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

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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 MmfwT4lv[XOnIHHzd4F6 MknnNk42KM7:TR?= MYLEUXNQ NWS4ZXkzcW6mdXPld{DPuS22dXL1cIlvKGi7cHXyZYNmfHmuYYTpc44> MlSzNlA3OTR7M{[=
neuron cultures NYPWbVVbTnWwY4Tpc44h[XO|YYm= M1:zeZ4yOCEQvF2= NHzuPXJFVVOR NUe4NGc{eHKxdHXjeJMh[WejaX7zeEBodHW2YYTobY9v\SCmZYDs[ZRqd25vaX7keYNm\CCxeHnkZZRqfmVic4Ty[ZN{ NH7CfYczODZzNEmzOi=>
134/04 Mnq2SpVv[3Srb36gZZN{[Xl? NWHGSGloPy53INM1US=> MYDpcZBicXK|IH35c5R2[mViZn;ycYF1cW:w M3\aNlIzOTd2OEO5
C2C12 MonUSpVv[3Srb36gZZN{[Xl? MlXFO{42KML3TR?= M{TtXolueGGrcoOgcZlwfHWkZTDmc5Ju[XSrb36= NH2xZ5czOjF5NEizPS=>
HaCaT keratinocytes M{\URWZ2dmO2aX;uJIF{e2G7 M4rGb|ExKM7:TR?= MkPwZoxw[2u|IHHyd4VvcXSnIH\yc40hcW6mdXPpcochVnKoMjDwdo91\WmwIITyZY5{dGG2aX;u NFjJT4QzOjN4N{[4PS=>
JURL-MK1 NWLVeWMyTnWwY4Tpc44h[XO|YYm= NUDhR2NMOTBizszN NYHvXZRN\W6qYX7j[ZMh[2WubDDh[Ihme2m4aYT5JJRwKG[rYoLvcoVkfGmw M1rGT|I{ODJ{NUiz
CML-T1 NHXhemJHfW6ldHnvckBie3OjeR?= Moj5NVAh|ryP MWjlcohidmOnczDj[YxtKGGmaHXzbZZqfHlidH:g[oljem:wZXP0bY4> MX6yN|AzOjV6Mx?=
K562 MnjBSpVv[3Srb36gZZN{[Xl? NGX2[|MyOCEQvF2= MX\lcohidmOnczDj[YxtKGGmaHXzbZZqfHlidH:g[oljem:wZXP0bY4> NU\udIRROjNyMkK1PFM>
HL-60 NGfzXZNHfW6ldHnvckBie3OjeR?= NFzaS4cyOCEQvF2= NV\TS|NG\W6qYX7j[ZMh[2WubDDh[Ihme2m4aYT5JJRwKG[rYoLvcoVkfGmw MoL5NlMxOjJ3OEO=
KMCH NYH6Vpp3T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M2W0T54yOCEQvF2= MWrk[YNz\WG|ZYOgdJJwdGmoZYLheIlwdiCjbnSgZY5kcG:{YXflMYlv\GWyZX7k[Y51KGe{b4f0bC=> M1mw[VI{OzdyM{K3
THP-1 M2S3d2Z2dmO2aX;uJIF{e2G7 M{TVe54yOCEQvF2= NY\HdVh5cW6qaXLpeJMhXE6ILd8xJIFv\CCLTD22JJNm[3KndHnvci=> MljTNlM2PDF4M{S=
RAW 264.7 MkCzSpVv[3Srb36gZZN{[Xl? M2DTPZ4yOCEQvF2= MVPheJRmdnWjdHXzJG5QKHC{b3T1Z5Rqd25? Moi0NlM2PDF4M{S=
HT3 MVjGeY5kfGmxbjDhd5NigQ>? MVL+OUDPxE1? M2C0SmROW09? NWfTXIRIcW6mdXPld{B1cGViZHnm[oVz\W62aXHsJO6yNXS3YoXsbY4h[WOndInsZZRqd25? M4rD[lI{Pjl6NE[4
