Thioguanine

SKU: orb1222647

Description

Tioguanine (INN, BAN), or thioguanine (AAN, USAN), commonly referred to as 6-thioguanine (6-TG) is a medication used to treat a number of types of leukemia. It has been used less frequently in recent years because of safety concerns. However, it is becoming more widely used for treating ulcerative colitis and some autoimmune diseases.(In Vitro):6-Thioguanine (Thioguanine; 2-Amino-6-purinethiol) is an anti-leukemia and immunosuppressant agent, acts as an inhibitor of SARS and MERS coronavirus papain-like proteases (PLpros) and also potently inhibits USP2 activity, with IC50s of 25 μM and 40 μM for Plpros and recombinant human USP2, respectively. 6-Thioguanine (Thioguanine) affects the methylation of cytosine residues by purified DNA methyltransferases including human DNMT1 and bacterial HpaII methylase. 6-Thioguanine (Thioguanine) (1 or 3 μM) decreases global cytosine methylation in Jurkat T cells and cytosine methylation in human cells at 3 μM. 6-Thioguanine (Thioguanine) (18.75, 37.50, or 75.00 μM) adversely affects cell viability, but with no effect on LDH or ALT activity.

Key Properties

• CAS Number: 154-42-7
• MW: 167.2
• Purity: >98% (HPLC)
• Formula: C₅H₅N₅S
• SMILES: c1nc2c([nH]1)c(=S)nc([nH]2)N
• Target: DNMT1
• Solubility: DMSO : 10 mg/mL 59.81 mM

Bioactivity

• In Vitro:
  6-Thioguanine (Thioguanine; 2-Amino-6-purinethiol) is an anti-leukemia and immunosuppressant agent, acts as an inhibitor of SARS and MERS coronavirus papain-like proteases (PLpros) and also potently inhibits USP2 activity, with IC50s of 25 μM and 40 μM for Plpros and recombinant human USP2, respectively. 6-Thioguanine (Thioguanine) affects the methylation of cytosine residues by purified DNA methyltransferases including human DNMT1 and bacterial HpaII methylase. 6-Thioguanine (Thioguanine) (1 or 3 μM) decreases global cytosine methylation in Jurkat T cells and cytosine methylation in human cells at 3 μM. 6-Thioguanine (Thioguanine) (18.75, 37.50, or 75.00 μM) adversely affects cell viability, but with no effect on LDH or ALT activity.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Quick Database Links

Gene Symbol

DNMT1