Tubastatin A HCl

Catalog No.S2627

Tubastatin A HCl Chemical Structure

Molecular Weight(MW): 371.86

Tubastatin A HCl is a potent and selective HDAC6 inhibitor with IC50 of 15 nM in a cell-free assay. It is selective (1000-fold more) against all other isozymes except HDAC8 (57-fold more).

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3 Customer Reviews

  • Control and MEC17 KD macrophages (RAW264.7) were treated with TBSA or DMSO for 12 hours followed by LPS treatment for indicated time. p38 phosphorylation were determined by immuno-blotting.

    Nat Commun 2014 5, 3479. Tubastatin A HCl purchased from Selleck.

    Tubastatin A gefitinib-induced apoptosis in NSCLC cells via activation of AKT. H358 cells were treated as described in Figure 4. Representative immunoblots of cleaved caspase-3, AKT and ERK1/2 and of their respective phosphorylated forms are shown. Actin was used as a protein-level control.

    Int J Cancer 2014 134(11):2560-71. Tubastatin A HCl purchased from Selleck.

  • GH cells were treated with 0.5 μM TSA or the DMSO solvent as indicated. Subsequently, Chromatin immunoprecipitation (ChIP) was performed with antibodies to NF-YB or a pre-immune control antibody. The DNA corresponding to the indicated promoters was quantified by real-time PCR and displayed in relation to the amount of input DNA. Bars indicate the standard error from three independent experiments.

    Oncotarget, 2016, 7(23):33484-97. Tubastatin A HCl purchased from Selleck.

Purity & Quality Control

Choose Selective HDAC Inhibitors

Biological Activity

Description Tubastatin A HCl is a potent and selective HDAC6 inhibitor with IC50 of 15 nM in a cell-free assay. It is selective (1000-fold more) against all other isozymes except HDAC8 (57-fold more).
Targets
HDAC6 [1]
(Cell-free assay)
HDAC8 [1]
(Cell-free assay)
15 nM 854 nM
In vitro

