Tubastatin A |
رقم الكتالوجGC10839
One-Click Copy Product Info
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Tubastatin A is a potent and selective HDAC6 inhibitor with an IC50 value of 15 nM . Tubastatin A is also a novel GPX4 inhibitor that directly binds to GPX4 and induces ferroptosis in breast cancer cells.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1252003-15-8
Sample solution is provided at 25 µL, 10mM.
Tubastatin A is a potent and selective HDAC6 inhibitor with an IC50 value of 15 nM [1]. Tubastatin A is also a novel GPX4 inhibitor that directly binds to GPX4 and induces ferroptosis in breast cancer cells[2].
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]. Tubastatin A (32.5µM, 30µM) can inhibit cell colony formation and migration ability and promote apoptosis[3]. Tubastatin A can effectively upregulate the levels of SOD1 and HO-1 and reduce the oxidative stress of chondrocytes [4]. Tubastatin A at 10 μM also significantly inhibited cell proliferation in cholangiocarcinoma cells[5].
Tubastatin A (50mg/kg/day) treatment effectively reduces the expression of HDAC6 in the cartilage of osteoarthritis mice and improves osteoarthritis in mice with surgically destroyed medial meniscus (DMM)[4]. Tubastatin A treatment reduced tumor growth and induces ciliogenesis in rat orthotopic model of cholangiocarcinoma at 10 mg/kg[5].
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] Liu, Shan., Zhang, Hai-Liang., Li, Jing., Ye, Zhi-Peng., Du, Tian. Tubastatin A potently inhibits GPX4 activity to potentiate cancer radiotherapy through boosting ferroptosis. Redox biology, 2023.
[3] Urdiciain A, Erausquin E, Meléndez B, Rey JA, Idoate MA, Castresana JS. Tubastatin A, an inhibitor of HDAC6, enhances temozolomide-induced apoptosis and reverses the malignant phenotype of glioblastoma cells. Int J Oncol. 2019 May;54(5):1797-1808.
[4] Shen Z, Ji K, Cai Z, Huang C, He X, Xu H, Chen G. Inhibition of HDAC6 by Tubastatin A reduces chondrocyte oxidative stress in chondrocytes and ameliorates mouse osteoarthritis by activating autophagy. Aging (Albany NY). 2021 Mar 19;13(7):9820-9837.
[5] 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.
| Cell experiment [1]: | |
Cell lines | LN405 and T98G cells |
Preparation Method | LN405 and T98G cells were treated with Tubastatin A at concentrations of 32.5 and 30 µM, respectively, and images were taken under a light microscope at 0, 8, 24, 32 and 48 hours after wounding. |
Reaction Conditions | 32.5 or 30 µM; 0, 8, 24, 32 and 48h |
Applications | Tubastatin A can reduce the migration ability of LN405 and T98G cells. |
| Animal experiment [2]: | |
Animal models | Mouse osteoarthritis model |
Preparation Method | The osteoarthritis mice were randomly divided into two groups and treated with or without tubastatin A (50 mg/kg intraperitoneally daily), and the mice were killed 8 weeks after surgery. |
Dosage form | 50 mg/kg/day,8 weeks, i.p. |
Applications | Tubastatin A significantly inhibited cartilage surface degradation, tissue and synovial tissue thickening, suppressed ROS levels, and increased the concentration of glycosaminoglycans in the joint cavity. |
References: [2]. Zheng Y, Chen Y, Lu X, Weng Q, Dai G, Yu Y, Yu K, Gao W. Inhibition of Histone Deacetylase 6 by Tubastatin A Attenuates the Progress of Osteoarthritis via Improving Mitochondrial Function. Am J Pathol. 2020 Dec;190(12):2376-2386. | |
| Cas No. | 1252003-15-8 | SDF | |
| Chemical Name | 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 | ||
| Formula | C20H21N3O2 | M.Wt | 335.4 |
| الذوبان | ≥ 10.75 mg/mL in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.9815 mL | 14.9076 mL | 29.8151 mL |
| 5 mM | 596.3 μL | 2.9815 mL | 5.963 mL |
| 10 mM | 298.2 μL | 1.4908 mL | 2.9815 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >98.00% Appearance: A solid
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- SDS (Safety Data Sheet)
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Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)