nmt1

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

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.

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.

GSK3685032 is a non-covalent and selective DNMT1 inhibitor(IC50 = 36 nM). The inhibitory effect is time-independent and reversible. GSK3685032 induces loss of DNA methylation and transcriptional activation and inhibits cancer cell growth.

CM-579 is a dual inhibitor of G9a and DNMT( IC50:16 nM, 32 nM for G9a and DNMT). It has potent in vitro cellular activity in a wide range of cancer cells.

GSK-3484862 is a non-covalent Dnmt1 inhibitor that induces DNA hypomethylation, offering potential therapeutic benefits against cancer.

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.

Genipin ((+)-Genipin), an active aglycone derived from an iridoid glycoside called geniposide, is found in the fruit of Gardenia jasminoides Ellis.

6-Thioguanine (2-Amino-6-purinethiol) is an antineoplastic compound which also has antimetabolite action. The drug is used in the therapy of acute leukemia.

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].

Isofistularin-3, a direct DNA-competitive DNMT1 inhibitor with an IC50 of 13.5 μM, functions as a DNA demethylating agent, leading to cell cycle arrest and increased sensitivity to TRAIL in cancer cells. Additionally, it can be employed as an ADC cytotoxin.

Guadecitabine sodium is a inhibitor of second-generation DNA methyltransferases (DNMT) .

DC-05 is an inhibitor of DNA methyltransferase 1 (DNMT1) (IC50 and a Kd: 10.3 μM and 1.09 μM, respectively).

DC_517 is an inhibitor of DNA methyltransferase 1 (DNMT1) ( IC50: 1.7 μM; Kd: 0.91 μM).

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.

RX-3117 (fluorocyclopentenylcytosine) is a novel a cytidine analog. RX-3117 displays anticancer activity in several cancer cell lines, including gemcitabine-resistant variants.

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.

SGI-1027 (DNA Methyltransferase Inhibitor II) is an effective and selective inhibitor of DNA methyltransferase (DNMT). The IC50 of SGI-1027(SGI1027) against DNMT1, DNMT3A, and DNMT3B are 6, 8, 7.5 μM, respectively.

MS9024 is a degrader of DNA methyltransferase 1 (DNMT1), facilitating its degradation in HCT116 cells via the ubiquitin-proteasome pathway, with a DC50 of 35 nM (DC50 values are 254 nM in MDA-MB-468 and 101 nM in H1299). Additionally, MS9024 inhibits DNMT1 with an IC50 of 0.43 μM.

CM-444 is an inhibitor of HDAC (IC50 ranging from 6 nM to 0.6 μM) and DNA methyltransferase (DNMT, IC50 ranging from 1.8 to 2.3 μM). This compound induces differentiation in acute myeloid leukemia cells, exhibits anti-leukemia activity, and enhances survival rates in mouse models.

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

Procainamide (Novocainamide) is a specific and potent DNA methyltransferase 1 (DNMT1) inhibitor and a Class 1A antiarrhythmic agent, with potential applications in cancer and arrhythmia research [1] [2].

DY-46-2 is a selective non-nucleoside DNA methyltransferase 3A (DNMT3A) inhibitor (IC50: 0.39 ± 0.23 μM) with anticancer activity for the study of cancer and tumors.