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Tubacin

Catalog No. T6327   CAS 537049-40-4

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

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.
Tubacin Chemical Structure
Tubacin, CAS 537049-40-4
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1 mg In stock $ 77.00
5 mg In stock $ 265.00
10 mg In stock $ 496.00
25 mg In stock $ 813.00
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1 mL * 10 mM (in DMSO) In stock $ 418.00
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Purity: 98.71%
Purity: 97.62%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Tubacin is a highly potent and selective, reversible, cell-permeable HDAC6 inhibitor with an IC50 of 4 nM, approximately 350-fold selectivity over HDAC1.
Targets&IC50 HDAC6(Cell-free assay):4nM
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. Tubacin, in combination with paclitaxel, synergistically enhances tubulin acetylation. 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.
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.
Kinase Assay 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 Research 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 Research Animal Models: Athymic nude mice implanted with angioreactorsFormulation: DMSODosages: --Administration: Tubacin is filled in semiclosed angioreactors, and then implanted into the mice.
Molecular Weight 721.86
Formula C41H43N3O7S
CAS No. 537049-40-4

Storage

store at low temperature

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 93 mg/mL (128.8 mM)

Ethanol: <1 mg/mL

H2O: <1 mg/mL

TargetMolReferences and Literature

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. 3. Marcus AI, et al. Cancer Res. 2005, 65(9), 3883-3893. 4. Hideshima T, et al. Proc Natl Acad Sci U S A. 2005, 102(24), 8567-8572. 5. Li D, et al. Protein Cell. 2011, 2(2), 150-160. 6. Lu CY, et al. Tubacin, an HDAC6 Selective Inhibitor, Reduces the Replication of the Japanese Encephalitis Virus via the Decrease of Viral RNA Synthesis. Int J Mol Sci. 2017 May 1;18(5).

TargetMolCitations

1. Wang C, Huang M, Lin Y, et al.ENO2-derived phosphoenolpyruvate functions as an endogenous inhibitor of HDAC1 and confers resistance to antiangiogenic therapy.Nature Metabolism.2023: 1-22.

Related compound libraries

This product is contained In the following compound libraries:
Chromatin Modification Compound Library

Related Products

Related compounds with same targets
HDAC6-IN-25 ITF3756 CHDI-390576 Tucidinostat Resminostat hydrochloride HDAC6-IN-24 HDAC6-IN-21 KPZ560

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Keywords

Tubacin 537049-40-4 Chromatin/Epigenetic DNA Damage/DNA Repair Microbiology/Virology Virus Protease HDAC Inhibitor inhibit Histone deacetylases inhibitor

 

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