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    Tubastatin A (TubA, AG-CR1-3900)
    Tubastatin A (TubA, AG-CR1-3900)

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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 #: V0275
    CAS #: 1252003-15-8Purity ≥98%

    Description: Tubastatin A (TubA, AG-CR13900), a tubacin derivative, is a potent and selective HDAC6 (Histone deacetylase 6) inhibitor (IC50 = 15 nM in a cell-free assay) with potential anticancer  and anti-inflammatory activity. It demonstrated the highest selectivity of over 1,000-fold for HDAC6 over other HDAC isoforms (excluding HDAC8 for which the IC50 is 0.9 μM). 

    References: Cancer Res. 2013 Apr 1;73(7):2259-70; Int Immunopharmacol. 2013 May;16(1):72-8; Blood. 2012 Mar 15;119(11):2579-89.

    Related CAS #: 1252003-15-8 (free base); 1310693-92-5 (HCl)


    Publications Citing Use of InvivoChem Tubastatin A HClScientific Reports | (2020) 10:6064 | https://doi.org/10.1038/s41598-020-62678-5


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    Molecular Weight (MW)335.4
    FormulaC20H21N3O2
    CAS No.1252003-15-8
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 67 mg/mL (199.8 mM)
    Water: <1 mg/mL
    Ethanol: <1 mg/mL
    Solubility (In vivo) 4% DMSO+30% PEG 300: 5mg/mL
    Synonyms

    Tubastatin A hydrochloride; Tubastatin A HCl; TSA HCl; Tubastatin A; TubA, AG-CR1-3900

    Chemical Name: N-hydroxy-4-((2-methyl-3,4-dihydro-1H-pyrido[4,3-b]indol-5(2H)-yl)methyl)benzamide

    InChi Key: GOVYBPLHWIEHEJ-UHFFFAOYSA-N

    InChi Code: InChI=1S/C20H21N3O2/c1-22-11-10-19-17(13-22)16-4-2-3-5-18(16)23(19)12-14-6-8-15(9-7-14)20(24)21-25/h2-9,25H,10-13H2,1H3,(H,21,24)

    SMILES Code: O=C(NO)C1=CC=C(CN2C3=C(CN(C)CC3)C4=C2C=CC=C4)C=C1


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    In Vitro

    In vitro activity: Tubastatin A is selective at all isozymes except HDAC8 and maintains over 1000-fold selectivity against all isoforms excluding HDAC8, where it has approximately 57-fold selectivity. Tubastatin A preferentially induces α-tubulin hyperacetylation at 2.5 μM. Slight induction of histone hyperacetylation is seen for Tubastatin A at 10 μM. Tubastatin A displays dose-dependent protection against homocysteic acid-induced neuronal cell death starting at 5 μM with near complete protection at 10 μM. Tubastatin A (10 μM) induces an increase in acetylated-α-tubulin levels and the restoration of primary cilia expression in the cholangiocarcinoma cell lines (18-fold); and the restoration of primary cilia correlated with downregulated Hedgehog (Hh) and MAPK signaling pathways, as well as decreased cell proliferation rates (in average by 50%) and invasion (by 40%). Tubastatin A shows significant inhibition of TNF-α and IL-6 in LPS stimulated human THP-1 macrophages with an IC50 of 272 nM and 712 nM. Tubastatin A inhibits nitric oxide (NO) secretion in murine Raw 264.7 macrophages dose depenndently with an IC50 of 4.2 μM.


    Kinase Assay: Tubastatin A is dissolved and diluted in assay buffer (50 mM HEPES, pH 7.4, 100 mM KCl, 0.001% Tween-20, 0.05% BSA, and 20 μM tris(2-carboxyethyl)phosphine) to 6-fold of the final concentration. HDAC enzymes are diluted to 1.5-fold of the final concentration in assay buffer and pre-incubated with Tubastatin A for 10 minutes before the addition of the substrate. The amount of FTS (HDAC1, HDAC2, HDAC3, and HDAC6) or MAZ-1675 (HDAC4, HDAC5, HDAC7, HDAC8, and HDAC9) used for each enzyme is equal to the Michaelis constant (Km), as determined by a titration curve. FTS or MAZ-1675 is diluted in assay buffer to 6-fold the final concentration with 0.3 μM sequencing grade trypsin. The substrate/trypsin mix is added to the enzyme/compound mix and the plate is shaken for 60 seconds and then placed into a SpectraMax M5 microtiter plate reader. The enzymatic reaction is monitored for release of 7-amino-4-methoxy-coumarin over 30 minutes, after deacetylation of the lysine side chain in the peptide substrate, and the linear rate of the reaction is calculated.


    Cell Assay: Anchorage-independent growth is assessed by growing cells in soft agar. About 25,000 cells suspended in 0.4% agar in culture media are layered over a 1% agar layer in a 6-well plate. Media are added twice a week and pictures are taken after 21 days of incubation. The number and size of colonies are analyzed using the Gel-Pro software.

    In VivoTubastatin A reduces the growth of cholangiocarcinoma in vivo. Tubastatin A (10 mg/kg) induces a 6-fold lower mean tumor weights in syngeneic rat orthotopic model of cholangiocarcinoma, and reduction of the ratios of tumor weight to liver weight and body weight (5- and 5.6-fold, respectively), as well as a greater frequency of ciliated cholangiocytes compared with controls (29% vs 1.4%). Tubastatin A significantly decreases the amount of PCNA-positive cells in the treated tumors compared with vehicle controls (34% vs 65%). Tubastat A shows significant inhibition of paw volume at 30 mg/kg i.p. in a Freund's complete adjuvant (FCA) induced animal model of inflammation. Tubastat A (30 mg/kg i.p.) significant attenuates clinical scores (~ 70%), and IL-6 expression in paw tissues of collagen induced arthritis DBA1 mouse.
    Animal modelWistar rats; DBA1 mice
    Formulation & DosageSolubilized in 10% Dimethyl sulfoxide (DMSO) 10% Polyethylene glycol (PEG) 400 and 80% (40% of hydroxy propyl beta cyclodextrin); Rats: 30 mg/kg/day i.p. for 5 days; mice: 30 mg/kg, q.d. from day 21 to day 36.
    References

    Cancer Res. 2013 Apr 1;73(7):2259-70; Int Immunopharmacol. 2013 May;16(1):72-8; Blood. 2012 Mar 15;119(11):2579-89.


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

     

    Tubastatin A

     

    Tubastatin A

     

    Tubastatin A


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