Tubastatin A

製品コードS8049

Tubastatin A化学構造

分子量(MW):335.4

Tubastatin A is a potent and selective HDAC6 inhibitor with IC50 of 15 nM in a cell-free assay. It is selective against all the other isozymes (1000-fold) except HDAC8 (57-fold).

サイズ 価格(税別)  
JPY 16102.00

カスタマーフィードバック(6)

  • 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 purchased from Selleck.

    HDACs inhibited gefitinib-induced apoptosis in NSCLC cells via a decrease in BAX/Ku70 interaction. H358 cells were treated with 5 umol/L tubastatin A (tubA), 0.5 lmol/L gefitinib or a combination of inhibitors for 96 hr as indicated. Endogenous BAX immunoprecipitations were performed and subjected to immunoblotting with Ku70-specific and BAX-specific antibodies. IgG: irrelevant immunoglobulin, used as negative controls. Input: cell lysate not subjected to immunoprecipitation.

    Int J Cancer 2014 134(11):2560-71. Tubastatin A purchased from Selleck.

  • Cells apoptosis was confirmed by H33342/PI double staining and representative images of PI-positive cells (red, top row) with H33342 counterstain (blue, middle row) are shown. TUB:Tubastatin A

    Cancer Lett, 2017, 391:89-99. Tubastatin A purchased from Selleck.

    J Biol Chem 2013 288(20), 14400-7. Tubastatin A purchased from Selleck.

  • J Biol Chem 2013 288(20), 14400-7. Tubastatin A purchased from Selleck.

    J Cell Biochem, 2018, 119(8):6623-6632. Tubastatin A purchased from Selleck.

製品安全説明書

HDAC阻害剤の選択性比較

生物活性

製品説明 Tubastatin A is a potent and selective HDAC6 inhibitor with IC50 of 15 nM in a cell-free assay. It is selective against all the other isozymes (1000-fold) except HDAC8 (57-fold).
ターゲット
HDAC6 [1]
(Cell-free assay)
15 nM
体外試験

Tubastatin A is selective at all isozymes except HDAC8 and maintains over 1000-fold selectivity against all isoforms excluding HDAC8, where it has approximately 57-fold selectivity. Tubastatin A preferentially induces α-tubulin hyperacetylation at 2.5 μM. Slight induction of histone hyperacetylation is seen for Tubastatin A at 10 μM. Tubastatin A displays dose-dependent protection against homocysteic acid-induced neuronal cell death starting at 5 μM with near complete protection at 10 μM. [1] Tubastatin A (10 μM) induces an increase in acetylated-α-tubulin levels and the restoration of primary cilia expression in the cholangiocarcinoma cell lines (18-fold); and the restoration of primary cilia correlated with downregulated Hedgehog (Hh) and MAPK signaling pathways, as well as decreased cell proliferation rates (in average by 50%) and invasion (by 40%). [2] Tubastatin A shows significant inhibition of TNF-α and IL-6 in LPS stimulated human THP-1 macrophages with an IC50 of 272 nM and 712 nM. Tubastatin A inhibits nitric oxide (NO) secretion in murine Raw 264.7 macrophages dose depenndently with an IC50 of 4.2 μM. [3]

