carm1

EZM 2302 (GSK3359088) is a selective, and orally available arginine methyltransferase CARM1 inhibitor (IC50: 6 nM).[1]

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

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

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.

PROTAC CARM1 IKZF3 degrader-1 (Compound 074) inhibits CARM1, reducing the methylation level of its substrate BAF155. This PROTAC degrader works by degrading IKZF 1 3 via a CRBN-dependent mechanism. It suppresses MYC protein expression, thereby inhibiting the proliferation of various multiple myeloma cells. Additionally, PROTAC CARM1 IKZF3 degrader-1 can induce apoptosis in H929 cells and overcomes resistance to immunomodulatory drugs (IMiDs, such as pomalidomide). It is applicable for cancer and immunology research. (Pink: ligand for target protein CARM1 IKZF3 ligand 1; Active form of target protein ligand: EZM 2302; Black: linker; Blue: ligand for E3 ligase Cereblon Thalidomide 4-fluoride)

CARM1-IN-3 dihydrochloride (compound 17b) is a potent and selective coactivator-associated arginine methyltransferase inhibitor, targeting CARM1 with an IC50 of 0.07 μM and exhibiting minimal activity on CARM3 (IC50 > 25 μM).

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].

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

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 arginine methyltransferase (CARM1). It promotes the degradation of CARM1 and prevents the methylation of its substrates, including poly(A)-binding protein PABP1 and BGR1-associated factor BAF155, consequently inhibiting breast cancer cell migration [1].

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

CARM1 IKZF3 ligand 1 functions as an inhibitor of CARM1 and serves as a target protein ligand for the synthesis of PROTAC CARM1 IKZF3 degrader-1.

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.

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

(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.

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

SKI-73, a chemical probe of CARM1 with prodrug properties, swiftly penetrates cell membranes and converts into an active inhibitor. It is capable of inhibiting breast cancer cell invasion, making it useful for tumor research.

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.

ZL-28-6, a type I PRMT inhibitor (IC50: 18 nM), effectively targets CARM1 (a member of PRMT) within cells and is suitable for cancer research [1].

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.

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.

Thalidomide-NH-C4-Boc is a compound that acts as a ligand and linker for the E3 ligase (Cereblon). It is utilized in the synthesis of PROTAC CARM1 IKZF3 degrader-1.