nmt

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.

DDD85646 is an inhibitor of T. brucei N-myristoyltransferase with a Ki of 1.44 nM, an IC50 of 2 nM and an EC50 of 2 nM. The IC50 of hNMT is 4 nM.

tris(dibenzylideneacetone)dipalladium (Tris DBA) is a N-myristoyltransferase-1 (NMT-1) inhibitor

PCLX-001 is a small-molecule compound that acts as an orally active inhibitor of N-myristoyltransferase (NMT), specifically targeting NMT1 and NMT2 with IC50 values of 5 nM and 8 nM, respectively. This compound demonstrates anti-tumor effects and effectively inhibits the early signaling of B-cell receptor (BCR). Consequently, PCLX-001 is a valuable tool for researching B-cell malignancies [1] [2].

IMP-1088 is a potent inhibitor of human N-myristoyltransferases NMT1 and NMT2 dual.

4-PivO-NMT chloride is an indole derivative-based regulator of the AMPK signaling pathway. It modulates neurogenesis or neurite outgrowth by influencing AMPK activity and holds potential for research in neurological disorders, pain, and inflammation.

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.

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

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).

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.

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.

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.

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.

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.

DNMT2-IN-1 (compound 80) is a novel DNMT2 (DNA methyltransferase 2) inhibitor with an IC50 of 1.2 μM, intended for research in neurological and metabolic disorders or cancer.

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.

DNMT2-IN-2 is a selective inhibitor of DNA methyltransferase 2 (DNMT2) with a KD value of 3.04 μM. It targets a concealed allosteric binding site of DNMT2 and reduces m5C levels in tRNA of MOLM-13 cells. This compound works synergistically with Doxorubicin to impair cell viability and is applicable in cancer research, including studies of cervical cancer and leukemia.

NMTCA (NMTPRO) is a sulfur-containing N-nitrosamino acid used as an endogenous nitrosation indicator in gas chromatography-thermal energy analysis (GC-TEA).

DNMT3A-IN-1 is a selective and potent DNMT3A inhibitor. DNMT3A-IN-1 exhibits inhibitory activity against DNMT3A with a KI ranging from 9.16-18.85 μM (AdoMet) and 11.37-23.34 μM (poly dI-dC).

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.

PNMT-IN-1 (inhibitor 4) is a selective second generation inhibitor [1] of phenylethanolamine N-methyltransferase (PNMT), exhibiting a Ki value of 1.2 nM and an IC50 value of 81 nM. Additionally, it disrupts the activity of DNMT1 and DNMT3b, with IC50 values of 61 μM and 17 μM, respectively, and antagonizes the action of epinephrine.