Tubastatin A is substantially selective for all 11 HDAC isoforms and maintains over 1000-fold selectivity against all isoforms excluding HDAC8, where it has approximately 57-fold selectivity. In homocysteic acid (HCA) induced neurodegeneration assays, Tubastatin A displays dose-dependent protection against HCA-induced neuronal cell death starting at 5 μM with near complete protection at 10 μM. [1] At 100 ng/mL Tubastatin A increases Foxp3+ T-regulatory cells (Tregs) suppression of T cell proliferation in vitro. [2] Tubastatin A treatment in C2C12 cells would lead to myotube formation impairment when alpha-tubulin is hyperacetylated early in the myogenic process; however, myotube elongation occurs when alpha-tubulin is hyeperacetylated in myotubes. [3] A recent study indicates that Tubastatin A treatment increases cell elasticity as revealed by atomic force microscopy (AFM) tests without exerting drastic changes to the actin microfilament or microtubule networks in mouse ovarian cancer cell lines, MOSE-E and MOSE-L. [4]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
neuron cultures NH;oUlBMcW6jc3WgZZN{[Xl? M17yNFIvPSEQvF2= NF;ZRVBFVVOR NHHZ[lhqdmS3Y3XzJO6yNXS3YoXsbY4hcHmyZYLhZ4V1gWyjdHnvci=> NV\5VZdGOjB4MUS5N|Y>
neuron cultures MmXTSpVv[3Srb36gZZN{[Xl? MXr+NVAh|ryP MV7EUXNQ Mn3jdJJwfGWldIOgZYdicW6|dDDncJV1[XSqaX;u[UBl\XCuZYTpc44ucW6mdXPl[EBwgGmmYYTpeoUhe3S{ZYPz M{fkRVIxPjF2OUO2
134/04 MmnWSpVv[3Srb36gZZN{[Xl? MWK3MlUhyrWP M1\ZOolueGGrcoOgcZlwfHWkZTDmc5Ju[XSrb36= Mo\hNlIyPzR6M{m=
C2C12 NYTxd|JrTnWwY4Tpc44h[XO|YYm= M1vONlcvPSEEtV2= MkXIbY1x[Wm{czDtfY91fWKnIH\vdo1ifGmxbh?= Mn;hNlIyPzR6M{m=
HaCaT keratinocytes NYPLS2d6TnWwY4Tpc44h[XO|YYm= MnPKNVAh|ryP Ml\JZoxw[2u|IHHyd4VvcXSnIH\yc40hcW6mdXPpcochVnKoMjDwdo91\WmwIITyZY5{dGG2aX;u NHzqXGgzOjN4N{[4PS=>
JURL-MK1 MkLwSpVv[3Srb36gZZN{[Xl? M1LwelExKM7:TR?= M3H2WYVvcGGwY3XzJINmdGxiYXTo[ZNqfmm2eTD0c{BncWK{b37lZ5Rqdg>? NGnzNWIzOzB{MkW4Ny=>
CML-T1 NEeyUXRHfW6ldHnvckBie3OjeR?= M4fCXlExKM7:TR?= NFPV[3ZmdmijbnPld{Bk\WyuIHHkbIV{cX[rdImgeI8h\mmkcn;u[YN1cW5? MUWyN|AzOjV6Mx?=
K562 M2rZOGZ2dmO2aX;uJIF{e2G7 NGrrW2oyOCEQvF2= M1H2VYVvcGGwY3XzJINmdGxiYXTo[ZNqfmm2eTD0c{BncWK{b37lZ5Rqdg>? NHrEfXQzOzB{MkW4Ny=>
HL-60 MV\GeY5kfGmxbjDhd5NigQ>? NIrrZmUyOCEQvF2= NWHzeo5T\W6qYX7j[ZMh[2WubDDh[Ihme2m4aYT5JJRwKG[rYoLvcoVkfGmw M4DITlI{ODJ{NUiz
KMCH MXLHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NGLHd3V,OTBizszN MnT5[IVkemWjc3XzJJBzd2yrZnXyZZRqd25iYX7kJIFv[2ixcnHn[U1qdmSncHXu[IVvfCCpcn;3eIg> MXmyN|M4ODN{Nx?=
THP-1 NUOzeY9[TnWwY4Tpc44h[XO|YYm= MXz+NVAh|ryP NEHQfY5qdmirYnn0d{BVVkZvzsGgZY5lKEmOLU[gd4VkemW2aX;u NELySXQzOzV2MU[zOC=>
RAW 264.7 M3XyWmZ2dmO2aX;uJIF{e2G7 M{jhfJ4yOCEQvF2= MUHheJRmdnWjdHXzJG5QKHC{b3T1Z5Rqd25? M{CzS|I{PTRzNkO0
HT3 MXXGeY5kfGmxbjDhd5NigQ>? M3vYWp42KM7:TR?= M{jiPWROW09? MVLpcoR2[2W|IITo[UBlcW[oZYLlcpRq[WxizsGteJVjfWyrbjDhZ4V1gWyjdHnvci=> M2XBcFI{Pjl6NE[4
