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 MU\LbY5ie2ViYYPzZZk> Ml3zNk42KM7:TR?= Mnq5SG1UVw>? MXzpcoR2[2W|IN8xMZR2[nWuaX6gbJlx\XKjY3X0fYxifGmxbh?= MUWyNFYyPDl|Nh?=
neuron cultures NX;BWWNkTnWwY4Tpc44h[XO|YYm= MWf+NVAh|ryP NX;mO3hrTE2VTx?= NWmxToxNeHKxdHXjeJMh[WejaX7zeEBodHW2YYTobY9v\SCmZYDs[ZRqd25vaX7keYNm\CCxeHnkZZRqfmVic4Ty[ZN{ NEL0SIUzODZzNEmzOi=>
134/04 NGX0bW1HfW6ldHnvckBie3OjeR?= MXy3MlUhyrWP NFnYSGhqdXCjaYLzJI16d3S3YnWg[o9zdWG2aX;u MljmNlIyPzR6M{m=
C2C12 NIXEeJpHfW6ldHnvckBie3OjeR?= NIPGXoM4NjViwsXN MlO5bY1x[Wm{czDtfY91fWKnIH\vdo1ifGmxbh?= NX[xS4JWOjJzN{S4N|k>
HaCaT keratinocytes NVO3S4U{TnWwY4Tpc44h[XO|YYm= M4DaS|ExKM7:TR?= NEfF[GljdG:la4OgZZJ{\W6rdHWg[pJwdSCrbnT1Z4lv\yCQcn[yJJBzd3SnaX6geJJidnOuYYTpc44> NH\GTHczOjN4N{[4PS=>
JURL-MK1 MoLkSpVv[3Srb36gZZN{[Xl? NVHadIxCOTBizszN M4PVboVvcGGwY3XzJINmdGxiYXTo[ZNqfmm2eTD0c{BncWK{b37lZ5Rqdg>? MVyyN|AzOjV6Mx?=
CML-T1 NWPGVYJFTnWwY4Tpc44h[XO|YYm= MWWxNEDPxE1? NILkbmJmdmijbnPld{Bk\WyuIHHkbIV{cX[rdImgeI8h\mmkcn;u[YN1cW5? NIrKZmkzOzB{MkW4Ny=>
K562 MWnGeY5kfGmxbjDhd5NigQ>? Ml7sNVAh|ryP MnTM[Y5p[W6lZYOgZ4VtdCCjZHjld4l3cXS7IITvJIZq[nKxbnXjeIlv MWmyN|AzOjV6Mx?=
HL-60 MYDGeY5kfGmxbjDhd5NigQ>? MUSxNEDPxE1? NFTzTZJmdmijbnPld{Bk\WyuIHHkbIV{cX[rdImgeI8h\mmkcn;u[YN1cW5? NGPFco8zOzB{MkW4Ny=>
KMCH M{TwfWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MnzRglExKM7:TR?= Mmfy[IVkemWjc3XzJJBzd2yrZnXyZZRqd25iYX7kJIFv[2ixcnHn[U1qdmSncHXu[IVvfCCpcn;3eIg> NVXTUmQxOjN|N{CzNlc>
THP-1 NHLIfFNHfW6ldHnvckBie3OjeR?= M3nLT54yOCEQvF2= NVvi[|JxcW6qaXLpeJMhXE6ILd8xJIFv\CCLTD22JJNm[3KndHnvci=> NW\CbXhsOjN3NEG2N|Q>
RAW 264.7 NEjjdXlHfW6ldHnvckBie3OjeR?= NFvFNXF,OTBizszN M2H1XoF1fGWwdXH0[ZMhVk9icILv[JVkfGmxbh?= MWCyN|U1OTZ|NB?=
HT3 M1X0PGZ2dmO2aX;uJIF{e2G7 Mo\oglUh|ryP MU\EUXNQ M4rnWIlv\HWlZYOgeIhmKGSrZn\ldoVvfGmjbDFOtU11fWK3bHnuJIFk\XS7bHH0bY9v NYS5OIJlOjN4OUi0Olg>
SiHa NHq5e2tHfW6ldHnvckBie3OjeR?= M1X6dZ42KM7:TR?= Mlq4SG1UVw>? Ml\1bY5lfWOnczD0bIUh\GmoZnXy[Y51cWGuIN8xMZR2[nWuaX6gZYNmfHmuYYTpc44> MlztNlM3QTh2Nki=
CaSki NF;JV|RHfW6ldHnvckBie3OjeR?= MkW5glUh|ryP MUPEUXNQ MmnybY5lfWOnczD0bIUh\GmoZnXy[Y51cWGuIN8xMZR2[nWuaX6gZYNmfHmuYYTpc44> NULLdXNZOjN4OUi0Olg>
SiHa MUPGeY5kfGmxbjDhd5NigQ>? M3zyV542KM7:TR?= NGDudJdFVVOR MlGxbY5pcWKrdIOgWIhieHOrZ3Hy[4lvNSCxcjDFS2YucW6mdXPl[EBUV0OHIHHjeIl3[XSrb36= MnTJNlM3QTh2Nki=
CaSki MVjGeY5kfGmxbjDhd5NigQ>? NEf3[|R,PSEQvF2= NE[1OpZFVVOR NFW0XIpqdmirYnn0d{BVcGGyc3nnZZJocW5vIH;yJGVITi2rbnT1Z4VlKFORQ1WgZYN1cX[jdHnvci=> M3zTNVI{Pjl6NE[4
MCF-7 NVfRbm5QT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MYqzNEDPxE1? Mom4SG1UVw>? MWXJR|UxRTF3IN88US=> NFHQd5ozOzd7OE[4NC=>
MCF-7 M{fpO2Z2dmO2aX;uJIF{e2G7 NGTaSGs{OCEQvF2= M3:5cGROW09? MUHpcoNz\WG|ZYOgeIhmKG2rY4LveJVjfWynIHHj[ZR6dGG2aX;uJIxmfmWuLh?= NFzpOnEzOzd7OE[4NC=>
MCF-7 NH3DWWdHfW6ldHnvckBie3OjeR?= NEn2VFI{OCEQvF2= NUHwT2FYTE2VTx?= NH\2Nox{fGGkaXzpfoV{KG2rY4LveJVjfWynczDh[4FqdnO2IHPvcIQucW6mdXPl[EBl\XCxbInt[ZJqgmG2aX;u M13DbFI{Pzl6Nkiw
MCF-7 NVPrUYhrTnWwY4Tpc44h[XO|YYm= NH7CdFIyPSEQvF2= MnPpSG1UVw>? MmLqd5Ri[mmuaYrld{BucWO{b4T1ZpVt\XNiYXfhbY5{fCCwb3Pv[IF7d2ynLXnu[JVk\WRiZHnzZZN{\W2kbIm= Mke2NlM4QTh4OEC=
MCF-7 NEj1SohHfW6ldHnvckBie3OjeR?= MW[zNEDPxE1? MmHFSG1UVw>? MYPhcJRmemW|IITo[UBie3OnbXLsfUBlgW6jbXnjd{Bw\iCrboTldpBp[XOnIH3pZ5JwfHWkdXzldy=> MX[yN|c6QDZ6MB?=
MCF-7 NGnYVHdHfW6ldHnvckBie3OjeR?= MmLjN|Ah|ryP NWPqSY16TE2VTx?= Mn7VbY5kemWjc3XzJJRp\SCkaX7kbY5oKG:oIFjERWM3KHerdHigbY51\XKyaHHz[UBucWO{b4T1ZpVt\XN? MnPINlM4QTh4OEC=
PC12 NY\3eHI3TnWwY4Tpc44h[XO|YYm= M3fkdZ4{KM7:TR?= NIP2VWdFVVOR Ml3OeZAuemWpdXzheIV{KGGwdHmtc5hq\GG2aY\lJIdmdmViZYjwdoV{e2mxbjDy[YxifGWmIITvJJRz[W6|Y4LpdJRqd25iZnHjeI9zKFiEUEHz M1npdFI1QTB7Nki2
PC12 NUn2T|ZFT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M2XvTZ4{KM7:TR?= M2XRfGROW09? M3XGWpJmfmW{c3WgTFJQOi2rbnT1Z4VlKGe{b4f0bEBqdmirYnn0bY9v M2XMflI1QTB7Nki2
HEK293T Mo\rSpVv[3Srb36gZZN{[Xl? Mke2glMh|ryP NU\2elFSTE2VTx?= NFTzU2J2eC2{ZXf1cIF1\WRiWFLQNZMheHKxdHXpckBt\X[nbB?= NV65dpliOjR7MEm2PFY>
HEK293T NULqV3M5TnWwY4Tpc44h[XO|YYm= MUf+N{DPxE1? MV\EUXNQ M3noVoRmdGG7czDYRnAyeyCycn;0[YlvKGSnZ4Lh[IF1cW:wII\pZUBi[2W2eXzheIlwdi2vZXTpZZRm\CCycn;0[YF{d22jbDDk[Ydz[WSjdHnvci=> M2PrNFI1QTB7Nki2
Huh7 NGK2ToNHfW6ldHnvckBie3OjeR?= NEnjVIt,PSEQvF2= MU\EUXNQ NIPyTXN{fXCycnXzd4V{KHC{b3zp[oVz[XSrb36gc4YhcGWyYYTpeIl{KENidnnyeZMhemWybHnjc44hf2m2aDDFR|UxKD1iMD6zJO69VQ>? NHj5VGQzPTFyOEOyOi=>
SKMEL21 M3nydWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M2PNNp42ODBibl2= NYC1eod1TE2VTx?= MUDpcohq[mm2czDj[YxtKHC{b3zp[oVz[XSrb36= MkH2NlU6PTd6MUK=
SKMEL103 NYDjNWhJT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NWPnTXJIhjVyMDDuUS=> MWjEUXNQ M2LST4lvcGmkaYTzJINmdGxicILvcIln\XKjdHnvci=> M2TO[FI2QTV5OEGy
SKMEL28 M2nVW2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M{Dp[J42ODBibl2= NGOzVo1FVVOR M4jiV4lvcGmkaYTzJINmdGxicILvcIln\XKjdHnvci=> MoLhNlU6PTd6MUK=
WM164 MWfHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MoL1glUxOCCwTR?= NXTEPYVWTE2VTx?= NFHtXINqdmirYnn0d{Bk\WyuIIDyc4xq\mW{YYTpc44> MXiyOVk2PzhzMh?=
WM1361a MW\Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NGqw[Vd,PTByIH7N Mlz1SG1UVw>? MnvFbY5pcWKrdIOgZ4VtdCCycn;sbYZmemG2aX;u MUCyOVk2PzhzMh?=
WM1366 NWjrd3dWT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MXr+OVAxKG6P NX;jRY04TE2VTx?= MY\pcohq[mm2czDj[YxtKHC{b3zp[oVz[XSrb36= NYrwWGp4OjV7NUe4NVI>
WM793 MUPHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MX;+OVAxKG6P M{OzWmROW09? NV3ZbI5RcW6qaXLpeJMh[2WubDDwdo9tcW[ncnH0bY9v MViyOVk2PzhzMh?=
WM35 M3;yV2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NWfkZZdXhjVyMDDuUS=> M1XaNGROW09? NIHIfHdqdmirYnn0d{Bk\WyuIIDyc4xq\mW{YYTpc44> NVv3bXNnOjV7NUe4NVI>
WM983a NYrxN3FFT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MkPRglUxOCCwTR?= MWfEUXNQ NITvZ3hqdmirYnn0d{Bk\WyuIIDyc4xq\mW{YYTpc44> M17WS|I2QTV5OEGy
WM793 M1Hr[GZ2dmO2aX;uJIF{e2G7 NHTPWYN,PiEQvF2= NF\IRoZFVVOR Mk\KbY5lfWOnIFexJIFzemW|dB?= NGK2S5czPTl3N{ixNi=>
WM164 M2W1Z2Z2dmO2aX;uJIF{e2G7 M{PtSJ43KM7:TR?= NWrEVHFDTE2VTx?= NFjPdZJqdmS3Y3WgS|Eh[XK{ZYP0 NV64ZW9IOjV7NUe4NVI>
WM983a MlPSSpVv[3Srb36gZZN{[Xl? NUXjOlB3hjZizszN Mn:2SG1UVw>? NEXkO3dqdmS3Y3WgS|Eh[XK{ZYP0 NEXoXY0zPTl3N{ixNi=>
WM164 MX\GeY5kfGmxbjDhd5NigQ>? M3\1S54{KM7:TR?= MUTEUXNQ NFe0fFdifWevZX70d{BmgHC{ZYPzbY9vKG:oIF3IR{BkdGG|czDJJIFv\CCvZXzhco9u[SCjc4PvZ4lifGWmIHHueIlo\W6| MnHONlU6PTd6MUK=
WM983a M3\PUWZ2dmO2aX;uJIF{e2G7 NVO1WGk2hjNizszN M{WzZmROW09? MX;heYdu\W62czDlfJBz\XO|aX;uJI9nKE2KQzDjcIF{eyCLIHHu[EBu\Wyjbn;tZUBie3OxY3nheIVlKGGwdHnn[Y5{ NXThdWkyOjV7NUe4NVI>
IPC298 NUfUcIFHTnWwY4Tpc44h[XO|YYm= MXr+N{DPxE1? M{PlbGROW09? MmXaZZVodWWwdIOg[ZhxemW|c3nvckBw\iCPSFOgZ4xie3NiSTDhcoQhdWWuYX7vcYEh[XO|b3PpZZRm\CCjboTp[4Vvew>? NVrBN2pbOjV7NUe4NVI>
SKMEL30 M3XzR2Z2dmO2aX;uJIF{e2G7 NYTnWJJHhjNizszN MUPEUXNQ MU\heYdu\W62czDlfJBz\XO|aX;uJI9nKE2KQzDjcIF{eyCLIHHu[EBu\Wyjbn;tZUBie3OxY3nheIVlKGGwdHnn[Y5{ M1XVO|I2QTV5OEGy
TCa83 NHLNUZFHfW6ldHnvckBie3OjeR?= MYrpcoR2[2W|IGDUSW4h\XiycnXzd4lwdiCjbnSgcYVu[nKjbnWgeJJidnOub3PheIlwdg>? M{ntOFI3Ojd7M{Cz
293T NX;FXFdSTnWwY4Tpc44h[XO|YYm= NUPQNJhxhjJizsznM41t NFX4b5lqdmS3Y3XzJHBVTU5iZYjwdoV{e2mxbjDhcoQhdWWvYoLhcoUhfHKjboPsc4NifGmxbh?= M2TaPFI3Ojd7M{Cz
SACC-83 NWrPb2V6TnWwY4Tpc44h[XO|YYm= NVrxXXZ2hjJizsznM41t M37wTolv\HWlZYOgVHRGViCneIDy[ZN{cW:wIHHu[EBu\W2kcnHu[UB1emGwc3zvZ4F1cW:w NFzFbHAzPjJ5OUOwNy=>
293T M2TTSGZ2dmO2aX;uJIF{e2G7 M333XZ4zKM7:Zz;tcC=> NELq[ZZqdmS3Y3XzJHBVTU5iYXPleJlt[XSrb36gZZQhUzF4Mx?= MYSyOlI4QTNyMx?=
U-87 MG MYTGeY5kfGmxbjDhd5NigQ>? NGiwZ4d,OiEQvHevcYw> MkHUbY5pcWKrdIOgeIhmKG2rZ4LheIlwdiCjbnSgbY53[XOrb36= MmPqNlYzPzl|MEO=
U-87 MG M4r6PGZ2dmO2aX;uJIF{e2G7 NVnD[XlOhjFyIN88US=> M3rF[4lvcGmkaYTzJGFMXCCyaH;zdIhwenmuYYTpc44> M2XyNVI3Ojd7M{Cz
U-87 MG M{DKZ2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M{j5[p4yOCEQvF2= MUXpcohq[mm2czDj[YxtKGe{b4f0bC=> M{f1dlI3Ojd7M{Cz

... 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