PRMT7 Inhibitor

SGC3027 is a histone methyltransferase inhibitor. SGC3027 is the first potent, selective and cell active chemical probe for PRMT7.

DS-437 is a dual PRMT5/7 inhibitor (IC₅₀s of PRMT5/7=6 μM). DS-437 is selective for PRMT5 and PRMT7 over 29 other human protein-, DNA-, and RNA-methyltransferases. DS-437 is a S-adenosylmethionine (SAM)-competitive inhibitor of PRMT5. DS-437 also inhibits DNMT3A and DNMT3B, with IC₅₀s of 52 and 62 μM, respectively. DS-437 inhibits the methylation of FOXP3.

SGC8158 is an inhibitor of PRMT7 and can be used to study the cellular function of PRMT7. SGC8158 decreases monomethylarginine levels of Hsp70 (the best characterized PRMT7 substrate). SGC8158 induces growth inhibition in various cancer cells (IC₅₀: 2-9 μM), as well as multidrug-resistant (MDR) cancer cells. SGC8158 also enhances Doxorubicin (HY-15142A) induced DNA damage and Its cytotoxicity.

MS2734 is a dual-substrate NNMT inhibitor that acts as a SAM (HY-B0617) competitor and a non-competitor of Nicotinamide (HY-B0150), with an IC₅₀ of 14 μM and a K_d of 2.7 μM against hNNMT. MS2734 inhibits the methyltransferase activities of DOT1L (IC₅₀ 1.3 μM), PRMT7 (IC₅₀ 20 μM), BCDIN3D (IC₅₀ 40 μM) and SMYD2 (IC₅₀ 62 μM). MS2734 is applicable to research related to diabetes, obesity and various cancers.

PRMT4-IN-1 is a selective inhibitor of PRMT4 (IC₅₀=3.2 nM). PRMT4-IN-1 inhibits MCF7 relative viability.

PRMT1-IN-3 is a potent protein arginine methyltransferase 1 (PRMT1) inhibitor with an IC₅₀ of 4.11 μM. PRMT1-IN-3 inhibits PRMT6 and PRMT8 with IC₅₀s of 23.3 and 30.1 μM. PRMT1-IN-3 suppresses asymmetric dimethylarginine (ADMA) levels and histone H4R3me2a modification in triple-negative breast cancer (TNBC) cells. PRMT1-IN-3 induces cell cycle arrest, apoptosis, and inhibits migration and colony formation in MDA-MB-231 cells. PRMT1-IN-3 acts as chemotherapeutic sensitizers for Paclitaxel (HY-B0015). PRMT1-IN-3 can be used for the study of TNBC.