carm1

CARM1-IN-1 (CARM1-IN-7G) is a selective inhibitor of CARM1 with IC50 of 8.6 μM. CARM1-IN-1 shows weak activity against PRMT1 and SET7 with IC50 > 600 μM.

CARM1-IN-1 hydrochloride is a potent and selective inhibitor of CARM1 (IC50: 8.6 μM) with low inhibition of PRMT1 and SET7.

PROTAC CARM1 degrader-1 (compound 3b) serves as a highly potent degrader (DC50=8.1 nM) of the co-activator associated arginine methyltransferase (CARM1). This compound facilitates the degradation of CARM1 via the VHL-proteasome pathway. By degrading CARM1, PROTAC CARM1 degrader-1 effectively reduces the methylation of its substrates, including poly(A)-binding protein PABP1 and BGR1-associated factor BAF155, subsequently inhibiting breast cancer cell migration [1].

CARM1-IN-3 (compound 17b) is a potent, selective inhibitor of co-activator associated arginine methyltransferase (CARM1), exhibiting IC50 values of 0.07 µM for CARM1 and greater than 25 µM for CARM3 [1].

CARM1-IN-3 dihydrochloride (compound 17b) CARM1-IN-3 dihydrochloride (compound 17b) is a potent, selective coactivator-associated arginine methyltransferase (CARM1) inhibitor that acts on CARM1 (IC50: 0.07 μM) and CARM3 ( IC50>25 μM).

PROTAC CARM1 degrader-2 (compound 3e), with a DC50 value of 8.8 nM, is a VHL- and proteasome-dependent degrader of co-activator associated argininemethyltransferase (CARM1). It not only promotes the degradation of CARM1 but also prevents the methylation of its substrates, including poly(A)-binding protein PABP1 and BGR1-associated factor BAF155, which consequently inhibits breast cancer cell migration [1].

EZM 2302 (GSK3359088) is a selective, and orally available arginine methyltransferase CARM1 inhibitor (IC50: 6 nM).

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.

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

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.

TP-064 is a potent and selective PRMT4 inhibitor. TP-064 includes inhibition of PRMT4 with IC50 < 10nM for methylation of H3 (1-25) and greater than 100-fold selectivity over other histone methyltransferases and non-epigenetic targets. TP-064 inhibits the

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

SGC2085 is an effective and selective coactivator-associated arginine methyltransferase 1 (CARM1) inhibitor (IC50: 50 nM).

Epigenetic Multiple Ligand is a cell-permeable inhibitor of substrate processing by several chromatin-associated enzymes, including SIRT1/2, H3/SET7, H3/p300/CBP, H4/RmtA, PABP1/CARM1, and H4/PRMT1. It acts by inducing either apoptosis or granulocytic differentiation.

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.