Tubastatin A HCl

For research use only.

Catalog No.S2627 Synonyms: TSA HCl

38 publications

Tubastatin A HCl Chemical Structure

CAS No. 1310693-92-5

Tubastatin A HCl (TSA) 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).

Selleck's Tubastatin A HCl has been cited by 38 publications

Purity & Quality Control

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Biological Activity

Description Tubastatin A HCl (TSA) 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 NV\DOJdLU2mwYYPlJIF{e2G7 Mm\1Nk42KM7:TR?= M2L2[2ROW09? NHjEZZlqdmS3Y3XzJO6yNXS3YoXsbY4hcHmyZYLhZ4V1gWyjdHnvci=> NVrRcnBIOjB4MUS5N|Y>
neuron cultures MUnGeY5kfGmxbjDhd5NigQ>? MVn+NVAh|ryP MlfHSG1UVw>? MnW1dJJwfGWldIOgZYdicW6|dDDncJV1[XSqaX;u[UBl\XCuZYTpc44ucW6mdXPl[EBwgGmmYYTpeoUhe3S{ZYPz NYnxeZVEOjB4MUS5N|Y>
134/04 MYrGeY5kfGmxbjDhd5NigQ>? NW\ObGJPPy53INM1US=> MnHUbY1x[Wm{czDtfY91fWKnIH\vdo1ifGmxbh?= MWqyNlE4PDh|OR?=
C2C12 NVjq[JFwTnWwY4Tpc44h[XO|YYm= NFrsNpk4NjViwsXN MmCzbY1x[Wm{czDtfY91fWKnIH\vdo1ifGmxbh?= Mn\INlIyPzR6M{m=
HaCaT keratinocytes MkL4SpVv[3Srb36gZZN{[Xl? M3XsU|ExKM7:TR?= MWDicI9kc3NiYYLz[Y5qfGViZoLvcUBqdmS3Y3nu[{BPemZ{IIDyc5RmcW5idILhcpNt[XSrb36= Mn\ENlI{Pjd4OEm=
JURL-MK1 M4rzOmZ2dmO2aX;uJIF{e2G7 NUK3d|lNOTBizszN M2PsU4VvcGGwY3XzJINmdGxiYXTo[ZNqfmm2eTD0c{BncWK{b37lZ5Rqdg>? MkHSNlMxOjJ3OEO=
CML-T1 NU\odnBZTnWwY4Tpc44h[XO|YYm= M1m0dlExKM7:TR?= NHXJTotmdmijbnPld{Bk\WyuIHHkbIV{cX[rdImgeI8h\mmkcn;u[YN1cW5? MoTpNlMxOjJ3OEO=
K562 MkHGSpVv[3Srb36gZZN{[Xl? MnO4NVAh|ryP MUXlcohidmOnczDj[YxtKGGmaHXzbZZqfHlidH:g[oljem:wZXP0bY4> MoC1NlMxOjJ3OEO=
HL-60 NYH6cZFGTnWwY4Tpc44h[XO|YYm= M1jZflExKM7:TR?= Mkjk[Y5p[W6lZYOgZ4VtdCCjZHjld4l3cXS7IITvJIZq[nKxbnXjeIlv MmLyNlMxOjJ3OEO=
KMCH MoG4S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MWH+NVAh|ryP MUXk[YNz\WG|ZYOgdJJwdGmoZYLheIlwdiCjbnSgZY5kcG:{YXflMYlv\GWyZX7k[Y51KGe{b4f0bC=> NVTtTIhXOjN|N{CzNlc>
THP-1 M{m5TGZ2dmO2aX;uJIF{e2G7 NIP3NJd,OTBizszN MkfPbY5pcWKrdIOgWG5HNc7zIHHu[EBKVC14IIPlZ5JmfGmxbh?= MlXqNlM2PDF4M{S=
RAW 264.7 NGTnZWFHfW6ldHnvckBie3OjeR?= MUL+NVAh|ryP MlzTZZR1\W63YYTld{BPVyCycn;keYN1cW:w M1;FVFI{PTRzNkO0
HT3 MX7GeY5kfGmxbjDhd5NigQ>? MmnFglUh|ryP MVfEUXNQ MXjpcoR2[2W|IITo[UBlcW[oZYLlcpRq[WxizsGteJVjfWyrbjDhZ4V1gWyjdHnvci=> MUOyN|Y6QDR4OB?=
SiHa M1\qUWZ2dmO2aX;uJIF{e2G7 NGLiNHJ,PSEQvF2= M{DxfGROW09? MULpcoR2[2W|IITo[UBlcW[oZYLlcpRq[WxizsGteJVjfWyrbjDhZ4V1gWyjdHnvci=> MVGyN|Y6QDR4OB?=
CaSki MXrGeY5kfGmxbjDhd5NigQ>? M1rGV542KM7:TR?= NHOxO3BFVVOR MYTpcoR2[2W|IITo[UBlcW[oZYLlcpRq[WxizsGteJVjfWyrbjDhZ4V1gWyjdHnvci=> NXq1bod[OjN4OUi0Olg>
SiHa NGCze3JHfW6ldHnvckBie3OjeR?= NUPhU2VWhjVizszN Mor4SG1UVw>? NXvQVlZrcW6qaXLpeJMhXGijcIPp[4Fz\2mwLTDvdkBGT0ZvaX7keYNm\CCVT1PFJIFkfGm4YYTpc44> M4nobVI{Pjl6NE[4
