mt1

MT1, a bivalent chemical probe targeting BET bromodomains, demonstrates an IC50 value of 0.789 nM for BRD4(1).

Agomelatine (Valdoxan) is structurally closely related to melatonin. Agomelatine is a potent agonist at melatonin receptors and an antagonist at serotonin-2C (5-HT2C) receptors, tested in an animal model of depression.

Ramelteon (TAK-375) is a Melatonin Receptor Agonist. The mechanism of action of ramelteon is as a Melatonin Receptor Agonist.

Tasimelteon (BMS-214778) is a melatonin receptor agonist that is used for the treatment of non-24 hour sleep-wake disorder in blind individuals.

ND-322 HCl (ND 322 Hydrochloride) is a selective inhibitor of MT1-MMP and MMP2 and reduces in vitro melanoma cell growth, migration and invasion.

Agomelatine hydrochloride (S-20098 hydrochloride) is a specific MT1 and MT2 receptor agonist with Ki values of 0.1 nM for CHO-hMT1, 0.06 nM for HEK-hMT1, 0.12 nM for CHO-hMT2, and 0.27 nM for HEK-hMT2, respectively [1]. Additionally, Agomelatine hydrochloride is a selective antagonist of the 5-HT2C receptor with pKi values of 6.4 and 6.2 for native (porcine) and cloned human 5-HT2C receptors, respectively [2].

8-M-PDOT (AH-002) is a selective and potent melatonin MT2 receptor agonist that also inhibits MT1 receptors. 8-M-PDOT exhibits anxiolytic activity and can be used to study MT2-induced neuropathic pain.

Agomelatine-D6 is a deuterium-labeled Agomelatine. Agomelatine (T1445) is a specific agonist of MT1 and MT2 receptors.

Chemically modified tetracyclines (CMTs) can inhibit MMPs, but lack antimicrobial activity. Nonantimicrobial derivative of tetracycline called incyclinide (COL-3, CMT-3). Incyclinide (CMT-3) has been shown to experimentally suppress prostate cancer, colon adenocarcinoma and melanoma invasiveness in cell culture and to inhibit tumor growth and metastasis.

Luzindole (N-0774) is a selective melatonin receptor antagonist that inhibits experimental autoimmune encephalomyelitis and exhibits antidepressant-like activity. It preferentially targets MT2 (Mel1b) over MT1 (Mel1a), with Ki values of 10.2 nM for human MT2 and 158 nM for MT1.

S26131 (N-[2-[7-[3-[8-(2-acetamidoethyl)naphthalen-2-yl]oxypropoxy]naphthalen-1-yl]ethyl]acetamide) behaves as an antagonist on MT1 and MT2 receptors with Ki of 0.5 and 112 nM respectively.

TIK-301 is a chlorinated melatonin derivative and a potent, high-affinity, and orally active melatonin MT1 and MT2 receptors agonist (Kis: 0.081 nM and 0.042 nM, respectively). TIK-301 is also a 5-HT2B/5-HT2C receptor antagonist with antidepressant action. TIK-301 has the potential for sleep disorders and other circadian rhythm disorders treatment.

NSC 405020 is a noncatalytic inhibitor of MT1-MMP.

glycine (2-Aminoacetic acid) is a non-essential amino acid. It is found primarily in gelatin and silk fibroin and used therapeutically as a nutrient. It is also a fast inhibitory neurotransmitter.

Piromelatine is an agonist of melatonin MT1/MT2 receptors, 5-HT1A and 5-HT1D, and an antagonist of 5-HT2B.Piromelatine has antinociceptive activity with inhibitory effects on P2X3, TRPV1, and Nav1.7 channels, and can be used in studies of sleep-promoting, pain-relieving, anti-neurodegenerative, and antidepressant diseases. diseases, and can be used to improve memory deficits associated with chronic mild stress-induced lack of pleasure in rats.

ACH-000143 have been identified as a novel agonist of the melatonin receptors MT1 and MT2.

DMT1 blocker 1 is a blocker of divalent metal transporter 1 (DMT1) with IC50 of 0.64 μM, which is expected to block the absorption of iron by intestinal cells in vivo.

IMT1B (LDC203974) is an orally administered, specific noncompetitive allosteric inhibitor of mitochondrial RNA polymerase (POLRMT), effectively suppressing mitochondrial DNA (mtDNA) expression and conferring anti-tumor properties.

DMT1 blocker 2, compound 12f, is a direct inhibitor of divalent metal transporter 1 (DMT1) with an IC50 hydrogen peroxide value of 0.83, which is expected to block iron uptake by intestinal epithelial cells in vivo.

DNMT1/HDAC-IN-1 (compound (R)-23a), a potent dual inhibitor targeting both DNMT1 and HDAC, exhibits impressive inhibitory effects specifically on HDAC1 (HDAC1:IC50=0.05 μM), a major HDAC isoform that interacts with DNMT1 across multiple protein complexes involved in the transcriptional silencing of TSGs. This compound has been shown to remodel the tumor immune microenvironment and induce tumor regression, effectively reversing cancer-specific epigenetic abnormalities.

DNMT1-IN-5 (Compound 55) is an inhibitor of DNMT, specifically targeting DNMT1 and DNMT3A, with IC50 values of 2.42 μM and 14.4 μM, respectively. It demonstrates antiproliferative effects across various cancer cell lines (TMD-8, DOHH2, MOLM-13, THP-1, RPIM-8226, and HCT116) with IC50 values ranging from 0.19 to 2.37 μM. The compound induces G2/M phase cell cycle arrest and apoptosis in TMD-8 and DOHH2 cells. Additionally, DNMT1-IN-5 exhibits antitumor efficacy in a TMD-8 xenograft mouse model.

MT-110 is a selective, potent, brain-permeable non-muscle myosin II (NMII) inhibitor with an EC50 of 0.68 uM in a cytokinesis assay, >70-fold selectivity over cardiac myosin II (CMII).

iPRMT1 is an effective and selective PRMT1 inhibitor useful for breast cancer research. It inhibits the growth of breast cancer cells both in vitro and in vivo, with EC50 values of 90 nM, 70 nM, and 9 nM for MCF7, T47D, and MDA-MB-231 cell lines, respectively.

PRMT1-IN-3 is a potent inhibitor of protein arginine methyltransferase 1 (PRMT1) with an IC50 of 4.11 μM. It also inhibits PRMT6 and PRMT8, with IC50 values of 23.3 and 30.1 μM, respectively. In triple-negative breast cancer (TNBC) cells, PRMT1-IN-3 reduces asymmetric dimethylarginine (ADMA) levels and the histone modification H4R3me2a. It induces cell cycle arrest and apoptosis in MDA-MB-231 cells and inhibits cell migration and colony formation. Furthermore, PRMT1-IN-3 serves as a chemosensitizer for Paclitaxel and is applicable in TNBC research.