mtap

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.

DMTAP, a cationic lipid, facilitates the delivery of DNA, RNAi, and drugs [1] [2] [3].

AGI-25696 is an inhibitor of methionine adenosyltransferase 2A (MATA2). AGI-25696 blocks the growth of MTAP-deleted tumors in vivo and can be used for studies about the treatment of cancer.

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.

MAT2A-IN-16 is a MAT2A inhibitor that effectively suppresses the proliferation of MTAP- -HCT-116 cells, with an IC50 value of 20 nM.

MAT2A-IN-21 (compound 28) is a potent inhibitor of methionine adenosyltransferase 2A (MAT2A), with an IC50 of 49 nM. It selectively inhibits cancer cells with MTAP deficiency.

PRMT5-MTA-IN-3 (Compound P2A) is an orally active and selective inhibitor of protein arginine methyltransferase 5 (PRMT5). It inhibits the proliferation of MTAP-deficient colorectal cancer HCT-116 cell line with an IC50 value of 5 nM. PRMT5-MTA-IN-3 holds potential for research in cancers, particularly in MTAP-deficient tumors such as colorectal cancer, non-small cell lung cancer, and pancreatic cancer.

MAT2A-IN-24 (Compound 9) is an inhibitor of methionine adenosyltransferase 2a (MAT2a), with an IC50 value of 20 nM for MAT2a inhibition and an antiproliferative IC50 value of 10 nM for HAP1MTAP–/– cells. MAT2A-IN-24 is applicable in the research of tumor diseases associated with MTAP deficiency.

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.

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

MTDIA (MT-DADMe-ImmA and methylthio-DADMe-Immucillin A) is an MTAP inhibitor.

MRTX9768 hydrochloride is a potent, orally active PRMT5 inhibitor. MRTX9768 hydrochloride is a synthetic lethal-based inhibitor binding the PRMT5-MTA complex[1]. MRTX9768 inhibits SDMA and cell proliferation in HCT116 MTAP-del cells (SDMA IC50 3 nM; prolif. IC50 11 nM) with marked selectivity over HCT116 MTAP-WT cells (SDMA IC50 544 nM; prolif. IC50 861 nM)[1].MRTX9768 selectively targets MTAP CDKN2A-deleted tumors[2][1]. In xenograft studies, oral administration of MRTX9768 demonstrates dose-dependent inhibition of SDMA in MTAP-del tumors, with less SDMA modulation observed in bone marrow[1]. [1]. Christopher R. Smith, et al. Abstract LB003: Fragment based discovery of MRTX9768, a synthetic lethal-based inhibitor designed to bind the PRMT5-MTA complex and selectively target MTAP CDKN2A-deleted tumors. AACR Annual Meeting 2021; April 10-15, 2021 and May 17-21, 2021; Philadelphia, PA.[2]. Yingqing Chen, et al. Targeting protein arginine methyltransferase 5 in cancers: Roles, inhibitors and mechanisms. Biomed Pharmacother. 2021 Oct 4;144:112252.

MAT2A-IN-5, a potent inhibitor of MAT2A, effectively targets the abnormally elevated expression of MAT2A found in various tumor types such as gastric, colon, liver, and pancreatic cancers. By reducing the proliferative activity of MTAP-deficient cancer cells, MAT2A-IN-5 exhibits potential in cancer research applications [1].

MAT2A-IN-7, a potent inhibitor of the enzyme MAT2A, demonstrates efficacy in targeting the abnormally elevated expression of MAT2A observed in gastric, colon, liver, and pancreatic cancers. Furthermore, MAT2A-IN-7 effectively reduces the proliferative activity specifically in MTAP-deficient cancer cells, thus highlighting its potential for cancer research applications [1].

MAT2A-IN-6 is a potent inhibitor of MAT2A that reduces the proliferative activity of MTAP-deficient cancer cells, demonstrating significant research potential in cancer diseases.

MAT2A-IN-2, a potent inhibitor of MAT2A, shows potential for cancer disease research.

MAT2A-IN-3, a potent MAT2A inhibitor, suppresses the proliferative activity of MTAP-deficient cancer cells and shows potential for cancer research [3=c₁(c(c(c(c(c₁cl)O)O)O)I)c₂c(NC(c(n₂)C(F)(F)F)Cl)=O].

MAT2A-IN-1 is a potent inhibitor of MAT2A, displaying proliferative activity in MTAP-deficient cancer cells. MAT2A is highly expressed in several tumours, including gastric, colon, liver, and pancreatic cancers. MAT2A-IN-1 shows significant potential for cancer research.

AGI-25696 is a MATA2 inhibitor that are useful as therapeutic agents for treating malignancies. AGI-25696 showed in vivo activity in MTAP null tumors. Note: The correct structure of AGI-25696 is CAS#2201065-84-9. Many vendors mistakenly listed CAS#2201066-35-3 as its AGI25696. J. Med. Chem. 2021, 64, 8, 4430–4449 published AGI25696 structure (it is CAS#2201065-84-9).

TNG908 is an orally active and selective MTAP-co-PRMT5 inhibitor that crosses the blood-brain barrier and kills MTAP-deficient cancers.

MAT2A Allosteric Inhibitor 2 is a potent, selective inhibitor exhibiting an IC50 of 5 nM and demonstrates nanomolar efficacy (IC50 = 5 μM) in proliferation assays utilizing the MTAP - - cell line [1].

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).

4-Methyl-2-oxopentanoic acid is an abnormal metabolite, a neurotoxin and a metabolic toxin.

MAT2A-IN-13 is a potent, orally active methionine adenosyltransferase 2A (MAT2A) inhibitor with a favorable pharmacokinetic profile, demonstrating in vivo efficacy in an HCT-116 MTAP-deleted xenograft model and potential use in MTAP-deleted tumors treatment research [1].