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Tubastatin A Sale

目录号 : GC10839

A potent HDAC6 inhibitor

Tubastatin A Chemical Structure

Cas No.:1252003-15-8

规格 价格 库存 购买数量
10mM (in 1mL DMSO)
¥389.00
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10mg
¥378.00
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50mg
¥504.00
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100mg
¥882.00
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200mg
¥1,512.00
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Sample solution is provided at 25 µL, 10mM.

产品文档

Quality Control & SDS

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实验参考方法

Cell experiment [1]:

Cell lines

Human breast cancer cells (MCF-7).

Preparation method

Soluble in DMSO > 10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months.

Reaction Conditions

15, 30 μM; 48 h.

Applications

In MCF-7 cells, tubastatin A inhibits cell proliferation in a dose-dependent way with IC50 value of 15 μM and increases the acetylation of cytoplasmic microtubules. Also, tubastatin A reduces the microtubule depolymerization rate induced by cold and 200 nM nocodazole, which is mediated by the inhibition of HDAC6.

Animal experiment [2]:

Animal models

Wistar rats; DBA1 mice

Dosage form

Rats: 30 mg/kg/day i.p. for 5 days; mice: 30 mg/kg, q.d. from day 21 to day 36.

Preparation method

Solubilized in 10% Dimethyl sulfoxide (DMSO) 10% Polyethylene glycol (PEG) 400 and 80% (40% of hydroxy propyl beta cyclodextrin).

Applications

In FCA injected rats, tubastatin significantly reduces paw volume by 71.9% at 2 h. In DBA1 arthritis mouse induced by semi-therapeutic collagen, tubastatin (30 mg/kg/day, i.p.) significantly reduces arthritic clinical scores by 73% and inhibits the production of IL-6 in paw tissues by 59%. Tubastatin treated mice shows insignificant changes in body weight.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

References:

[1]. Asthana J, Kapoor S, Mohan R, et al. Inhibition of HDAC6 deacetylase activity increases its binding with microtubules and suppresses microtubule dynamic instability in MCF-7 cells. J Biol Chem, 2013, 288(31): 22516-22526.

[2]. Vishwakarma S, Iyer LR, Muley M, et al. Tubastatin, a selective histone deacetylase 6 inhibitor shows anti-inflammatory and anti-rheumatic effects. Int Immunopharmacol, 2013, 16(1): 72-78.

产品描述

Tubastatin A is a potent and selective inhibitor of HDAC6 with IC50 value of 15 nM [1].
Histone deacetylases (HDACs) and histone acetyltransferases (HATs) mediates the balance between histone deacetylation and acetylation. HDACs also regulate the acetylation status of signaling molecules, chaperones, and transcription factors that are non-histone proteins [2]. HDAC6 interacts with the HSP90 which is a molecular chaperone. The deacetylation of HSP90 by HDAC6 is important for the stability and of many client proteins including Bcr-Abl, c-Raf, and AKT. So, HDAC inhibitors have anti-cancer function [2].
Tubastatin A is a selective inhibitor of HDAC6 compared with other HDACs. Tubastatin A maintained an average 200-fold selectivity compared with class I HDACs. Tubastatin A displayed selectivity against all isoforms excluding HDAC8 over 1000-fold.
Tubastatin A protected against HCA induced neuronal cell death in a dose-dependent manner. Tubastatin A induced the hyperacetylation of  α-tubulin at 2.5 μM[1]. In LPS stimulated human THP-1 macrophages, Tubastatin A displayed significant inhibition of IL-6 and TNF with an IC50 of 712 nM and 212 nM [3]. Tubastatin A showed the inhibition of nitric oxide (NO) secretion with an IC50 of 4.2μM in murine Raw 264.7 macrophages [3]. Tubastatin-A also significantly inhibit cell proliferation at 10μM in KMCH cells [4].
Tubastatin A showed inhibition of paw volume at 30 mg/kg in an animal model of inflammation[3]. Tubastatin-A treatment reduced tumor growth and induces ciliogenesis in rat orthotopic model of cholangiocarcinoma at 10 mg/kg [4].
References:
1.Butler KV, Kalin J, Brochier C, Vistoli G, Langley B, Kozikowski AP: Rational design and simple chemistry yield a superior, neuroprotective HDAC6 inhibitor, tubastatin A. J Am Chem Soc 2010, 132(31):10842-10846.
2.Kim HJ, Bae SC: Histone deacetylase inhibitors: molecular mechanisms of action and clinical trials as anti-cancer drugs. Am J Transl Res 2011, 3(2):166-179.
3.Vishwakarma S, Iyer LR, Muley M, Singh PK, Shastry A, Saxena A, Kulathingal J, Vijaykanth G, Raghul J, Rajesh N et al: Tubastatin, a selective histone deacetylase 6 inhibitor shows anti-inflammatory and anti-rheumatic effects. Int Immunopharmacol 2013, 16(1):72-78.
4.Gradilone SA, Radtke BN, Bogert PS, Huang BQ, Gajdos GB, LaRusso NF: HDAC6 inhibition restores ciliary expression and decreases tumor growth. Cancer Res 2013, 73(7):2259-2270.

Chemical Properties

Cas No. 1252003-15-8 SDF
化学名 N-hydroxy-4-((2-methyl-3,4-dihydro-1H-pyrido[4,3-b]indol-5(2H)-yl)methyl)benzamide
Canonical SMILES CN(C1)CCC2=C1C3=C(N2CC4=CC=C(C(NO)=O)C=C4)C=CC=C3
分子式 C20H21N3O2 分子量 335.4
溶解度 ≥ 10.75 mg/mL in DMSO 储存条件 Store at -20°C
General tips 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。
储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。
Shipping Condition 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。

溶解性数据

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1 mg 5 mg 10 mg
1 mM 2.9815 mL 14.9076 mL 29.8151 mL
5 mM 0.5963 mL 2.9815 mL 5.963 mL
10 mM 0.2982 mL 1.4908 mL 2.9815 mL
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