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 MVjLbY5ie2ViYYPzZZk> NVXlRoFlOi53IN88US=> M1PUZmROW09? MUnpcoR2[2W|IN8xMZR2[nWuaX6gbJlx\XKjY3X0fYxifGmxbh?= MkLCNlA3OTR7M{[=
neuron cultures NGnDTplHfW6ldHnvckBie3OjeR?= NYPBepFzhjFyIN88US=> NUPCUodsTE2VTx?= MV7wdo91\WO2czDh[4FqdnO2IHfseZRifGirb37lJIRmeGyndHnvck1qdmS3Y3XkJI95cWSjdHn2[UB{fHKnc4O= NFjCbG8zODZzNEmzOi=>
134/04 Mn7MSpVv[3Srb36gZZN{[Xl? MV63MlUhyrWP NWPIelJScW2yYXnyd{BugW:2dXLlJIZwem2jdHnvci=> NGPqcm4zOjF5NEizPS=>
C2C12 NUSwR4hkTnWwY4Tpc44h[XO|YYm= NFnadGc4NjViwsXN MkHhbY1x[Wm{czDtfY91fWKnIH\vdo1ifGmxbh?= Mn\MNlIyPzR6M{m=
HaCaT keratinocytes NYn1RoY3TnWwY4Tpc44h[XO|YYm= MXmxNEDPxE1? NGLsSGxjdG:la4OgZZJ{\W6rdHWg[pJwdSCrbnT1Z4lv\yCQcn[yJJBzd3SnaX6geJJidnOuYYTpc44> MXmyNlM3PzZ6OR?=
JURL-MK1 NWHFRWdxTnWwY4Tpc44h[XO|YYm= NEXv[VAyOCEQvF2= NGXkVmlmdmijbnPld{Bk\WyuIHHkbIV{cX[rdImgeI8h\mmkcn;u[YN1cW5? MnT0NlMxOjJ3OEO=
CML-T1 MWrGeY5kfGmxbjDhd5NigQ>? MXmxNEDPxE1? NX[5cY5[\W6qYX7j[ZMh[2WubDDh[Ihme2m4aYT5JJRwKG[rYoLvcoVkfGmw NGPNbnMzOzB{MkW4Ny=>
K562 MmrGSpVv[3Srb36gZZN{[Xl? MUexNEDPxE1? M3n2dIVvcGGwY3XzJINmdGxiYXTo[ZNqfmm2eTD0c{BncWK{b37lZ5Rqdg>? NYHHOGhZOjNyMkK1PFM>
HL-60 MoTjSpVv[3Srb36gZZN{[Xl? NHj6ZYUyOCEQvF2= M2OzToVvcGGwY3XzJINmdGxiYXTo[ZNqfmm2eTD0c{BncWK{b37lZ5Rqdg>? NXnmcnhVOjNyMkK1PFM>
KMCH MWDHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MoWyglExKM7:TR?= NYfad5h2\GWlcnXhd4V{KHC{b3zp[oVz[XSrb36gZY5lKGGwY3jvdoFo\S2rbnTldIVv\GWwdDDndo94fGh? MXKyN|M4ODN{Nx?=
THP-1 NFnsSZBHfW6ldHnvckBie3OjeR?= M1vUcJ4yOCEQvF2= NYnINFY6cW6qaXLpeJMhXE6ILd8xJIFv\CCLTD22JJNm[3KndHnvci=> NEPTOpAzOzV2MU[zOC=>
RAW 264.7 MX;GeY5kfGmxbjDhd5NigQ>? Mm\3glExKM7:TR?= M2K1SoF1fGWwdXH0[ZMhVk9icILv[JVkfGmxbh?= MmPlNlM2PDF4M{S=
HT3 NFLXN5FHfW6ldHnvckBie3OjeR?= MorLglUh|ryP NV\aSpR1TE2VTx?= MWXpcoR2[2W|IITo[UBlcW[oZYLlcpRq[WxizsGteJVjfWyrbjDhZ4V1gWyjdHnvci=> MViyN|Y6QDR4OB?=
SiHa M2XYZmZ2dmO2aX;uJIF{e2G7 Mo\lglUh|ryP MlrmSG1UVw>? NYfNeXlCcW6mdXPld{B1cGViZHnm[oVz\W62aXHsJO6yNXS3YoXsbY4h[WOndInsZZRqd25? NELObGQzOzZ7OES2PC=>
