prmt

PRMT5-IN-1 is a covalent inhibitor of protein arginine methyltransferase 5 (PRMT5)(IC50 of 11 nM for PRMT5 MEP50).

PRMT5-IN-2 is an inhibitor of protein arginine methyltransferase 5.

PRMT1-IN-1, a PRMT1 inhibitor, selectively targets the protein arginine methyltransferase 1 enzyme, which plays a pivotal role in various cellular processes, such as gene regulation and signal transduction [1].

PRMT5-IN-4 (compound AAA-1) is a PRMT5 inhibitor. This chemical compound specifically impedes the activity of PRMT5, an enzyme involved in the methylation of arginine residues on target proteins, which plays a critical role in various cellular processes.

PRMT5-IN-14 is a PRMT5 inhibitor used to treat cancer, sickle cell, and hereditary persistence of foetal hemoglobin (HPFH) mutations.

PRMT5-IN-13 is a selective inhibitor of protein arginine methyltransferase 5 (PRMT5).

PRMT5-IN-15, a PRMT5 inhibitor, has an IC50 value of 0.84 nM.

PRMT5-IN-11 demonstrates potent structure-dependent inhibition against the protein methyltransferase PRMT5:MEP50 complex at submicromolar concentrations.

PRMT5-IN-12 demonstrates significant inhibitory activity on PRMT5.

PRMT5-IN-9 is a novel PRMT5 inhibitor for treating cancer, with an IC50 of 0.01 μM.

PRMT4-IN-3 (compound 56) is a potent class I protein arginine methyltransferase (PRMT) inhibitor, specifically targeting PRMT4 with an IC50 of 37 nM, while exhibiting weaker inhibition of PRMT6 with an IC50 of 253 nM [1].

PRMT4-IN-2 (compound 55) acts as a pan-inhibitor across various protein arginine methyltransferase (PRMT) isoforms, exhibiting inhibitory potencies with IC50 values of 92 nM for PRMT4, 436 nM for PRMT6, 460 nM for PRMT1, 823 nM for PRMT8, and 1.386 μM for PRMT3 [1].

PRMT3-IN-4 (intermediate 15) is an inhibitor of Protein arginine methyltransferase 3 (PRMT3) and serves as the active control for SGC707. It can be utilized in the synthesis of PROTACs targeting PRMT3 and is applicable in research related to leukemia.

PROTAC PRMT3 degrader 1 (compound 11) is a PROTAC molecule targeting PRMT3 for degradation. It effectively inhibits the growth of acute leukemia cells.

PRMT5-IN-45 (compound 36) is a potent and selective inhibitor of PRMT5, exhibiting an IC50 value of 3 nM. This compound effectively reduces the levels of symmetrical dimethylarginine (sDMA) and inhibits the proliferation of the MOLM-13 cell line by inducing apoptosis and causing cell cycle arrest.

PRMT5-MTA-IN-2 (compound 1) is a synergistic inhibitor of PRMT5 with an IC50 of less than 1.5 nM.

PRMT5-IN-49 (Compound 4b16) is an inhibitor of PRMT5.

PRMT5-IN-47 (compound 20) is a potent, selective, and orally active MTA co-operative PRMT5 inhibitor, with an IC50 value of 15 nM. It exhibits antiproliferative and anticancer activity.

PRMT5-IN-46 (compound 278) inhibits PRMT5 with an IC50 range of 1.001-10.000 μM. PRMT5 is a methyltransferase associated with specific genetic alterations. PRMT5-IN-46 is applicable in the study of proliferative diseases, metabolic disorders, and hematological conditions.

PRMT3-IN-5 (Compound 14) is an allosteric inhibitor of PRMT3 with an IC50 of 291 nM. It is utilized in research to explore the biological functions and disease associations of PRMT3.

PRMT5ligand 1 is a ligand of PRMT5, used as a target protein ligand in the synthesis of the PROTAC degrader MS4322.

PRMT5-IN-48 (compound D3) is an orally active PRMT5 inhibitor with an IC50 of 20.7 nM, displaying antitumor activity. It effectively suppresses the growth of various cancer cells, induces apoptosis, and causes cell cycle arrest at the G0 G1 phase. PRMT5-IN-48 is applicable for research in non-Hodgkin's lymphoma (NHL).

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.

PRMT5-IN-50 is an orally active selective inhibitor of PRMT5, demonstrating good metabolic stability and low clearance in human liver microsomes. It inhibits SDMA/HCT116-MTAPdel and SDMA/HCT116-MTAPwt with IC50 values for symmetric arginine methylation inhibition at 1.0 and 536 nM, respectively, and antiproliferative IC50 values at 19 and 1620 nM, respectively. Additionally, PRMT5-IN-50 suppresses tumor growth in mice.