Formal Name: 2-Amino-6-mercaptopurine
Alternate Names: 6-TG; NSC 752; NSC 76504
Molecular Formula: C5H5N5S
Formula Weight: 167.19
CAS Number: 154-42-7
Purity: >98%
Formulation: powder
Solubility: Soluble in DMF (up to 1.5 mg/ml with warming)
Storage: -20°C
Stability: ≥ 1 year.
Applications
Anticancer agent; Downregulates DNMT1
Functions
After incorporation into DNA, it disrupts cytosine methylation by DNA methyltransferases in vitro and acts as a DNA demethylating agent in vivo. It reactivates epigenetically silenced genes in acute lymphoblastic leukemia cells by facilitating proteasome-mediated degradation of DNA methyltransferase (DNMT1). Incorporates into DNA and induces double strand breaks which destabilize DNA structure resulting in cytotoxicity. Selectively kills BRCA2-defective tumors and overcomes PARP inhibitor resistance in a xenograft model. Anticancer and immunosuppressive activity.
Application Procedures
First dissolved in DMF (up to 1.5 mg/ml with warming), then diluted to aqueous buffer. Solutions in DMF may be stored at -20°C for up to 1 month.