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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. Also induces pancreatic beta cell proliferation. Exhibits antidiabetic activity. Orally bioavailable.
|Storage||Store at RT|
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
|ethanol||1.06||5 with gentle warming|
Preparing Stock Solutions
The following data is based on the product molecular weight 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.
|Concentration / Solvent Volume / Mass||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|
References are publications that support the biological activity of the product.
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
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1 Citation for Harmine
Citations are publications that use Tocris products. Selected citations for Harmine include:
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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Literature in this Area
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
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Alzheimer's disease (AD) is a degenerative brain disease and the most common cause of dementia, affecting approximately 47 million people worldwide. Updated in 2015, this poster summarizes the structural and functional changes observed in the progression of this neurodegenerative disease, as well as classic AD drug targets.
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.