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.

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

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

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

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/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.

CARM1/HDAC2-IN-1 (Compound CH-1) is a dual inhibitor targeting CARM1 and HDAC2, with IC50 values of 3.71 nM and 4.07 nM, respectively. This compound exhibits antitumor activity.

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].

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].

CARM1-IN-5 (Compound 17e) is a potent and selective inhibitor of CARM1, exhibiting an IC50 of 2 nM. By directly interacting with CARM1, CARM1-IN-5 effectively inhibits the methylation of substrate proteins. Additionally, CARM1-IN-5 demonstrates significant antiproliferative effects on melanoma cell lines.

CARM1-IN-6 (Compound iCARM1) dihydrochloride is a potent and selective inhibitor of CARM1, with an IC50 value of 12.3 μM. It demonstrates cell growth inhibitory activity and is applicable in cancer research.

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

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-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-6 (iCARM1) is a potent and selective inhibitor of CARM1. It possesses activity that inhibits cell growth and is applicable for cancer research.

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.

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.

(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.

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.

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.

Tert-Butyl 6-aminocaproate (Tert-butyl 6-aminohexanoate) is a PROTAC linker. It is utilized in the synthesis of the PROTAC CARM1/IKZF3 degrader-1.

PROTAC EZH2Degrader-44 (compound 60) is a potent PROTAC degrader that targets the EZH2-PRC2 complex. It functions by recruiting the CRBN E3 ligase, relying on the proteasome system to degrade the core components EZH2, SUZ12, and EED, effectively reducing H3K27me3 and CARM1 levels. This compound exhibits antiproliferative effects through a dual mechanism: inducing mitochondrial dysfunction, which leads to decreased membrane potential, and regulating Bcl-2 family proteins (by upregulating Bax, Caspase-3, and PARP and downregulating Bcl-2), thereby significantly promoting apoptosis. PROTAC EZH2Degrader-44 demonstrates minimal cytotoxicity in human normal breast epithelial, liver, and kidney cells, providing a favorable safety profile. It is an ideal tool molecule for exploring targeted therapy mechanisms for triple-negative breast cancer.