細胞データ
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
Sf9 cells MYfGeY5kfGmxbjDhd5NigQ>? MVzJcohq[mm2aX;uJI9nKGi3bXHuJJJm[2:vYnnuZY51KEiGQVO2JIV5eHKnc4Pl[EBqdiCVZkmgZ4VtdHNiaX7jeYJifGWmIH\vdkAzKGi{czD1d4lv\yCUSFvLMWFkKG[udX;yc4dmdmmlIIP1ZpN1emG2ZTygTWM2OD1zNTDuUU4> NIX1WXMzOzByOUKwNy=>
human HeLa cells MUjGeY5kfGmxbjDhd5NigQ>? M2XUPVYhcA>? NWThRZo6UW6qaXLpeIlwdiCxZjDISGFEPiCrbjDoeY1idiCKZVzhJINmdGy|IHHzd4V{e2WmIHHzJJJm\HWldHnvckBqdiCNNECgbJlx\XKjY3X0fYxifGmxbjDv[kBidHCqYT30eYJ2dGmwIHnuZ5Vj[XSnZDDmc5IhPiCqcoOgZpkhcW2vdX7v[ox2d3Knc3PlcoNmKGG|c3H5MEBKSzVyPUKuOUDPxE1w MUSyOVQ2PDJ5MB?=
human Jurkat cells MV3DfZRwfG:6aXRCpIF{e2G7 MX23NkBp NFPwbodEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBLfXKtYYSgZ4VtdHNiYYPz[ZN{\WRiYYOg[5Jwf3SqIHnubIljcXSrb36gZYZ1\XJiN{KgbJJ{KGK7IF3UV{Bie3OjeTygTWM2OD1|LkO4JO69VS5? M{XPU|I1OzB2M{S4
human LNCAP cells M4PDOmN6fG:2b4jpZ:Kh[XO|YYm= Mo\oO|IhcA>? Ml;aR5l1d3SxeHnjbZR6KGGpYXnud5Qh[W6mcn;n[Y4u\GWyZX7k[Y51KGi3bXHuJGxPS0GSIHPlcIx{KGG|c3Xzd4VlKGG|IHfyc5d1cCCrbnjpZol1cW:wIHHmeIVzKDd{IHjyd{BjgSCPVGOgZZN{[XluIFnDOVA:OTBwOEig{txONg>? MnvXNlQ{ODR|NEi=
human KB cells NInqNnZEgXSxdH;4bYPDqGG|c3H5 MnTFO|IhcA>? NH3MfoFEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBMSiClZXzsd{Bi\nSncjC3NkBpenNiYomgUXRUKGG|c3H5MEBKSzVyPUG0MlgyKM7:TT6= NFvHcFEzPTh7OUOzPC=>
mouse B16 cells M2rxbWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MWLHdo94fGhiaX7obYJqfGmxbjDv[kBud3W|ZTDCNVYh[2WubIOgbY5kfWKjdHXkJIZweiB2ODDodpMh[nliTWTUJIF{e2G7LDDHTVUxRTRyLkWg{txONg>? NVXjTJFKOjNyMEmyNFM>

他の多くの細胞株試験データをご覧になる場合はこちらをクリックして下さい

体内試験 Tubastatin A reduces the growth of cholangiocarcinoma in vivo. Tubastatin A (10 mg/kg) induces a 6-fold lower mean tumor weights in syngeneic rat orthotopic model of cholangiocarcinoma, and reduction of the ratios of tumor weight to liver weight and body weight (5- and 5.6-fold, respectively), as well as a greater frequency of ciliated cholangiocytes compared with controls (29% vs 1.4%). Tubastatin A significantly decreases the amount of PCNA-positive cells in the treated tumors compared with vehicle controls (34% vs 65%). [2] Tubastat A shows significant inhibition of paw volume at 30 mg/kg i.p. in a Freund's complete adjuvant (FCA) induced animal model of inflammation. Tubastat A (30 mg/kg i.p.) significant attenuates clinical scores (~ 70%), and IL-6 expression in paw tissues of collagen induced arthritis DBA1 mouse. [3]

お薦めの試験操作(参考用のみ)

キナーゼ試験:

[4]

+ 展開

HDAC enzymatic assays:

Tubastatin A is dissolved and diluted in assay buffer (50 mM HEPES, pH 7.4, 100 mM KCl, 0.001% Tween-20, 0.05% BSA, and 20 μM tris(2-carboxyethyl)phosphine) to 6-fold of the final concentration. HDAC enzymes are diluted to 1.5-fold of the final concentration in assay buffer and pre-incubated with Tubastatin A for 10 minutes before the addition of the substrate. The amount of FTS (HDAC1, HDAC2, HDAC3, and HDAC6) or MAZ-1675 (HDAC4, HDAC5, HDAC7, HDAC8, and HDAC9) used for each enzyme is equal to the Michaelis constant (Km), as determined by a titration curve. FTS or MAZ-1675 is diluted in assay buffer to 6-fold the final concentration with 0.3 μM sequencing grade trypsin. The substrate/trypsin mix is added to the enzyme/compound mix and the plate is shaken for 60 seconds and then placed into a SpectraMax M5 microtiter plate reader. The enzymatic reaction is monitored for release of 7-amino-4-methoxy-coumarin over 30 minutes, after deacetylation of the lysine side chain in the peptide substrate, and the linear rate of the reaction is calculated.
細胞試験:

[2]

+ 展開
  • 細胞株: Human cholangiocarcinoma cell lines HuCCT-1
  • 濃度: ~10 μM
  • 反応時間: 21 days
  • 実験の流れ:

    Anchorage-independent growth is assessed by growing cells in soft agar. About 25,000 cells suspended in 0.4% agar in culture media are layered over a 1% agar layer in a 6-well plate. Media are added twice a week and pictures are taken after 21 days of incubation. The number and size of colonies are analyzed using the Gel-Pro software.


