prmt8

MS023 trihydrochloride (MS023 3HCl) is a selective and potent human type I protein arginine methyltransferase (PRMT) inhibitor with potential anticancer activity against PRMT1, PRMT3, PRMT4, PRMT6, and PRMT8 for cancer research.

GSK3368715, a potent inhibitor of type I protein arginine methyltransferases (PRMT), could inhibit PRMT1, 3, 4, 6 and 8 with Kiapp vaules ranging from 1.5 to 81 nM.

GSK3368715 is an orally active, reversible, and S-adenosyl-L-methionine (SAM) uncompetitive type I protein arginine methyltransferases (PRMTs) inhibitor (IC50s: 3.1 nM (PRMT1), 48 nM (PRMT3), 1148 nM (PRMT4), 5.7 nM (PRMT6), 1.7 nM (PRMT8)). It has strong anti-cancer activity.

Spermine (Neuridine) is a biogenic polyamine formed from spermidine. It is found in a wide variety of organisms and tissues and is an essential growth factor in some bacteria.

PRMT4-IN-1 is a selective inhibitor of PRMT4, demonstrating an IC50 value of 3.2 nM, and has been shown to reduce the relative viability of MCF7 cells [1].

MS023 dihydrochloride (MS023 2HCl) is a selective, cytosolic and highly potent inhibitor of human type I protein arginine methyltransferases (PRMTs) with antitumour activity, inhibits PRMT1, PRMT3, PRMT4, PRMT6, and PRMT8, and increases the proliferative capacity of isolated cultured MuSC. It can be used to study breast cancer.

MS049 is a potent and selective inhibitor of PRMT4 (IC50 = 34 nM) and PRMT6 (IC50 = 43 nM). It is less active against additional type I PRMTs (IC50s = >130, >220, and 1.6 μM for PRMT1, PRMT3, and PRMT8, respectively) and displays no inhibition against typ

EPZ020411 is a specific and effective inhibitor of PRMT6 (IC50=10 nM).

CARM1-IN-4 (compound 11f) serves as a potent inhibitor of CARM1, exhibiting IC50 values of 9 nM for CARM1 and 56 nM for PRMT1. This compound significantly inhibits the proliferation of colorectal cancer cell lines and curtails the methyltransferase activity of CARM1, blocking the methylation of downstream proteins. Moreover, CARM1-IN-4 induces apoptosis and demonstrates notable antitumor activity [1].

EPZ020411 is an effective and specific small molecule PRMT6 inhibitor (IC50=10 nM).

GSK3368715 dihydrochloride (EPZ019997 dihydrochloride) is an orally active and potent inhibitor of type I protein arginine methyltransferases (PRMTs), including PRMT1, PRMT3, PRMT4, PRMT6, and PRMT8. It exhibits anticancer and antitumor activity and can be used to study advanced solid tumors.

MS023 is a potent, selective, and cell-active Type I PRMT inhibitor with IC50 values of 30 nM, 119 nM, 83 nM, 4 nM, and 5 nM for PRMT1, PRMT3, PRMT4, PRMT6, and PRMT8, respectively.

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].

EPZ020411 hydrochloride is a selective and potent small molecule PRMT6 inhibitor with an IC50 value of 10 nM.

MS 049 is a potent, selective, and cell-active dual inhibitor of PRMT4 and PRMT6 with IC 50 of 34 nM and 43 nM, respectively.

(1-Nitroethene-1,2-diyl)dibenzene (alpha-Nitrostilbene; α-Nitrostilbene) serves as an inhibitor of protein arginine methyltransferase 1 (PRMT1; histone H4 methylation assay with an IC50 of 11 μM). At concentrations of 10 and 100 μM, it also inhibits histone H4 methylation caused by PRMT8 but does not affect methylation of histone H3.1 induced by CARM1 or Set7 9.