CaSki M4fFfmZ2dmO2aX;uJIF{e2G7 M4PEXp42KM7:TR?= NIHQOVFFVVOR NGC2OXVqdmirYnn0d{BVcGGyc3nnZZJocW5vIH;yJGVITi2rbnT1Z4VlKFORQ1WgZYN1cX[jdHnvci=> MV6yN|Y6QDR4OB?=
MCF-7 MlzXS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MYSzNEDPxE1? NEfEdXFFVVOR MXnJR|UxRTF3IN88US=> M1riXlI{Pzl6Nkiw
MCF-7 NVr1coJpTnWwY4Tpc44h[XO|YYm= M3PzbFMxKM7:TR?= NXLybm9YTE2VTx?= MWjpcoNz\WG|ZYOgeIhmKG2rY4LveJVjfWynIHHj[ZR6dGG2aX;uJIxmfmWuLh?= NYm3bFIzOjN5OUi2PFA>
MCF-7 NVHKXI42TnWwY4Tpc44h[XO|YYm= MlfiN|Ah|ryP M1zzd2ROW09? MmfTd5Ri[mmuaYrld{BucWO{b4T1ZpVt\XNiYXfhbY5{fCClb3zkMYlv\HWlZXSg[IVxd2y7bXXybZpifGmxbh?= M1SwSVI{Pzl6Nkiw
MCF-7 M4T6U2Z2dmO2aX;uJIF{e2G7 M4K2bVE2KM7:TR?= NVrTfWlzTE2VTx?= NVfXOmpme3SjYnnsbZpmeyCvaXPyc5R2[nWuZYOgZYdicW6|dDDuc4Nw\GG8b3zlMYlv\HWlZXSg[Il{[XO|ZX3icJk> MnnPNlM4QTh4OEC=
MCF-7 NEHpcGhHfW6ldHnvckBie3OjeR?= M3vxV|MxKM7:TR?= M2C2VWROW09? NWPVNVBT[Wy2ZYLld{B1cGViYYPz[Y1jdHliZInuZY1q[3Nib3[gbY51\XKyaHHz[UBucWO{b4T1ZpVt\XN? NXXpUW5iOjN5OUi2PFA>
MCF-7 NUD4PJNDTnWwY4Tpc44h[XO|YYm= MWSzNEDPxE1? NVv0XmJvTE2VTx?= MXTpcoNz\WG|ZYOgeIhmKGKrbnTpcochd2ZiSFTBR|Yhf2m2aDDpcpRmenCqYYPlJI1q[3KxdIXieYxmew>? NXjsSnBIOjN5OUi2PFA>
PC12 M321R2Z2dmO2aX;uJIF{e2G7 NEfyd4t,OyEQvF2= MWrEUXNQ NXTrXFFmfXBvcnXneYxifGW|IHHueIkud3irZHH0bZZmKGenbnWg[ZhxemW|c3nvckBz\WyjdHXkJJRwKHS{YX7zZ5JqeHSrb36g[oFkfG:{IGjCVFF{ MkTkNlQ6ODl4OE[=
PC12 MnPxS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MU\+N{DPxE1? NGLUdIFFVVOR NYjob4VTemW4ZYLz[UBJOk9{LXnu[JVk\WRiZ4Lve5RpKGmwaHnibZRqd25? NU[zT4dWOjR7MEm2PFY>
HEK293T M2npbmZ2dmO2aX;uJIF{e2G7 M{HrUp4{KM7:TR?= NGTSUoZFVVOR NEn6THJ2eC2{ZXf1cIF1\WRiWFLQNZMheHKxdHXpckBt\X[nbB?= M{LsSFI1QTB7Nki2
HEK293T MlrOSpVv[3Srb36gZZN{[Xl? NUHkeYlDhjNizszN NEHGbVNFVVOR NUKxVZNU\GWuYYnzJHhDWDG|IIDyc5RmcW5iZHXndoFl[XSrb36geoliKGGlZYT5cIF1cW:wLX3l[IlifGWmIIDyc5Rm[XOxbXHsJIRm\3KjZHH0bY9v MXWyOFkxQTZ6Nh?=
Huh7 M2nDN2Z2dmO2aX;uJIF{e2G7 NFHGWXR,PSEQvF2= M{n3VWROW09? NUjFOolTe3WycILld5NmeyCycn;sbYZmemG2aX;uJI9nKGincHH0bZRqeyCFII\pdpV{KHKncHzpZ49vKHerdHigSWM2OCB;IECuN{DPxE1? MmS0NlUyODh|Mk[=
SKMEL21 NGnqbnRIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NETKW2Z,PTByIH7N MXnEUXNQ MlXxbY5pcWKrdIOgZ4VtdCCycn;sbYZmemG2aX;u NI\LTVMzPTl3N{ixNi=>
SKMEL103 M2n0dWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MnL3glUxOCCwTR?= NEe0NW9FVVOR M2DKeolvcGmkaYTzJINmdGxicILvcIln\XKjdHnvci=> MUiyOVk2PzhzMh?=
SKMEL28 NEXRfXhIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NH7ydI1,PTByIH7N M{fXTGROW09? MkXwbY5pcWKrdIOgZ4VtdCCycn;sbYZmemG2aX;u Mlf2NlU6PTd6MUK=
WM164 M3vPSWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MXL+OVAxKG6P MUXEUXNQ NHPEeZBqdmirYnn0d{Bk\WyuIIDyc4xq\mW{YYTpc44> MYKyOVk2PzhzMh?=
