DNA Methyltransferase Inhibitor

CM-579 is a first-in-class reversible, dual inhibitor of G9a and DNMT, with IC₅₀ values of 16 nM, 32 nM for G9a and DNMT, respectively. Has potent in vitro cellular activity in a wide range of cancer cells.

BM30 is a selective peptidomimetic NTMT1 and NTMT2 inhibitor (IC₅₀: 0.89 μM for NTMT1).

NV914 is an inhibitor of FTSJ1 (tryptophan tRNA-specific 2'-O-methyltransferase) that inhibits the methyltransferase activity of FTSJ1, induces translational readthrough of premature termination codons, and enables genes carrying nonsense mutations to synthesize full-length proteins. NV914 belongs to translational readthrough-inducing compounds (TRIDs). NV914 exhibits translational readthrough activity against nonsense mutations in in vitro systems, does not induce readthrough of natural termination codons, and restores CFTR protein expression. NV914 shows favorable acute oral tolerance in mice, with low health risks and good safety profiles. NV914 is applicable to research related to cystic fibrosis and Shwachman-Diamond syndrome.

Hydralazine-d4 hydrochloride is the deuterium labeled Hydralazine hydrochloride. Hydralazine hydrochloride is an orally active, blood-brain barrier-permeable DNA methyltransferase inhibitor with vasodilatory, arterial smooth muscle relaxant and hypotensive activities. Hydralazine hydrochloride reactivates silenced tumor suppressor genes via mediating DNA demethylation, while exerting neuroprotective and anti-inflammatory properties. Hydralazine hydrochloride inhibits NOS-2 (iNOS) and COX-2, and reduces the production of NO and PGE_E2; meanwhile, Hydralazine hydrochloride scavenges reactive oxygen species and inhibits macrophage activation. Hydralazine hydrochloride alleviates motor dysfunction, neuropathic inflammatory pain, and formalin-induced somatic and emotional pain responses. In addition, Hydralazine hydrochloride directly induces DNA strand breaks and sister chromatid exchange, exhibiting certain mutagenic characteristics. Hydralazine hydrochloride has been widely used in studies on hypertension, various cancers (such as cervical cancer, leukemia), spinal cord injury and the mechanisms of inflammatory pain.

MC3817 is a selective DNMT1 inhibitor. MC3817 inhibits DNMT1 and DNMT3A/3L with IC₅₀s of 0.044 μM and > 10μM, respectively. MC3817 inhibits P53-dependent cancer cell proliferation, induces apoptosis and DNA damage MC3817 elevates cleaved Caspase 3, P53, and γH2AX. MC3817 can be used in non-small cell lung cancer, colon cancer, cervical cancer, triple-negative breast cancer and histiocytic lymphoma research.

DNMT1/HDAC-IN-1 (compound (R)-23a) is a DNMT1/HDAC dual inhibitor (HDAC1:IC₅₀=0.05 μM), HDAC1 is a major HDAC isoform that interacts with DNMT1 in multiple protein complexes for transcriptional silencing of TSGs. DNMT1/HDAC-IN-1 can reshape the tumor immune microenvironment and induce tumor regression, and effectively reverse cancer-specific epigenetic abnormalities.

Decitabine-¹³C₅ (5-Aza-2'-deoxycytidine-¹³C₅) is ¹³C labeled Decitabine. Decitabine (NSC 127716) is an orally active deoxycytidine analogue antimetabolite and a DNA methyltransferase inhibitor. Decitabine incorporates into DNA in place of cytosine can covalently trap DNA methyltransferase to DNA causing irreversible inhibition of the enzyme. Decitabine induces cell G2/M arrest and cell apoptosis. Decitabine has potent anticancer activity.

AT-1965 is a selective CMTR2 inhibitor that suppresses methyltransferase activity. AT-1965 triggers the intrinsic antiviral immune response in cancer cells, promotes the infiltration and activation of B cells into tumors, and thereby induces antitumor immune memory to prevent tumor recurrence. AT-1965 can be formulated into lipid nanoparticles to achieve rapid tumor regression. AT-1965 is widely used in studies of immunologically "cold" tumors, triple-negative breast cancer, melanoma, Lewis lung cancer, and other malignancies.

