Tubastatin A HCl

製品コード：S2627 純度：99.30%

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).

CAS No. 1310693-92-5

サイズ	価格(税別)	在庫状況
10mM (1mL in DMSO)	JPY 29500	国内在庫あり
10mg	JPY 22000	国内在庫あり
50mg	JPY 44500	国内在庫あり
1g	JPY 448500	国内在庫なし(納期7~10日)

代表番号: 045-509-1970\|電子メール：[email protected] よく尋ねられる質問

文献中Selleckの製品使用例（47）

製品安全説明書

現在のバッチを見る：純度： 99.30%

99.30

Tubastatin A HCl関連製品

関連ターゲット	HDAC1 HDAC2 HDAC3 HDAC4 HDAC5 HDAC6 HDAC7 HDAC8 HDAC9 HDAC10 HDAC11 HD1 HD2	もっと見る
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関連化合物ライブラリー	Kinase Inhibitor Library FDA-approved Drug Library Natural Product Library Bioactive Compound Library-I Highly Selective Inhibitor Library	もっと見る

シグナル伝達経路

HDACシグナル伝達経路

HDAC阻害剤の選択性比較

Cell Data

Cell Lines	Assay Type	Concentration	活性情報	PMID
neuron cultures	Kinase assay	2.5 μM	induces α-tubulin hyperacetylation	20614936
neuron cultures	Function assay	~10 μM	protects against glutathione depletion-induced oxidative stress	20614936
134/04	Function assay	7.5 µM	impairs myotube formation	22174839
C2C12	Function assay	7.5 µM	impairs myotube formation	22174839
HaCaT keratinocytes	Function assay	10 μM	blocks arsenite from inducing Nrf2 protein translation	22367689
JURL-MK1	Function assay	10 μM	enhances cell adhesivity to fibronectin	23022583
CML-T1	Function assay	10 μM	enhances cell adhesivity to fibronectin	23022583
K562	Function assay	10 μM	enhances cell adhesivity to fibronectin	23022583
HL-60	Function assay	10 μM	enhances cell adhesivity to fibronectin	23022583
KMCH	Growth inhibitory assay	~10 μM	decreases proliferation and anchorage-independent growth	23370327
THP-1	Function assay	~10 μM	inhibits TNF-α and IL-6 secretion	23541634
RAW 264.7	Function assay	~10 μM	attenuates NO production	23541634
HT3	Function assay	~5 μM	induces the differential α-tubulin acetylation	23698468
SiHa	Function assay	~5 μM	induces the differential α-tubulin acetylation	23698468
CaSki	Function assay	~5 μM	induces the differential α-tubulin acetylation	23698468
SiHa	Function assay	~5 μM	inhibits Thapsigargin- or EGF-induced SOCE activation	23698468
CaSki	Function assay	~5 μM	inhibits Thapsigargin- or EGF-induced SOCE activation	23698468
MCF-7	Growth inhibitory assay	30 μM	IC50=15 μM	23798680
MCF-7	Function assay	30 μM	increases the microtubule acetylation level.	23798680
MCF-7	Function assay	30 μM	stabilizes microtubules against cold-induced depolymerization	23798680
MCF-7	Function assay	15 μM	stabilizes microtubules against nocodazole-induced disassembly	23798680
MCF-7	Function assay	30 μM	alteres the assembly dynamics of interphase microtubules	23798680
MCF-7	Function assay	30 μM	increases the binding of HDAC6 with interphase microtubules	23798680
PC12	Function assay	~3 μM	up-regulates anti-oxidative gene expression related to transcription factor XBP1s	24909686
PC12	Growth inhibitory assay	~3 μM	reverse H2O2-induced growth inhibition	24909686
HEK293T	Function assay	~3 μM	up-regulated XBP1s protein level	24909686
HEK293T	Function assay	~3 μM	delays XBP1s protein degradation via acetylation-mediated proteasomal degradation	24909686
Huh7	Function assay	~5 μM	suppresses proliferation of hepatitis C virus replicon with EC50 = 0.3 μM	25108326
SKMEL21	Growth inhibitory assay	~500 nM	inhibits cell proliferation	25957812
SKMEL103	Growth inhibitory assay	~500 nM	inhibits cell proliferation	25957812
SKMEL28	Growth inhibitory assay	~500 nM	inhibits cell proliferation	25957812
WM164	Growth inhibitory assay	~500 nM	inhibits cell proliferation	25957812
WM1361a	Growth inhibitory assay	~500 nM	inhibits cell proliferation	25957812
WM1366	Growth inhibitory assay	~500 nM	inhibits cell proliferation	25957812
WM793	Growth inhibitory assay	~500 nM	inhibits cell proliferation	25957812
WM35	Growth inhibitory assay	~500 nM	inhibits cell proliferation	25957812
WM983a	Growth inhibitory assay	~500 nM	inhibits cell proliferation	25957812
WM793	Function assay	~6 μM	induce G1 arrest	25957812
WM164	Function assay	~6 μM	induce G1 arrest	25957812
WM983a	Function assay	~6 μM	induce G1 arrest	25957812
WM164	Function assay	~3 μM	augments expression of MHC class I and melanoma associated antigens	25957812
WM983a	Function assay	~3 μM	augments expression of MHC class I and melanoma associated antigens	25957812
IPC298	Function assay	~3 μM	augments expression of MHC class I and melanoma associated antigens	25957812
SKMEL30	Function assay	~3 μM	augments expression of MHC class I and melanoma associated antigens	25957812
293T	Function assay	~2 μg/ml	induces PTEN expression and membrane translocation	26279303
SACC-83	Function assay	~2 μg/ml	induces PTEN expression and membrane translocation	26279303
293T	Function assay	~2 μg/ml	induces PTEN acetylation at K163	26279303
U-87 MG	Function assay	~2 μg/ml	inhibits the migration and invasion	26279303
U-87 MG	Function assay	~10 μM	inhibits AKT phosphorylation	26279303
U-87 MG	Growth inhibitory assay	~10 μM	inhibits cell growth	26279303
TCa83	Function assay		induces PTEN expression and membrane translocation	26279303
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生物活性

