mt-i

Dinotefuran (MTI-446) is an insecticide of the neonicotinoid class for control of insect pests such as aphids, whiteflies, thrips, leafhoppers, leafminers. Its mechanism of action involves disruption of the insect's nervous system by inhibiting nicotinic acetylcholine receptors.

MTI-31 (LXI-15029) is a potent, orally active, and highly selective inhibitor of mTORC1 and mTORC2, exhibiting a Kd of 0.20 nM for mTOR and >5,000-fold selectivity over PIK3CA, PIK3CB, and PIK3G in binding assays, with an IC50 of 39 nM for mTOR in a LANCE assay of mTOR substrate phosphorylation with 100 μM ATP [1].

SHMT-IN-1 is a potent plasmodial serine hydroxymethyltransferase (SHMT) inhibitor with antitumor activity.

NMT-IN-1 is a potent inhibitor of N-nutyltransferase (NMT), with IC50 of 31μM for TbNMT and 66μM for hNMT. NMT-IN-1 is a potential compound for the treatment of African trypanosomiasis.

COMT-IN-2 (compound 9) is the most potent inhibitor of COMT, exhibiting selective inhibition for brain (IC50=24 nM) and liver (IC50=81 nM) MB-COMT compared to the liver S-COMT isoform (IC50=620 nM).

NMT-IN-7 is an inhibitor of N-myristoyltransferase (NMT) with an IC50 of 2.1 nM for HsNMT1M and demonstrates toxicity with an IC50 of 0.6 nM against SU-DHL-10 cells. It can be utilized as an ADC cytotoxin.

SHMT-IN-3 (Hit 1) is an inhibitor of SHMT1 and SHMT2, exhibiting an IC50 value of 0.53 µM for human SHMT1. It acts as a non-competitive inhibitor with respect to serine.

NNMT-IN-7 (Compound 4e) is an NNMT inhibitor with an IC50 of 505.7 µM. It is useful for research in metabolic and chronic diseases.

CpNMT-IN-1 (Compound 11e) is an inhibitor of N-myristoyltransferase (CpNMT) with an IC50 value of 2.5 μM. It also inhibits the growth of microsporidia, demonstrating an EC50 value of 6.9 μM.

DNMT-IN-4 (Compound 4d) is a DNMT inhibitor with an IC50 value of 5.78 µM. It induces apoptosis and exhibits anticancer activity.

NNMT-IN-6 hydrochloride (compound 78) is a potent inhibitor of nicotinamide N-methyltransferase (NNMT), exhibiting an IC50 of 1.41 μM and a Kd of 5.6 μM. It effectively suppresses the proliferation of HSC-2 human oral cancer cell lines.

NNMT-IN-5 (Compound 3-12) is a potent inhibitor of nicotinamide N-methyltransferase (NNMT) with an IC50 value of 47.9 ± 0.6 nM. This compound exhibits exceptional selectivity for a set of human methyltransferases. NNMT-IN-5 is applicable in research related to cancer, diabetes, metabolic disorders, and neurodegenerative diseases.

NMT-IN-3 is an inhibitor of N-myristoyltransferase (NMT), displaying an IC50 of 38 mM against Plasmodium vivax NMT.

POLRMT-IN-2 is a potent inhibitor of POLRMT, exhibiting significant antiproliferative activity in MOLM-13 cells with an IC50 of 1.01 μM. It disrupts mitochondrial function and induces apoptosis, making it a valuable candidate for research in acute myeloid leukemia (AML).

NMT-IN-8 (Compound Ex.129) is an orally active and highly selective N-myristoyltransferase (NMT) inhibitor with an IC50 value of less than 10 nM. It binds to the peptide binding pocket of NMT, blocking the enzyme-catalyzed protein N-myristoylation, thereby disrupting key pathways such as protein transport, signal transduction, and viral replication. NMT-IN-8 shows promise for research in oncology (including MYC-dependent cancers and B-cell lymphoma) and infectious diseases (such as malaria, HIV, and rhinovirus infections).

DNMT-IN-5 is a potent and stable inhibitor of DNA methyltransferase (DNMT), with an IC50 of 0.78 nM. It exhibits submicromolar inhibitory activity against DNMT3A, upregulates the expression of target genes, inhibits cell proliferation, and induces key cell cycle arrest. DNMT-IN-5 is suitable for research on p53-deficient colorectal cancer.

Mal-PEG2-amide-C2-amide-Phenyl(β-D-glucuronide)-NMT-IN-7 is a drug-linker conjugate intended for use in antibody-drug conjugates (ADCs). This compound is composed of an NMT inhibitor and a stable cleavable linker [Mal-PEG2-amide-C2-amide-Phenyl(β-D-glucuronide)]. It can be utilized in the synthesis of ADCs.

5'-O-DMT-ibu-dC [5'-O-(4,4'-Dimethoxytrityl)-N4-isobutyryl-2'-deoxycytidine] can be utilized in the synthesis of oligodeoxyribonucleotides.

5'-O-DMT-ibu-rG is a valuable model for a novel category of DNA binding compounds, offering potential for the creation of highly effective and specifically targeted anti-cancer medications.

hMAO-B/MB-COMT-IN-1 is a dual MAO-B/MB-COMT inhibitor with IC50s of 2.5 μΜ for hMAO-B and 3.84 μΜ for MB-COMT. hMAO-B/MB-COMT-IN-1 protects cells from oxidative damage and can be utilized in neurodegenerative disease research, such as Parkinson's Disease (PD) [1].

hMAO-B/MB-COMT-IN-2 is a dual inhibitor of MAO-B/MB-COMT with IC50s of 4.27 μM and 2.69 μM for hMAO-B and MB-COMT, respectively. hMAO-B/MB-COMT-IN-2 protects cells from oxidative damage and can be used in neurodegeneration disease research, such as Parkinson's Disease (PD) [1].

SHMT-IN-2 (compound 2) is a specific human SHMT1/2 small molecule inhibitor that acts on SHMT1 (IC50: 13 nM) and SHMT2 (IC50: 66 nM). SHMT-IN-2 inhibits the growth of many human cancer cells and is sensitive to B-cell lymphoma.

NNMT-IN-3 (compound 14) is a potent and selective inhibitor of nicotinamide N-methyltransferase (NNMT), with IC50 values of 1.1 nM in cell-free assays and 0.4 μM in cell-based assays. NNMT-IN-3 can be utilized in studies of obesity, cancer, type II diabetes, and skeletal sarcopenia, among other diseases.

IHMT-IDH1-053 (compound 16) is an irreversible inhibitor highly selective for the IDH1 R132H mutant, with an IC50 of 4.7 nM. It preferentially targets IDH1 mutants over wild-type IDH1 and IDH2, in both their wild-type and mutant forms. In 293T cells transfected with the IDH1 R132H mutant, IHMT-IDH1-053 reduces 2-hydroxyglutarate (2-HG) production with an IC50 of 28 nM. The compound binds to the R132H protein at an allosteric site near the NADPH binding region, forming a covalent linkage with Cys269. Additionally, IHMT-IDH1-053 inhibits the growth of both the HT1080 cell line and primary acute myeloid leukemia (AML) cells harboring IDH1 R132 mutations [1].