CaSki MYjGeY5kfGmxbjDhd5NigQ>? M37PR542KM7:TR?= NXz1V3U4TE2VTx?= MWrpcoR2[2W|IITo[UBlcW[oZYLlcpRq[WxizsGteJVjfWyrbjDhZ4V1gWyjdHnvci=> M4LTVVI{Pjl6NE[4
SiHa NHr6WlJHfW6ldHnvckBie3OjeR?= MonVglUh|ryP NH\sSIVFVVOR NUHvPGg{cW6qaXLpeJMhXGijcIPp[4Fz\2mwLTDvdkBGT0ZvaX7keYNm\CCVT1PFJIFkfGm4YYTpc44> NWnSU4JQOjN4OUi0Olg>
CaSki M{PhUWZ2dmO2aX;uJIF{e2G7 M13Vcp42KM7:TR?= MknsSG1UVw>? MlzzbY5pcWKrdIOgWIhieHOrZ3Hy[4lvNSCxcjDFS2YucW6mdXPl[EBUV0OHIHHjeIl3[XSrb36= Mmn4NlM3QTh2Nki=
MCF-7 M4q1Zmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NW[2e4RmOzBizszN M1vibGROW09? M13PemlEPTB;MUWg{txO NW\w[pNIOjN5OUi2PFA>
MCF-7 NWnmdZhuTnWwY4Tpc44h[XO|YYm= NFfsdlk{OCEQvF2= MlHSSG1UVw>? NEn5XWNqdmO{ZXHz[ZMhfGinIH3pZ5JwfHWkdXzlJIFk\XS7bHH0bY9vKGyndnXsMi=> NIjUSoYzOzd7OE[4NC=>
MCF-7 NV\s[WFwTnWwY4Tpc44h[XO|YYm= MnLwN|Ah|ryP M{\2[WROW09? MlPWd5Ri[mmuaYrld{BucWO{b4T1ZpVt\XNiYXfhbY5{fCClb3zkMYlv\HWlZXSg[IVxd2y7bXXybZpifGmxbh?= MoO1NlM4QTh4OEC=
MCF-7 M4rOXGZ2dmO2aX;uJIF{e2G7 NXjRd4x4OTVizszN MlLHSG1UVw>? NIP6eIt{fGGkaXzpfoV{KG2rY4LveJVjfWynczDh[4FqdnO2IH7vZ49l[XqxbHWtbY5lfWOnZDDkbZNie3OnbXLsfS=> M4nIN|I{Pzl6Nkiw
MCF-7 NHmyT3VHfW6ldHnvckBie3OjeR?= MkDhN|Ah|ryP Mmf5SG1UVw>? NIKyXppidHSncnXzJJRp\SCjc4PlcYJtgSCmeX7hcYlkeyCxZjDpcpRmenCqYYPlJI1q[3KxdIXieYxmew>? NXv4dldOOjN5OUi2PFA>
MCF-7 NGHEU3RHfW6ldHnvckBie3OjeR?= M1P0T|MxKM7:TR?= Mmi2SG1UVw>? MmPBbY5kemWjc3XzJJRp\SCkaX7kbY5oKG:oIFjERWM3KHerdHigbY51\XKyaHHz[UBucWO{b4T1ZpVt\XN? MVSyN|c6QDZ6MB?=
PC12 NFLmbG1HfW6ldHnvckBie3OjeR?= Ml\BglMh|ryP MXzEUXNQ NIXaenR2eC2{ZXf1cIF1\XNiYX70bU1wgGmmYYTpeoUh\2WwZTDlfJBz\XO|aX;uJJJmdGG2ZXSgeI8hfHKjboPjdolxfGmxbjDmZYN1d3JiWFLQNZM> MVmyOFkxQTZ6Nh?=
PC12 MoLoS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MkDhglMh|ryP NV3oTZBETE2VTx?= MliwdoV3\XK|ZTDINm8zNWmwZIXj[YQh\3Kxd4ToJIlvcGmkaYTpc44> MVuyOFkxQTZ6Nh?=
HEK293T NVrOU5o1TnWwY4Tpc44h[XO|YYm= MmHsglMh|ryP M{H2VmROW09? MWj1dE1z\We3bHH0[YQhYEKSMYOgdJJwfGWrbjDs[ZZmdA>? MXWyOFkxQTZ6Nh?=