WM1361a MWHHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NIm2b4x,PTByIH7N M3u3[2ROW09? MXPpcohq[mm2czDj[YxtKHC{b3zp[oVz[XSrb36= MlLQNlU6PTd6MUK=
WM1366 NIHib4NIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NIjPSmV,PTByIH7N NVq0WItWTE2VTx?= NWHjeHpVcW6qaXLpeJMh[2WubDDwdo9tcW[ncnH0bY9v M4PK[FI2QTV5OEGy
WM793 M33zSGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NIT0NXR,PTByIH7N NGTucpBFVVOR M4X5[olvcGmkaYTzJINmdGxicILvcIln\XKjdHnvci=> MXWyOVk2PzhzMh?=
WM35 MoTuS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NH;UR3V,PTByIH7N MXfEUXNQ MUDpcohq[mm2czDj[YxtKHC{b3zp[oVz[XSrb36= MVuyOVk2PzhzMh?=
WM983a MYfHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NUTmXodvhjVyMDDuUS=> M4jhZWROW09? M2fw[olvcGmkaYTzJINmdGxicILvcIln\XKjdHnvci=> MVKyOVk2PzhzMh?=
WM793 NYXnWVUyTnWwY4Tpc44h[XO|YYm= MXr+OkDPxE1? MUfEUXNQ MoXGbY5lfWOnIFexJIFzemW|dB?= MUiyOVk2PzhzMh?=
WM164 M{jlZmZ2dmO2aX;uJIF{e2G7 MYr+OkDPxE1? Ml[xSG1UVw>? NIPHdIFqdmS3Y3WgS|Eh[XK{ZYP0 MlPwNlU6PTd6MUK=
WM983a NXH2eodNTnWwY4Tpc44h[XO|YYm= MXj+OkDPxE1? MVzEUXNQ NWXObGN{cW6mdXPlJGcyKGG{cnXzeC=> MUCyOVk2PzhzMh?=
WM164 MV7GeY5kfGmxbjDhd5NigQ>? M2H5[Z4{KM7:TR?= NEX4VJVFVVOR M4TkUIF2\22nboTzJIV5eHKnc4Ppc44hd2ZiTVjDJINt[XO|IFmgZY5lKG2nbHHuc41iKGG|c3;jbYF1\WRiYX70bYdmdnN? M1y1VVI2QTV5OEGy
WM983a M2q1cGZ2dmO2aX;uJIF{e2G7 Moq0glMh|ryP MYXEUXNQ NYLTemxF[XWpbXXueJMh\XiycnXzd4lwdiCxZjDNTGMh[2yjc4OgTUBidmRibXXsZY5wdWFiYYPzc4Nq[XSnZDDhcpRq\2Wwcx?= M4O0[|I2QTV5OEGy
IPC298 NVLaXnM6TnWwY4Tpc44h[XO|YYm= NFWzZWZ,OyEQvF2= Ml\aSG1UVw>? MVHheYdu\W62czDlfJBz\XO|aX;uJI9nKE2KQzDjcIF{eyCLIHHu[EBu\Wyjbn;tZUBie3OxY3nheIVlKGGwdHnn[Y5{ NEDZb|kzPTl3N{ixNi=>
SKMEL30 NUHVbFJUTnWwY4Tpc44h[XO|YYm= MW\+N{DPxE1? NE\jVmFFVVOR MVXheYdu\W62czDlfJBz\XO|aX;uJI9nKE2KQzDjcIF{eyCLIHHu[EBu\Wyjbn;tZUBie3OxY3nheIVlKGGwdHnn[Y5{ NYPudIZHOjV7NUe4NVI>
TCa83 NGXE[mNHfW6ldHnvckBie3OjeR?= MlHpbY5lfWOnczDQWGVPKGW6cILld5Nqd25iYX7kJI1mdWK{YX7lJJRz[W6|bH;jZZRqd25? NVvCTWRCOjZ{N{mzNFM>
293T MlnQSpVv[3Srb36gZZN{[Xl? NXfCOo1nhjJizsznM41t NVPvUYV[cW6mdXPld{BRXEWQIHX4dJJme3Orb36gZY5lKG2nbXLyZY5mKHS{YX7zcI9k[XSrb36= MVGyOlI4QTNyMx?=
SACC-83 MnvkSpVv[3Srb36gZZN{[Xl? MkDPglIh|rypL33s MVHpcoR2[2W|IGDUSW4h\XiycnXzd4lwdiCjbnSgcYVu[nKjbnWgeJJidnOub3PheIlwdg>? MojHNlYzPzl|MEO=
293T MXHGeY5kfGmxbjDhd5NigQ>? MlmyglIh|rypL33s NWLmNI9pcW6mdXPld{BRXEWQIHHj[ZR6dGG2aX;uJIF1KEtzNkO= NGnBUIwzPjJ5OUOwNy=>
U-87 MG NVjvXI5FTnWwY4Tpc44h[XO|YYm= MmLCglIh|rypL33s MWXpcohq[mm2czD0bIUhdWmpcnH0bY9vKGGwZDDpcpZie2mxbh?= NFP5[|YzPjJ5OUOwNy=>
U-87 MG M1Kwb2Z2dmO2aX;uJIF{e2G7 MYL+NVAh|ryP NF\WOohqdmirYnn0d{BCU1RicHjvd5Bpd3K7bHH0bY9v M1zR[FI3Ojd7M{Cz
U-87 MG MnfZS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M4PRTp4yOCEQvF2= MkLDbY5pcWKrdIOgZ4VtdCCpcn;3eIg> Mo\3NlYzPzl|MEO=

