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 MoL2T4lv[XOnIHHzd4F6 MojKNk42KM7:TR?= MoWwSG1UVw>? NGG4RpNqdmS3Y3XzJO6yNXS3YoXsbY4hcHmyZYLhZ4V1gWyjdHnvci=> NIfVTmozODZzNEmzOi=>
neuron cultures MUHGeY5kfGmxbjDhd5NigQ>? M33h[54yOCEQvF2= MV3EUXNQ MknRdJJwfGWldIOgZYdicW6|dDDncJV1[XSqaX;u[UBl\XCuZYTpc44ucW6mdXPl[EBwgGmmYYTpeoUhe3S{ZYPz NH2wSWIzODZzNEmzOi=>
134/04 NYXCV5dOTnWwY4Tpc44h[XO|YYm= NXPjcWJFPy53INM1US=> MUXpcZBicXK|IH35c5R2[mViZn;ycYF1cW:w M3fqZVIzOTd2OEO5
C2C12 NEDaUllHfW6ldHnvckBie3OjeR?= Mk\QO{42KML3TR?= M2D1fIlueGGrcoOgcZlwfHWkZTDmc5Ju[XSrb36= MWGyNlE4PDh|OR?=
HaCaT keratinocytes M37QTGZ2dmO2aX;uJIF{e2G7 NED3OJAyOCEQvF2= MkjVZoxw[2u|IHHyd4VvcXSnIH\yc40hcW6mdXPpcochVnKoMjDwdo91\WmwIITyZY5{dGG2aX;u M3\kRVIzOzZ5Nki5
JURL-MK1 NXXFclB3TnWwY4Tpc44h[XO|YYm= NGLCe4gyOCEQvF2= M2XzNoVvcGGwY3XzJINmdGxiYXTo[ZNqfmm2eTD0c{BncWK{b37lZ5Rqdg>? MkjhNlMxOjJ3OEO=
CML-T1 NIrxU|FHfW6ldHnvckBie3OjeR?= NVXUSW9EOTBizszN MV3lcohidmOnczDj[YxtKGGmaHXzbZZqfHlidH:g[oljem:wZXP0bY4> M4PMbVI{ODJ{NUiz
K562 MX7GeY5kfGmxbjDhd5NigQ>? MUSxNEDPxE1? NV62c4hC\W6qYX7j[ZMh[2WubDDh[Ihme2m4aYT5JJRwKG[rYoLvcoVkfGmw MmW0NlMxOjJ3OEO=
HL-60 NXHMUFJSTnWwY4Tpc44h[XO|YYm= MYmxNEDPxE1? MWPlcohidmOnczDj[YxtKGGmaHXzbZZqfHlidH:g[oljem:wZXP0bY4> NXTJbmNrOjNyMkK1PFM>
KMCH MX7Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MlLLglExKM7:TR?= MWTk[YNz\WG|ZYOgdJJwdGmoZYLheIlwdiCjbnSgZY5kcG:{YXflMYlv\GWyZX7k[Y51KGe{b4f0bC=> MUSyN|M4ODN{Nx?=
THP-1 NGj5NIVHfW6ldHnvckBie3OjeR?= M3rtcZ4yOCEQvF2= NFLmR3lqdmirYnn0d{BVVkZvzsGgZY5lKEmOLU[gd4VkemW2aX;u NELEXZkzOzV2MU[zOC=>
RAW 264.7 MmLISpVv[3Srb36gZZN{[Xl? NFPoNph,OTBizszN NX7mV4J{[XS2ZX71ZZRmeyCQTzDwdo9lfWO2aX;u NFS1cpYzOzV2MU[zOC=>
HT3 M3;1N2Z2dmO2aX;uJIF{e2G7 NIHkU|F,PSEQvF2= NIDWZYxFVVOR M3LFc4lv\HWlZYOgeIhmKGSrZn\ldoVvfGmjbDFOtU11fWK3bHnuJIFk\XS7bHH0bY9v M3S1SVI{Pjl6NE[4
SiHa MlfFSpVv[3Srb36gZZN{[Xl? NXzTcFF3hjVizszN Mmq5SG1UVw>? M3H4folv\HWlZYOgeIhmKGSrZn\ldoVvfGmjbDFOtU11fWK3bHnuJIFk\XS7bHH0bY9v M1zCZVI{Pjl6NE[4
