arm 1

ARM1 is a potent inhibitor of aminopeptidase and epoxide hydrolase. The IC50 values are 7.61 µM for aminopeptidase and 12.4 µM for epoxide hydrolase.

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.

Isoquinoline, 5-iodo- is a potent and selective inhibitor of SARM1(IC50 = 75 nM) by preventing axonal degeneration and by allowing functional recovery of a metastable pool of damaged, but viable, axons.

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/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.

SARM1-IN-4 (Compound 7) is an orally active SARM1 inhibitor that reduces plasma neurofilament light chain (NfL) levels in a mouse model following a 50 mg/kg oral dose. By inhibiting the NAD+ hydrolase activity of SARM1, it prevents programmed axon degeneration, making it useful for research in neurodegenerative and neurological diseases such as multiple sclerosis, amyotrophic lateral sclerosis, Parkinson's disease, and peripheral neuropathy.

SARM1-IN-5 (compound 1-23-a) is an inhibitor of SARM1, useful for researching diseases related to axonal degeneration, including Alzheimer's disease, Parkinson's disease, amyotrophic lateral sclerosis (ALS), and multiple sclerosis (MS).

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.

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.

ARM165 is a heterobifunctional molecule that degrades the protein PIK3CG and inhibits the PI3Kγ-Akt signaling pathway, thereby exerting anti-leukemic effects. It is capable of suppressing the proliferation of AML cells, with an IC50 of less than 1 μM.

SARM1-IN-6 (Compound 17a) is a brain-penetrant orthosteric inhibitor of SARM1. It exhibits an IC50 of 14 nM against NAM and 74 nM against HEK cells.

SARM1-IN-7 is a potent, orally active inhibitor of SARM1, targeting its active site (orthosteric). This compound persistently enhances SARM1's enzymatic activity, leading to exacerbated NAD depletion at suboptimal concentrations. In both cell and mouse models with activated SARM1, SARM1-IN-7 exhibits dual effects: high doses provide cell/neuron protection, whereas low doses intensify cell/neuron damage. SARM1-IN-7 is applicable in studies of axonal degeneration.

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.

SARM1-IN-8 (compound 6) is a competitive base-exchange inhibitor of SARM1. It competitively inhibits the activity of the NAD+ substrate SARM1Δ1-27.

AR-M 1896 Acetate is the selective agonist of GalR2.

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

AR-M 1000390 hydrochloride (ARM-390 HCl) , also known as ARM-390, is a low-internalizing nonpeptidic δ-selective opioid receptor agonist; derivative of SNC 80. Does not trigger acute desensitization of the analgesic response; reduces CFA-induced hyperalgesia. Brain penetrant following systemic administration.

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

SARM1-IN-2 is a potent SARM1 inhibitor for the study of metabolic and neurological related diseases.

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.

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