SiHa NGLFe5FHfW6ldHnvckBie3OjeR?= NHnaUJl,PSEQvF2= Mo\kSG1UVw>? NWHRSJN4cW6mdXPld{B1cGViZHnm[oVz\W62aXHsJO6yNXS3YoXsbY4h[WOndInsZZRqd25? Mn3MNlM3QTh2Nki=
CaSki MWfGeY5kfGmxbjDhd5NigQ>? M{HCS542KM7:TR?= MVXEUXNQ MWDpcoR2[2W|IITo[UBlcW[oZYLlcpRq[WxizsGteJVjfWyrbjDhZ4V1gWyjdHnvci=> M{j2WlI{Pjl6NE[4
SiHa NVrtPVNvTnWwY4Tpc44h[XO|YYm= MnrPglUh|ryP NHrkVm5FVVOR NF\CbYxqdmirYnn0d{BVcGGyc3nnZZJocW5vIH;yJGVITi2rbnT1Z4VlKFORQ1WgZYN1cX[jdHnvci=> Mmm2NlM3QTh2Nki=
CaSki NVfqenhITnWwY4Tpc44h[XO|YYm= NHmwVFN,PSEQvF2= M4Hu[2ROW09? NULhZ2xqcW6qaXLpeJMhXGijcIPp[4Fz\2mwLTDvdkBGT0ZvaX7keYNm\CCVT1PFJIFkfGm4YYTpc44> NUD5VnhIOjN4OUi0Olg>
MCF-7 NIjlWXpIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MUOzNEDPxE1? NFKy[phFVVOR MkO2TWM2OD1zNTFOwG0> NICweJEzOzd7OE[4NC=>
MCF-7 NFy3cm5HfW6ldHnvckBie3OjeR?= MXyzNEDPxE1? MUfEUXNQ MlH3bY5kemWjc3XzJJRp\SCvaXPyc5R2[nWuZTDhZ4V1gWyjdHnvckBt\X[nbD6= NH\YSpczOzd7OE[4NC=>
MCF-7 NV[0NlFOTnWwY4Tpc44h[XO|YYm= NWWyW4JkOzBizszN MXTEUXNQ MV7zeIFjcWyrenXzJI1q[3KxdIXieYxmeyCjZ3HpcpN1KGOxbHStbY5lfWOnZDDk[ZBwdHmvZYLpfoF1cW:w MVuyN|c6QDZ6MB?=
MCF-7 M{m3UGZ2dmO2aX;uJIF{e2G7 M17zT|E2KM7:TR?= MVnEUXNQ MlfDd5Ri[mmuaYrld{BucWO{b4T1ZpVt\XNiYXfhbY5{fCCwb3Pv[IF7d2ynLXnu[JVk\WRiZHnzZZN{\W2kbIm= M2HBV|I{Pzl6Nkiw
MCF-7 NG[4fWdHfW6ldHnvckBie3OjeR?= M4HUcVMxKM7:TR?= M{PNNWROW09? M3:5e4FtfGW{ZYOgeIhmKGG|c3XtZox6KGS7bnHtbYN{KG:oIHnueIVzeGijc3WgcYlkem:2dXL1cIV{ MUeyN|c6QDZ6MB?=
MCF-7 MnS4SpVv[3Srb36gZZN{[Xl? NGj5OnI{OCEQvF2= M4fhfGROW09? M{jOOIlv[3KnYYPld{B1cGViYnnu[Ilv\yCxZjDISGFEPiC5aYToJIlvfGW{cHjhd4UhdWmlcn;0eYJ2dGW| NWTXTWxXOjN5OUi2PFA>
PC12 MVPGeY5kfGmxbjDhd5NigQ>? NES5TmN,OyEQvF2= M3jJbmROW09? MV31dE1z\We3bHH0[ZMh[W62aT3vfIll[XSrdnWg[4Vv\SCneIDy[ZN{cW:wIILlcIF1\WRidH:geJJidnOlcnnweIlwdiCoYXP0c5IhYEKSMYO= NFLk[JczPDlyOU[4Oi=>
PC12 M4TNWmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M1:5cp4{KM7:TR?= M2PNUGROW09? MnjNdoV3\XK|ZTDINm8zNWmwZIXj[YQh\3Kxd4ToJIlvcGmkaYTpc44> NWrGcVhHOjR7MEm2PFY>
HEK293T MV3GeY5kfGmxbjDhd5NigQ>? NUez[YRbhjNizszN M3zCbmROW09? NWnqSWpPfXBvcnXneYxifGWmIGjCVFF{KHC{b4TlbY4hdGW4ZXy= MlXKNlQ6ODl4OE[=
HEK293T NIPkOY5HfW6ldHnvckBie3OjeR?= NEfhdXd,OyEQvF2= MlflSG1UVw>? MlTl[IVt[Xm|IGjCVFF{KHC{b4TlbY4h\GWpcnHkZZRqd25idnnhJIFk\XS7bHH0bY9vNW2nZHnheIVlKHC{b4TlZZNwdWGuIHTl[5Ji\GG2aX;u NXy5SYFuOjR7MEm2PFY>
Huh7 NUPlZmQ6TnWwY4Tpc44h[XO|YYm= MmDtglUh|ryP M4DKfGROW09? NH:wc3R{fXCycnXzd4V{KHC{b3zp[oVz[XSrb36gc4YhcGWyYYTpeIl{KENidnnyeZMhemWybHnjc44hf2m2aDDFR|UxKD1iMD6zJO69VQ>? NVLnRXh5OjVzMEizNlY>
SKMEL21 NUTsSGVKT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NYTselN[hjVyMDDuUS=> M4mxXWROW09? M4jzcIlvcGmkaYTzJINmdGxicILvcIln\XKjdHnvci=> M1X2TFI2QTV5OEGy
SKMEL103 M3m3R2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MYj+OVAxKG6P NX3XcJE6TE2VTx?= Mn\LbY5pcWKrdIOgZ4VtdCCycn;sbYZmemG2aX;u MX6yOVk2PzhzMh?=
SKMEL28 MUDHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M4TDUp42ODBibl2= NX3S[mZHTE2VTx?= MkL3bY5pcWKrdIOgZ4VtdCCycn;sbYZmemG2aX;u NXn1XmFIOjV7NUe4NVI>
