Stemcell, 100-1640, 3-Deazaneplanocin A (Hydrochloride)

Regulate tumor suppressor genes with 3-Deazaneplanocin A (Hydrochloride), an S-adenosyl-L-homocysteine hydrolase (SAHase) inhibitor (IC50 = 0.08 - 0.24 ­µM). SAHase inhibition reduces the protein levels of enhancer of zeste homolog 2 (EZH2), a histone methyltransferase (Tseng et al. J Med Chem, 1989). Part of the polycomb repressive complex 2 (PRC2), EZH2 is an important regulator of tumor suppressor genes and is associated with regulation of cell proliferation, apoptosis, senescence, and DNA damage repair. EZH2 can be selectively targeted by 3-Deazaneplanocin A (Hydrochloride), making it an attractive target for cancer therapy (Duan et al. J Hematol Oncol, 2020; Tan et al. Genes Dev, 2007). This product is supplied as the hydrochloride salt of the molecule.

3-Deazaneplanocin A (Hydrochloride) has been used for:

DIFFERENTIATION

· Support differentiation of reprogrammed urine-derived cells into myotubes by promoting expression of myogenin (Takizawa et al. Sci Rep, 2019).

· Contribute to erythroid differentiation of human leukemia cells by promoting expression of erythroid-related genes (Fujiwara et al. J Biol Chem, 2014).

CANCER RESEARCH

· Induce cell death and reduce cell migration in human chondrosarcoma cell lines (Girard et al. PLoS One, 2014).

· Increase apoptosis in human gastric cancer cells with high expression of EZH2 (Pan et al. Mol Cancer, 2016).