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
EGFR / p-AKT / AKT / p-ERK / ERK ; 

PubMed: 29665050     


In KYSE140 (C) and KYSE180 (D), Tubastatin treatment EGFR, AKT, phospho-AKT and phospho-ERK levels were decreased in tubastatin-treated cells compared with control group.

29665050
Immunofluorescence
α-tubulin / Acetylated tubulin ; 

PubMed: 23798680     


Effects of tubastatin A on microtubules and microtubule acetylation level are shown. MCF-7 cells were treated with different concentrations of tubastatin A for 24 h and processed for immunostaining with antibodies against α-tubulin (green) and acetylated tubulin (red). Scale bars, 10 μm.

HDAC6; 

PubMed: 23798680     


MCF-7 cells are treated with vehicle, 30 μm tubastatin A (TBA), or 240 nm TSA for 24 h and fixed and processed to visualize microtubules (red) and HDAC6 (green). Scale bar, 20 μm.

23798680
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]
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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]
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  • 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]
- Collapse
  • Animal Models: Na?ve CD45RBhi CD4+ CD25- cells (1 × 106) from WT or HDAC6-/- mice Are injected i.p. into B6/Rag1-/-mice.
  • 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):
5%DMSO+40%PEG300+5%Tween80+50%ddH2O
For best results, use promptly after mixing.
1 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 TSA HCl
Smiles CN1CCC2=C(C1)C3=CC=CC=C3N2CC4=CC=C(C=C4)C(=O)NO.Cl

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Tech Support

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID