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 MUTLbY5ie2ViYYPzZZk> MWOyMlUh|ryP NYfPboV{TE2VTx?= NXO2fJZrcW6mdXPld{DPuS22dXL1cIlvKGi7cHXyZYNmfHmuYYTpc44> NXj6dVYzOjB4MUS5N|Y>
neuron cultures NVHTWG1GTnWwY4Tpc44h[XO|YYm= NFzPTHV,OTBizszN MWPEUXNQ MmDZdJJwfGWldIOgZYdicW6|dDDncJV1[XSqaX;u[UBl\XCuZYTpc44ucW6mdXPl[EBwgGmmYYTpeoUhe3S{ZYPz MUGyNFYyPDl|Nh?=
134/04 MYfGeY5kfGmxbjDhd5NigQ>? MoGyO{42KML3TR?= MnHibY1x[Wm{czDtfY91fWKnIH\vdo1ifGmxbh?= M{HPU|IzOTd2OEO5
C2C12 MVnGeY5kfGmxbjDhd5NigQ>? MnLyO{42KML3TR?= MW\pcZBicXK|IH35c5R2[mViZn;ycYF1cW:w NYj0[Y93OjJzN{S4N|k>
HaCaT keratinocytes MYPGeY5kfGmxbjDhd5NigQ>? M3nhSlExKM7:TR?= MnS5Zoxw[2u|IHHyd4VvcXSnIH\yc40hcW6mdXPpcochVnKoMjDwdo91\WmwIITyZY5{dGG2aX;u MX:yNlM3PzZ6OR?=
JURL-MK1 MlvhSpVv[3Srb36gZZN{[Xl? NEjhT2kyOCEQvF2= M2\aRoVvcGGwY3XzJINmdGxiYXTo[ZNqfmm2eTD0c{BncWK{b37lZ5Rqdg>? MlHoNlMxOjJ3OEO=
CML-T1 NYLGc245TnWwY4Tpc44h[XO|YYm= NFP6[5QyOCEQvF2= NVXhT|NH\W6qYX7j[ZMh[2WubDDh[Ihme2m4aYT5JJRwKG[rYoLvcoVkfGmw MUiyN|AzOjV6Mx?=
K562 M3\ZcGZ2dmO2aX;uJIF{e2G7 MkPJNVAh|ryP NIHLfllmdmijbnPld{Bk\WyuIHHkbIV{cX[rdImgeI8h\mmkcn;u[YN1cW5? NG\LeVYzOzB{MkW4Ny=>
HL-60 Mlv4SpVv[3Srb36gZZN{[Xl? NGr0PI0yOCEQvF2= M2P2RYVvcGGwY3XzJINmdGxiYXTo[ZNqfmm2eTD0c{BncWK{b37lZ5Rqdg>? Ml6xNlMxOjJ3OEO=
KMCH M{fQ[2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NYXYfnJ4hjFyIN88US=> MWHk[YNz\WG|ZYOgdJJwdGmoZYLheIlwdiCjbnSgZY5kcG:{YXflMYlv\GWyZX7k[Y51KGe{b4f0bC=> MXyyN|M4ODN{Nx?=
THP-1 M{SyRWZ2dmO2aX;uJIF{e2G7 MnzyglExKM7:TR?= NYjJeZp{cW6qaXLpeJMhXE6ILd8xJIFv\CCLTD22JJNm[3KndHnvci=> M3HsRlI{PTRzNkO0
RAW 264.7 NGLa[IxHfW6ldHnvckBie3OjeR?= MVf+NVAh|ryP NUjQOlB{[XS2ZX71ZZRmeyCQTzDwdo9lfWO2aX;u NIWw[ngzOzV2MU[zOC=>
HT3 M4DZSGZ2dmO2aX;uJIF{e2G7 MUf+OUDPxE1? MmfBSG1UVw>? NYDxcG97cW6mdXPld{B1cGViZHnm[oVz\W62aXHsJO6yNXS3YoXsbY4h[WOndInsZZRqd25? MmfxNlM3QTh2Nki=
SiHa M4XHbmZ2dmO2aX;uJIF{e2G7 MVH+OUDPxE1? MWTEUXNQ NGnTVpFqdmS3Y3XzJJRp\SCmaX\m[ZJmdnSrYXyg{tEufHWkdXzpckBi[2W2eXzheIlwdg>? NHvndJEzOzZ7OES2PC=>