SARS-CoV-2-IN-87 (compound 138968421) is a potent inhibitor of methyltransferases (nsp14 and nsp16) of SARS-CoV-2.

MC3817 free base is a selective DNMT1 inhibitor. MC3817 free base inhibits DNMT1 and DNMT3A/3L with IC₅₀s of 0.044 μM and > 10μM, respectively. MC3817 free base inhibits P53-dependent cancer cell proliferation, induces apoptosis and DNA damage. MC3817 free base elevates cleaved Caspase 3, P53, and γH2AX. MC3817 free base can be used in non-small cell lung cancer, colon cancer, cervical cancer, triple-negative breast cancer and histiocytic lymphoma research.

DNMT1 aptamer sodium is a DNA aptamer for binding and inhibition of DNA methyltransferase 1 (DNMT1).

DNMT-IN-3 is an DNA Methyltransferase (DNMT) inhibitor, and plays an antimalarial role with IC₅₀ of 60 nM against Plasmodium falciparum (Plasmodium). DNMT-IN-3 can be used for malaria related research.

DNMT-IN-6 is a DNA methyltransferase inhibitor with activity against DNMT1, DNMT3A, and DNMT3B. DNMT-IN-6 drives demethylation, and restores TMS1 tumor suppressor gene expression. DNMT-IN-6 induces apoptosis, causes G2/M phase arrest, disrupts mitochondrial integrity, and activates the intrinsic caspase cascade (3/7/9). DNMT-IN-6 inhibits tumor growth, and improves survival in xenograft models. DNMT-IN-6 can be used for the research of cancer, such as diffuse large B-cell lymphoma.

Isofistularin-3 is a direct, DNA-competitive DNMT1 inhibitor, with an IC₅₀ of 13.5 μM. Isofistularin-3, as a DNA demethylating agent, induces cell cycle arrest and sensitization to TRAIL in cancer cells. Isofistularin-3 can be used as an ADC cytotoxin.

DNMT1-IN-3 (compound 7t-S) is an effective DNA methyltransferase 1 (DNMT1) inhibitor with an IC₅₀ value of 0.777 μM and a K_D value of 0.183 μM. DNMT1-IN-3 can bind to the methyl donor S-adenosyl-l-methionine (SAM) site in DNMT1. DNMT1-IN-3 can inhibit cell proliferation in K562 cells by inducing cells apoptosis and arresting cell cycle at G0 / G1 phase, which has the potential to be used for the research of hematologic tumor.

Levetiracetam-d₆ is the deuterium labeled Levetiracetam. Levetiracetam, an antiepileptic agent, binds the synaptic vesicle protein SV2A. Levetiracetam enhances Temozolomide effect on glioblastoma stem cell proliferation and apoptosis. Levetiracetam modulates HDAC levels ultimately silencing MGMT, thus increasing Temozolomide effectiveness. A chemosensitizer agent.

DNMT1-IN-5 (Compound 55) is the inhibitor for DNMT that inhibits DNMT1 and DNMT3A with IC₅₀ of 2.42 μM and 14.4 μM. DNMT1-IN-5 exhibits antiproliferative activity in a variety of cancer cell lines (IC₅₀s for TMD-8, DOHH2, MOLM-13, THP-1, RPIM-8226 and HCT116 are 0.19-2.37 μM), arrests the cell cycle at G2/M phase, and induces apoptosis in TMD-8 and DOHH2 cells. DNMT1-IN-5 exhibits antitumor efficacy in TMD-8 xenograft mouse models.

J208 is a dual inhibitor for histone deacetylase (HDAC) and DNA methyltransferase (DNMT). J208 inhibits proliferation of cancer cells, as well as the migration/invasion of triple-negative breast cancer (TNBC) cells. J208 induces apoptosis, arrests the cell cycle at G0/G1 phase. J2008 activates the innate immune signalling pathway in TNBC, by inducing the expression of endogenous retroviruses (ERVs).

(S)-Kaempferide (ZINC167686681) is a DNA methyltransferase (DNMT) inhibitor. (S)-Kaempferide can be used in tumor research.