Harmine
Harmine, also known as telepathine, is an alkaloid of the β-carboline family that regulates PPARγ expression through inhibition of the Wnt signaling pathway. It also selectively binds to MAO-A and reversibly inhibits monoamine oxidase A (MAO-A) but not the variant MAO-B[3].Harmine has a severe cytotoxicity in hepatoma cells and holds great promise as an oncologic drug for anticancer treatment[4].
References:
[1] Smith B, Medda F, Gokhale V, et al. Recent Advances in theDesign, Synthesis, and BiologicalEvaluation of Selective DYRK1A Inhibitors: A New Avenue for a DiseaseModifying Treatment of Alzheimer’s?[J]. Acs Chemical Neuroscience, 2012, 3(11):857-72.
[2] Waki H, Park K W, Mitro N, et al. The small molecule harmine is an antidiabetic cell-type-specific regulator of PPARgamma expression.[J]. Cell Metabolism, 2007, 5(5):357-370.
[3] Ginovart N, Meyer J H, Boovariwala A, et al. Positron emission tomography quantification of |[lsqb]|11C|[rsqb]|-harmine binding to monoamine oxidase-A in the human brain[J]. Journal of Cerebral Blood Flow & Metabolism Official Journal of the International Society of Cerebral Blood Flow & Metabolism, 2006, 26(3):330-44.
[4] Zhang L, Zhang F, Zhang W, et al. Harmine suppresses homologous recombination repair and inhibits proliferation of hepatoma cells[J]. Cancer Biology & Therapy, 2015, 16(11):1585-1592.
Physical Appearance | A solid |
Storage | Store at -20°C |
M.Wt | 212.25 |
Cas No. | 442-51-3 |
Formula | C13H12N2O |
Solubility | insoluble in H2O; ≥33 mg/mL in DMSO with ultrasonic; ≥6.35 mg/mL in EtOH with gentle warming and ultrasonic |
Chemical Name | 7-methoxy-1-methyl-9H-pyrido[3,4-b]indole |
SDF | Download SDF |
Canonical SMILES | CC1=NC=CC2=C1NC3=C2C=CC(OC)=C3 |
Shipping Condition | Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice. |
General tips | We do not recommend long-term storage for the solution, please use it up soon. |
Potent and selective inhibitor of DYRK1A (IC50 values are 80, 800 and 900 nM for DYRK1A, DYRK3 and DYRK2 respectively)[1]. It can also regulate PPARγ expression through inhibition of the Wnt signaling pathway[2]. | ||||||
Targets | DYRK1A | DYRK3 | DYRK2 | PPARγ | ||
IC50 | 80nM | 800nM | 900nM | -- |
Quality Control & MSDS
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Chemical structure
