DNA Methyltransferase

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.

Decitabine (Deoxycytidine) is a deoxycytidine analog, a DNA methyltransferase inhibitor with oral activity. Decitabine has antitumor activity and antimetabolic activity. Decitabine induces cell cycle arrest and apoptosis.

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

5-Azacytidine (Ladakamycin) is a cytidine nucleoside analog, a DNA methylation inhibitor with specificity. 5-Azacytidine regulates gene expression by decreasing the level of DNA methylation. 5-Azacytidine induces autophagy and has antitumor activity.

CM-272 is a dual G9a DNA methyltransferases (DNMTs) inhibitor.

Bobcat339 is a novel cytosine-based TET enzyme inhibitor (IC50s: 33 73 uM for TET1 2), but not DNMT3a, does not inhibit the DNA methyltransferase DNMT3a.

Bobcat339 hydrochloride is a selective 10 11 translocation (TET) dioxygenase inhibitor that inhibits TET1 and TET2.Bobcat339 hydrochloride induces TET3 protein degradation and also stimulates the expression of AGRP, NPY, and VGAT in a TET3-dependent manner in mouse and human neuronal cells. VGAT expression, which can be used to study transient anorexia nervosa.

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.

RG108 (N-Phthalyl-L-tryptophan) is a DNA methyltransferase inhibitor with an IC50 of 115 nM.

Cedazuridine ((4R)-2'-Deoxy-2',2'-difluoro-3,4,5,6-tetrahydrouridine) is an oral inhibitor of cytidine deaminase with antineoplastic properties.

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

5-Fluoro-2'-deoxycytidine (2'-DEOXY-5-FLUOROCYTIDINE) is an inhibitor of DNA methyltransferase (DNMT) .

Lomeguatrib (PaTrin-2), a modified guanine base, inhibits the activity of DNA repair protein O(6)-alkylguanine-DNA alkyltransferase (MGMT) .

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.

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.

Zebularine (4-Deoxyuridine) is a DNA methylation inhibitor. Acts as a transition state analog inhibitor of cytidine deaminase by binding to the active size as covalent hydrates. It also inhibits cytidine deaminase (Ki: 2 μM, in a cell-free assay).

Levetiracetam (SIB-S1) is a relatively unique anticonvulsant that is typically used in combination with other antiepileptic medications for partial onset seizures. Levetiracetam has been linked to rare instances of serum aminotransferase and alkaline phosphatase elevations during treatment and to rare cases of clinically apparent drug induced liver disease.

γ-Oryzanol (Gamma-Oryzanol) is a natural nutrient extract isolated from rice bran oil that contains a mixture of sterols and ferulic acids, which may aid in the destruction of free radicals in the skin. It has recently been researched for its ability to slow the progress of melanin pigmentation by intercepting the ultraviolet rays at the skin's surface and hindering their transmission.

Sarmustine (SarCNU) is an alkylating agent with anticancer activity that inhibits the growth of prostate cancer cells via p53-dependent and p53-independent pathways.Sarmustine mediates the selection of P140K methylguanine-DNA-methyltransferase-transduced human CD34(+) cells in vitro.

Procainamide Hydrochloride (Procapan) is the hydrochloride salt form of procainamide, an amide derivative exhibiting class 1A antiarrhythmic property and analog of procaine. Procainamide hydrochloride reversibly binds to and blocks activated (open) voltage-gated sodium channels, thereby blocks the influx of sodium ions into the cell, which leads to an increase in threshold for excitation and inhibit depolarization during phase 0 of the action potential.

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].

TFMB-(S)-2-HG (TFMB S 2 HG) is a highly effective inhibitor of TET2, the 5'-methylcytosine hydroxylase. Additionally, it significantly inhibits the EglN prolyl hydroxylases. With its unique properties, TFMB-(S)-2-HG holds great promise for advancing research in the field of acute myeloid leukemia (AML).

SW155246 is a potent and selective inhibitor of DNMT1 (DNA methyltransferase 1; IC50 of 1.2 μM). SW155246 induces re-expression of the tumor suppressor geneRASSF1 in A549 cells.

Dihydro-5-azacytidine FA (DHAC) is a pyrimidine analog that has antitumor activity, inhibits cell growth, inhibits DNA methylation, and may be used in the study of malignant mesothelioma.

2’-Deoxy-2’-fluoro-β-D-arabinocytidine hydrochloride is a cytosine nucleoside analog with inhibitory effects on DNA methyltransferase , with potential antimetabolic and antitumor activity.

2',3',5'-triacetyl-5-Azacytidine (Nsc291930) is a prodrug form of 5-azacytidine that may be rapidly absorbed orally.

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.

Nanaomycin A, a quinone antibiotics, reactivates silenced tumor suppressor genes in human cancer cells. Nanaomycin A is a selective inhibitor of DNMT3B (IC50 = 500 nM).

Dihydro-5-azacytidine (DHAC) is an active nucleoside analog with anti-leukemic activity that inhibits cell growth and induces DNA hypomethylation.Dihydro-5-azacytidine is used in the study of leukemia and tumors.

Tetrahydrouridine (NSC-112907; THU) is a multidrug resistance modulator. It can be used in cancer treatment to make tumor cells more sensitive to radiation therapy. THU is a competitive cytidine deaminase(CDA) inhibitor that inhibits deamination in the catabolism of cytotoxic deoxycytidine analogs such as ara-C and Gemcitabine.

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

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.

Isomaltotriose is a sugar compound derived from the enzymic hydrolyzates of dextran obtained from the Leuconostoc mesenteroides NRRL B-512.

CM-579 trihydrochloride is a first-in-class reversible and dual inhibitor of G9a and DNMT (IC50s: 16 nM, 32 nM) with potent in vitro cellular activity in a wide range of cancer cells.

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