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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Cited by 8 Publications

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 NFvLfo5McW6jc3WgZZN{[Xl? NI\yWpUzNjVizszN NUDD[FNHTE2VTx?= MoLMbY5lfWOnczFOtU11fWK3bHnuJIh6eGW{YXPleJlt[XSrb36= M1zaOlIxPjF2OUO2
neuron cultures NVP2c5plTnWwY4Tpc44h[XO|YYm= MlSyglExKM7:TR?= M{Xk[GROW09? M{XjPZBzd3SnY4TzJIFo[Wmwc4Sg[4x2fGG2aHnvcoUh\GWybHX0bY9vNWmwZIXj[YQhd3irZHH0bZZmKHO2cnXzdy=> MoL0NlA3OTR7M{[=
134/04 NVzm[XhjTnWwY4Tpc44h[XO|YYm= NFPIW2c4NjViwsXN MmnRbY1x[Wm{czDtfY91fWKnIH\vdo1ifGmxbh?= MoC2NlIyPzR6M{m=
C2C12 M1HDbWZ2dmO2aX;uJIF{e2G7 MkjrO{42KML3TR?= NES1WXpqdXCjaYLzJI16d3S3YnWg[o9zdWG2aX;u NHryN24zOjF5NEizPS=>
HaCaT keratinocytes NE\lfFRHfW6ldHnvckBie3OjeR?= Mn3YNVAh|ryP NIjnfotjdG:la4OgZZJ{\W6rdHWg[pJwdSCrbnT1Z4lv\yCQcn[yJJBzd3SnaX6geJJidnOuYYTpc44> MVqyNlM3PzZ6OR?=
JURL-MK1 NY[xemlpTnWwY4Tpc44h[XO|YYm= NVqwdGZzOTBizszN NGL6eZlmdmijbnPld{Bk\WyuIHHkbIV{cX[rdImgeI8h\mmkcn;u[YN1cW5? NF\2VVEzOzB{MkW4Ny=>
CML-T1 MlznSpVv[3Srb36gZZN{[Xl? NFXSPJEyOCEQvF2= NULVPXVN\W6qYX7j[ZMh[2WubDDh[Ihme2m4aYT5JJRwKG[rYoLvcoVkfGmw NIHIUnYzOzB{MkW4Ny=>
K562 MWLGeY5kfGmxbjDhd5NigQ>? NF[0WGgyOCEQvF2= MlvU[Y5p[W6lZYOgZ4VtdCCjZHjld4l3cXS7IITvJIZq[nKxbnXjeIlv M2\xN|I{ODJ{NUiz
HL-60 Mn3ZSpVv[3Srb36gZZN{[Xl? MYCxNEDPxE1? MV\lcohidmOnczDj[YxtKGGmaHXzbZZqfHlidH:g[oljem:wZXP0bY4> MoTUNlMxOjJ3OEO=
KMCH M{PVU2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MXX+NVAh|ryP MkL1[IVkemWjc3XzJJBzd2yrZnXyZZRqd25iYX7kJIFv[2ixcnHn[U1qdmSncHXu[IVvfCCpcn;3eIg> NHnhfm8zOzN5MEOyOy=>
THP-1 NGjPSIlHfW6ldHnvckBie3OjeR?= NVLwNpd[hjFyIN88US=> MW\pcohq[mm2czDUUmYu|rFiYX7kJGlNNTZic3XjdoV1cW:w Ml\QNlM2PDF4M{S=
RAW 264.7 M33Pe2Z2dmO2aX;uJIF{e2G7 MkjmglExKM7:TR?= NGS0XWxifHSnboXheIV{KE6RIIDyc4R2[3Srb36= NXziSGdyOjN3NEG2N|Q>
HT3 NH;NW3RHfW6ldHnvckBie3OjeR?= NVzNVVd{hjVizszN M4S0ZmROW09? NUHvZZo4cW6mdXPld{B1cGViZHnm[oVz\W62aXHsJO6yNXS3YoXsbY4h[WOndInsZZRqd25? NUO5NJdoOjN4OUi0Olg>