SiHa M1;ofGZ2dmO2aX;uJIF{e2G7 MmnRglUh|ryP MYnEUXNQ NWXvW2p5cW6mdXPld{B1cGViZHnm[oVz\W62aXHsJO6yNXS3YoXsbY4h[WOndInsZZRqd25? MX[yN|Y6QDR4OB?=
CaSki NH75eJNHfW6ldHnvckBie3OjeR?= MWL+OUDPxE1? MlHUSG1UVw>? NUj3eJBJcW6mdXPld{B1cGViZHnm[oVz\W62aXHsJO6yNXS3YoXsbY4h[WOndInsZZRqd25? NWP3[3dVOjN4OUi0Olg>
SiHa M3\rTWZ2dmO2aX;uJIF{e2G7 Ml;DglUh|ryP NVfx[Vd6TE2VTx?= NF\wPWNqdmirYnn0d{BVcGGyc3nnZZJocW5vIH;yJGVITi2rbnT1Z4VlKFORQ1WgZYN1cX[jdHnvci=> NIDweoMzOzZ7OES2PC=>
CaSki Mn\SSpVv[3Srb36gZZN{[Xl? NF;JdGp,PSEQvF2= Mo\0SG1UVw>? MlPqbY5pcWKrdIOgWIhieHOrZ3Hy[4lvNSCxcjDFS2YucW6mdXPl[EBUV0OHIHHjeIl3[XSrb36= M{\qN|I{Pjl6NE[4
MCF-7 MmT6S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MnSwN|Ah|ryP NV;jVYp7TE2VTx?= NIfBb3hKSzVyPUG1JO69VQ>? NYXaTZBwOjN5OUi2PFA>
MCF-7 NXWyOFZWTnWwY4Tpc44h[XO|YYm= MYOzNEDPxE1? MWjEUXNQ M{CzTIlv[3KnYYPld{B1cGVibXnjdo91fWK3bHWgZYNmfHmuYYTpc44hdGW4ZXyu NEfMVXczOzd7OE[4NC=>
MCF-7 NUm0UHpUTnWwY4Tpc44h[XO|YYm= Mo\DN|Ah|ryP NYrVUWM6TE2VTx?= NIX3VIV{fGGkaXzpfoV{KG2rY4LveJVjfWynczDh[4FqdnO2IHPvcIQucW6mdXPl[EBl\XCxbInt[ZJqgmG2aX;u MlLzNlM4QTh4OEC=
MCF-7 M2GxSGZ2dmO2aX;uJIF{e2G7 NYnGb5N3OTVizszN NE\0[FdFVVOR M3HzU5N1[WKrbHn6[ZMhdWmlcn;0eYJ2dGW|IHHnZYlve3Ribn;jc4Rigm:uZT3pcoR2[2WmIHTpd4F{e2WvYnz5 MVKyN|c6QDZ6MB?=
MCF-7 NXT1SpBLTnWwY4Tpc44h[XO|YYm= MXGzNEDPxE1? MlzFSG1UVw>? MYfhcJRmemW|IITo[UBie3OnbXLsfUBlgW6jbXnjd{Bw\iCrboTldpBp[XOnIH3pZ5JwfHWkdXzldy=> MWeyN|c6QDZ6MB?=
MCF-7 MnjoSpVv[3Srb36gZZN{[Xl? NWTp[GEzOzBizszN M1TmPGROW09? MVvpcoNz\WG|ZYOgeIhmKGKrbnTpcochd2ZiSFTBR|Yhf2m2aDDpcpRmenCqYYPlJI1q[3KxdIXieYxmew>? MYqyN|c6QDZ6MB?=
PC12 NGi1eY9HfW6ldHnvckBie3OjeR?= MmC1glMh|ryP NETPUIVFVVOR M3HCZ5VxNXKnZ4XsZZRmeyCjboTpMY95cWSjdHn2[UBo\W6nIHX4dJJme3Orb36gdoVt[XSnZDD0c{B1emGwc3PybZB1cW:wIH\hZ5RweiC[QmCxdy=> NXnRXZZ4OjR7MEm2PFY>
PC12 MWnHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NUnRdWJ1hjNizszN NF7RUldFVVOR Ml:zdoV3\XK|ZTDINm8zNWmwZIXj[YQh\3Kxd4ToJIlvcGmkaYTpc44> NVnO[3FmOjR7MEm2PFY>
HEK293T NXrBSVVVTnWwY4Tpc44h[XO|YYm= M1KwXJ4{KM7:TR?= M1r2cmROW09? MlXseZAuemWpdXzheIVlKFiEUEHzJJBzd3SnaX6gcIV3\Wx? NF\wb4IzPDlyOU[4Oi=>
