Tubastatin A
目录号 : GC10839
Tubastatin A 是一种有效的选择性 HDAC6 抑制剂，IC50 值为 15 nM。并且Tubastatin A也是一种新型GPX4抑制剂，Tubastatin A 直接与 GPX4 结合，诱导乳腺癌细胞铁死亡。
Cas No.:1252003-15-8
Sample solution is provided at 25 µL, 10mM.
;)
,-1-7$$$37316672.jpg');)
;)
;)
$$$36806353.jpg');)
;33(7)%EF%BC%9A546-561$$$37156877.jpg');)
;)
;)
;)
%201124-1138.$$$35908550.jpg');)
%20766-780.$$$37100057.jpg');)
%20418-432.$$$36893736.jpg');)
%EF%BC%9A-240-255.$$$35108512.jpg');)
533-545$$$36543525.jpg');)
%201-13.$$$36600053.jpg');)
;)
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.
Tubastatin A 是一种有效的选择性 HDAC6 抑制剂，IC50 值为 15 nM [1]。并且Tubastatin A也是一种新型GPX4抑制剂，Tubastatin A 直接与 GPX4 结合，诱导乳腺癌细胞铁死亡[2]。
Tubastatin A以剂量依赖性方式防止 HCA 诱导的神经元细胞死亡，在 2.5 μM 浓度下可以诱导 α-微管蛋白过度乙酰化[1] 。Tubastatin A（32.5µM，30µM）可抑制细胞的集落形成、迁移能力并促进其凋亡[3]。Tubastatin A 能够有效上调SOD1和HO-1的水平，减少软骨细胞的氧化应激[4]。10μM 的 Tubastatin A 还可显着抑制胆管癌细胞的增殖[5]。
Tubastatin A (50mg/kg/day)治疗有效降低骨关节炎小鼠软骨中 HDAC6 的表达，改善被手术破坏内侧半月板（ DMM）小鼠的骨关节炎[4]。在胆管癌大鼠原位模型中，10 mg/kg 的 Tubastatin A 治疗可减少肿瘤生长并诱导纤毛生成[5] 。
| 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 | |
| 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。 | ||
| 制备储备液 | |||
 |
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 |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet