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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2 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.

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)
HDAC1 [1]
(Cell-free assay)
HDAC2 [1]
(Cell-free assay)
HDAC3 [1]
(Cell-free assay)
15 nM 854 nM 16.4 μM >30 μM >30 μM
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 NFS3[mRMcW6jc3WgZZN{[Xl? MnPpNk42KM7:TR?= NF7sVIdFVVOR MljDbY5lfWOnczFOtU11fWK3bHnuJIh6eGW{YXPleJlt[XSrb36= M3K5SFIxPjF2OUO2
neuron cultures MWrGeY5kfGmxbjDhd5NigQ>? NFzDfW9,OTBizszN MYXEUXNQ MWXwdo91\WO2czDh[4FqdnO2IHfseZRifGirb37lJIRmeGyndHnvck1qdmS3Y3XkJI95cWSjdHn2[UB{fHKnc4O= NIe2VlUzODZzNEmzOi=>
134/04 MkPuSpVv[3Srb36gZZN{[Xl? NEKzXm44NjViwsXN M2DDXIlueGGrcoOgcZlwfHWkZTDmc5Ju[XSrb36= MVSyNlE4PDh|OR?=
C2C12 MonqSpVv[3Srb36gZZN{[Xl? MUC3MlUhyrWP M1PmbolueGGrcoOgcZlwfHWkZTDmc5Ju[XSrb36= NEP4NVkzOjF5NEizPS=>
HaCaT keratinocytes NHfmWG5HfW6ldHnvckBie3OjeR?= M{ThSVExKM7:TR?= NIDISVVjdG:la4OgZZJ{\W6rdHWg[pJwdSCrbnT1Z4lv\yCQcn[yJJBzd3SnaX6geJJidnOuYYTpc44> MoK5NlI{Pjd4OEm=
JURL-MK1 NUPIOIR6TnWwY4Tpc44h[XO|YYm= MXGxNEDPxE1? NV72cVJJ\W6qYX7j[ZMh[2WubDDh[Ihme2m4aYT5JJRwKG[rYoLvcoVkfGmw MonaNlMxOjJ3OEO=
CML-T1 NEn0U5hHfW6ldHnvckBie3OjeR?= NHTrOpQyOCEQvF2= NXL5WWFM\W6qYX7j[ZMh[2WubDDh[Ihme2m4aYT5JJRwKG[rYoLvcoVkfGmw NUn1UmI4OjNyMkK1PFM>
K562 NHzhV5NHfW6ldHnvckBie3OjeR?= NIfqZ40yOCEQvF2= NGX3R2pmdmijbnPld{Bk\WyuIHHkbIV{cX[rdImgeI8h\mmkcn;u[YN1cW5? MXSyN|AzOjV6Mx?=
HL-60 MWfGeY5kfGmxbjDhd5NigQ>? NHvyWocyOCEQvF2= NGfndnRmdmijbnPld{Bk\WyuIHHkbIV{cX[rdImgeI8h\mmkcn;u[YN1cW5? MUSyN|AzOjV6Mx?=
KMCH M3T2cmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NGG1dnB,OTBizszN M4ezdIRm[3KnYYPld{Bxem:uaX\ldoF1cW:wIHHu[EBidmOqb4Lh[4UucW6mZYDlcoRmdnRiZ4Lve5Rp NW\acmhtOjN|N{CzNlc>
THP-1 MoDUSpVv[3Srb36gZZN{[Xl? MmDzglExKM7:TR?= MXPpcohq[mm2czDUUmYu|rFiYX7kJGlNNTZic3XjdoV1cW:w MXiyN|U1OTZ|NB?=
RAW 264.7 NXTzcZBtTnWwY4Tpc44h[XO|YYm= NYTic3h3hjFyIN88US=> NXfjdFM3[XS2ZX71ZZRmeyCQTzDwdo9lfWO2aX;u NWnPSZdEOjN3NEG2N|Q>
HT3 NX;w[Yd2TnWwY4Tpc44h[XO|YYm= NHPiTVh,PSEQvF2= MWnEUXNQ MYnpcoR2[2W|IITo[UBlcW[oZYLlcpRq[WxizsGteJVjfWyrbjDhZ4V1gWyjdHnvci=> NEK4NFUzOzZ7OES2PC=>