HEK293T MoDCSpVv[3Srb36gZZN{[Xl? Mmq3glMh|ryP M1zsfGROW09? NIfET|Bl\WyjeYOgXGJROXNicILveIVqdiCmZXfyZYRifGmxbjD2bYEh[WOndInsZZRqd25vbXXkbYF1\WRicILveIVie2:vYXyg[IVoemGmYYTpc44> MUiyOFkxQTZ6Nh?=
Huh7 NUXrbIhkTnWwY4Tpc44h[XO|YYm= NGW3fJd,PSEQvF2= NU\tT|ByTE2VTx?= NFzyOWt{fXCycnXzd4V{KHC{b3zp[oVz[XSrb36gc4YhcGWyYYTpeIl{KENidnnyeZMhemWybHnjc44hf2m2aDDFR|UxKD1iMD6zJO69VQ>? MX2yOVExQDN{Nh?=
SKMEL21 M2XUN2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MXv+OVAxKG6P NXnXdHA5TE2VTx?= NUjjSWZxcW6qaXLpeJMh[2WubDDwdo9tcW[ncnH0bY9v NEDCW4IzPTl3N{ixNi=>
SKMEL103 M17QTmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M3yzSp42ODBibl2= MkK0SG1UVw>? M4nVVIlvcGmkaYTzJINmdGxicILvcIln\XKjdHnvci=> MnjONlU6PTd6MUK=
SKMEL28 NFHLPWRIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MmHVglUxOCCwTR?= NWLXXpM4TE2VTx?= NU\4ZmRNcW6qaXLpeJMh[2WubDDwdo9tcW[ncnH0bY9v NFOxbmIzPTl3N{ixNi=>
WM164 MnL1S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? Mo[zglUxOCCwTR?= MkLwSG1UVw>? MXvpcohq[mm2czDj[YxtKHC{b3zp[oVz[XSrb36= M3eyblI2QTV5OEGy
WM1361a NHXqXpRIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NF36XmV,PTByIH7N NXG2XW9sTE2VTx?= NXfMTmpQcW6qaXLpeJMh[2WubDDwdo9tcW[ncnH0bY9v NVXHNnBOOjV7NUe4NVI>
WM1366 MnvrS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MVf+OVAxKG6P MYXEUXNQ NUnyTWdJcW6qaXLpeJMh[2WubDDwdo9tcW[ncnH0bY9v NH70VYEzPTl3N{ixNi=>
WM793 NHzHeW1Iem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MmmzglUxOCCwTR?= M3;YOGROW09? MXfpcohq[mm2czDj[YxtKHC{b3zp[oVz[XSrb36= NWfVOYt5OjV7NUe4NVI>
WM35 MlfNS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NGXnVlN,PTByIH7N M3PVUmROW09? MX;pcohq[mm2czDj[YxtKHC{b3zp[oVz[XSrb36= M1niUlI2QTV5OEGy
WM983a MYHHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MU\+OVAxKG6P MoPGSG1UVw>? MVnpcohq[mm2czDj[YxtKHC{b3zp[oVz[XSrb36= MmfDNlU6PTd6MUK=
WM793 MVzGeY5kfGmxbjDhd5NigQ>? M1nvTZ43KM7:TR?= NITwOZNFVVOR M4rVbolv\HWlZTDHNUBienKnc4S= NVjER2dmOjV7NUe4NVI>
