mercaptopurine

6-Mercaptopurine (6-MP) is an antimetabolite antineoplastic agent with immunosuppressant properties. It interferes with nucleic acid synthesis by inhibiting purine metabolism and is used, usually in combination with other drugs, in the treatment of or in remission maintenance programs for leukemia.

7-Methyl-6-mercaptopurine (7-Methyl-6-thiopurine) is an inhibitor of PRPP aminotransferase, inhibits IMP metabolism and prevents purine, DNA and RNA synthesis.

6-Mercaptopurine hydrate (6-Mercaptopurine monohydrate) is a Nucleoside Metabolic Inhibitor. It interferes with nucleic acid synthesis by inhibiting purine metabolism and is used, usually in combination with other drugs, in the treatment of or in remission maintenance programs for leukemia.

2',3'-O-Isopropylidene-6-mercaptopurine riboside is a compound with excellent metal complexation activity. It is utilized in the study of mechanisms involving metal complexation.

Azathioprine (BW 57-322), an immunosuppressive agent, inhibits purine synthesis and GTP-binding protein Rac1 activation.

6-Thioguanine (2-Amino-6-purinethiol) is an antineoplastic compound which also has antimetabolite action. The drug is used in the therapy of acute leukemia.

Ansatrienin A is an ansamycin antibiotic and antifungal agent first isolated from S. collinus and S. rishiriensis. In fetal rat long bones, it is an inhibitor of parathyroid hormone-induced calcium release (IC50 = 64 nM), which is a measure of bone resorption, and pp60c-srcM kinase (IC50 = 100 nM). It also inhibits TNF-α-induced expression of intercellular adhesion molecule-1 (ICAM-1; IC50 = 570 nM). Early in vitro studies showed that ansatrienin A potentiates the chemotherapeutic action of 5-fluorouracil , cisplatin , bleomycin , mitomycin C , and 6-mercaptopurine. It is an oxidized form of ansatrienin B .

Ansatrienin B is an ansamycin antibiotic and antifungal agent first isolated from S. collinus and S. rishiriensis., In fetal rat long bones, it is an inhibitor of parathyroid hormone-induced calcium release (IC50 = 21 nM), which is a measure of bone resorption, and pp60c-src kinase (IC50 = 50 nM). It is an inhibitor of translation at the protein synthesis stage by specific inhibition of L-leucine incorporation (IC50 = 58 nM in A549 cells). It also inhibits TNF-α-induced expression of intercellular adhesion molecule-1 (ICAM-1; IC50 = 300 nM). Early in vitro studies showed that ansatrienin B potentiates the chemotherapeutic action of 5-fluorouracil , cisplatin , bleomycin , mitomycin C , and 6-mercaptopurine. Ansatrienin B is a hydroquinone form of ansatrienin A .

Thio-ITP, also known as 6-Thioinosine 5'-triphosphate, is a competitive inhibitor of RNA polymerase activity. It exhibits a strong apparent affinity towards the polymerases, with Ki values of 40.9 μM for RNA polymerase I and 38.0 μM for RNA polymerase II.

Azathioprine Sodium is the sodium salt form of azathioprine, a pro-drug of purine analogue with immunosuppressive activity. Azathioprine is converted in vivo to its active metabolite 6-mercaptopurine (6-MP), which substitutes for the normal nucleoside and mistakenly gets incorporated into DNA sequences. This leads to inhibition of DNA, RNA, and protein synthesis. As a result, cell proliferation may be inhibited, particularly in lymphocytes and leukocytes.

6-Thioinosine (6TI) is a purine antimetabolite, acts as an anti-adipogenesis agent.

PU 23 is an inhibitor of multidrug-resistant protein 4 (MRP4).