prmt5

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.

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.

CMP-5 is a PRMT5 inhibitor with antiviral activity, inhibits PRMT5 methyltransferase activity, and can be used in the study of SARS virus infection.

DW14800 is an inhibitor of PRMT5 (IC50 = 17 nM), enhances the transcription of HNF4α, and reduces the level of H4R3me2s.

(Iso)-MS4322 ((Iso)-YS43-22) is a selective and potent protein arginine methyltransferase 5 (PRMT5) degrader with potential anticancer activity that effectively reduces PRMT5 protein levels in MCF-7 cells and inhibits the growth of a wide range of cancer cells.

GSK3326595 (EPZ015938) is an inhibitor of protein arginine methyltransferase 5 (PRMT5)(IC50:6.2 nM.).

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.

JNJ-64619178 is a selective, orally active, and pseudo-irreversible inhibitor of protein arginine methyltransferase 5 (IC50: 0.14 nM). It has effective activity In lung cancer.

LLY-283 is a potent, selective, and oral protein arginine methyltransferase 5 (PRMT5) inhibitor, exhibiting an IC50 of 22 nM and a Kd of 6 nM for the PRMT5:MEP50 complex, and demonstrates antitumor activity.

EPZ015666 (GSK3235025) is an orally available inhibitor of PRMT5 enzymatic activity.

GSK591 (GSK3203591), Alternative Names are EPZ015866, GSK3203591, is a potent selective inhibitor of the arginine methyltransferase PRMT5 (IC50=11 nM).

HLCL-61 hydrochloride (HLCL-61 HCL) is a potent and selective PRMT5 inhibitor for the treatment of acute myeloid leukemia.

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

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

BRD0639 is a pioneering inhibitor targeting the interaction between PRMT5 and its substrate adaptor. As a competitive inhibitor of the PRMT5 binding motif (PBM), BRD0639 facilitates the investigation of activities dependent on PBM-associated PRMT5 functions [1].

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

PRMT5-IN-46 (compound 278) is a PRMT5 inhibitor (IC50 = 1–10 μM) applicable for studying proliferative diseases, metabolic disorders, and hematological conditions.

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

PRMT5/EGFR-IN-1 (Compound 10p) is an orally active dual inhibitor targeting PRMT5 and EGFR, with IC50 values of 15.47 μM and 19.31 μM, respectively. It demonstrates antiproliferative activity against the A549, MCF7, HeLa, and MDA-MB-231 cell lines. This compound also exhibits favorable pharmacokinetic (PK) and pharmacodynamic (PD) properties in vivo and significantly inhibits the growth of MCF7 orthotopic xenograft tumors.

PRMT5:MEP50 PPI, a pioneering inhibitor of the PRMT5:MEP50 protein-protein interaction (PRMT5:MEP50 PPI), demonstrates anti-tumor and anti-proliferative effects in lung and prostate cancer cells.

PRMT5ligand 2 (Compound 38) is a ligand used for target proteins in PROTACs (Ligands for Target Protein for PROTACs). It is utilized in the synthesis of MS115.

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.