164
MicroRNA-22 represses glioma development via activation of macrophage-mediated innate and adaptive immune responses [ Oncogene, 2022, 10.1038/s41388-022-02236-7] PubMed: 35279703
Dual Blockade of Misfolded Alpha-Sarcoglycan Degradation by Bortezomib and Givinostat Combination [ Front Pharmacol, 2022, 13:856804] PubMed: 35571097
Dual Blockade of Misfolded Alpha-Sarcoglycan Degradation by Bortezomib and Givinostat Combination [ Front Pharmacol, 2022, 13:856804] PubMed: 35571097
Hypoxia Selectively Increases a SMAD3 Signaling Axis to Promote Cancer Cell Invasion [ Cancers (Basel), 2022, 14(11)2751] PubMed: 35681731
Targeting cancer cell plasticity by HDAC inhibition to reverse EBV-induced dedifferentiation in nasopharyngeal carcinoma [ Signal Transduct Target Ther, 2021, 6(1):333] PubMed: 34482361
A protocol to visualize cytosolic aggresome-like bodies using confocal microscopy [ STAR Protoc, 2021, 2(3):100674] PubMed: 34337443
Protein acetylation derepresses Serotonin Synthesis to potentiate Pancreatic Beta-Cell Function through HDAC1-PKA-Tph1 signaling [ Theranostics, 2020, 10(16):7351-7368] PubMed: 32641996

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.