CaSki MonYSpVv[3Srb36gZZN{[Xl? NFXuTot,PSEQvF2= NXP1N4d4TE2VTx?= NXP0Z5h4cW6mdXPld{B1cGViZHnm[oVz\W62aXHsJO6yNXS3YoXsbY4h[WOndInsZZRqd25? NGK5bGYzOzZ7OES2PC=>
SiHa NIr0To1HfW6ldHnvckBie3OjeR?= M3S3Tp42KM7:TR?= NWnzTJJMTE2VTx?= MVXpcohq[mm2czDUbIFxe2mpYYLnbY4uKG:{IFXHSk1qdmS3Y3XkJHNQS0ViYXP0bZZifGmxbh?= MlSyNlM3QTh2Nki=
CaSki NVPVWnV5TnWwY4Tpc44h[XO|YYm= NXfRfXhHhjVizszN MnzNSG1UVw>? NGLsPJZqdmirYnn0d{BVcGGyc3nnZZJocW5vIH;yJGVITi2rbnT1Z4VlKFORQ1WgZYN1cX[jdHnvci=> NILQWVgzOzZ7OES2PC=>
MCF-7 MnrIS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NH2zZ5E{OCEQvF2= M2fvdmROW09? MXPJR|UxRTF3IN88US=> NVLS[pJmOjN5OUi2PFA>
MCF-7 NVrVO4twTnWwY4Tpc44h[XO|YYm= Mlv6N|Ah|ryP MoeySG1UVw>? NIewbYJqdmO{ZXHz[ZMhfGinIH3pZ5JwfHWkdXzlJIFk\XS7bHH0bY9vKGyndnXsMi=> MnrRNlM4QTh4OEC=
MCF-7 NXu1fHFFTnWwY4Tpc44h[XO|YYm= MmG5N|Ah|ryP NIrnVolFVVOR M3WxcpN1[WKrbHn6[ZMhdWmlcn;0eYJ2dGW|IHHnZYlve3RiY3;s[E1qdmS3Y3XkJIRmeG:ueX3ldol7[XSrb36= MlXwNlM4QTh4OEC=
MCF-7 M2LaWmZ2dmO2aX;uJIF{e2G7 NVHUWlA3OTVizszN MmrFSG1UVw>? MXvzeIFjcWyrenXzJI1q[3KxdIXieYxmeyCjZ3HpcpN1KG6xY3;kZZpwdGVvaX7keYNm\CCmaYPhd5NmdWKueR?= NGTPb|YzOzd7OE[4NC=>
MCF-7 NX3LcpVbTnWwY4Tpc44h[XO|YYm= NGPRdYM{OCEQvF2= NXPUVpJ6TE2VTx?= MXvhcJRmemW|IITo[UBie3OnbXLsfUBlgW6jbXnjd{Bw\iCrboTldpBp[XOnIH3pZ5JwfHWkdXzldy=> MWOyN|c6QDZ6MB?=
MCF-7 MkC0SpVv[3Srb36gZZN{[Xl? NHnNV5o{OCEQvF2= MmfRSG1UVw>? MlvCbY5kemWjc3XzJJRp\SCkaX7kbY5oKG:oIFjERWM3KHerdHigbY51\XKyaHHz[UBucWO{b4T1ZpVt\XN? MUGyN|c6QDZ6MB?=
PC12 NYDFZ2lnTnWwY4Tpc44h[XO|YYm= Mk\mglMh|ryP MUTEUXNQ MnvQeZAuemWpdXzheIV{KGGwdHmtc5hq\GG2aY\lJIdmdmViZYjwdoV{e2mxbjDy[YxifGWmIITvJJRz[W6|Y4LpdJRqd25iZnHjeI9zKFiEUEHz NHjETY8zPDlyOU[4Oi=>
PC12 M2HWOWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M1zNVZ4{KM7:TR?= MYDEUXNQ NFK2XVJz\X[ncoPlJGgzVzJvaX7keYNm\CCpcn;3eIghcW6qaXLpeIlwdg>? MUWyOFkxQTZ6Nh?=
HEK293T NIfJbZlHfW6ldHnvckBie3OjeR?= M{LJPZ4{KM7:TR?= NFq1[INFVVOR NUfZT4JvfXBvcnXneYxifGWmIGjCVFF{KHC{b4TlbY4hdGW4ZXy= NXXLenVGOjR7MEm2PFY>