SiHa MYnGeY5kfGmxbjDhd5NigQ>? M1HDNp42KM7:TR?= M3fBPGROW09? MlTIbY5lfWOnczD0bIUh\GmoZnXy[Y51cWGuIN8xMZR2[nWuaX6gZYNmfHmuYYTpc44> NYGwUW1iOjN4OUi0Olg>
CaSki NUPIUWVQTnWwY4Tpc44h[XO|YYm= MmrFglUh|ryP NFv4eJpFVVOR M37Ydolv\HWlZYOgeIhmKGSrZn\ldoVvfGmjbDFOtU11fWK3bHnuJIFk\XS7bHH0bY9v NY\XfG57OjN4OUi0Olg>
SiHa MWXGeY5kfGmxbjDhd5NigQ>? M4foRp42KM7:TR?= NYLmOIl3TE2VTx?= M3[1cYlvcGmkaYTzJHRp[XC|aXfhdodqdi1ib4KgSWdHNWmwZIXj[YQhW0:FRTDhZ5RqfmG2aX;u M{jQXVI{Pjl6NE[4
CaSki MkWwSpVv[3Srb36gZZN{[Xl? M2q5ep42KM7:TR?= NXPxU5RsTE2VTx?= MlXjbY5pcWKrdIOgWIhieHOrZ3Hy[4lvNSCxcjDFS2YucW6mdXPl[EBUV0OHIHHjeIl3[XSrb36= MnrlNlM3QTh2Nki=
MCF-7 MlH3S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NVG5[VNPOzBizszN M3rGd2ROW09? NF[yNlhKSzVyPUG1JO69VQ>? NWrLdIdEOjN5OUi2PFA>
MCF-7 NX7Ne4N[TnWwY4Tpc44h[XO|YYm= MoX6N|Ah|ryP MnnISG1UVw>? M2LNWYlv[3KnYYPld{B1cGVibXnjdo91fWK3bHWgZYNmfHmuYYTpc44hdGW4ZXyu NYLRcnB2OjN5OUi2PFA>
MCF-7 M37ROGZ2dmO2aX;uJIF{e2G7 NFW4O4Q{OCEQvF2= MnfsSG1UVw>? MVfzeIFjcWyrenXzJI1q[3KxdIXieYxmeyCjZ3HpcpN1KGOxbHStbY5lfWOnZDDk[ZBwdHmvZYLpfoF1cW:w M3i0N|I{Pzl6Nkiw
MCF-7 NW[yWIxZTnWwY4Tpc44h[XO|YYm= MWWxOUDPxE1? NIrlSJVFVVOR MknSd5Ri[mmuaYrld{BucWO{b4T1ZpVt\XNiYXfhbY5{fCCwb3Pv[IF7d2ynLXnu[JVk\WRiZHnzZZN{\W2kbIm= MVOyN|c6QDZ6MB?=
MCF-7 MUDGeY5kfGmxbjDhd5NigQ>? M3TxfFMxKM7:TR?= MWPEUXNQ MYLhcJRmemW|IITo[UBie3OnbXLsfUBlgW6jbXnjd{Bw\iCrboTldpBp[XOnIH3pZ5JwfHWkdXzldy=> Mlf2NlM4QTh4OEC=
MCF-7 MlPFSpVv[3Srb36gZZN{[Xl? NIKycWY{OCEQvF2= MlvYSG1UVw>? NHfZ[WJqdmO{ZXHz[ZMhfGinIHLpcoRqdmdib3[gTGRCSzZid3n0bEBqdnSncoDoZZNmKG2rY4LveJVjfWyncx?= MmnFNlM4QTh4OEC=
PC12 MUDGeY5kfGmxbjDhd5NigQ>? MmnqglMh|ryP NEnyN|lFVVOR MnTZeZAuemWpdXzheIV{KGGwdHmtc5hq\GG2aY\lJIdmdmViZYjwdoV{e2mxbjDy[YxifGWmIITvJJRz[W6|Y4LpdJRqd25iZnHjeI9zKFiEUEHz MnPtNlQ6ODl4OE[=
PC12 MW\Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M{HjcZ4{KM7:TR?= Ml;jSG1UVw>? NXzkXXMxemW4ZYLz[UBJOk9{LXnu[JVk\WRiZ4Lve5RpKGmwaHnibZRqd25? NHr1SW0zPDlyOU[4Oi=>