SiHa MkfsSpVv[3Srb36gZZN{[Xl? NVLseHBChjVizszN MVXEUXNQ MU\pcoR2[2W|IITo[UBlcW[oZYLlcpRq[WxizsGteJVjfWyrbjDhZ4V1gWyjdHnvci=> NVvqWmk4OjN4OUi0Olg>
CaSki NWLWV4c4TnWwY4Tpc44h[XO|YYm= MoPEglUh|ryP MYLEUXNQ MnjxbY5lfWOnczD0bIUh\GmoZnXy[Y51cWGuIN8xMZR2[nWuaX6gZYNmfHmuYYTpc44> M1zFWlI{Pjl6NE[4
SiHa MlzuSpVv[3Srb36gZZN{[Xl? M2exPZ42KM7:TR?= M4\meWROW09? NH\SO3ZqdmirYnn0d{BVcGGyc3nnZZJocW5vIH;yJGVITi2rbnT1Z4VlKFORQ1WgZYN1cX[jdHnvci=> MYGyN|Y6QDR4OB?=
CaSki M37MN2Z2dmO2aX;uJIF{e2G7 MXH+OUDPxE1? MknBSG1UVw>? MlKwbY5pcWKrdIOgWIhieHOrZ3Hy[4lvNSCxcjDFS2YucW6mdXPl[EBUV0OHIHHjeIl3[XSrb36= NWDrWFZ1OjN4OUi0Olg>
MCF-7 MV7Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NXfM[XNHOzBizszN NX2xRod6TE2VTx?= NHjaUZVKSzVyPUG1JO69VQ>? MkWyNlM4QTh4OEC=
MCF-7 MXPGeY5kfGmxbjDhd5NigQ>? M{H0OFMxKM7:TR?= MXXEUXNQ MlK4bY5kemWjc3XzJJRp\SCvaXPyc5R2[nWuZTDhZ4V1gWyjdHnvckBt\X[nbD6= MUiyN|c6QDZ6MB?=
MCF-7 M2rubmZ2dmO2aX;uJIF{e2G7 M1vOZVMxKM7:TR?= M2DK[GROW09? NVfJbFl2e3SjYnnsbZpmeyCvaXPyc5R2[nWuZYOgZYdicW6|dDDjc4xlNWmwZIXj[YQh\GWyb3z5cYVzcXqjdHnvci=> NY\1bmJmOjN5OUi2PFA>
MCF-7 NXj2NnFQTnWwY4Tpc44h[XO|YYm= MVOxOUDPxE1? MX\EUXNQ MWHzeIFjcWyrenXzJI1q[3KxdIXieYxmeyCjZ3HpcpN1KG6xY3;kZZpwdGVvaX7keYNm\CCmaYPhd5NmdWKueR?= NVrJeFNmOjN5OUi2PFA>
MCF-7 M33IcmZ2dmO2aX;uJIF{e2G7 NEDhU2Q{OCEQvF2= M2e1eWROW09? MYDhcJRmemW|IITo[UBie3OnbXLsfUBlgW6jbXnjd{Bw\iCrboTldpBp[XOnIH3pZ5JwfHWkdXzldy=> NHXtS5UzOzd7OE[4NC=>
MCF-7 M2WwUmZ2dmO2aX;uJIF{e2G7 MkjkN|Ah|ryP MXHEUXNQ M4\IOIlv[3KnYYPld{B1cGViYnnu[Ilv\yCxZjDISGFEPiC5aYToJIlvfGW{cHjhd4UhdWmlcn;0eYJ2dGW| MY[yN|c6QDZ6MB?=
PC12 MmfXSpVv[3Srb36gZZN{[Xl? NUHyO3FOhjNizszN NF3BfpRFVVOR MUL1dE1z\We3bHH0[ZMh[W62aT3vfIll[XSrdnWg[4Vv\SCneIDy[ZN{cW:wIILlcIF1\WRidH:geJJidnOlcnnweIlwdiCoYXP0c5IhYEKSMYO= NUTjbo1yOjR7MEm2PFY>
PC12 NXjpbVQ{T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MWf+N{DPxE1? MYjEUXNQ MXzy[ZZmenOnIFiyU|IucW6mdXPl[EBoem:5dHigbY5pcWKrdHnvci=> MV6yOFkxQTZ6Nh?=
HEK293T MV\GeY5kfGmxbjDhd5NigQ>? M2XLbZ4{KM7:TR?= MkHQSG1UVw>? M{m1WpVxNXKnZ4XsZZRm\CC[QmCxd{Bxem:2ZXnuJIxmfmWu M{LDeVI1QTB7Nki2
HEK293T MYjGeY5kfGmxbjDhd5NigQ>? Mmi1glMh|ryP NHPJcmZFVVOR MmS5[IVt[Xm|IGjCVFF{KHC{b4TlbY4h\GWpcnHkZZRqd25idnnhJIFk\XS7bHH0bY9vNW2nZHnheIVlKHC{b4TlZZNwdWGuIHTl[5Ji\GG2aX;u NFLFUlIzPDlyOU[4Oi=>
Huh7 NGXxNWxHfW6ldHnvckBie3OjeR?= MX\+OUDPxE1? NWXwS2ZoTE2VTx?= NYHiR2Y5e3WycILld5NmeyCycn;sbYZmemG2aX;uJI9nKGincHH0bZRqeyCFII\pdpV{KHKncHzpZ49vKHerdHigSWM2OCB;IECuN{DPxE1? MU[yOVExQDN{Nh?=
SKMEL21 NEeyW3FIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MWP+OVAxKG6P NXzDVIlxTE2VTx?= NYXGdnhWcW6qaXLpeJMh[2WubDDwdo9tcW[ncnH0bY9v MnH4NlU6PTd6MUK=
SKMEL103 NYPzd4hDT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= Mn71glUxOCCwTR?= NGe4RlFFVVOR NVz2VYtQcW6qaXLpeJMh[2WubDDwdo9tcW[ncnH0bY9v NELGRoQzPTl3N{ixNi=>
SKMEL28 Mmj4S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NF;Ke2t,PTByIH7N MV;EUXNQ NVjUPGV{cW6qaXLpeJMh[2WubDDwdo9tcW[ncnH0bY9v MVyyOVk2PzhzMh?=
WM164 NUnXNldnT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M1\F[J42ODBibl2= NWjUPXc3TE2VTx?= NIO4[4dqdmirYnn0d{Bk\WyuIIDyc4xq\mW{YYTpc44> M2HUZ|I2QTV5OEGy
WM1361a NG\qd4xIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MXr+OVAxKG6P MVLEUXNQ NW\tdWpucW6qaXLpeJMh[2WubDDwdo9tcW[ncnH0bY9v MkXPNlU6PTd6MUK=
WM1366 MUfHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NU\IXINDhjVyMDDuUS=> Mk\iSG1UVw>? NGrQb2ZqdmirYnn0d{Bk\WyuIIDyc4xq\mW{YYTpc44> MVGyOVk2PzhzMh?=
WM793 NVz4dGlLT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MlHiglUxOCCwTR?= MnXISG1UVw>? MVPpcohq[mm2czDj[YxtKHC{b3zp[oVz[XSrb36= MXqyOVk2PzhzMh?=
WM35 MnzhS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MYr+OVAxKG6P MlnqSG1UVw>? NVrBbJAxcW6qaXLpeJMh[2WubDDwdo9tcW[ncnH0bY9v MVGyOVk2PzhzMh?=
WM983a MoLUS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MnjJglUxOCCwTR?= NF3FS3ZFVVOR M3fPU4lvcGmkaYTzJINmdGxicILvcIln\XKjdHnvci=> M{TiTlI2QTV5OEGy
WM793 NU\scWt7TnWwY4Tpc44h[XO|YYm= NFXM[o5,PiEQvF2= NIO0cpRFVVOR MkHpbY5lfWOnIFexJIFzemW|dB?= NEXDNlUzPTl3N{ixNi=>
WM164 MoriSpVv[3Srb36gZZN{[Xl? M1jiZZ43KM7:TR?= NFLESGNFVVOR NIT2eHdqdmS3Y3WgS|Eh[XK{ZYP0 NH7rOpgzPTl3N{ixNi=>
WM983a NGD5ZVZHfW6ldHnvckBie3OjeR?= M1W0TJ43KM7:TR?= NIP5SFdFVVOR MX;pcoR2[2ViR{GgZZJz\XO2 NX3xdmRKOjV7NUe4NVI>
WM164 MYLGeY5kfGmxbjDhd5NigQ>? NVrEXJlMhjNizszN NXfIbpVKTE2VTx?= MWjheYdu\W62czDlfJBz\XO|aX;uJI9nKE2KQzDjcIF{eyCLIHHu[EBu\Wyjbn;tZUBie3OxY3nheIVlKGGwdHnn[Y5{ Mlj6NlU6PTd6MUK=
WM983a MmfmSpVv[3Srb36gZZN{[Xl? MmfuglMh|ryP MVXEUXNQ NFKwZoxifWevZX70d{BmgHC{ZYPzbY9vKG:oIF3IR{BkdGG|czDJJIFv\CCvZXzhco9u[SCjc4PvZ4lifGWmIHHueIlo\W6| M4i3[FI2QTV5OEGy
IPC298 M3XoTmZ2dmO2aX;uJIF{e2G7 MXn+N{DPxE1? MknFSG1UVw>? NYWwN5RP[XWpbXXueJMh\XiycnXzd4lwdiCxZjDNTGMh[2yjc4OgTUBidmRibXXsZY5wdWFiYYPzc4Nq[XSnZDDhcpRq\2Wwcx?= M33JS|I2QTV5OEGy
SKMEL30 Mkn5SpVv[3Srb36gZZN{[Xl? NUTqVJR1hjNizszN M{jrOmROW09? NVjpcY8z[XWpbXXueJMh\XiycnXzd4lwdiCxZjDNTGMh[2yjc4OgTUBidmRibXXsZY5wdWFiYYPzc4Nq[XSnZDDhcpRq\2Wwcx?= MWWyOVk2PzhzMh?=
TCa83 NVvCeZZZTnWwY4Tpc44h[XO|YYm= NVjMcXhNcW6mdXPld{BRXEWQIHX4dJJme3Orb36gZY5lKG2nbXLyZY5mKHS{YX7zcI9k[XSrb36= NVnidVRTOjZ{N{mzNFM>
293T NXPUWokyTnWwY4Tpc44h[XO|YYm= M1LseZ4zKM7:Zz;tcC=> MWfpcoR2[2W|IGDUSW4h\XiycnXzd4lwdiCjbnSgcYVu[nKjbnWgeJJidnOub3PheIlwdg>? M1u2VFI3Ojd7M{Cz
SACC-83 M3nIRWZ2dmO2aX;uJIF{e2G7 MmjjglIh|rypL33s NUHlU2h4cW6mdXPld{BRXEWQIHX4dJJme3Orb36gZY5lKG2nbXLyZY5mKHS{YX7zcI9k[XSrb36= NYfEbYI6OjZ{N{mzNFM>
293T MVXGeY5kfGmxbjDhd5NigQ>? MYf+NkDPxGdxbXy= MUXpcoR2[2W|IGDUSW4h[WOndInsZZRqd25iYYSgT|E3Ow>? MWKyOlI4QTNyMx?=
U-87 MG NEm4U5BHfW6ldHnvckBie3OjeR?= MkPrglIh|rypL33s MUTpcohq[mm2czD0bIUhdWmpcnH0bY9vKGGwZDDpcpZie2mxbh?= NGTybWkzPjJ5OUOwNy=>
U-87 MG MVzGeY5kfGmxbjDhd5NigQ>? M3HCeZ4yOCEQvF2= Mly1bY5pcWKrdIOgRWtVKHCqb4PwbI9zgWyjdHnvci=> NHvH[ZYzPjJ5OUOwNy=>
U-87 MG Mom2S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NYPVbpRVhjFyIN88US=> M33TPYlvcGmkaYTzJINmdGxiZ4Lve5Rp Mo[zNlYzPzl|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 slightly soluble or insoluble
Ethanol slightly soluble or insoluble
In vivo 1% DMSO+30% polyethylene glycol+1% Tween 80 30 mg/mL

* 1 mg/ml means slightly soluble or insoluble.
* 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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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.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID