Harmine

Name: Harmine
Brand: Tocris Bioscience
SKU: 5075

Tocris Bioscience, part of Bio-Techne | Catalog # 5075

Citations (16)

COA / SDS

Potent and selective DYRK1A inhibitor

Key Product Details

Description:	Potent and selective DYRK1A inhibitor
Chemical Name:	7-Methoxy-1-methyl-9H-pyrido[3,4-b]indole
Purity:	≥98% (HPLC)
Molecular Weight:	212.25

View Full Technical Details for Harmine

Technical Data
Citations

Biological Activity 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 (K_d = 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.

Technical Data for Harmine

M. Wt	212.25
Formula	C₁₃H₁₂N₂O
Storage	Store at RT
Purity	≥98% (HPLC)
CAS Number	442-51-3
PubChem ID	5280953
InChi Key	BXNJHAXVSOCGBA-UHFFFAOYSA-N
Smiles	CC1=NC=CC2=C1NC3=C2C=CC(OC)=C3

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.

Solubility for Harmine

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
	DMSO	21.23	100
	ethanol	1.06	5 with gentle warming

Preparing Stock Solutions for Harmine

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

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References for Harmine

References are publications that support the biological activity of the product.

Li The yjdF riboswitch candidate regulates gene expression by binding diverse azaaromatic compounds. RNA 2016 PMID: 26843526
Wang A high-throughput chemical screen reveals that harmine-mediated inhibition of DYRK1A increases human pancreatic beta cell replication. Nat.Med. 2015 PMID: 25751815
Bain The selectivity of protein kinase inhibitors: a further update. Biochem.J. 2007 PMID: 17850214
Waki The small molecule harmine is an antidiabetic cell-type-specific regulator of PPARγ expression. Cell Metab. 2007 PMID: 17488638
Smith 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. 2012 PMID: 23173067