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 MXHLbY5ie2ViYYPzZZk> MoLzNk42KM7:TR?= NEnKOGNFVVOR NV76dIJocW6mdXPld{DPuS22dXL1cIlvKGi7cHXyZYNmfHmuYYTpc44> M1vz[VIxPjF2OUO2
neuron cultures NYD2fGJ[TnWwY4Tpc44h[XO|YYm= MW\+NVAh|ryP M2LRZWROW09? NYfCZ3J4eHKxdHXjeJMh[WejaX7zeEBodHW2YYTobY9v\SCmZYDs[ZRqd25vaX7keYNm\CCxeHnkZZRqfmVic4Ty[ZN{ Mor4NlA3OTR7M{[=
134/04 MkOxSpVv[3Srb36gZZN{[Xl? NHi3d2g4NjViwsXN MX\pcZBicXK|IH35c5R2[mViZn;ycYF1cW:w MnjGNlIyPzR6M{m=
C2C12 MWHGeY5kfGmxbjDhd5NigQ>? NUm3c21{Py53INM1US=> NHvWe3BqdXCjaYLzJI16d3S3YnWg[o9zdWG2aX;u NYDCXI1WOjJzN{S4N|k>
HaCaT keratinocytes MXXGeY5kfGmxbjDhd5NigQ>? MYmxNEDPxE1? MV;icI9kc3NiYYLz[Y5qfGViZoLvcUBqdmS3Y3nu[{BPemZ{IIDyc5RmcW5idILhcpNt[XSrb36= NXfEeZlLOjJ|Nke2PFk>
JURL-MK1 MofaSpVv[3Srb36gZZN{[Xl? MkTSNVAh|ryP NHHEXVlmdmijbnPld{Bk\WyuIHHkbIV{cX[rdImgeI8h\mmkcn;u[YN1cW5? M2PIWlI{ODJ{NUiz
CML-T1 M1v4O2Z2dmO2aX;uJIF{e2G7 MV2xNEDPxE1? Mnrm[Y5p[W6lZYOgZ4VtdCCjZHjld4l3cXS7IITvJIZq[nKxbnXjeIlv MojQNlMxOjJ3OEO=
K562 M3HvU2Z2dmO2aX;uJIF{e2G7 Mm\1NVAh|ryP MknQ[Y5p[W6lZYOgZ4VtdCCjZHjld4l3cXS7IITvJIZq[nKxbnXjeIlv MUeyN|AzOjV6Mx?=
HL-60 M2\WRWZ2dmO2aX;uJIF{e2G7 MWmxNEDPxE1? MWrlcohidmOnczDj[YxtKGGmaHXzbZZqfHlidH:g[oljem:wZXP0bY4> NXXmTWZ7OjNyMkK1PFM>
KMCH NIS2VFFIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NWK5cWdThjFyIN88US=> NIPaVFFl\WO{ZXHz[ZMheHKxbHnm[ZJifGmxbjDhcoQh[W6laH;yZYdmNWmwZHXw[Y5l\W62IHfyc5d1cA>? MnXFNlM{PzB|Mke=
THP-1 M1PxT2Z2dmO2aX;uJIF{e2G7 MkH0glExKM7:TR?= NHjNOIZqdmirYnn0d{BVVkZvzsGgZY5lKEmOLU[gd4VkemW2aX;u M2HoWVI{PTRzNkO0
RAW 264.7 NUHFcZRiTnWwY4Tpc44h[XO|YYm= MlO0glExKM7:TR?= MVrheJRmdnWjdHXzJG5QKHC{b3T1Z5Rqd25? MWGyN|U1OTZ|NB?=
HT3 NEHDUXpHfW6ldHnvckBie3OjeR?= MYL+OUDPxE1? MoLiSG1UVw>? MVnpcoR2[2W|IITo[UBlcW[oZYLlcpRq[WxizsGteJVjfWyrbjDhZ4V1gWyjdHnvci=> MXOyN|Y6QDR4OB?=
SiHa MnvTSpVv[3Srb36gZZN{[Xl? MlTrglUh|ryP NWjVTlJpTE2VTx?= MXHpcoR2[2W|IITo[UBlcW[oZYLlcpRq[WxizsGteJVjfWyrbjDhZ4V1gWyjdHnvci=> NFzV[|gzOzZ7OES2PC=>
CaSki NF\ER4VHfW6ldHnvckBie3OjeR?= NWLYfm9NhjVizszN Ml\USG1UVw>? NVzSfnZTcW6mdXPld{B1cGViZHnm[oVz\W62aXHsJO6yNXS3YoXsbY4h[WOndInsZZRqd25? NWW4OYZoOjN4OUi0Olg>
SiHa M2P2WWZ2dmO2aX;uJIF{e2G7 MVv+OUDPxE1? MojoSG1UVw>? Mlj3bY5pcWKrdIOgWIhieHOrZ3Hy[4lvNSCxcjDFS2YucW6mdXPl[EBUV0OHIHHjeIl3[XSrb36= M2XlOlI{Pjl6NE[4
CaSki MV;GeY5kfGmxbjDhd5NigQ>? Ml:4glUh|ryP MmHVSG1UVw>? NELNPVBqdmirYnn0d{BVcGGyc3nnZZJocW5vIH;yJGVITi2rbnT1Z4VlKFORQ1WgZYN1cX[jdHnvci=> NUXMXG51OjN4OUi0Olg>
MCF-7 NEL5dIhIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M1juTlMxKM7:TR?= M{LzfGROW09? NX3IVJJkUUN3ME2xOUDPxE1? M2eyfFI{Pzl6Nkiw
MCF-7 NFX0TVdHfW6ldHnvckBie3OjeR?= NUPFS3hFOzBizszN MonrSG1UVw>? MVjpcoNz\WG|ZYOgeIhmKG2rY4LveJVjfWynIHHj[ZR6dGG2aX;uJIxmfmWuLh?= NVnoVXBQOjN5OUi2PFA>
MCF-7 MnnSSpVv[3Srb36gZZN{[Xl? MUizNEDPxE1? MYjEUXNQ NHu0R|N{fGGkaXzpfoV{KG2rY4LveJVjfWynczDh[4FqdnO2IHPvcIQucW6mdXPl[EBl\XCxbInt[ZJqgmG2aX;u MVqyN|c6QDZ6MB?=
MCF-7 M1LodGZ2dmO2aX;uJIF{e2G7 MW[xOUDPxE1? NUDJcIRGTE2VTx?= M3\4dJN1[WKrbHn6[ZMhdWmlcn;0eYJ2dGW|IHHnZYlve3Ribn;jc4Rigm:uZT3pcoR2[2WmIHTpd4F{e2WvYnz5 NYTGWYlROjN5OUi2PFA>
MCF-7 M4HQZWZ2dmO2aX;uJIF{e2G7 M1nVNFMxKM7:TR?= MoDESG1UVw>? M2nBcIFtfGW{ZYOgeIhmKGG|c3XtZox6KGS7bnHtbYN{KG:oIHnueIVzeGijc3WgcYlkem:2dXL1cIV{ MoWzNlM4QTh4OEC=
MCF-7 Mlf2SpVv[3Srb36gZZN{[Xl? M1S3clMxKM7:TR?= M2mwN2ROW09? MoTobY5kemWjc3XzJJRp\SCkaX7kbY5oKG:oIFjERWM3KHerdHigbY51\XKyaHHz[UBucWO{b4T1ZpVt\XN? NVS5e|l[OjN5OUi2PFA>
PC12 MX7GeY5kfGmxbjDhd5NigQ>? NF\iU|J,OyEQvF2= MnT3SG1UVw>? NFTXR3l2eC2{ZXf1cIF1\XNiYX70bU1wgGmmYYTpeoUh\2WwZTDlfJBz\XO|aX;uJJJmdGG2ZXSgeI8hfHKjboPjdolxfGmxbjDmZYN1d3JiWFLQNZM> MXWyOFkxQTZ6Nh?=
PC12 M3TtcWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MoXYglMh|ryP MXHEUXNQ MlzSdoV3\XK|ZTDINm8zNWmwZIXj[YQh\3Kxd4ToJIlvcGmkaYTpc44> MoGzNlQ6ODl4OE[=
HEK293T NIDmSlJHfW6ldHnvckBie3OjeR?= M{XrT54{KM7:TR?= NWjaRVF2TE2VTx?= NUXGb5E6fXBvcnXneYxifGWmIGjCVFF{KHC{b4TlbY4hdGW4ZXy= NWftWo9vOjR7MEm2PFY>
HEK293T MYfGeY5kfGmxbjDhd5NigQ>? MlPVglMh|ryP NYH2N2JNTE2VTx?= M4rsZ4RmdGG7czDYRnAyeyCycn;0[YlvKGSnZ4Lh[IF1cW:wII\pZUBi[2W2eXzheIlwdi2vZXTpZZRm\CCycn;0[YF{d22jbDDk[Ydz[WSjdHnvci=> MmruNlQ6ODl4OE[=
Huh7 M3;qNGZ2dmO2aX;uJIF{e2G7 MmT3glUh|ryP M1fxNmROW09? NEPPXHd{fXCycnXzd4V{KHC{b3zp[oVz[XSrb36gc4YhcGWyYYTpeIl{KENidnnyeZMhemWybHnjc44hf2m2aDDFR|UxKD1iMD6zJO69VQ>? MYGyOVExQDN{Nh?=
SKMEL21 M12xUGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MmfGglUxOCCwTR?= NX7pcXM6TE2VTx?= MmP0bY5pcWKrdIOgZ4VtdCCycn;sbYZmemG2aX;u MUeyOVk2PzhzMh?=
SKMEL103 NHXncoVIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MmXjglUxOCCwTR?= M3LBT2ROW09? MlXBbY5pcWKrdIOgZ4VtdCCycn;sbYZmemG2aX;u NWewfFZyOjV7NUe4NVI>
SKMEL28 MkD6S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NHK5XlB,PTByIH7N NUi0NHh6TE2VTx?= MkewbY5pcWKrdIOgZ4VtdCCycn;sbYZmemG2aX;u NGrwTFgzPTl3N{ixNi=>
WM164 MYfHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M4\KU542ODBibl2= M1rZcGROW09? MX3pcohq[mm2czDj[YxtKHC{b3zp[oVz[XSrb36= NGfSOWUzPTl3N{ixNi=>
WM1361a Mo[4S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MlH4glUxOCCwTR?= MYLEUXNQ MonRbY5pcWKrdIOgZ4VtdCCycn;sbYZmemG2aX;u MkP5NlU6PTd6MUK=
WM1366 NHPUSFNIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NXzP[WluhjVyMDDuUS=> MXLEUXNQ NVvyOXREcW6qaXLpeJMh[2WubDDwdo9tcW[ncnH0bY9v MnX3NlU6PTd6MUK=
WM793 MY\Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NXHxfYZLhjVyMDDuUS=> MoXjSG1UVw>? NG\lfmhqdmirYnn0d{Bk\WyuIIDyc4xq\mW{YYTpc44> MkKzNlU6PTd6MUK=
WM35 NE\ES4xIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= Ml\HglUxOCCwTR?= NIi3WmVFVVOR NEPIVJZqdmirYnn0d{Bk\WyuIIDyc4xq\mW{YYTpc44> NH7ZUWUzPTl3N{ixNi=>
WM983a M2rTXmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NIHVTZR,PTByIH7N MmjPSG1UVw>? NU\Kb|lMcW6qaXLpeJMh[2WubDDwdo9tcW[ncnH0bY9v MknyNlU6PTd6MUK=
WM793 MmLHSpVv[3Srb36gZZN{[Xl? MWP+OkDPxE1? MkDCSG1UVw>? NW\iVIxCcW6mdXPlJGcyKGG{cnXzeC=> NV3WUpRPOjV7NUe4NVI>
WM164 NVG5OplxTnWwY4Tpc44h[XO|YYm= MXj+OkDPxE1? M1\qSGROW09? MXLpcoR2[2ViR{GgZZJz\XO2 M3vlWFI2QTV5OEGy
WM983a MVLGeY5kfGmxbjDhd5NigQ>? MmPoglYh|ryP MV3EUXNQ MmG5bY5lfWOnIFexJIFzemW|dB?= MYGyOVk2PzhzMh?=
WM164 NX\jT2EyTnWwY4Tpc44h[XO|YYm= NUK2NmdvhjNizszN NES3TXFFVVOR NIH3WlFifWevZX70d{BmgHC{ZYPzbY9vKG:oIF3IR{BkdGG|czDJJIFv\CCvZXzhco9u[SCjc4PvZ4lifGWmIHHueIlo\W6| MV[yOVk2PzhzMh?=
WM983a MULGeY5kfGmxbjDhd5NigQ>? NGLLbHh,OyEQvF2= NF7tZmRFVVOR NX\Y[nB{[XWpbXXueJMh\XiycnXzd4lwdiCxZjDNTGMh[2yjc4OgTUBidmRibXXsZY5wdWFiYYPzc4Nq[XSnZDDhcpRq\2Wwcx?= NVvwempHOjV7NUe4NVI>
IPC298 MlPySpVv[3Srb36gZZN{[Xl? NHeweGZ,OyEQvF2= NFG5NFdFVVOR MXrheYdu\W62czDlfJBz\XO|aX;uJI9nKE2KQzDjcIF{eyCLIHHu[EBu\Wyjbn;tZUBie3OxY3nheIVlKGGwdHnn[Y5{ NFnuSXUzPTl3N{ixNi=>
SKMEL30 NX\5WlhtTnWwY4Tpc44h[XO|YYm= M4TkPZ4{KM7:TR?= NHv3OJFFVVOR Mne3ZZVodWWwdIOg[ZhxemW|c3nvckBw\iCPSFOgZ4xie3NiSTDhcoQhdWWuYX7vcYEh[XO|b3PpZZRm\CCjboTp[4Vvew>? NVK4b5VTOjV7NUe4NVI>
TCa83 M3XuVGZ2dmO2aX;uJIF{e2G7 NUK0ZZlHcW6mdXPld{BRXEWQIHX4dJJme3Orb36gZY5lKG2nbXLyZY5mKHS{YX7zcI9k[XSrb36= M4TKOFI3Ojd7M{Cz
293T M125b2Z2dmO2aX;uJIF{e2G7 NUTCW45rhjJizsznM41t M123Zolv\HWlZYOgVHRGViCneIDy[ZN{cW:wIHHu[EBu\W2kcnHu[UB1emGwc3zvZ4F1cW:w M3PaeVI3Ojd7M{Cz
SACC-83 NF7oOZBHfW6ldHnvckBie3OjeR?= MmmxglIh|rypL33s NUXsOog{cW6mdXPld{BRXEWQIHX4dJJme3Orb36gZY5lKG2nbXLyZY5mKHS{YX7zcI9k[XSrb36= NVXkS3ZCOjZ{N{mzNFM>
293T MlrTSpVv[3Srb36gZZN{[Xl? MlzJglIh|rypL33s NIDTT|BqdmS3Y3XzJHBVTU5iYXPleJlt[XSrb36gZZQhUzF4Mx?= M1zpRVI3Ojd7M{Cz
U-87 MG NIewZpBHfW6ldHnvckBie3OjeR?= Mk\SglIh|rypL33s NWj3SIh{cW6qaXLpeJMhfGinIH3p[5JifGmxbjDhcoQhcW64YYPpc44> M123b|I3Ojd7M{Cz
U-87 MG MWDGeY5kfGmxbjDhd5NigQ>? NGS0XXN,OTBizszN NEXpeo9qdmirYnn0d{BCU1RicHjvd5Bpd3K7bHH0bY9v MorXNlYzPzl|MEO=
U-87 MG NUTLNIROT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MY\+NVAh|ryP MWDpcohq[mm2czDj[YxtKGe{b4f0bC=> M1foVFI3Ojd7M{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 individually and in order:
1% DMSO+30% polyethylene glycol+1% Tween 80
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