HEK293T Mki4SpVv[3Srb36gZZN{[Xl? M3r5TJ4{KM7:TR?= MVnEUXNQ NYO0cpB{fXBvcnXneYxifGWmIGjCVFF{KHC{b4TlbY4hdGW4ZXy= M4TObFI1QTB7Nki2
HEK293T NFHpOWZHfW6ldHnvckBie3OjeR?= MmXjglMh|ryP NFrpNoFFVVOR NGrSdlRl\WyjeYOgXGJROXNicILveIVqdiCmZXfyZYRifGmxbjD2bYEh[WOndInsZZRqd25vbXXkbYF1\WRicILveIVie2:vYXyg[IVoemGmYYTpc44> MXeyOFkxQTZ6Nh?=
Huh7 NIi3SnZHfW6ldHnvckBie3OjeR?= MmrTglUh|ryP NYnxe5Q3TE2VTx?= MV7zeZBxemW|c3XzJJBzd2yrZnXyZZRqd25ib3[gbIVx[XSrdHnzJGMhfmm{dYOgdoVxdGmlb36ge4l1cCCHQ{WwJF0hOC5|IN88US=> MmC4NlUyODh|Mk[=
SKMEL21 M1PmWGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MmDRglUxOCCwTR?= NWWyem9JTE2VTx?= MV3pcohq[mm2czDj[YxtKHC{b3zp[oVz[XSrb36= M2jUR|I2QTV5OEGy
SKMEL103 NHTsRolIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M2j3fZ42ODBibl2= MnvrSG1UVw>? M1;VbYlvcGmkaYTzJINmdGxicILvcIln\XKjdHnvci=> NF;4Z3gzPTl3N{ixNi=>
SKMEL28 MlP1S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MonBglUxOCCwTR?= M3\BW2ROW09? MUfpcohq[mm2czDj[YxtKHC{b3zp[oVz[XSrb36= NEjXZ2kzPTl3N{ixNi=>
WM164 NVzxfYNiT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MmT4glUxOCCwTR?= MknlSG1UVw>? M2H5SolvcGmkaYTzJINmdGxicILvcIln\XKjdHnvci=> NUnk[WpKOjV7NUe4NVI>
WM1361a NVrIOYpwT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MVL+OVAxKG6P NULvWIZ7TE2VTx?= MoLQbY5pcWKrdIOgZ4VtdCCycn;sbYZmemG2aX;u NXHSWHZvOjV7NUe4NVI>
WM1366 M4facmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MoDaglUxOCCwTR?= M4nyNGROW09? NEjVZmdqdmirYnn0d{Bk\WyuIIDyc4xq\mW{YYTpc44> NXq1PVVNOjV7NUe4NVI>
WM793 NVXCdlVVT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= Mm\kglUxOCCwTR?= MUnEUXNQ MYHpcohq[mm2czDj[YxtKHC{b3zp[oVz[XSrb36= M1HwNlI2QTV5OEGy
WM35 NWKxSnFQT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MX\+OVAxKG6P NVjKTVE6TE2VTx?= MnPmbY5pcWKrdIOgZ4VtdCCycn;sbYZmemG2aX;u NFLJXY4zPTl3N{ixNi=>
WM983a MUXHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MlfLglUxOCCwTR?= M3LMUmROW09? MnWxbY5pcWKrdIOgZ4VtdCCycn;sbYZmemG2aX;u Ml[3NlU6PTd6MUK=