HEK293T MXLGeY5kfGmxbjDhd5NigQ>? NFfhVot,OyEQvF2= M2LIZWROW09? MkX6[IVt[Xm|IGjCVFF{KHC{b4TlbY4h\GWpcnHkZZRqd25idnnhJIFk\XS7bHH0bY9vNW2nZHnheIVlKHC{b4TlZZNwdWGuIHTl[5Ji\GG2aX;u MXSyOFkxQTZ6Nh?=
Huh7 MoXzSpVv[3Srb36gZZN{[Xl? MlXxglUh|ryP NHrkbllFVVOR NUTTbJROe3WycILld5NmeyCycn;sbYZmemG2aX;uJI9nKGincHH0bZRqeyCFII\pdpV{KHKncHzpZ49vKHerdHigSWM2OCB;IECuN{DPxE1? M3fJWlI2OTB6M{K2
SKMEL21 MnPnS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M2izbZ42ODBibl2= MkC3SG1UVw>? NGDHcolqdmirYnn0d{Bk\WyuIIDyc4xq\mW{YYTpc44> MWqyOVk2PzhzMh?=
SKMEL103 M4rzWmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 Mn3EglUxOCCwTR?= MWnEUXNQ NFTL[Y9qdmirYnn0d{Bk\WyuIIDyc4xq\mW{YYTpc44> MYWyOVk2PzhzMh?=
SKMEL28 MX;Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NGDMSFF,PTByIH7N MoTzSG1UVw>? NX\Ve4hxcW6qaXLpeJMh[2WubDDwdo9tcW[ncnH0bY9v MlPVNlU6PTd6MUK=
WM164 NWfMW|l2T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MlvHglUxOCCwTR?= NWDKV|BXTE2VTx?= M1XsV4lvcGmkaYTzJINmdGxicILvcIln\XKjdHnvci=> NGXoWVMzPTl3N{ixNi=>
WM1361a M33jZmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NVu0RXBEhjVyMDDuUS=> NXTQ[JZyTE2VTx?= M364Z4lvcGmkaYTzJINmdGxicILvcIln\XKjdHnvci=> MWqyOVk2PzhzMh?=
WM1366 MUTHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NV73ZZM2hjVyMDDuUS=> MkPzSG1UVw>? NVvnW5BEcW6qaXLpeJMh[2WubDDwdo9tcW[ncnH0bY9v NELXdIEzPTl3N{ixNi=>
WM793 NVrWNo9xT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NF3GOZN,PTByIH7N MVLEUXNQ NFqyWYRqdmirYnn0d{Bk\WyuIIDyc4xq\mW{YYTpc44> NV3JbGo1OjV7NUe4NVI>
WM35 NYjJPZVpT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MkO4glUxOCCwTR?= NF7H[XlFVVOR MW\pcohq[mm2czDj[YxtKHC{b3zp[oVz[XSrb36= NHjRbY4zPTl3N{ixNi=>
WM983a MX3Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MnjpglUxOCCwTR?= NYS3fmo3TE2VTx?= M4\reYlvcGmkaYTzJINmdGxicILvcIln\XKjdHnvci=> NV7oNVF2OjV7NUe4NVI>
WM793 NUSxeHpHTnWwY4Tpc44h[XO|YYm= M1ixO543KM7:TR?= M1XCR2ROW09? NVXmdG05cW6mdXPlJGcyKGG{cnXzeC=> MlPvNlU6PTd6MUK=
WM164 Mn;HSpVv[3Srb36gZZN{[Xl? MlTwglYh|ryP MlTPSG1UVw>? NEXSdY5qdmS3Y3WgS|Eh[XK{ZYP0 NUPHXHpzOjV7NUe4NVI>
WM983a MXfGeY5kfGmxbjDhd5NigQ>? M330PZ43KM7:TR?= M37RdGROW09? M4rlNolv\HWlZTDHNUBienKnc4S= MmqwNlU6PTd6MUK=
WM164 MUfGeY5kfGmxbjDhd5NigQ>? NGfweol,OyEQvF2= M{ja[GROW09? NITXWWlifWevZX70d{BmgHC{ZYPzbY9vKG:oIF3IR{BkdGG|czDJJIFv\CCvZXzhco9u[SCjc4PvZ4lifGWmIHHueIlo\W6| NH\y[W8zPTl3N{ixNi=>
WM983a NInRTpNHfW6ldHnvckBie3OjeR?= MoT4glMh|ryP NVHM[lBbTE2VTx?= NXrac4x4[XWpbXXueJMh\XiycnXzd4lwdiCxZjDNTGMh[2yjc4OgTUBidmRibXXsZY5wdWFiYYPzc4Nq[XSnZDDhcpRq\2Wwcx?= NVvJNpdLOjV7NUe4NVI>
IPC298 M4fie2Z2dmO2aX;uJIF{e2G7 MY\+N{DPxE1? M4\JOmROW09? M4fKe4F2\22nboTzJIV5eHKnc4Ppc44hd2ZiTVjDJINt[XO|IFmgZY5lKG2nbHHuc41iKGG|c3;jbYF1\WRiYX70bYdmdnN? MmjQNlU6PTd6MUK=
SKMEL30 M3\nPGZ2dmO2aX;uJIF{e2G7 M1Tn[p4{KM7:TR?= M{nXOmROW09? NXjxOG17[XWpbXXueJMh\XiycnXzd4lwdiCxZjDNTGMh[2yjc4OgTUBidmRibXXsZY5wdWFiYYPzc4Nq[XSnZDDhcpRq\2Wwcx?= MX:yOVk2PzhzMh?=
TCa83 NFzoV|VHfW6ldHnvckBie3OjeR?= MlnGbY5lfWOnczDQWGVPKGW6cILld5Nqd25iYX7kJI1mdWK{YX7lJJRz[W6|bH;jZZRqd25? NYjp[21zOjZ{N{mzNFM>
293T Moq1SpVv[3Srb36gZZN{[Xl? NXu5XGlPhjJizsznM41t MYDpcoR2[2W|IGDUSW4h\XiycnXzd4lwdiCjbnSgcYVu[nKjbnWgeJJidnOub3PheIlwdg>? M3HDT|I3Ojd7M{Cz
SACC-83 NX\KenpqTnWwY4Tpc44h[XO|YYm= NXjsWlFLhjJizsznM41t MkXjbY5lfWOnczDQWGVPKGW6cILld5Nqd25iYX7kJI1mdWK{YX7lJJRz[W6|bH;jZZRqd25? NWm3WnlXOjZ{N{mzNFM>
293T M3PZW2Z2dmO2aX;uJIF{e2G7 NHPCe5J,OiEQvHevcYw> Ml:4bY5lfWOnczDQWGVPKGGlZYT5cIF1cW:wIHH0JGsyPjN? NH\BdXIzPjJ5OUOwNy=>
U-87 MG M2[xe2Z2dmO2aX;uJIF{e2G7 M{LzfJ4zKM7:Zz;tcC=> MnfpbY5pcWKrdIOgeIhmKG2rZ4LheIlwdiCjbnSgbY53[XOrb36= NXzoVYI6OjZ{N{mzNFM>
U-87 MG M3jjOWZ2dmO2aX;uJIF{e2G7 MXr+NVAh|ryP MoPLbY5pcWKrdIOgRWtVKHCqb4PwbI9zgWyjdHnvci=> MWOyOlI4QTNyMx?=
U-87 MG NX7Qbmo4T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NX;4RmhphjFyIN88US=> NHTFSIpqdmirYnn0d{Bk\WyuIHfyc5d1cA>? NV;tNVh[OjZ{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 <1 mg/mL
Ethanol <1 mg/mL
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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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