WM164 MUTHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NYrkfItYhjVyMDDuUS=> MXzEUXNQ NYXBT4NScW6qaXLpeJMh[2WubDDwdo9tcW[ncnH0bY9v M4rpWlI2QTV5OEGy
WM1361a MmHlS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MXz+OVAxKG6P NHnob|JFVVOR MYLpcohq[mm2czDj[YxtKHC{b3zp[oVz[XSrb36= MVyyOVk2PzhzMh?=
WM1366 NH3w[lZIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MUH+OVAxKG6P NWLjVVk1TE2VTx?= NUfoVIF3cW6qaXLpeJMh[2WubDDwdo9tcW[ncnH0bY9v MVSyOVk2PzhzMh?=
WM793 MXXHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NHLvdmp,PTByIH7N NHXoSIZFVVOR NX3oeVlXcW6qaXLpeJMh[2WubDDwdo9tcW[ncnH0bY9v NXvwXG1zOjV7NUe4NVI>
WM35 MX\Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NEnsSXd,PTByIH7N NVTYVnB2TE2VTx?= NYi4UmNXcW6qaXLpeJMh[2WubDDwdo9tcW[ncnH0bY9v MnjINlU6PTd6MUK=
WM983a MoSyS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MljKglUxOCCwTR?= MWTEUXNQ MmD1bY5pcWKrdIOgZ4VtdCCycn;sbYZmemG2aX;u Mmf3NlU6PTd6MUK=
WM793 MkjmSpVv[3Srb36gZZN{[Xl? NVzQ[GtEhjZizszN MUfEUXNQ MV3pcoR2[2ViR{GgZZJz\XO2 NFH0RmozPTl3N{ixNi=>
WM164 M2\Q[WZ2dmO2aX;uJIF{e2G7 MUj+OkDPxE1? NHm3O|FFVVOR MXTpcoR2[2ViR{GgZZJz\XO2 M{C4RVI2QTV5OEGy
WM983a MYXGeY5kfGmxbjDhd5NigQ>? NXPjZZFthjZizszN NEf6NYFFVVOR MnnYbY5lfWOnIFexJIFzemW|dB?= MWGyOVk2PzhzMh?=
WM164 NVm0[Jh4TnWwY4Tpc44h[XO|YYm= M3joOp4{KM7:TR?= MVjEUXNQ MYrheYdu\W62czDlfJBz\XO|aX;uJI9nKE2KQzDjcIF{eyCLIHHu[EBu\Wyjbn;tZUBie3OxY3nheIVlKGGwdHnn[Y5{ MmS2NlU6PTd6MUK=
WM983a NHvZ[mlHfW6ldHnvckBie3OjeR?= MWX+N{DPxE1? NGDTXo9FVVOR MUPheYdu\W62czDlfJBz\XO|aX;uJI9nKE2KQzDjcIF{eyCLIHHu[EBu\Wyjbn;tZUBie3OxY3nheIVlKGGwdHnn[Y5{ NIe1N2czPTl3N{ixNi=>
IPC298 MW\GeY5kfGmxbjDhd5NigQ>? M4LLU54{KM7:TR?= NGXrdohFVVOR MnGzZZVodWWwdIOg[ZhxemW|c3nvckBw\iCPSFOgZ4xie3NiSTDhcoQhdWWuYX7vcYEh[XO|b3PpZZRm\CCjboTp[4Vvew>? NIHMZ4gzPTl3N{ixNi=>
SKMEL30 NF71dW5HfW6ldHnvckBie3OjeR?= NInGRmJ,OyEQvF2= NFXyeZpFVVOR NWPQRZdP[XWpbXXueJMh\XiycnXzd4lwdiCxZjDNTGMh[2yjc4OgTUBidmRibXXsZY5wdWFiYYPzc4Nq[XSnZDDhcpRq\2Wwcx?= NHz2SpIzPTl3N{ixNi=>
TCa83 M321WWZ2dmO2aX;uJIF{e2G7 NXn3UphKcW6mdXPld{BRXEWQIHX4dJJme3Orb36gZY5lKG2nbXLyZY5mKHS{YX7zcI9k[XSrb36= MWSyOlI4QTNyMx?=
293T MlP3SpVv[3Srb36gZZN{[Xl? NEPnXZZ,OiEQvHevcYw> NWqyTVhocW6mdXPld{BRXEWQIHX4dJJme3Orb36gZY5lKG2nbXLyZY5mKHS{YX7zcI9k[XSrb36= NVnqdnMyOjZ{N{mzNFM>
SACC-83 MWDGeY5kfGmxbjDhd5NigQ>? M1[3XZ4zKM7:Zz;tcC=> NGnpRmtqdmS3Y3XzJHBVTU5iZYjwdoV{e2mxbjDhcoQhdWWvYoLhcoUhfHKjboPsc4NifGmxbh?= NIn0RZIzPjJ5OUOwNy=>
293T MXjGeY5kfGmxbjDhd5NigQ>? MVv+NkDPxGdxbXy= NHu4T3pqdmS3Y3XzJHBVTU5iYXPleJlt[XSrb36gZZQhUzF4Mx?= MYKyOlI4QTNyMx?=
U-87 MG NFm1UFNHfW6ldHnvckBie3OjeR?= NVLQTW1OhjJizsznM41t MUTpcohq[mm2czD0bIUhdWmpcnH0bY9vKGGwZDDpcpZie2mxbh?= MmHlNlYzPzl|MEO=
U-87 MG M4mxTWZ2dmO2aX;uJIF{e2G7 MoXJglExKM7:TR?= MULpcohq[mm2czDBT3QheGixc4Doc5J6dGG2aX;u MVGyOlI4QTNyMx?=
U-87 MG NYnJZ4h6T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MW\+NVAh|ryP MkPQbY5pcWKrdIOgZ4VtdCCpcn;3eIg> MnzPNlYzPzl|MEO=

