prmt6

PRMT6-IN-3 is a selective PRMT6 inhibitor with an IC50 value of 192 nM.PRMT6-IN-3 has anticancer activity and induces apoptosis in cancer cells.

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.

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

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.

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.

DC_C66 DC_C66 has good selectivity for CARM1, PRMT1 (IC50 = 21μM), PRMT6 (IC50 = 47μM) and PRMT5. It is a cell-permeable, selective co-activator related arginine methyltransferase 1 (CARM1) inhibitor with IC50 of 1.8 μM.

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.

EPZ020411 is a potent and selective PRMT6 inhibitor tool compound. EPZ020411 shows good bioavailability following subcutaneous dosing in rats making it a suitable tool for in vivo studies. EPZ020411 suppresses RCC1 arginine methylation and improves the cytotoxic activity of radiotherapy against GSC brain tumor xenografts.

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].

DCLX069 is a selective protein arginine methyltransferase 1 (PRMT1) inhibitor with an IC50 value of 17.9 µM, occupying the SAM binding pocket to exert its inhibitory effect. It effectively blocks cell proliferation in breast cancer, liver cancer, and acute myeloid leukemia cell lines.

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

Furamidine is a cell-permeable, selective inhibitor of protein arginine methyltransferase 1 (PRMT1). Furamidine binds to strings of AT base pair sequences in DNA′s minor groove. Furamidine targets the enzyme active site and is primarily competitive with t

SGC6870 is a novel potent, selective, and cell-active inhibitor of PRMT6 with IC50 of 77 ± 6 nM, being selective over all other PRMTs and 23 methyltransferases.

PRMT4-IN-3 (compound 56) is a potent class I protein arginine methyltransferase (PRMT) inhibitor, specifically targeting PRMT4 with an IC50 of 37 nM, while exhibiting weaker inhibition of PRMT6 with an IC50 of 253 nM [1].

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].

EPZ-025654 is an effective and selective inhibitor of arginine methyltransferase CARM1.

C-MS023 is a photoactivatable prodrug of MS023, designed to achieve spatiotemporal inhibition of Histone Arginine Asymmetric Dimethylation. It specifically inhibits PRMT6-mediated asymmetric dimethylation of H3 Arginine 2 (H3R2me2a) with an IC50 of approximately 0.2224 μM. The photolysis of C-MS023 can be triggered by exposure to 420 nm visible light, releasing MS023, which effectively downregulates histone arginine asymmetric dimethylation and transcriptional activities related to DNA replication.

Selective protein arginine methyltransferase 1 (PRMT1) inhibitor (IC50 = 1.8 μM). Exhibits five-fold selectivity for PRMT1 over PRMT6 and >250-fold selectivity over PRMT3 and CARM1.

MS117 is a first-in-class, cell-active, irreversible covalent inhibitor of protein arginine methyltransferase 6 (PRMT6) with an IC50 of 18 nM [1].

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].

MS-049 oxalate salt is a potent and selective inhibitor of protein arginine methyltransferases (PRMTs) PRMT 4 and PRMT6.

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