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    Tubacin (tubulin acetylation inducer)
    Tubacin (tubulin acetylation inducer)

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V0286
    CAS #: 537049-40-4Purity ≥98%

    Description: Tubacin (known also as tubulin acetylation inducer) is a specific HDAC6 (histone deacetylase 6) inhibitor with potential anticancer activity. It inhibits HDAC6 with IC50 of 4 nM in a cell-free assay, and exhibits ~350-fold higher selectivity for HDAC6 over HDAC1.

    References: J Am Chem Soc. 2010 Aug 11;132(31):10842-6; Proc Natl Acad Sci U S A. 2003 Apr 15;100(8):4389-94; Protein Cell. 2011 Feb;2(2):150-60.

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    Molecular Weight (MW)721.86
    FormulaC41H43N3O7S
    CAS No.537049-40-4
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 100 mg/mL (138.5 mM)
    Water: <1 mg/mL
    Ethanol: <1 mg/mL
    Solubility (In vivo)2% DMSO+30% PEG 300+5% Tween 80+ddH2O: 10 mg/mL  
    Synonyms

    Tubacin; tubulin acetylation inducer.

    Chemical Name: N1-(4-((2R,4R,6S)-4-(((4,5-diphenyloxazol-2-yl)thio)methyl)-6-(4-(hydroxymethyl)phenyl)-1,3-dioxan-2-yl)phenyl)-N8-hydroxyoctanediamide

    InChi Key: BHUZLJOUHMBZQY-YXQOSMAKSA-N

    InChi Code: InChI=1S/C41H43N3O7S/c45-26-28-17-19-29(20-18-28)35-25-34(27-52-41-43-38(30-11-5-3-6-12-30)39(51-41)31-13-7-4-8-14-31)49-40(50-35)32-21-23-33(24-22-32)42-36(46)15-9-1-2-10-16-37(47)44-48/h3-8,11-14,17-24,34-35,40,45,48H,1-2,9-10,15-16,25-27H2,(H,42,46)(H,44,47)/t34-,35+,40+/m1/s1

    SMILES Code: O=C(NC1=CC=C([[email protected]@H]2O[[email protected]](C3=CC=C(CO)C=C3)C[[email protected]](CSC4=NC(C5=CC=CC=C5)=C(C6=CC=CC=C6)O4)O2)C=C1)CCCCCCC(NO)=O


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    In Vitro

    In vitro activity: 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.


    Kinase 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: 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. Cell lines used: Drug-sensitive (MM.1S, U266, INA-6, and RPMI8226) and drug-resistant (RPMI-LR5 and RPMI-Dox40) MM cell lines

    In VivoIn 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.
    Animal modelMice
    Formulation & DosageN/A
    References

    J Am Chem Soc. 2010 Aug 11;132(31):10842-6; Proc Natl Acad Sci U S A. 2003 Apr 15;100(8):4389-94; Protein Cell. 2011 Feb;2(2):150-60.


    These protocols are for reference only. InvivoChem does not independently validate these methods.

     

    Tubacin

    Inhibition of HDAC6 deacetylase activity by tubacin. Proc Natl Acad Sci U S A. 2003 Apr 15;100(8):4389-94.
     

    Tubacin

    Phenotypic effects of tubacin. Proc Natl Acad Sci U S A. 2003 Apr 15;100(8):4389-94.
     

    Tubacin

    Characterization of tubacin, an inhibitor of α-tubulin deacetylation. Proc Natl Acad Sci U S A. 2003 Apr 15;100(8):4389-94. 


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