製品説明

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
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]
Kinase Assay	Enzyme Inhibition Assays
Kinase Assay	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.
細胞実験	細胞株	Primary cortical neuron of fetal Sprague-Dawley rats (embryonic day 17)
	濃度	0-10 μM
	反応時間	24 hours
	実験の流れ	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.
実験結果図	Methods	Biomarkers	結果図	PMID
	Western blot	EGFR / p-AKT / AKT / p-ERK / ERK		29665050
	Immunofluorescence	α-tubulin / Acetylated tubulin HDAC6		23798680

In Vivo
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]
動物実験	動物モデル	Na?ve CD45RBhi CD4+ CD25- cells (1 × 10⁶) from WT or HDAC6-/- mice Are injected i.p. into B6/Rag1-/-mice.
	投与量	0.5 mg/kg
	投与経路	Tubastatin A is injected i.p. daily.

参考
[1] Butler KV, et al, J Am Chem Soc, 2010, 132(31), 10842-10846. [2] de Zoeten EF, et al, Mol Cell Biol, 2011, 31(10), 2066-2078. [3] Di Fulvio S, et al, PloS One, 2011, 6(12):e28563. [4] Ketene AN, et al, Integr Biol (Camb), 2012, 4(5), 540-549. + 展開

参考

[4] Ketene AN, et al, Integr Biol (Camb), 2012, 4(5), 540-549.

+ 展開

化学情報

分子量	371.86	化学式	C₂₀H₂₁N₃O₂.HCl
CAS No.	1310693-92-5	SDF	Download Tubastatin A HCl SDFをダウンロードする
Smiles	CN1CCC2=C(C1)C3=CC=CC=C3N2CC4=CC=C(C=C4)C(=O)NO.Cl
保管	3年-20°C粉	溶液の保管冷凍と解凍の繰り返しを避けるため小分けにしてください	1年-80°Cin solvent
保管	3年-20°C粉	溶液の保管冷凍と解凍の繰り返しを避けるため小分けにしてください	１ケ月-20°Cin solvent

In vitro
Batch:

DMSO : 100 mg/mL ( (268.91 mM)； Warmed with 50℃ water bath; Ultrasonicated; 吸湿したDMSOは溶解度を減少させます。新しいDMSOをご使用ください。)

Water : Insoluble

Ethanol : Insoluble

モル濃度計算器

in vivo
Batch:

Add solvents to the product individually and in order.

投与溶液組成計算機

実験計算

モル濃度計算器

質量	濃度	体積	分子量
=	×	×

希釈計算器分子量計算器

投与溶液組成計算機(クリア溶液)

ステップ１：実験データを入力してください。（実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します）

投与量 mg/kg 動物平均体重 g 投与体積（動物毎）μL 動物数匹

ステップ２：投与溶媒の組成を入力してください。（ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください）

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

計算結果：

投与溶媒濃度： mg/ml;

DMSOストック溶液調製方法： mg 試薬を μL DMSOに溶解する（濃度 mg/mL, 注：濃度が当該ロットのDMSO溶解度を超える場合はご連絡ください。 )

投与溶媒調製方法：Take μL DMSOストック溶液に μL PEG300，を加え、完全溶解後μL Tween 80，を加えて完全溶解させた後 μL ddH₂O，を加え完全に溶解させます。

投与溶媒調製方法：μL DMSOストック溶液に μL Corn oil，を加え、完全溶解。

注意：１.ストック溶液に沈殿、混濁などがないことをご確認ください；
２.順番通りに溶剤を加えてください。次のステップに進む前に溶液に沈殿、混濁などがないことを確認してから加えてください。ボルテックス、ソニケーション、水浴加熱など物理的な方法で溶解を早めることは可能です。

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