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Submit ReviewTasquinimod
说明： High affinity HDAC4 negative allosteric modulator; also binds S100A9; antiangiogenic
化学名： 1,2-dihydro-4-hydroxy-5-methoxy-N,1-dimethyl-2-oxo-N-[4-(trifluoromethyl)phenyl]-3-quinolinecarboxamide
纯度： ≥98% (HPLC)
生物活性 for Tasquinimod
Tasquinimod is a high affinity negative allosteric modulator of HDAC4 (Kd = 10 - 30 nM). Binds the regulatory Zn2+ binding domain of HDAC4. Suppresses hypoxia-induced decrease in histone acetylation in human prostate cancer cells in vitro. Also binds S100A9. Antiangiogenic. Inhibits endothelial sprouting in vitro and growth of prostate tumor xenografts in nude mice. Orally bioavailable.
化合物库 for Tasquinimod
Tasquinimod is also offered as part of the Tocriscreen Antiviral Library and Tocriscreen Epigenetics Library. 了解 Tocris 化合物库的更多信息。
技术数据 for Tasquinimod
| 分子量 | 406.36 |
| 公式 | C20H17F3N2O4 |
| 储存 | Store at -20°C |
| 纯度 | ≥98% (HPLC) |
| CAS Number | 254964-60-8 |
| PubChem ID | 54682876 |
| InChI Key | ONDYALNGTUAJDX-UHFFFAOYSA-N |
| Smiles | COC1=C2C(O)=C(C(=O)N(C)C3=CC=C(C=C3)C(F)(F)F)C(=O)N(C)C2=CC=C1 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶解性数据 for Tasquinimod
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| DMSO | 40.64 | 100 | |
| ethanol | 8.13 | 20 |
制备储备液 for Tasquinimod
以下数据基于产品分子量 406.36。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| 浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 2.46 mL | 12.3 mL | 24.61 mL |
| 5 mM | 0.49 mL | 2.46 mL | 4.92 mL |
| 10 mM | 0.25 mL | 1.23 mL | 2.46 mL |
| 50 mM | 0.05 mL | 0.25 mL | 0.49 mL |
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产品说明书 for Tasquinimod
参考文献 for Tasquinimod
参考文献是支持产品生物活性的出版物。
Isaacs et al (2013) Tasquinimod is an allosteric modulator of HDAC4 survival signaling within the compromised cancer microenvironment. Cancer Res. 73 1386 PMID: 23149916
Isaacs et al (2014) Anti-cancer potency of Tasquinimod is enhanced via albumin-binding facilitating increased uptake in the tumor microenvironment. Oncotarget 5 8093 PMID: 25193858
If you know of a relevant reference for Tasquinimod, please let us know.
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关键词: Tasquinimod, Tasquinimod supplier, High, affinity, HDAC4, histone, deacetylase, negative, allosteric, modulators, modulates, NAM, orally, bioavailable, antiangiogenic, binds, S100A9, Class, II, HDACs, 7051, Tocris Bioscience
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该领域的文献
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*请注意，Tocris 仅会向正规科研企业/机构地址发送文献。
Epigenetics Scientific Review
Written by Susanne Müller-Knapp and Peter J. Brown, this review gives an overview of the development of chemical probes for epigenetic targets, as well as the impact of these tool compounds being made available to the scientific community. In addition, their biological effects are also discussed. Epigenetic compounds available from Tocris are listed.
Cell Cycle & DNA Damage Repair Poster
In normal cells, each stage of the cell cycle is tightly regulated, however in cancer cells many genes and proteins that are involved in the regulation of the cell cycle are mutated or over expressed. This poster summarizes the stages of the cell cycle and DNA repair. It also highlights strategies for enhancing replicative stress in cancer cells to force mitotic catastrophe and cell death.
Epigenetics in Cancer Poster
This poster summarizes the main epigenetic targets in cancer. The dysregulation of epigenetic modifications has been shown to result in oncogenesis and cancer progression. Unlike genetic mutations, epigenetic alterations are considered to be reversible and thus make promising therapeutic targets.
Rheumatoid Arthritis Poster
Rheumatoid arthritis (RA) is a chronic destructive inflammatory autoimmune disease that results from a breakdown in immune tolerance, for reasons that are as yet unknown. This poster summarizes the pathology of RA and the inflammatory processes involved, as well as describing some of the epigenetic modifications associated with the disease and the potential for targeting these changes in the discovery of new treatments.