... Click to View More Cell Line Experimental Data

In vivo Daily treatment of Tubastatin A at 0.5mg/kg inhibits HDAC6 to promote Tregs suppressive activity in mouse models of inflammation and autoimmunity, including multiple forms of experimental colitis and fully major histocompatibility complex (MHC)-incompatible cardiac allograft rejection. [2]

Protocol

Kinase Assay:[1]
+ Expand

Enzyme Inhibition Assays:

Enzyme inhibition assays are performed by the Reaction Biology Corporation, Malvern, PA, using the Reaction Biology HDAC Spectrum platform. (www.reactionbiology.com) The HDAC1, 2, 4, 5, 6, 7, 8, 9, 10, and 11 assays use 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. Tubastatin A is 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:[1]
+ Expand
  • Cell lines: Primary cortical neuron of fetal Sprague-Dawley rats (embryonic day 17)
  • Concentrations: 0-10 μM
  • Incubation Time: 24 hours
  • Method: Primary cortical neuron cultures are obtained from the cerebral cortex of fetal Sprague-Dawley rats (embryonic day 17) as described previously. All experiments are initiated 24 hours after plating. Under these conditions, the cells are not susceptible to glutamate-mediated excitotoxicity. For cytotoxicity studies, cells are rinsed with warm PBS and then placed in minimum essential medium (Invitrogen) containing 5.5 g/L glucose, 10% fetal calf serum, 2 mM L-glutamine, and 100 μM cystine. Oxidative stress is induced by the addition of the glutamate analogue homocysteate (HCA; 5 mM) to the media. HCA is diluted from 100-fold concentrated solutions that are adjusted to pH 7.5. In combination with HCA, neurons are treated with Tubastatin A at the indicated concentrations. Viability is assessed after 24 hours by MTT assay (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide) method.
    (Only for Reference)
Animal Research:[2]
+ Expand
  • Animal Models: Na?ve CD45RBhi CD4+ CD25- cells (1 × 106) from WT or HDAC6-/- mice Are injected i.p. into B6/Rag1-/-mice.
  • Formulation: Tubastatin A is dissolved in dimethyl sulfoxide (DMSO).
  • Dosages: 0.5 mg/kg
  • Administration: Tubastatin A is injected i.p. daily.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 74 mg/mL (198.99 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
1% DMSO+30% polyethylene glycol+1% Tween 80
For best results, use promptly after mixing.
30 mg/mL

* 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 Information

Molecular Weight 371.86
Formula

C20H21N3O2.HCl

CAS No. 1310693-92-5
Storage powder
in solvent
Synonyms N/A

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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.

Handling Instructions

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID