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.

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).

PRMT1-IN-1, a PRMT1 inhibitor, selectively targets the protein arginine methyltransferase 1 enzyme, which plays a pivotal role in various cellular processes, such as gene regulation and signal transduction [1].

MT189 (Antiproliferative agent-14) is a potent tubulin polymerization inhibitor, with an IC50 of 3.41 μM. Antiproliferative agent-14 has excellent antiproliferative activity. Antiproliferative agent-14 possess the ability to arrest cells at G2 M phases of the cell cycle.

PTPMT1-IN-1 is a PTEN-like mitochondrial phosphatase PTPMT1 inhibitor.

DNMT1-IN-3 (compound 7t-S), a DNMT1 inhibitor, exhibits an IC50 of 0.777 μM. It induces cell apoptosis and leads to G0 G1 phase arrest.

IMT1 (Propanamide, N,N-dimethyl-2-[[4-(2-methylphenyl)-2-oxo-2H-1-benzopyran-7-yl]oxy]-) has anticancer activity.

2-Iodomelatonin is a potent agonist of melatonin receptor 1 (MT1) with a Ki value of 28 pM, exhibiting over 5-fold selectivity for MT1 compared to MT2. It can be used to identify, characterize, and localize melatonin binding sites in the brain and peripheral tissues.

6-Chloromelatonin is a potent melatonin receptor agonist, a 5-methoxyindole compound that competes for presynaptic melatonin receptor sites in the rabbit retina, inhibiting the calcium-dependent release of [3H]dopamine with higher metabolic stability than melatonin. Chloromelatonin competitively binds to [3H]melatonin at MT2 receptors (pKi=9.77) and may be used to study insomnia and sleep disorders associated with depression.

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].

Agomelatine (S-20098) L(+)-Tartaric acid is a specific agonist of MT1 and MT2 receptors (Kis: 0.1, 0.06, 0.12, and 0.27 nM for CHO-hMT1, HEK-hMT1, CHO-hMT2, and HEK-hMT2). It also is a selective 5-HT2C receptor antagonist (pKis: 6.4 and 6.2 at native (porcine) and cloned (human) 5-HT2C receptors).

4-P-PDOT (4-phenyl-2- propionamidotetralin) is a potent, selective and affinity Melatonin receptor (MT2) antagonist.

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.

7-Desmethyl-3-hydroxyagomelatine is a metabolite of Agomelatine and has less activity than Agomelatine. Agomelatine is a melatonergic (MT1 and MT2) agonist and 5-HT2C antagonist.

7-Desmethyl-agomelatine, a metabolite of Agomelatine, exhibits lower activity than Agomelatine, which functions as a melatonergic (MT1 and MT2) agonist and 5-HT2C antagonist.

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.