methylthioadenosine phosphorylase

AGI-24512 is a potent inhibitor of methionine adenylyltransferase 2α (MAT2A) (IC50: 8 nM).AGI-24512 shows antiproliferative activity in MTAP-deficient cancer cells.AGI-24512 inhibits MAT2A, which causes DNA damage in MTAP, and is often used in conjunction with anticancer compounds in cancer research.

SIBA (5'-Deoxy-5'-isobutylthioadenosine) is a synthetic analogue of SAH, acts as an inhibitor of S-adenosylmethionine-mediated transmethylation. SIBA can interfere with a variety of enzymatic activities in vitro, such as SAH hydrolase, methylthioadenosine phosphorylase and cAMP phosphodiesterase. SIBA reversibly blocks the multiplication of herpes simplex type 1 virus (HSV)

L-Alanosine, an antibiotic isolated from the fermentation product of Streptomyces alanosinicus, inhibits tumor cell proliferation by blocking the adenylosuccinate synthetic pathway through the inhibition of adenylosuccinate synthetase and Methylthioadenosine phosphorylase.

m-APTA (5'-S-(3-aminophenyl)-5'-thioadenosine) is a selective chemoprotective agent targeting methylthioadenosine phosphorylase (MTAP). It can be converted into adenine, which is a crucial step in shielding normal cells from the toxicity of nucleobase analogs (NBA). m-APTA holds potential for research in MTAP-deficient cancers.

ZS34 is a potent, orally active, and selective inhibitor of MAT2A, with an IC50 value of 13.7 nM, and it exhibits minimal inhibition of hERG and UGT1A1. By inhibiting SAM synthesis, reducing SDMA levels, and inducing DNA damage, ZS34 selectively inhibits the growth of methylthioadenosine phosphorylase (MTAP)-deficient cancer cells. It demonstrates antitumor activity in HCT116 MTAP-/- xenograft mouse models and is suitable for research on MTAP-deficient cancers.

Erythrofuranosyladenine(9-beta-D-Erythrofuranosyladenine, ETA) is a nontoxic MTAP substrate. Erythrofuranosyladenine is an effective salvage agent for methylthioadenosine phosphorylase–selective therapy of T-cell acute lymphoblastic leukemia with L-alanos

TNG-462 is a potent and selective PRMT5 inhibitor with antitumor activity and oral activity, primarily for the treatment of methylthioadenosine phosphorylase (MTAP)-deficient and/or methylthioadenosine (MTA)-accumulating cancers (e.g., non-small-cell lung cancer, pancreatic cancer, bladder cancer, and hematologic malignancies).

MT-DADMe-ImmA (MTDIA) is an inhibitor of human 5'-methylthioadenosine phosphorylase (MTAP, Ki: 90 pM).