CaSki MonNSpVv[3Srb36gZZN{[Xl? M4PGbZ42KM7:TR?= MlnSSG1UVw>? MnzmbY5lfWOnczD0bIUh\GmoZnXy[Y51cWGuIN8xMZR2[nWuaX6gZYNmfHmuYYTpc44> NFGw[ZYzOzZ7OES2PC=>
SiHa MXjGeY5kfGmxbjDhd5NigQ>? NFf0PWh,PSEQvF2= NHvY[JNFVVOR MmPZbY5pcWKrdIOgWIhieHOrZ3Hy[4lvNSCxcjDFS2YucW6mdXPl[EBUV0OHIHHjeIl3[XSrb36= MVWyN|Y6QDR4OB?=
CaSki MoPESpVv[3Srb36gZZN{[Xl? MljxglUh|ryP NY[0ZVZRTE2VTx?= MUTpcohq[mm2czDUbIFxe2mpYYLnbY4uKG:{IFXHSk1qdmS3Y3XkJHNQS0ViYXP0bZZifGmxbh?= MXGyN|Y6QDR4OB?=
MCF-7 MUDHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NVHXc4FFOzBizszN MX3EUXNQ M1HlOWlEPTB;MUWg{txO MnPSNlM4QTh4OEC=
MCF-7 Mlj0SpVv[3Srb36gZZN{[Xl? NUnNfnJlOzBizszN M{\BeGROW09? MofSbY5kemWjc3XzJJRp\SCvaXPyc5R2[nWuZTDhZ4V1gWyjdHnvckBt\X[nbD6= MX:yN|c6QDZ6MB?=
MCF-7 NVK0WZdMTnWwY4Tpc44h[XO|YYm= M{mxVFMxKM7:TR?= NH;aUJJFVVOR MXvzeIFjcWyrenXzJI1q[3KxdIXieYxmeyCjZ3HpcpN1KGOxbHStbY5lfWOnZDDk[ZBwdHmvZYLpfoF1cW:w MmXINlM4QTh4OEC=
MCF-7 M2P6Z2Z2dmO2aX;uJIF{e2G7 NWTvfGs5OTVizszN MnjvSG1UVw>? NVXGT3g3e3SjYnnsbZpmeyCvaXPyc5R2[nWuZYOgZYdicW6|dDDuc4Nw\GG8b3zlMYlv\HWlZXSg[Il{[XO|ZX3icJk> MVWyN|c6QDZ6MB?=
MCF-7 NELPbHJHfW6ldHnvckBie3OjeR?= NYXje3p2OzBizszN NHLtZ3VFVVOR NFTSdJFidHSncnXzJJRp\SCjc4PlcYJtgSCmeX7hcYlkeyCxZjDpcpRmenCqYYPlJI1q[3KxdIXieYxmew>? M{fOfFI{Pzl6Nkiw
MCF-7 NIG1NmJHfW6ldHnvckBie3OjeR?= NEWyNG8{OCEQvF2= MVrEUXNQ NHLmRoxqdmO{ZXHz[ZMhfGinIHLpcoRqdmdib3[gTGRCSzZid3n0bEBqdnSncoDoZZNmKG2rY4LveJVjfWyncx?= M2C4RVI{Pzl6Nkiw
PC12 NYm0ZXlETnWwY4Tpc44h[XO|YYm= NWXRUFVShjNizszN NUL4enVqTE2VTx?= NVzP[|VifXBvcnXneYxifGW|IHHueIkud3irZHH0bZZmKGenbnWg[ZhxemW|c3nvckBz\WyjdHXkJJRwKHS{YX7zZ5JqeHSrb36g[oFkfG:{IGjCVFF{ NUC0bnBVOjR7MEm2PFY>
PC12 MV\Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M{PJPZ4{KM7:TR?= NVSxVmtjTE2VTx?= MXfy[ZZmenOnIFiyU|IucW6mdXPl[EBoem:5dHigbY5pcWKrdHnvci=> NXfGTVFkOjR7MEm2PFY>
HEK293T Mn;zSpVv[3Srb36gZZN{[Xl? MVj+N{DPxE1? MVzEUXNQ M2LJepVxNXKnZ4XsZZRm\CC[QmCxd{Bxem:2ZXnuJIxmfmWu M17TflI1QTB7Nki2
HEK293T MoTUSpVv[3Srb36gZZN{[Xl? M{PlNp4{KM7:TR?= Ml:3SG1UVw>? MWHk[YxigXNiWFLQNZMheHKxdHXpckBl\We{YXTheIlwdiC4aXGgZYNmfHmuYYTpc44udWWmaXH0[YQheHKxdHXhd49u[WxiZHXndoFl[XSrb36= M2DiZ|I1QTB7Nki2
Huh7 MXPGeY5kfGmxbjDhd5NigQ>? NGHqVYt,PSEQvF2= NV7MR29lTE2VTx?= MYDzeZBxemW|c3XzJJBzd2yrZnXyZZRqd25ib3[gbIVx[XSrdHnzJGMhfmm{dYOgdoVxdGmlb36ge4l1cCCHQ{WwJF0hOC5|IN88US=> NXyyVHB{OjVzMEizNlY>
SKMEL21 MYHHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MUH+OVAxKG6P MVTEUXNQ M1XUcolvcGmkaYTzJINmdGxicILvcIln\XKjdHnvci=> MnTKNlU6PTd6MUK=
SKMEL103 M37kW2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MkLmglUxOCCwTR?= M1\WSGROW09? M3;ubYlvcGmkaYTzJINmdGxicILvcIln\XKjdHnvci=> MXiyOVk2PzhzMh?=
SKMEL28 NVjZ[4tGT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M4rvO542ODBibl2= NITz[2hFVVOR NIroVVhqdmirYnn0d{Bk\WyuIIDyc4xq\mW{YYTpc44> NEL3RXQzPTl3N{ixNi=>
WM164 Ml76S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NF35RoN,PTByIH7N MmLMSG1UVw>? MkSwbY5pcWKrdIOgZ4VtdCCycn;sbYZmemG2aX;u M{\nPFI2QTV5OEGy
WM1361a MUHHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NIK4bVZ,PTByIH7N M4q0XmROW09? NFLPVFJqdmirYnn0d{Bk\WyuIIDyc4xq\mW{YYTpc44> M2Dad|I2QTV5OEGy
WM1366 MmOzS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MlO0glUxOCCwTR?= MoTqSG1UVw>? MoTzbY5pcWKrdIOgZ4VtdCCycn;sbYZmemG2aX;u NWDlPVlXOjV7NUe4NVI>
WM793 NIrJRWJIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MVn+OVAxKG6P NVfER|c6TE2VTx?= NVjjdXJUcW6qaXLpeJMh[2WubDDwdo9tcW[ncnH0bY9v MmPyNlU6PTd6MUK=
WM35 MlvlS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MmXUglUxOCCwTR?= Mli5SG1UVw>? MV3pcohq[mm2czDj[YxtKHC{b3zp[oVz[XSrb36= MXeyOVk2PzhzMh?=
WM983a NWLCZlBQT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MUP+OVAxKG6P M1ztb2ROW09? M2H2S4lvcGmkaYTzJINmdGxicILvcIln\XKjdHnvci=> NEPVTpMzPTl3N{ixNi=>
WM793 MV\GeY5kfGmxbjDhd5NigQ>? NWfKfo9ohjZizszN NIHXdI9FVVOR MXHpcoR2[2ViR{GgZZJz\XO2 M4fNe|I2QTV5OEGy
