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Niltubacin

目录号 M1738 所有产品仅供科研使用,严禁用于人或动物的治疗等任何其他用途,不为任何个人提供产品和服务  


Niltubacin, as an inactive derivative of Tubacin, is a highly potent and selective, reversible cell-permeable inhibitor of HDAC6.

Niltubacin结构式

别名:MAZ-1391

包装 价格 库存状态
1mg 原价 ¥ 3840
促销价 ¥ 3648
中国库存现货
2mg 原价 ¥ 7200
促销价 ¥ 6840
中国库存现货
其他规格数量报价?

质量控制及产品安全说明书
  • 当前批次:
  • 纯度 >98%
  • COA
  • MSDS
生物活性

Niltubacin, as an inactive derivative of Tubacinis, is a highly potent and selective, reversible cell-permeable inhibitor of HDAC6. Histone deacetylase 6 (HDAC6) is structurally and functionally unique among the 11 human zinc-dependent histone deacetylases. HDAC6-selective inhibitor tubacin significantly enhances cell death induced by the topoisomerase II inhibitors etoposide and doxorubicin and the pan-HDAC inhibitor SAHA (vorinostat) in transformed cells (LNCaP, MCF-7), an effect not observed in normal cells. The inactive analogue of tubacin, nil-tubacin, does not sensitize transformed cells to these anticancer agents.

实验操作 来自于公开的文献,仅供相同实验参考(如实验材料、目的不同,请参考其他文献)
细胞实验
细胞系 Raji cells
方法 Cell adhesion assay Prior to SDF-1α (100 ng/ml) stimulation, Raji cells were treated with DMSO, NaB (1 μM), or tubacin (1 μM) for 3 hours. Then cells were plated into a 96-well plate which were precoated with Fibronectin (50 ng/ml) to allow cell adherence for 30 minutes. Subsequently cells were washed with PBS three times to remove the non-adherent cells, and adherent cells were measured by CellTiter-Glo luminescent cell viability assay kit.
浓度 1μM
处理时间 3h
动物实验
动物模型 PLD animal model 3-week-old PCK rats
配制 saline
剂量 30 mg/kg body
给药处理 intraperitoneally
不同实验动物依据体表面积的等效剂量转换表(数据来源于FDA指南)
小鼠 大鼠 豚鼠 仓鼠
重量 (kg) 0.02 0.15 1.8 0.4 0.08 10
体表面积 (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km 系数 3 6 12 8 5 20
动物 A (mg/kg) = 动物 B (mg/kg) ×  动物 B的Km系数
动物 A的Km系数

例如,依据体表面积折算法,将白藜芦醇用于小鼠的剂量22.4 mg/kg 换算成大鼠的剂量,需要将22.4 mg/kg 乘以小鼠的Km系数(3),再除以大鼠的Km系数(6),得到白藜芦醇用于大鼠的等效剂量为11.2 mg/kg。

化学数据
分子量 706.85
分子式 C41H42N2O7S
CAS号
纯度 >98%
溶解性(25°C) DMSO ≥5 mg/mL
储存和运输条件 固体粉末: -20°C 冷藏长期储存
常温运输及临时存放
储备液配制

以下数据基于产品分子量,对于特殊产品,请参照COA中的储备液配制条件和说明进行操作。

Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.4147 mL 7.0736 mL 14.1473 mL
5 mM 0.2829 mL 1.4147 mL 2.8295 mL
10 mM 0.1415 mL 0.7074 mL 1.4147 mL
使用AbMole产品发表的文献
客户产品验证及相关生物数据
数据来源 J Cell Biochem (2017). Figure 5. Niltubacin (Abmole Bioscience Inc.)
方法 Clonogenic survival assay
细胞系 FEMX-I cell line
浓度 200 µm
处理时间 24 h
实验结果 This effect was specific for tubacin, as TSA, niltubacin and ACY-1215 did not inhibit the formation of cell aggregates. Similar effects were observed in Caco-2 cell line (Supplementary Fig. S5).
数据来源 J Cell Biochem (2017). Figure 2. Niltubacin (Abmole Bioscience Inc.)
方法 Cell Aggregation Assay
细胞系 FEMX-I cell line
浓度
处理时间 24 h
实验结果 The effect was specific, as the inactive analog of tubacin, niltubacin, at the same concentration did not increase CD133, CD9, or b-actin levels (Fig. 2c).
数据来源 Mol. Cell. Biol. (2016). Figure 9. Tubacin and Niltubacin for animal studies were obtained from AbMole Bioscience Inc. (Houston, TX)
方法 BK-SS mice
细胞系
浓度 0.5mg/kg i.p.
处理时间 5 or 10 or 30 days
实验结果 These drug regimens showed a time dependent reduction of PlGF (Fig. 9C) and ET-1 (Fig. 9D) in plasma, compared to Niltubacin. The 30 day drug treatment effectively reduced plasma levels of PlGF by ~60% (p <0.001, Fig. 9C) and plasma levels of ET-1 by ~60% (p<0.001, Fig. 9D).
数据来源 Mol. Cell. Biol. (2016). Figure 7. Tubacin and Niltubacin for animal studies were obtained from AbMole Bioscience Inc. (Houston, TX)
方法 FAIRE-qPCR
细胞系 HMEC-1 cells
浓度 5 µM
处理时间 30 min
实验结果 Taken together, these data showed PlGF induced chromatin condensation to repress DNM3os transcription, while Tubacin prevented the repressive effect following PlGF signaling.
数据来源 Mol. Cell. Biol. (2016). Figure 6. Tubacin and Niltubacin for animal studies were obtained from AbMole Bioscience Inc. (Houston, TX)
方法 qRT-PCR and reporter luciferase activity
细胞系 HMEC-1 cells
浓度 5 µM
处理时间 30 min
实验结果 We concluded that HDAC6 required functional ATF3 binding sites in the DNM3os promoter and any antagonism of PlGF effects by Tubacin was not due to a general effect on transcription of the endogenous DNM3os gene or the wt DNM3os reporter construct.
参考文献

Selective inhibition of histone deacetylase 6 (HDAC6) induces DNA damage and sensitizes transformed cells to anticancer agents.
Namdar et al. Proc Natl Acad Sci U S A. 2010 Nov 16;107(46):20003-8. PMID: 21037108.

Histone deacetylase 6 interacts with the microtubule-associated protein tau.
Ding et al. J Neurochem. 2008 Sep;106(5):2119-30. PMID: 18636984.

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