    (参考用のみ)
動物試験:

[2]

+ 展開
  • 動物モデル: Rat cholangiocarcinoma xenografts BDEneu
  • 製剤: --
  • 投薬量: 10 mg/kg
  • 投与方法: i.p. daily
    (参考用のみ)

溶解度 (25°C)

体外 DMSO 67 mg/mL (199.76 mM)
Water Insoluble
Ethanol Insoluble
体内 左から(NMPから)右の順に溶剤を製品に加えます(文献ではなく、Selleckの実験によるデータ):
4% DMSO+30% PEG 300+ddH2O
混合させたのち直ちに使用することを推奨します。
5mg/mL

* 溶解度測定はSelleck技術部門によって行われており、その他文献に示されている溶解度と差異がある可能性がありますが、同一ロットの生産工程で起きる正常な現象ですからご安心ください。

化学情報

分子量 335.4
化学式

C20H21N3O2

CAS No. 1252003-15-8
保管
in solvent
別名 N/A

便利ツール

モル濃度計算器

モル濃度計算器

求めたい質量、体積または濃度を計算してください。

質量 (g) = 濃度 (mol/L) x 体積 (L) x 分子量 (g/mol)

モル濃度計算器方程式

  • 質量
    濃度
    体積
    分子量

*貯蔵液を準備するとき、常に、オンであるとわかる製品のバッチに特有の分子量を使って、を通してラベルとMSDS/COA(製品ページで利用可能な)。

希釈計算器

希釈計算器

貯蔵液を準備するために必要な希釈率を計算してください。Selleck希釈計算器は、以下の方程式に基づきます:

開始濃度 x 開始体積 = 最終濃度 x 最終体積

希釈の計算式

この方程式は、一般に略語を使われます:C1V1 = C2V2 ( 入力 出力 )

  • C1
    V1
    C2
    V2

常に貯蔵液を準備するとき、小びんラベルとMSDS/COA(オンラインで利用できる)で見つかる製品のバッチに特有の分子量を使ってください。

連続希釈計算器方程式

  • 連続希釈剤

  • 計算結果

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
分子量計算器

分子量计算器

そのモル質量と元素組成を計算するために、合成物の化学式を入力してください:

総分子量:g/mol

チップス: 化学式は大文字と小文字の区別ができます。C10H16N2O2 c10h16n2o2

モル濃度計算器

質量 濃度 体積 分子量

技術サポート

ストックの作り方、阻害剤の保管方法、細胞実験や動物実験の際に注意すべき点など、製品を取扱う時に問い合わせが多かった質問に対しては取扱説明書でお答えしています。

Handling Instructions

他に質問がある場合は、お気軽にお問い合わせください。

  • * 必須

よくある質問(FAQ)

  • 質問1:

    We are planning to order some tubastatin A but I found out there are two versions of it. One has HCl and one does not. Which one do you recommend for live cell use? Will the HCl containing version significantly change the pH?

  • 回答:

    S8049 and S2627 have same molecular structure. The only difference is S2627 containing HCl and has higher solubility in DMSO (74 mg/mL vs. S8049 9 mg/mL). Since they are the same molecule, the biological function should be similar. I would recommend to use S2627 for cell culture study.

  • 質問2:

    What’s the vehicle do you recommend to dissolve the compound for in vivo experiments?

  • 回答:

    S8049 Tubastatin A can be dissolved in 2% DMSO/30% PEG 300/PBS at 2.5 mg/mL as a clear solution, and it is also a clear solution in 2% DMSO/ corn oil at 2.5 mg/mL. The drug in 2% DMSO/0.5% Tween 80/PBS is a homogeneous suspension at 2.5 mg/mL at first. After stay for a while, the precipitation goes out at the bottom of the tube.

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細胞株 試験類型 濃度 培養時間 溶剤類型 活性叙述 PMID