Decitabine (NSC 127716) is a DNA methyltransferase inhibitor commonly used to treat myelodysplastic syndromes (MDS) and acute myeloid leukemia (AML).
5-Aza-4'-thio-2'-deoxycytidine (5-Aza-T-dCyd) is an orally active DNA methyltransferase I (DNMT1) inhibitor. 5-Aza-4'-thio-2'-deoxycytidine, a sulfur-containing deoxy-cytidine analog, has the potential for DNA hypomethylating and has antitumor effects[1].
Hinokitiol is a component of essential oils isolated from Chymacyparis obtusa, reduces Nrf2 expression, and decreases DNMT1 and UHRF1 mRNA and protein expression, with anti-infective, anti-oxidative, and anti-tumor activities.
5-Fluoro-2'-deoxycytidine, a fluoropyrimidine nucleoside analogue, is a DNA methyltransferase (DNMT) inhibitor. 5-Fluoro-2'-deoxycytidine is a tumor-selective prodrug of the potent thymidylate synthase inhibitor 5-fluoro-2′-dUMP[1][2].
Dihydro-5-azacytidine acetate (DHAC), the nucleoside analog, is incorporated into DNA and inhibits DNA methylation. Dihydro-5-azacytidine acetate has an antitumor activity[1][2].
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[1].
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[1].
Glucose-conjugated MGMT inhibitor is a potent O6-methylguanine-DNAmethyl-transferase (MGMT) inhibitor, with IC50s of 32 nM in vitro (cell extracts) and 10 nM in HeLa S3 cells.
AluI Methyltransferase (AluI) is a methyltransferase used as the interference enzymes to investigate the selectivity[1].
Laccaic acid A is a orally active and DNA-competitive inhibitor of DNA methyltransferase 1 (Dnmt1) (Ki=310 nM; IC50=650 nM). Laccaic acid A has stronger Dnmt1 inhibitory effect than SG-1027 (HY-13962). Laccaic acid A combined with Phenethyl isothiocyanate has a strong synergistic effect on colorectal cancer[1][2].
5-Methyl-2'-deoxycytidine in single-stranded DNA can act in cis to signal de novo DNA methylation[1][2].
(R)-GSK-3685032 is the R-enantiomer of GSK-3685032. GSK-3685032 is a non-time-dependent, noncovalently, first-in-class reversible DNMT1-selective inhibitor, with an IC50 of 0.036 μM. GSK-3685032 induces robust loss of DNA methylation, transcriptional activation, and cancer cell growth inhibition[1][2].
GSK-3685032 is a non-time-dependent, noncovalently, first-in-class reversible DNMT1-selective inhibitor, whit an IC50 of 0.036 μM. GSK-3685032 induces robust loss of DNA methylation, transcriptional activation and cancer cell growth inhibition[1].
DNMT3A-IN-2 (compound 2) is a potent and allosteric inhibitor of DNMT3A. DNMT3A-IN-2 inhibits DNMT3A activity by disrupting protein-protein interactions. DNMT3A-IN-2 induces apoptosis of acute myeloid leukemia (AML) cell lines. DNMT3A-IN-2 induces differentiation of distinct AML cell lines including cells with mutated DNMT3A R882[1].
CM-272 (CM272) is a novel potent, selective and reversible dual inhibitor of G9a/DNMTs with IC50 of 8 nM and 382 nM for G9a and DNMT1, respectively; also inhibits DNMT3A/3B/GLP with IC50 of 85/1,200/2 nM, respectively; inhibits cell proliferation and promotes apoptosis in different haematological neoplasias (AML, ALL and DLBCL); significantly prolongs survival of AML, ALL and DLBCL xenogeneic models.
Lomeguatrib is a O6-methylguanine-DNA methyltransferase (MGMT) inhibitor, with IC50s of 9 nM in cell-free assay and ∼6 nM in MCF-7 cells.
5-Azacytidine is a nucleoside analogue of cytidine that specifically inhibits DNA methylation by trapping DNA methyltransferases.
RSC133 exhibits dual activity by inhibiting histone deacetylase and DNA methyltransferase. RSC133 effectively facilitates reprogramming of human somatic cells to pluripotent stem cells and supports the maintenance of an undifferentiated state of human pluripotent stem cells[1].