bs-60241C

DATASHEET

Formulation Powder

Storage: Store in dry, dark place at -20C for 1 year.

Product Information:

Molecular Weight: 212.25

Formula: C13 H12 N2 O

CAS Number: 442-51-3

InChi Key: BXNJHAXVSOCGBA-UHFFFAOYSA-N

InChi: InChI=1S/C13H12N2O/c1-8-13-11(5-6-14-8)10-4-3-9(16-2)7-12(10)15-13/h3-7,15H,1-2H3

Smiles: CC1=NC=CC2=C1NC1=CC(=CC=C21)OC

Purity: 98.0

Solubility: DMSO up to 100 mM

Appearance: Solid Power.

Shelf Life: 1.0 years

Description:

Harmine is a potent, selective and orally bioavailable DYRK1A inhibitor with IC50 of 80 nM. It inhibits phosphorylation of tau directly by DYRK1A (IC50 ~700 nM). It has >10-fold selectivity over DYRK3 and DYRK2 (IC50 ~800 nM and 900 nM respectively. Harmine is also a unique regulator of PPARγ expression that acts by inhibiting the Wnt signalling pathway in a cell-specific manner. It attenuates inflammatory gene expression (TNFα, IL-1β, iNOS) and macrophage accumulation in adipose tissue. Administration of harmine (30 mg/kg) to obese db/db mice resulted in reduced blood glucose, free fatty acids, and triglyceride levels, delayed hyperglycemia, and improved insulin sensitivity. Being function as a new class of human beta cell mitogenic compound, by using three different mouse and human islet in vivo-based models, harmine is able to induce beta cell proliferation, increase islet mass and improve glycemic control. The nuclear factors of activated T cells (NFAT) family of transcription factors are defined as likely mediators of human beta cell proliferation and differentiation.