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 MkPET4lv[XOnIHHzd4F6 MnS1Nk42KM7:TR?= MVPEUXNQ M1\uUIlv\HWlZYOg{tEufHWkdXzpckBpgXCncnHj[ZR6dGG2aX;u MWiyNFYyPDl|Nh?=
neuron cultures NX6wT4pkTnWwY4Tpc44h[XO|YYm= MkL2glExKM7:TR?= NHmxWFJFVVOR NYXNTop3eHKxdHXjeJMh[WejaX7zeEBodHW2YYTobY9v\SCmZYDs[ZRqd25vaX7keYNm\CCxeHnkZZRqfmVic4Ty[ZN{ M2XKbVIxPjF2OUO2
134/04 MXHGeY5kfGmxbjDhd5NigQ>? NXPmeHNKPy53INM1US=> M4qyXIlueGGrcoOgcZlwfHWkZTDmc5Ju[XSrb36= Ml3zNlIyPzR6M{m=
C2C12 NHO0PZNHfW6ldHnvckBie3OjeR?= M1vMN|cvPSEEtV2= NVjvZXVDcW2yYXnyd{BugW:2dXLlJIZwem2jdHnvci=> Mk\2NlIyPzR6M{m=
HaCaT keratinocytes MWrGeY5kfGmxbjDhd5NigQ>? M3TUcVExKM7:TR?= M3joWYJtd2OtczDhdpNmdmm2ZTDmdo9uKGmwZIXjbY5oKE6{ZkKgdJJwfGWrbjD0doFve2yjdHnvci=> NVXHXFE5OjJ|Nke2PFk>
JURL-MK1 MnzjSpVv[3Srb36gZZN{[Xl? NHjaRmEyOCEQvF2= M4\LPYVvcGGwY3XzJINmdGxiYXTo[ZNqfmm2eTD0c{BncWK{b37lZ5Rqdg>? MmPyNlMxOjJ3OEO=
CML-T1 M1:zT2Z2dmO2aX;uJIF{e2G7 M2D3bVExKM7:TR?= MYXlcohidmOnczDj[YxtKGGmaHXzbZZqfHlidH:g[oljem:wZXP0bY4> MUCyN|AzOjV6Mx?=
K562 M3;0b2Z2dmO2aX;uJIF{e2G7 NVnyRpZ7OTBizszN MWTlcohidmOnczDj[YxtKGGmaHXzbZZqfHlidH:g[oljem:wZXP0bY4> MVyyN|AzOjV6Mx?=
HL-60 MYTGeY5kfGmxbjDhd5NigQ>? MVmxNEDPxE1? NGXNe|ZmdmijbnPld{Bk\WyuIHHkbIV{cX[rdImgeI8h\mmkcn;u[YN1cW5? NEDReIkzOzB{MkW4Ny=>
KMCH NVv3[mE{T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M4rHSJ4yOCEQvF2= Mmrz[IVkemWjc3XzJJBzd2yrZnXyZZRqd25iYX7kJIFv[2ixcnHn[U1qdmSncHXu[IVvfCCpcn;3eIg> MVqyN|M4ODN{Nx?=
THP-1 M3jjc2Z2dmO2aX;uJIF{e2G7 MlvuglExKM7:TR?= MVrpcohq[mm2czDUUmYu|rFiYX7kJGlNNTZic3XjdoV1cW:w MXyyN|U1OTZ|NB?=
RAW 264.7 MoXuSpVv[3Srb36gZZN{[Xl? NUDNcFQ1hjFyIN88US=> NHr2XIhifHSnboXheIV{KE6RIIDyc4R2[3Srb36= NWfkWXhKOjN3NEG2N|Q>
HT3 MVzGeY5kfGmxbjDhd5NigQ>? M17EOZ42KM7:TR?= MUfEUXNQ NGrqSFhqdmS3Y3XzJJRp\SCmaX\m[ZJmdnSrYXyg{tEufHWkdXzpckBi[2W2eXzheIlwdg>? MXuyN|Y6QDR4OB?=
SiHa MV;GeY5kfGmxbjDhd5NigQ>? NXfscXVnhjVizszN MYfEUXNQ MoPZbY5lfWOnczD0bIUh\GmoZnXy[Y51cWGuIN8xMZR2[nWuaX6gZYNmfHmuYYTpc44> NGG2U5UzOzZ7OES2PC=>
CaSki NF;uN4FHfW6ldHnvckBie3OjeR?= MknqglUh|ryP MmHZSG1UVw>? NHj4OnVqdmS3Y3XzJJRp\SCmaX\m[ZJmdnSrYXyg{tEufHWkdXzpckBi[2W2eXzheIlwdg>? NXL4UplJOjN4OUi0Olg>
SiHa MmPoSpVv[3Srb36gZZN{[Xl? NEHyRWV,PSEQvF2= MXTEUXNQ NVjTPItrcW6qaXLpeJMhXGijcIPp[4Fz\2mwLTDvdkBGT0ZvaX7keYNm\CCVT1PFJIFkfGm4YYTpc44> NVjNfo9QOjN4OUi0Olg>
CaSki NVi3UVd1TnWwY4Tpc44h[XO|YYm= MUL+OUDPxE1? MomzSG1UVw>? NV\oeWhvcW6qaXLpeJMhXGijcIPp[4Fz\2mwLTDvdkBGT0ZvaX7keYNm\CCVT1PFJIFkfGm4YYTpc44> NXTyenVJOjN4OUi0Olg>
MCF-7 M3PDfmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M4LOPVMxKM7:TR?= M2HodWROW09? MlzsTWM2OD1zNTFOwG0> MUSyN|c6QDZ6MB?=
MCF-7 Mk\DSpVv[3Srb36gZZN{[Xl? NYH1dYl1OzBizszN NEjKNJFFVVOR MXHpcoNz\WG|ZYOgeIhmKG2rY4LveJVjfWynIHHj[ZR6dGG2aX;uJIxmfmWuLh?= M3zJNVI{Pzl6Nkiw
MCF-7 NH;tWnFHfW6ldHnvckBie3OjeR?= Mn3QN|Ah|ryP NUOwZnluTE2VTx?= NILlU2x{fGGkaXzpfoV{KG2rY4LveJVjfWynczDh[4FqdnO2IHPvcIQucW6mdXPl[EBl\XCxbInt[ZJqgmG2aX;u NVfjUWVbOjN5OUi2PFA>
MCF-7 NHfJNpZHfW6ldHnvckBie3OjeR?= M2HTZVE2KM7:TR?= MmfMSG1UVw>? NFXmRZV{fGGkaXzpfoV{KG2rY4LveJVjfWynczDh[4FqdnO2IH7vZ49l[XqxbHWtbY5lfWOnZDDkbZNie3OnbXLsfS=> MVOyN|c6QDZ6MB?=
MCF-7 NF;FOoxHfW6ldHnvckBie3OjeR?= NVzXUVdNOzBizszN MmqwSG1UVw>? MofDZYx1\XKnczD0bIUh[XO|ZX3icJkh\HmwYX3pZ5Mhd2ZiaX70[ZJxcGG|ZTDtbYNzd3S3YoXs[ZM> MkK0NlM4QTh4OEC=
MCF-7 M{jpV2Z2dmO2aX;uJIF{e2G7 M4X4NlMxKM7:TR?= NITyW4FFVVOR NHTH[FRqdmO{ZXHz[ZMhfGinIHLpcoRqdmdib3[gTGRCSzZid3n0bEBqdnSncoDoZZNmKG2rY4LveJVjfWyncx?= MkDmNlM4QTh4OEC=
PC12 NYXHS4d3TnWwY4Tpc44h[XO|YYm= NWXERnoyhjNizszN NFj3SI5FVVOR MYH1dE1z\We3bHH0[ZMh[W62aT3vfIll[XSrdnWg[4Vv\SCneIDy[ZN{cW:wIILlcIF1\WRidH:geJJidnOlcnnweIlwdiCoYXP0c5IhYEKSMYO= Moj2NlQ6ODl4OE[=
PC12 MnPLS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? Mlm3glMh|ryP M4D0TWROW09? MYHy[ZZmenOnIFiyU|IucW6mdXPl[EBoem:5dHigbY5pcWKrdHnvci=> M1vOdVI1QTB7Nki2
HEK293T MXjGeY5kfGmxbjDhd5NigQ>? NHPpOm9,OyEQvF2= MYDEUXNQ MVX1dE1z\We3bHH0[YQhYEKSMYOgdJJwfGWrbjDs[ZZmdA>? NGHoUXYzPDlyOU[4Oi=>
HEK293T MYnGeY5kfGmxbjDhd5NigQ>? NIr5O|h,OyEQvF2= NHjRVIRFVVOR NF;0cXVl\WyjeYOgXGJROXNicILveIVqdiCmZXfyZYRifGmxbjD2bYEh[WOndInsZZRqd25vbXXkbYF1\WRicILveIVie2:vYXyg[IVoemGmYYTpc44> Ml3LNlQ6ODl4OE[=
Huh7 M33zWGZ2dmO2aX;uJIF{e2G7 NV\nRVlohjVizszN NYPmbpJzTE2VTx?= MVHzeZBxemW|c3XzJJBzd2yrZnXyZZRqd25ib3[gbIVx[XSrdHnzJGMhfmm{dYOgdoVxdGmlb36ge4l1cCCHQ{WwJF0hOC5|IN88US=> NEDSS|QzPTFyOEOyOi=>
SKMEL21 NIrLdFFIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NUTVOHg1hjVyMDDuUS=> MlTVSG1UVw>? NEDHcnNqdmirYnn0d{Bk\WyuIIDyc4xq\mW{YYTpc44> M{fuTlI2QTV5OEGy
SKMEL103 NXPDTIl6T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MX;+OVAxKG6P NVvLb4lRTE2VTx?= MVjpcohq[mm2czDj[YxtKHC{b3zp[oVz[XSrb36= MYiyOVk2PzhzMh?=
SKMEL28 NWL3bVZ3T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MUn+OVAxKG6P Mn3mSG1UVw>? MoTybY5pcWKrdIOgZ4VtdCCycn;sbYZmemG2aX;u NXXoSVFFOjV7NUe4NVI>
WM164 NWXNfFZET3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= Mn7LglUxOCCwTR?= MX7EUXNQ Mof3bY5pcWKrdIOgZ4VtdCCycn;sbYZmemG2aX;u M4XRXVI2QTV5OEGy
WM1361a NF2zZoVIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MWT+OVAxKG6P M2PaeWROW09? MkTvbY5pcWKrdIOgZ4VtdCCycn;sbYZmemG2aX;u M3f6cFI2QTV5OEGy
WM1366 M{\zUGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M4DLd542ODBibl2= MoP5SG1UVw>? NHX1NY5qdmirYnn0d{Bk\WyuIIDyc4xq\mW{YYTpc44> NUW2bXhnOjV7NUe4NVI>
WM793 NHjUUZhIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NU[yPVM3hjVyMDDuUS=> MmThSG1UVw>? NX7QcpB1cW6qaXLpeJMh[2WubDDwdo9tcW[ncnH0bY9v MnHUNlU6PTd6MUK=
WM35 MWfHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MoHJglUxOCCwTR?= M3LORWROW09? MXfpcohq[mm2czDj[YxtKHC{b3zp[oVz[XSrb36= NFv1dXkzPTl3N{ixNi=>
WM983a NIfBW2RIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MVT+OVAxKG6P NFOzb|BFVVOR M{LZbYlvcGmkaYTzJINmdGxicILvcIln\XKjdHnvci=> M{T2NlI2QTV5OEGy
WM793 M1TEN2Z2dmO2aX;uJIF{e2G7 MoH0glYh|ryP NF\PRY1FVVOR NXTPb|ZGcW6mdXPlJGcyKGG{cnXzeC=> NFnFTVAzPTl3N{ixNi=>
