prmt5-mta

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

MRTX-1719 is a potent and selective inhibitor of the PRMT5 MTA complex with an IC50 value of <10 nM against PRMT5 MTAMTAPDELSDMA cell lines.

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.

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.

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).

AMG-193 is an inhibitor of the MTA-PRMT5 complex and is used in the study of cancer, respiratory diseases and digestive disorders.

AZ-PRMT5i-1 (Compound 28) is an effective, orally-active MTAP-selective PRMT5 inhibitor. It exhibits synergistic properties with MTA and demonstrates anti-tumor activity both in vivo and in vitro, making it suitable for research in cancers lacking MTAP.

MRTX-9768 is a synthetic lethal-based inhibitor designed to bind the PRMT5-MTA complex and selectively target MTAP CDKN2A-deleted tumors.