6-Thioguanine, Anticancer agent; Downregulates DNMT1 (TBI1282)

Description

Product Details

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.