Methionine Adenosyltransferase (MAT) Inhibitor

3-TYP is an inhibitor of SIRT3 (IC₅₀of 38 μM) and an inhibitor of Methionine Adenosyltransferase (MAT) 2 and Indoleamine 2,3-Dioxygenase (IDO). There may be many off-target sites for 3-TYP that need to be examined, such as NAD-dependent enzymes, including dehydrogenases.

AGI-24512 is a potent methionine adenosyltransferase 2α (MAT2A) inhibitor, with an IC₅₀ of 8 nM. AGI-24512 triggers DNA damage response. AGI-24512 can block proliferation of MTAP-deleted cancer cells in vitro. AGI-24512 can be used for researching anticancer.

AGI-25696 is an orally active ethionine adenosyltransferase 2A (MAT2A) inhibitor with an IC₅₀ of 97 nM. AGI-25696 reduces intracellular SAM levels in cancer cells. AGI-25696 inhibits tumor growth in mice bearing subcutaneous KP4 MTAP-null pancreatic xenografts. AGI-25696 can be used for the research of mtap-deleted pancreatic cancer.

MAT2A-IN-26 is an orally active MAT2A inhibitor with a human IC₅₀ of 17.53 nM. MAT2A-IN-26 inhibits the enzymatic activity of MAT2A, thereby reducing the levels of S-adenosylmethionine (SAM) and symmetric dimethylarginine (sDMA). MAT2A-IN-26 inhibits the proliferation of MTAP-deficient cancer cells and induces anti-tumor efficacy in xenograft models. MAT2A-IN-26 can be used in non-small cell lung cancer research.

AGI-41998 is a potent and orally active inhibitor of methionine adenosyltransferase 2A (MAT2A) that effectively penetrates the blood-brain barrier. AGI-41998 exhibits inhibitory activities against MAT2A and S-adenosyl methionine (SAM) in HCT-116 MTAP-null cells with IC₅₀s of 22 nM and 34 nM. AGI-41998 can significantly inhibit the proliferation of HCT-116 cells and tumor growth. AGI-41998 can be used to study the role of SAM regulation in the central nervous system (CNS) and colon cancer.

SCR-7952 is a MAT2A inhibitor, with IC₅₀ of 18.7 nM. SCR-7952 can be used in anti-cancer research.

AGI-43192 is a potent and orally active inhibitor of methionine adenosyltransferase 2A (MAT2A) that limitedly penetrates the blood-brain barrier. AGI-43192 exhibits inhibitory activitity against MAT2A and S-adenosyl methionine (SAM) in HCT-116 MTAP-null cells with IC₅₀s of 32 and 14 nM. AGI-43192 can significantly inhibit the proliferation of HCT-116 cells and tumor growth. AGI-43192 can be used to study the role of SAM regulation in the central nervous system (CNS) and colon cancer.

MAT2A-IN-18 (Compound 15) is an inhibitor for methionine adenosyltransferase 2A (MAT2A) with an IC₅₀≤50 nM.

MAT2A-IN-14 (compound H3) is a MAT2A inhibitor, and generates reactive oxygen species after sonication to specifically degrade cellular MAT2A via rapid oxidative reactions. Combination of MAT2A-IN-14 and sonication induces 87% MAT2A depletion in human colon cancer cell.

MAT2A-IN-23 (compound 39) is a MAT2A inhibitor, with an IC₅₀ of 4 nM. MAT2A-IN-23 inhibits SAM in the HCT-116 (MTAP^−/−) and in the HCT-116 WT cell line with IC₅₀s of 3 and 2 nM, respectively. MAT2A-IN-23 inhibits SDMA in the HCT-116 (MTAP^−/−) and in the HCT-116 WT cell line with IC₅₀s of 2 and >3000 nM, respectively. MAT2A-IN-23 inhibits HCT-116 (MTAP^−/−) cell proliferation with with an IC₅₀ of 47 nM.

MAT2A-IN-17 is a potent MAT2A inhibitor with an IC₅₀ < 100 nM. MAT2A-IN-17 can be used in the study of cancer.

MAT2A-IN-20 (Compound A49) is an inhibitor for methionine adenosyltransferase 2A (MAT2A) with an IC₅₀ ≤50 nM. MAT2A-IN-20 inhibits human UGT1A1 with an IC₅₀ of 28.45 μM. MAT2A-IN-20 exhibits antitumor in mouse models.

MAT2A-IN-6 is a potent inhibitor of MAT2A. The expression level of MAT2A is abnormally elevated in several types of tumors, including gastric, colon, liver and pancreatic cancers. MAT2A-IN-6 reduces the proliferative activity of MTAP-deficient cancer cells. MAT2A-IN-6 has the potential for the potential for the research of cancer diseases (extracted from patent WO2021254529A1, compound 18).

MAT2A-IN-7 is a potent inhibitor of MAT2A. The expression level of MAT2A is abnormally elevated in several types of tumors, including gastric, colon, liver and pancreatic cancers. MAT2A-IN-7 reduces the proliferative activity of MTAP-deficient cancer cells. MAT2A-IN-7 has the potential for the potential for the research of cancer diseases (extracted from patent WO2021254529A1, compound 24).

MAT2A-IN-22 (Compound 29-1) is a BBB-penetrable and orally active MAT2A inhibitor with an IC₅₀ of 4 nM. MAT2A-IN-22 shows selectivity and inhibitory activity against MTAP-deficient cancer cell lines. MAT2A-IN-22 has anti-tumor effects.

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

MAT2A-IN-19 (Compound I-3) is an inhibitor for methionine adenosyltransferase 2A (MAT2A) with an IC₅₀ of 32.93 nM.

MAT2A-IN-13 is a potent and orally active methionine adenosyltransferase 2A (MAT2A) inhibitor with a favorable pharmacokinetic profile. MAT2A-IN-13 shows in vivo potency in an HCT-116 MTAP-deleted xenograft model. MAT2A-IN-13 can be used for MTAP-Deleted tumors research.

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

MAT2A-IN-5 is a potent inhibitor of MAT2A. The expression level of MAT2A is abnormally elevated in several types of tumors, including gastric, colon, liver and pancreatic cancers. MAT2A-IN-5 reduces the proliferative activity of MTAP-deficient cancer cells. MAT2A-IN-5 has the potential for the potential for the research of cancer diseases (extracted from patent WO2021254529A1, compound 1).