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.

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.

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.

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

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

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

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.

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.

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.

Spermine (Neuridine) is an endogenous polyamine in the human body. As a direct free radical scavenger, it exhibits antiviral activity and protects DNA from free radical damage; it is also a key regulator of cell proliferation, differentiation, and apoptosis. Spermine inhibits certain bacteria, particularly strains of Staphylococcus aureus. Spermine induces striatal neurotoxicity in a dose-dependent manner. Spermine reversibly inhibits DNA synthesis, mixed lymphocyte reactions, and the induction of cytolytic lymphocyte reactions in primary cultures of mouse splenocytes.

Furamidine is also a selective and cell-permeable protein arginine methyltransferase 1 (PRMT1) inhibitor with an IC50 of 9.4 μM. Furamidine is selective for PRMT1 over PRMT5, PRMT6, and PRMT4 (CARM1) (IC50s of 166 μM, 283 μM, and >400 μM, respectively). Furamidine (DB75) is abisbenzamidine derivative and an antiparasite agent. Furamidine is a potent, reversible and competitive tyrosyl-DNA phosphodiesterase 1 (TDP-1) inhibitor. Inhibition of TDP-1 by Furamidine is effective both with single- and double-stranded DNA substrates but is slightly stronger with the duplex DNA.

SKLB06329 is a potent and selective inhibitor of type I PRMTs. It demonstrates strong selectivity for PRMT6 (IC50= 3.86 nM) without significantly inhibiting type II/III PRMTs (such as PRMT5/7) or various protein lysine methyltransferases [PKMTs]. SKLB06329 effectively suppresses the proliferation of triple-negative breast cancer [TNBC] cells, induces apoptosis, and inhibits the expression of asymmetric dimethylarginine [ADMA] within cells. This compound is applicable for research related to triple-negative breast cancer.

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

Furamidine dihydrochloride (DB75 dihydrochloride) is a cell-permeable, selective small molecule inhibitor of protein arginine methyltransferase 1 (PRMT1) that also binds preferentially to strings of AT base pair sequences within the minor groove of DNA; it targets the PRMT1 enzyme active site primarily through a competitive mechanism with the protein substrate and is noncompetitive toward the cofactor, ultimately leading to the blockade of cell proliferation in various leukemia cell lines irrespective of their genetic lesions.

TP-064 is a potent and selective PRMT4 inhibitor, featuring an IC50 < 10nM for methylation of H3 (1-25) and over 100-fold selectivity compared to other histone methyltransferases and non-epigenetic targets. It inhibits the methylation of MED12 in cells with an IC50 of 43 nM.

SGC2085 is a potent and selective coactivator associated arginine methyltransferase 1 (CARM1) Inhibitor with an IC50 of 50 nM and more than undred-fold selectivity over other PRMTs. CARM1 is an important positive modulator of Wnt/β-catenin transcription a

MS049 dihydrochloride is a selective and cell-active dual inhibitor of PRMT4 and PRMT6 (IC50=34/43 nM), capable of reducing Med12me2a and H3R2me2a levels in HEK293 cells.

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].

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].

SKLB-0124 is a potent degrader of PRMT6, exhibiting DC50 values of 15.4 μM in HCC827 cells and 16.4 μM in MDA-MB-435 cells. It does not degrade PRMT1 or PRMT8. SKLB-0124 has an IC50 value of 1.6 μM for PRMT6. It induces proteasome-dependent degradation of PRMT6 and significantly inhibits cell proliferation. Additionally, SKLB-0124 effectively induces apoptosis and cell cycle arrest, making it suitable for research in lung cancer and breast cancer.

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.

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.