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Submit ReviewHarmine
说明： Potent and selective DYRK1A inhibitor
化学名： 7-Methoxy-1-methyl-9H-pyrido[3,4-b]indole
纯度： ≥98% (HPLC)
生物活性 for Harmine
Harmine is a potent and selective inhibitor of DYRK1A (IC50 values are 80, 800 and 900 nM for DYRK1A, DYRK3 and DYRK2 respectively). Inhibits DYRK1A-mediated tau phosphorylation and regulates PPARγ expression. Harmine also induces pancreatic β cell proliferation and exhibits antidiabetic activity. Orally bioavailable. Harmine has high affinity (Kd = 100 nM) for the yjdF aptamer. The riboswitch function of yjdF motif RNAs is activated by Harmine and leads to robust reporter gene expressions in B. subtilis.
技术数据 for Harmine
| 分子量 | 212.25 |
| 公式 | C13H12N2O |
| 储存 | Store at RT |
| 纯度 | ≥98% (HPLC) |
| CAS Number | 442-51-3 |
| PubChem ID | 5280953 |
| InChI Key | BXNJHAXVSOCGBA-UHFFFAOYSA-N |
| Smiles | CC1=NC=CC2=C1NC3=C2C=CC(OC)=C3 |
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 Harmine
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| DMSO | 21.23 | 100 | |
| ethanol | 1.06 | 5 温和加热 |
制备储备液 for Harmine
以下数据基于产品分子量 212.25。 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 | 4.71 mL | 23.56 mL | 47.11 mL |
| 5 mM | 0.94 mL | 4.71 mL | 9.42 mL |
| 10 mM | 0.47 mL | 2.36 mL | 4.71 mL |
| 50 mM | 0.09 mL | 0.47 mL | 0.94 mL |
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产品说明书 for Harmine
参考文献 for Harmine
参考文献是支持产品生物活性的出版物。
Smith et al (2012) Recent advances in the design, synthesis, and biological evaluation of selective DYRK1A inhibitors: a new avenue for a disease modifying treatment of Alzheimer's? ACS Chem.Neurosci. 3 857 PMID: 23173067
Bain et al (2007) The selectivity of protein kinase inhibitors: a further update. Biochem.J. 408 297 PMID: 17850214
Waki et al (2007) The small molecule harmine is an antidiabetic cell-type-specific regulator of PPARγ expression. Cell Metab. 5 357 PMID: 17488638
Wang et al (2015) A high-throughput chemical screen reveals that harmine-mediated inhibition of DYRK1A increases human pancreatic beta cell replication. Nat.Med. 21 383 PMID: 25751815
Li et al (2016) The yjdF riboswitch candidate regulates gene expression by binding diverse azaaromatic compounds. RNA 22 530 PMID: 26843526
If you know of a relevant reference for Harmine, please let us know.
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2 篇 Harmine 的引用文献
引用文献是使用了 Tocris 产品的出版物。 Harmine 的部分引用包括：
Sourav et al (2021) The stress-responsive kinase DYRK2 activates heat shock factor 1 promoting resistance to proteotoxic stress. Cell Death Differ 28 1563-1578 PMID: 33268814
Singh et al (2017) Different developmental histories of beta-cells generate functional and proliferative heterogeneity during islet growth. Nat Commun 8 664 PMID: 28939870
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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。
Alzheimer's Disease Poster
Alzheimer's disease (AD) is a debilitating and progressive neurodegenerative disease and the most common cause of dementia, affecting approximately 30% of individuals aged over 85 years. This poster summarizes the cellular and molecular mechanisms of AD.
Parkinson's Disease Poster
Parkinson's disease (PD) causes chronic disability and is the second most common neurodegenerative condition. This poster outlines the neurobiology of the disease, as well as highlighting current therapeutic treatments for symptomatic PD, and emerging therapeutic strategies to delay PD onset and progression.