Tubastatin A

製品コード：S8049 純度：99.63%

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). Tubastatin A promotes autophagy and increases apoptosis.

CAS No. 1252003-15-8

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Tubastatin A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
関連製品	Entinostat (MS-275) TSA (Trichostatin A) Mocetinostat (MGCD0103) RGFP966 Ricolinostat (ACY-1215) Quisinostat (JNJ-26481585) 2HCl MC1568 Tubastatin A HCl PCI-34051 Tacedinaline (CI994) LMK-235 Fimepinostat (CUDC-907) Tubacin Givinostat hydrochloride monohydrate TMP269 AR-42 Sodium butyrate Pracinostat (SB939) Santacruzamate A (CAY10683) Abexinostat (PCI-24781) (-)-Parthenolide CUDC-101 Dacinostat (LAQ824) CAY10603 RG2833 (RGFP109) Tasquinimod Tucidinostat (Chidamide) TMP195 Nexturastat A Droxinostat Domatinostat (4SC-202) Scriptaid 4-PBA (4-Phenylbutyric acid) M344 Resminostat Citarinostat (ACY-241) BG45 WT161 ACY-738 HPOB ITSA-1 (ITSA1) Tubastatin A TFA TC-H 106 SIS17 ACY-775 BML-210 (CAY10433) TH34 Raddeanin A	もっと見る
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

阻害剤	Citation	HDAC	HDAC1	HDAC2	HDAC3	HDAC4	HDAC5	HDAC6	HDAC7	HDAC8	HDAC9	HDAC10	HDAC11	HD1	HD2	その他
Entinostat (MS-275)	406		+		+
TSA (Trichostatin A)	281	++++
Mocetinostat (MGCD0103)	114		++	++	+								+
MC1568	50													++
Tubastatin A HCl	47							+++		+
Givinostat hydrochloride monohydrate	32													++++	+++
Dacinostat (LAQ824)	22	+++
CUDC-101	23	++++	++++	+++	+++	+++	+++	++++	+	++	++	+++				EGFR,HER2
Quisinostat (JNJ-26481585) 2HCl	59		++++	++++	++++	++++	++++			++++		++++	++++
Pracinostat (SB939)	23		+++	++	+++	++	+++	+	++	++	++	+++	++
PCI-34051	52									+++
Droxinostat	14				+			+		+
Abexinostat (PCI-24781)	24		++++	+++	++++			+++		++		+++
RGFP966	111				++
AR-42	29	+++
Ricolinostat (ACY-1215)	70		++	+++	++			++++		++
Tacedinaline (CI994)	41		+	+	+
Fimepinostat (CUDC-907)	36		++++	++++	++++			+++				++++	++++			PI3Kα,PI3Kδ,PI3Kβ
M344	11	++
Tubacin	35							++++
RG2833 (RGFP109)	22		++		+++
Resminostat	7		+++		+++			++
Tubastatin A	103							+++
SW-100	0							++++
KT-531	0							++++
CXD101	0		++	+	+
KA2507	0							++++
BRD-6929	1		+++	++
ACY-775	2							++++
Tubastatin A TFA	2							+++
BRD3308	0		+	+	++
SIS17	4												+
SR-4370	0		++	+	++++			+		+
TC-H 106	3		++	++	+++
NKL 22	0	+
Tinostamustine(EDO-S101)	0		++++	++++	+++			++++		++		++
SKLB-23bb	0							++
TH34	2							+		+		+
Suberohydroxamic acid	0		++		++
UF010	1		++++	++++	++++			+++		++++		+++
WT161	4		++++	+++				++++
ACY-738	4							++++
Tucidinostat (Chidamide)	25		++	++	++							++
TMP195	18					++	++		+++		+++
Citarinostat (ACY-241)	5		+++	+++	+++			++++		++
BRD73954	0							+++		++
BG45	7		+	+	++
Domatinostat (4SC-202)	13		+	+	+		+				+	+	+
CAY10603	24							++++
LMK-235	39					+++	++++
Splitomicin	0	+
Santacruzamate A (CAY10683)	25			++++
Nexturastat A	14							++++
TMP269	30					++	++		+++		+++
HPOB	3		+	+	+			++		+		+
Pyroxamide (NSC 696085)	0		++
Sodium butyrate	33	✔
Curcumin	47	✔														NF-κB,Nrf2,Ferroptosis
Scriptaid	13	✔
TNG260	0		✔
Tefinostat(CHR-2845)	0	✔
ITF3756	0							✔
4-PBA (4-Phenylbutyric acid)	18	✔
GSK3117391	0	✔
BML-210 (CAY10433)	1	✔
Sulforaphane	18	✔														ROS,NF-κB,Nrf2
Raddeanin A	1	✔
Isoguanosine	0				✔											FLT3
Sinapinic Acid	1	✔														ACE1
Tasquinimod	18					✔
(-)-Parthenolide	22		✔													NF-κB,p53,MDM2

1. "+" indicates inhibitory effect. Increased inhibition is marked by a higher "+" designation. 2. "✔" indicates inhibitory effect, but without specific value.

Cell Data

Cell Lines	Assay Type	Concentration	Incubation Time	活性情報	PMID
KB	Function assay	14 uM	24 hrs	Inhibition of HDAC1 in human KB cells assessed as increase in histone H4 acetylation at 14 uM after 24 hrs by Western blotting analysis	25899338
KMS-12-BM	Function assay	15 uM	up to 48 hrs	Inhibition of HDAC6 in human KMS-12-BM cells assessed as increase in acetylated tubulin level at 15 uM up to 48 hrs by immunoblot method	27541357
MOLM14	Function assay	15 uM	up to 48 hrs	Inhibition of HDAC6 in human MOLM14 cells assessed as increase in acetylated tubulin level at 15 uM up to 48 hrs by immunoblot method	27541357
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生物活性

製品説明

Targets

HDAC6 ^[1]
(Cell-free assay)

15 nM

In Vitro
In vitro	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]
Kinase Assay	HDAC enzymatic assays
Kinase Assay	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 (K_m), 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.
細胞実験	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.
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	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]
動物実験	動物モデル	Rat cholangiocarcinoma xenografts BDEneu
	投与量	10 mg/kg
	投与経路	i.p. daily

参考
[1] Butler KV, et al. J Am Chem Soc, 2010, 132(31), 10842-10846. [2] Gradilone SA, et al. Cancer Res, 2013, 73(7), 2259-2270. [3] Vishwakarma S, et al. Int Immunopharmacol, 2013, 16(1), 72-78. [4] Santo L, et al. Blood, 2012, 119(11), 2579-2589. + 展開

参考

[4] Santo L, et al. Blood, 2012, 119(11), 2579-2589.

+ 展開

化学情報

分子量	335.4	化学式	C₂₀H₂₁N₃O₂
CAS No.	1252003-15-8	SDF	Download Tubastatin A 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
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 : 16.7 mg/mL ( (49.79 mM)；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

Clear solution

5%DMSO 1 40%PEG300 Click to order 2 5%Tween 80 Click to order 3 50%ddH2O

1.67mg/ml (4.98mM)

Taking the 1 mL working solution as an example, add 50 μL of 33.4 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to make it clear. Volume up to 1 mL. The mixed solution should be used immediately for optimal results.

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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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.

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):