WM164 MYnGeY5kfGmxbjDhd5NigQ>? NG\2WWt,PiEQvF2= MWjEUXNQ NV\LdXg2cW6mdXPlJGcyKGG{cnXzeC=> NF[1c2ozPTl3N{ixNi=>
WM983a M3PR[mZ2dmO2aX;uJIF{e2G7 M1X4Np43KM7:TR?= M4nx[GROW09? MWfpcoR2[2ViR{GgZZJz\XO2 MlTnNlU6PTd6MUK=
WM164 NGXkV|NHfW6ldHnvckBie3OjeR?= M1qz[p4{KM7:TR?= NVTCR4tvTE2VTx?= NWXVeZhk[XWpbXXueJMh\XiycnXzd4lwdiCxZjDNTGMh[2yjc4OgTUBidmRibXXsZY5wdWFiYYPzc4Nq[XSnZDDhcpRq\2Wwcx?= Mk\5NlU6PTd6MUK=
WM983a MWDGeY5kfGmxbjDhd5NigQ>? MUj+N{DPxE1? NUPPeZJGTE2VTx?= MVjheYdu\W62czDlfJBz\XO|aX;uJI9nKE2KQzDjcIF{eyCLIHHu[EBu\Wyjbn;tZUBie3OxY3nheIVlKGGwdHnn[Y5{ NF74eVAzPTl3N{ixNi=>
IPC298 NWDJTYpnTnWwY4Tpc44h[XO|YYm= NX7MSIgzhjNizszN MYfEUXNQ M3TKbYF2\22nboTzJIV5eHKnc4Ppc44hd2ZiTVjDJINt[XO|IFmgZY5lKG2nbHHuc41iKGG|c3;jbYF1\WRiYX70bYdmdnN? NIrnZ5MzPTl3N{ixNi=>
SKMEL30 NXX0PYVmTnWwY4Tpc44h[XO|YYm= M4PKRp4{KM7:TR?= NFTvXZhFVVOR NIDmSZpifWevZX70d{BmgHC{ZYPzbY9vKG:oIF3IR{BkdGG|czDJJIFv\CCvZXzhco9u[SCjc4PvZ4lifGWmIHHueIlo\W6| NXva[Xk3OjV7NUe4NVI>
TCa83 MWXGeY5kfGmxbjDhd5NigQ>? Ml\SbY5lfWOnczDQWGVPKGW6cILld5Nqd25iYX7kJI1mdWK{YX7lJJRz[W6|bH;jZZRqd25? MlX0NlYzPzl|MEO=
293T M3PS[2Z2dmO2aX;uJIF{e2G7 M3f2XJ4zKM7:Zz;tcC=> NIGzcYpqdmS3Y3XzJHBVTU5iZYjwdoV{e2mxbjDhcoQhdWWvYoLhcoUhfHKjboPsc4NifGmxbh?= M4TXXlI3Ojd7M{Cz
SACC-83 NVPFcWpvTnWwY4Tpc44h[XO|YYm= MlnsglIh|rypL33s MWDpcoR2[2W|IGDUSW4h\XiycnXzd4lwdiCjbnSgcYVu[nKjbnWgeJJidnOub3PheIlwdg>? M{\Ld|I3Ojd7M{Cz
293T NGDQXY9HfW6ldHnvckBie3OjeR?= MXL+NkDPxGdxbXy= Mom1bY5lfWOnczDQWGVPKGGlZYT5cIF1cW:wIHH0JGsyPjN? M37Hc|I3Ojd7M{Cz
U-87 MG MmmwSpVv[3Srb36gZZN{[Xl? MUD+NkDPxGdxbXy= NF:zOZdqdmirYnn0d{B1cGVibXnndoF1cW:wIHHu[EBqdn[jc3nvci=> Mo\DNlYzPzl|MEO=
U-87 MG M{XhUWZ2dmO2aX;uJIF{e2G7 NXvtXphkhjFyIN88US=> NEXYUnhqdmirYnn0d{BCU1RicHjvd5Bpd3K7bHH0bY9v M2G3S|I3Ojd7M{Cz
U-87 MG MoT5S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NGfTd3N,OTBizszN MYfpcohq[mm2czDj[YxtKGe{b4f0bC=> MnLwNlYzPzl|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 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