WM164 M3i5OWZ2dmO2aX;uJIF{e2G7 MUj+OkDPxE1? MUHEUXNQ MkH6bY5lfWOnIFexJIFzemW|dB?= NHqwSoMzPTl3N{ixNi=>
WM983a NUf4XnJmTnWwY4Tpc44h[XO|YYm= NIDnUJV,PiEQvF2= NUfVdWFHTE2VTx?= M4XTVolv\HWlZTDHNUBienKnc4S= MlXXNlU6PTd6MUK=
WM164 NX[weWlLTnWwY4Tpc44h[XO|YYm= MoG2glMh|ryP NH\z[2hFVVOR NUXMWnlk[XWpbXXueJMh\XiycnXzd4lwdiCxZjDNTGMh[2yjc4OgTUBidmRibXXsZY5wdWFiYYPzc4Nq[XSnZDDhcpRq\2Wwcx?= NFj6SZYzPTl3N{ixNi=>
WM983a MVTGeY5kfGmxbjDhd5NigQ>? MoW1glMh|ryP NEmyRpBFVVOR NXLIZm9n[XWpbXXueJMh\XiycnXzd4lwdiCxZjDNTGMh[2yjc4OgTUBidmRibXXsZY5wdWFiYYPzc4Nq[XSnZDDhcpRq\2Wwcx?= NVLHXXo3OjV7NUe4NVI>
IPC298 NGrV[YtHfW6ldHnvckBie3OjeR?= MVX+N{DPxE1? MYLEUXNQ NVGxfGFn[XWpbXXueJMh\XiycnXzd4lwdiCxZjDNTGMh[2yjc4OgTUBidmRibXXsZY5wdWFiYYPzc4Nq[XSnZDDhcpRq\2Wwcx?= NIXNbpozPTl3N{ixNi=>
SKMEL30 MleySpVv[3Srb36gZZN{[Xl? NY\wNYNphjNizszN Ml:3SG1UVw>? MVfheYdu\W62czDlfJBz\XO|aX;uJI9nKE2KQzDjcIF{eyCLIHHu[EBu\Wyjbn;tZUBie3OxY3nheIVlKGGwdHnn[Y5{ MXiyOVk2PzhzMh?=
TCa83 NH3tV2pHfW6ldHnvckBie3OjeR?= NHXEPI1qdmS3Y3XzJHBVTU5iZYjwdoV{e2mxbjDhcoQhdWWvYoLhcoUhfHKjboPsc4NifGmxbh?= MXyyOlI4QTNyMx?=
293T MVLGeY5kfGmxbjDhd5NigQ>? NYLPfWlNhjJizsznM41t M3jjVIlv\HWlZYOgVHRGViCneIDy[ZN{cW:wIHHu[EBu\W2kcnHu[UB1emGwc3zvZ4F1cW:w M2nVelI3Ojd7M{Cz
SACC-83 M2rveGZ2dmO2aX;uJIF{e2G7 MXv+NkDPxGdxbXy= NUL2OXh5cW6mdXPld{BRXEWQIHX4dJJme3Orb36gZY5lKG2nbXLyZY5mKHS{YX7zcI9k[XSrb36= NVjpUVl4OjZ{N{mzNFM>
293T NGTuSWlHfW6ldHnvckBie3OjeR?= M2r0PJ4zKM7:Zz;tcC=> NYLBRW9bcW6mdXPld{BRXEWQIHHj[ZR6dGG2aX;uJIF1KEtzNkO= MUGyOlI4QTNyMx?=
U-87 MG M3zOd2Z2dmO2aX;uJIF{e2G7 M1LtPJ4zKM7:Zz;tcC=> MXzpcohq[mm2czD0bIUhdWmpcnH0bY9vKGGwZDDpcpZie2mxbh?= M2H2RlI3Ojd7M{Cz
U-87 MG M1nkPGZ2dmO2aX;uJIF{e2G7 MYL+NVAh|ryP MXTpcohq[mm2czDBT3QheGixc4Doc5J6dGG2aX;u M{HpWVI3Ojd7M{Cz
U-87 MG M3XSeWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NFrJT2x,OTBizszN MYPpcohq[mm2czDj[YxtKGe{b4f0bC=> MUOyOlI4QTNyMx?=

... 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