WM164 NVKzZVRHTnWwY4Tpc44h[XO|YYm= NXLzd|lZhjZizszN MYDEUXNQ NV[1epJ6cW6mdXPlJGcyKGG{cnXzeC=> M1i1dFI2QTV5OEGy
WM983a MXnGeY5kfGmxbjDhd5NigQ>? NF7G[2F,PiEQvF2= NInpZmZFVVOR NWS4O2F[cW6mdXPlJGcyKGG{cnXzeC=> M{W4TlI2QTV5OEGy
WM164 MVHGeY5kfGmxbjDhd5NigQ>? MoXWglMh|ryP M364dGROW09? M{P4RoF2\22nboTzJIV5eHKnc4Ppc44hd2ZiTVjDJINt[XO|IFmgZY5lKG2nbHHuc41iKGG|c3;jbYF1\WRiYX70bYdmdnN? M3PYbFI2QTV5OEGy
WM983a NHTk[oxHfW6ldHnvckBie3OjeR?= M2O2cJ4{KM7:TR?= M4jQUWROW09? NUeyOHM6[XWpbXXueJMh\XiycnXzd4lwdiCxZjDNTGMh[2yjc4OgTUBidmRibXXsZY5wdWFiYYPzc4Nq[XSnZDDhcpRq\2Wwcx?= M2LlV|I2QTV5OEGy
IPC298 NFfGR2pHfW6ldHnvckBie3OjeR?= M2\hfZ4{KM7:TR?= MoDhSG1UVw>? M3jFO4F2\22nboTzJIV5eHKnc4Ppc44hd2ZiTVjDJINt[XO|IFmgZY5lKG2nbHHuc41iKGG|c3;jbYF1\WRiYX70bYdmdnN? M3HteVI2QTV5OEGy
SKMEL30 M{XZ[mZ2dmO2aX;uJIF{e2G7 NHf3UXB,OyEQvF2= MYjEUXNQ NUfJcGxN[XWpbXXueJMh\XiycnXzd4lwdiCxZjDNTGMh[2yjc4OgTUBidmRibXXsZY5wdWFiYYPzc4Nq[XSnZDDhcpRq\2Wwcx?= M3zlU|I2QTV5OEGy
TCa83 NF\FVVFHfW6ldHnvckBie3OjeR?= MWDpcoR2[2W|IGDUSW4h\XiycnXzd4lwdiCjbnSgcYVu[nKjbnWgeJJidnOub3PheIlwdg>? NVPo[mxROjZ{N{mzNFM>
293T MVvGeY5kfGmxbjDhd5NigQ>? M2rYe54zKM7:Zz;tcC=> NXfENW5tcW6mdXPld{BRXEWQIHX4dJJme3Orb36gZY5lKG2nbXLyZY5mKHS{YX7zcI9k[XSrb36= MkjBNlYzPzl|MEO=
SACC-83 MlLNSpVv[3Srb36gZZN{[Xl? NFvid4Z,OiEQvHevcYw> NUXwOmU3cW6mdXPld{BRXEWQIHX4dJJme3Orb36gZY5lKG2nbXLyZY5mKHS{YX7zcI9k[XSrb36= MYqyOlI4QTNyMx?=
293T NGX5blhHfW6ldHnvckBie3OjeR?= NXPVSFVrhjJizsznM41t M3nwTIlv\HWlZYOgVHRGViCjY3X0fYxifGmxbjDheEBMOTZ| MV:yOlI4QTNyMx?=
U-87 MG MoX1SpVv[3Srb36gZZN{[Xl? M{jW[J4zKM7:Zz;tcC=> MVXpcohq[mm2czD0bIUhdWmpcnH0bY9vKGGwZDDpcpZie2mxbh?= NWfD[2hFOjZ{N{mzNFM>
U-87 MG NXq3TYxMTnWwY4Tpc44h[XO|YYm= M174fZ4yOCEQvF2= MVLpcohq[mm2czDBT3QheGixc4Doc5J6dGG2aX;u MYGyOlI4QTNyMx?=
U-87 MG MWjHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MYT+NVAh|ryP NYn1PXJRcW6qaXLpeJMh[2WubDDndo94fGh? Mn[4NlYzPzl|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:
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
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