pa-21

6-Acryloyloxyhexyl phosphater (PA21) is a novel phosphate-binding agent, which is an iron-based reagent, and can be used for the treatment of hyperphosphatemia in chronic kidney disease.

PA21A092 is an inhibitor of PfATP4 and exhibits specific biochemical effects.

Benzazepinoquinoline-spermine (Compound PA-3) is a potent complexing agent for pre-miR-372 that specifically inhibits its processing mediated by Dicer, with an IC₅₀ of 0.58 μM. It exhibits strong affinity for pre-miR-372, with a KD of 0.11 μM, and shows high activity against pre-miR-373 (IC₅₀= 0.29 μM). However, its inhibitory effect is significantly reduced for pre-miR-17, pre-miR-21, and pre-miR-155, with IC₅₀ values of 0.84 μM, 1.43 μM, and 1.07 μM, respectively. Benzazepinoquinoline-spermine is applicable in cancer research.

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.