Tubastatin A

製品コードS8049

Tubastatin A化学構造

分子量(MW):335.4

Tubastatin Aは一種の有効的で、選択性HDAC6阻害剤で、無細胞試験でIC50値が15 nMです。Tubastatin Aは、HDAC6に作用する選択性は全ての他のイソ酵素に作用する選択性より1000倍が高くなリますが、HDAC8に作用する選択性より57倍が高くなります。

サイズ 価格 在庫  
JPY 13966.83 あり

カスタマーフィードバック(5)

  • 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.

    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.

  • 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.

    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.

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は一種の有効的で、選択性HDAC6阻害剤で、無細胞試験でIC50値が15 nMです。Tubastatin Aは、HDAC6に作用する選択性は全ての他のイソ酵素に作用する選択性より1000倍が高くなリますが、HDAC8に作用する選択性より57倍が高くなります。
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 M3ewOWZ2dmO2aX;uJIF{e2G7 M3zESGlvcGmkaYTpc44hd2ZiaIXtZY4hemWlb33ibY5idnRiSFTBR|Yh\XiycnXzd4VlKGmwIGPmPUBk\WyuczDpcoN2[mG2ZXSg[o9zKDJiaILzJJV{cW6pIGLIT2suSWNiZnz1c5Jw\2WwaXOgd5Vje3S{YYTlMEBKSzVyPUG1JI5ONg>? NXrlUIdXOjNyMEmyNFM>
human HeLa cells NEntNGhHfW6ldHnvckBie3OjeR?= M{WxeFYhcA>? NIfrenpKdmirYnn0bY9vKG:oIFjERWM3KGmwIHj1cYFvKEinTHGgZ4VtdHNiYYPz[ZN{\WRiYYOgdoVlfWO2aX;uJIlvKEt2MDDofZBmemGlZYT5cIF1cW:wIH;mJIFteGijLYT1ZpVtcW5iaX7jeYJifGWmIH\vdkA3KGi{czDifUBqdW23bn;mcJVwemW|Y3XuZ4Uh[XO|YYmsJGlEPTB;Mj61JO69VS5? MXeyOVQ2PDJ5MB?=
human Jurkat cells MVfDfZRwfG:6aXRCpIF{e2G7 MoTQO|IhcA>? MUTDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDKeZJs[XRiY3XscJMh[XO|ZYPz[YQh[XNiZ4Lve5RpKGmwaHnibZRqd25iYX\0[ZIhPzJiaILzJIJ6KE2WUzDhd5NigSxiSVO1NF0{NjN6IN88UU4> NXzTfmNuOjR|MESzOFg>
human LNCAP cells NGTKbotEgXSxdH;4bYPDqGG|c3H5 NUiwS2dOPzJiaB?= NHzr[phEgXSxdH;4bYNqfHliYXfhbY5{fCCjbnTyc4dmdi2mZYDlcoRmdnRiaIXtZY4hVE6FQWCgZ4VtdHNiYYPz[ZN{\WRiYYOg[5Jwf3SqIHnubIljcXSrb36gZYZ1\XJiN{KgbJJ{KGK7IF3UV{Bie3OjeTygTWM2OD1zMD64PEDPxE1w NGH1V4kzPDNyNEO0PC=>
human KB cells M3jaNmN6fG:2b4jpZ:Kh[XO|YYm= NHH5O|Y4OiCq M3fybWN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGtDKGOnbHzzJIFnfGW{IEeyJIhzeyCkeTDNWHMh[XO|YYmsJGlEPTB;MUSuPFEh|ryPLh?= NIXwUYMzPTh7OUOzPC=>
mouse B16 cells MXTHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NWHC[JR7T3Kxd4ToJIlvcGmkaYTpc44hd2ZibX;1d4UhSjF4IHPlcIx{KGmwY4XiZZRm\CCob4KgOFghcHK|IHL5JG1VXCCjc4PhfUwhT0l3ME20NE42KM7:TT6= NEXJcFgzOzByOUKwNy=>

多くの細胞株試験データを見る場合、クリックしてください

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)

溶解度 (25°C)

体外 DMSO 67 mg/mL (199.76 mM)
Water Insoluble
Ethanol Insoluble
体内 順序で溶剤を入れること:
4% DMSO+30% PEG 300
5mg/mL

* 溶解度検測はSelleck技術部門によって行いますので、文献より提供された溶解度と差異がある可能性がありますが、生産工芸と不同ロット(lot)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

解決のために必要とされるマス、ボリュームまたは濃度を計算してください。

マス (g) = 濃度 (mol/L) x ボリューム (L) x 分子量 (g/mol)

モル濃度計算器方程式

  • マス
    濃度
    ボリューム
    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

貯蔵液を準備することを要求される希釈剤を計算してください. セレック希釈計算器は、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 ( 輸入 輸出 )

  • 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

マス 濃度 ボリューム 分子量

技術サポート

ストックの作り方、阻害剤の保管する方法、細胞実験や動物実験に注意すべきな点を全部含めており、製品を取扱う時よくあった質問に対して取扱説明書でお答えいたします。

Handling Instructions

他の質問がある場合は、お気軽くお問合せください。

  • * 必須

よくある質問(FAQ)

  • 問題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.

  • 問題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.

HDAC信号経路図

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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