WM793 Mki0SpVv[3Srb36gZZN{[Xl? NYj1bYZ4hjZizszN M3vGV2ROW09? NUO1NIlxcW6mdXPlJGcyKGG{cnXzeC=> MUWyOVk2PzhzMh?=
WM164 NWjpZoJKTnWwY4Tpc44h[XO|YYm= NEjPPJV,PiEQvF2= MVXEUXNQ NHPZV3pqdmS3Y3WgS|Eh[XK{ZYP0 NVL1THJ{OjV7NUe4NVI>
WM983a NXTTVGQzTnWwY4Tpc44h[XO|YYm= MmLNglYh|ryP M3i4cGROW09? NIex[W1qdmS3Y3WgS|Eh[XK{ZYP0 MoC1NlU6PTd6MUK=
WM164 NIrN[oZHfW6ldHnvckBie3OjeR?= NWi5S29XhjNizszN Mom5SG1UVw>? M3;teIF2\22nboTzJIV5eHKnc4Ppc44hd2ZiTVjDJINt[XO|IFmgZY5lKG2nbHHuc41iKGG|c3;jbYF1\WRiYX70bYdmdnN? NXXneJE5OjV7NUe4NVI>
WM983a NXTZXI9lTnWwY4Tpc44h[XO|YYm= NHPPPJp,OyEQvF2= NULabWVSTE2VTx?= MoSzZZVodWWwdIOg[ZhxemW|c3nvckBw\iCPSFOgZ4xie3NiSTDhcoQhdWWuYX7vcYEh[XO|b3PpZZRm\CCjboTp[4Vvew>? NVPscmtNOjV7NUe4NVI>
IPC298 MWDGeY5kfGmxbjDhd5NigQ>? MmnmglMh|ryP MXPEUXNQ NGfPbpBifWevZX70d{BmgHC{ZYPzbY9vKG:oIF3IR{BkdGG|czDJJIFv\CCvZXzhco9u[SCjc4PvZ4lifGWmIHHueIlo\W6| M3O2TlI2QTV5OEGy
SKMEL30 MkfKSpVv[3Srb36gZZN{[Xl? M1\rdZ4{KM7:TR?= M4GwZWROW09? MWnheYdu\W62czDlfJBz\XO|aX;uJI9nKE2KQzDjcIF{eyCLIHHu[EBu\Wyjbn;tZUBie3OxY3nheIVlKGGwdHnn[Y5{ NX[3SlhOOjV7NUe4NVI>
TCa83 NGTnV3lHfW6ldHnvckBie3OjeR?= MnTzbY5lfWOnczDQWGVPKGW6cILld5Nqd25iYX7kJI1mdWK{YX7lJJRz[W6|bH;jZZRqd25? MWWyOlI4QTNyMx?=
293T M2HX[WZ2dmO2aX;uJIF{e2G7 MWD+NkDPxGdxbXy= M4fOSolv\HWlZYOgVHRGViCneIDy[ZN{cW:wIHHu[EBu\W2kcnHu[UB1emGwc3zvZ4F1cW:w MVyyOlI4QTNyMx?=
SACC-83 MVrGeY5kfGmxbjDhd5NigQ>? MoXoglIh|rypL33s MX3pcoR2[2W|IGDUSW4h\XiycnXzd4lwdiCjbnSgcYVu[nKjbnWgeJJidnOub3PheIlwdg>? M{[1dVI3Ojd7M{Cz
293T MWnGeY5kfGmxbjDhd5NigQ>? NFTFV2d,OiEQvHevcYw> NWe0O2JUcW6mdXPld{BRXEWQIHHj[ZR6dGG2aX;uJIF1KEtzNkO= M3XmeFI3Ojd7M{Cz
U-87 MG MYHGeY5kfGmxbjDhd5NigQ>? NELLNo9,OiEQvHevcYw> M1rjV4lvcGmkaYTzJJRp\SCvaXfyZZRqd25iYX7kJIlvfmG|aX;u NXXFVWMyOjZ{N{mzNFM>
U-87 MG NX\kWZo1TnWwY4Tpc44h[XO|YYm= M4rucp4yOCEQvF2= NInsZWxqdmirYnn0d{BCU1RicHjvd5Bpd3K7bHH0bY9v M13IN|I3Ojd7M{Cz
U-87 MG MXXHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MmL6glExKM7:TR?= M{XWOIlvcGmkaYTzJINmdGxiZ4Lve5Rp Ml:2NlYzPzl|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