HEK293T M332WmZ2dmO2aX;uJIF{e2G7 MVL+N{DPxE1? M2j3UmROW09? MYrk[YxigXNiWFLQNZMheHKxdHXpckBl\We{YXTheIlwdiC4aXGgZYNmfHmuYYTpc44udWWmaXH0[YQheHKxdHXhd49u[WxiZHXndoFl[XSrb36= MUSyOFkxQTZ6Nh?=
Huh7 MnXFSpVv[3Srb36gZZN{[Xl? Mk\yglUh|ryP NH\l[3ZFVVOR M3TxZ5N2eHC{ZYPz[ZMheHKxbHnm[ZJifGmxbjDv[kBp\XCjdHn0bZMhSyC4aYL1d{Bz\XCuaXPvckB4cXSqIFXDOVAhRSByLkOg{txO MY[yOVExQDN{Nh?=
SKMEL21 M2q5N2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MojmglUxOCCwTR?= NGDueYpFVVOR NYm5XFAxcW6qaXLpeJMh[2WubDDwdo9tcW[ncnH0bY9v NGjvSGQzPTl3N{ixNi=>
SKMEL103 NHTJdnBIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MonPglUxOCCwTR?= NYfwblNzTE2VTx?= M3f4[4lvcGmkaYTzJINmdGxicILvcIln\XKjdHnvci=> M1;1cFI2QTV5OEGy
SKMEL28 Ml32S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NXzWTpAyhjVyMDDuUS=> NY\JWlNHTE2VTx?= MnzEbY5pcWKrdIOgZ4VtdCCycn;sbYZmemG2aX;u M4jGblI2QTV5OEGy
WM164 MX7Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NYnBNmNZhjVyMDDuUS=> M{PJXmROW09? MWTpcohq[mm2czDj[YxtKHC{b3zp[oVz[XSrb36= MmfBNlU6PTd6MUK=
WM1361a NIPTfmJIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M1rFZp42ODBibl2= M1HqbGROW09? NIXqXWxqdmirYnn0d{Bk\WyuIIDyc4xq\mW{YYTpc44> M{\hUFI2QTV5OEGy
WM1366 NFnO[XdIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NIjlN4p,PTByIH7N NXrpOHA5TE2VTx?= M1izOYlvcGmkaYTzJINmdGxicILvcIln\XKjdHnvci=> MnPlNlU6PTd6MUK=
WM793 Ml3RS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NG[3SHB,PTByIH7N Ml3vSG1UVw>? NUntbWVlcW6qaXLpeJMh[2WubDDwdo9tcW[ncnH0bY9v NUnidnNwOjV7NUe4NVI>
WM35 M1vWXmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MnrGglUxOCCwTR?= NIrNe3pFVVOR NXPKUWtVcW6qaXLpeJMh[2WubDDwdo9tcW[ncnH0bY9v NF\2RnUzPTl3N{ixNi=>
WM983a MUfHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? Mnj1glUxOCCwTR?= MVzEUXNQ MkXlbY5pcWKrdIOgZ4VtdCCycn;sbYZmemG2aX;u M3PucVI2QTV5OEGy
WM793 MlPFSpVv[3Srb36gZZN{[Xl? NHTYUHZ,PiEQvF2= MoDmSG1UVw>? M1zscYlv\HWlZTDHNUBienKnc4S= MXKyOVk2PzhzMh?=
WM164 NX7l[FlZTnWwY4Tpc44h[XO|YYm= MXz+OkDPxE1? M1nKZmROW09? NUCwNoFRcW6mdXPlJGcyKGG{cnXzeC=> MXOyOVk2PzhzMh?=
WM983a M1\I[GZ2dmO2aX;uJIF{e2G7 NHPlfWh,PiEQvF2= M4PqbGROW09? NF65T|dqdmS3Y3WgS|Eh[XK{ZYP0 MonoNlU6PTd6MUK=
WM164 M2LibGZ2dmO2aX;uJIF{e2G7 M{DqUp4{KM7:TR?= MXXEUXNQ MV\heYdu\W62czDlfJBz\XO|aX;uJI9nKE2KQzDjcIF{eyCLIHHu[EBu\Wyjbn;tZUBie3OxY3nheIVlKGGwdHnn[Y5{ NGLPO4UzPTl3N{ixNi=>
WM983a NFvnfZlHfW6ldHnvckBie3OjeR?= MlfiglMh|ryP MXnEUXNQ MUfheYdu\W62czDlfJBz\XO|aX;uJI9nKE2KQzDjcIF{eyCLIHHu[EBu\Wyjbn;tZUBie3OxY3nheIVlKGGwdHnn[Y5{ MoHSNlU6PTd6MUK=
IPC298 MljOSpVv[3Srb36gZZN{[Xl? NUDRWYlOhjNizszN MU\EUXNQ MnTaZZVodWWwdIOg[ZhxemW|c3nvckBw\iCPSFOgZ4xie3NiSTDhcoQhdWWuYX7vcYEh[XO|b3PpZZRm\CCjboTp[4Vvew>? MYSyOVk2PzhzMh?=
SKMEL30 M3fLU2Z2dmO2aX;uJIF{e2G7 MnuzglMh|ryP NVX3[2xWTE2VTx?= MoDpZZVodWWwdIOg[ZhxemW|c3nvckBw\iCPSFOgZ4xie3NiSTDhcoQhdWWuYX7vcYEh[XO|b3PpZZRm\CCjboTp[4Vvew>? MkCwNlU6PTd6MUK=
TCa83 NGC3NJFHfW6ldHnvckBie3OjeR?= NHPhTWFqdmS3Y3XzJHBVTU5iZYjwdoV{e2mxbjDhcoQhdWWvYoLhcoUhfHKjboPsc4NifGmxbh?= NVHaTGZFOjZ{N{mzNFM>
293T NVLBXZU2TnWwY4Tpc44h[XO|YYm= NFO0fIp,OiEQvHevcYw> NXrIW|ducW6mdXPld{BRXEWQIHX4dJJme3Orb36gZY5lKG2nbXLyZY5mKHS{YX7zcI9k[XSrb36= M1f3WFI3Ojd7M{Cz
SACC-83 MkTlSpVv[3Srb36gZZN{[Xl? NFX0VGt,OiEQvHevcYw> MmDZbY5lfWOnczDQWGVPKGW6cILld5Nqd25iYX7kJI1mdWK{YX7lJJRz[W6|bH;jZZRqd25? M2Hvc|I3Ojd7M{Cz
293T NXPHb|RtTnWwY4Tpc44h[XO|YYm= NWjjco1xhjJizsznM41t NH;NdYRqdmS3Y3XzJHBVTU5iYXPleJlt[XSrb36gZZQhUzF4Mx?= MYGyOlI4QTNyMx?=
U-87 MG M2nNVmZ2dmO2aX;uJIF{e2G7 MYD+NkDPxGdxbXy= MmjmbY5pcWKrdIOgeIhmKG2rZ4LheIlwdiCjbnSgbY53[XOrb36= NXzMUYFUOjZ{N{mzNFM>
U-87 MG NX3DUI06TnWwY4Tpc44h[XO|YYm= MVf+NVAh|ryP MlXnbY5pcWKrdIOgRWtVKHCqb4PwbI9zgWyjdHnvci=> MVOyOlI4QTNyMx?=
U-87 MG M1XHTmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 Mmn4glExKM7:TR?= MWrpcohq[mm2czDj[YxtKGe{b4f0bC=> NXz3TIk6OjZ{N{mzNFM>

... 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