dnmt3a

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).

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.

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.

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.

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.

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

EML741 also inhibits DNMT1 (IC50, 3.1 μM), with no effect on DNMT3a or DNMT3b. EML741 exhibits low cell toxicity, and is membrane permeable and blood-brain barrier penetrated. EML741 is a histone lysine methyltransferase G9a/GLP inhibitor, with an IC50 of 23 nM, Kd of 1.13 μM for G9a.

DS-437 is a dual PRMT5 7 inhibitor with IC50 values of 6 μM and also inhibits DNMT3A and DNMT3B with IC50 values of 52 μM and 62 μM, respectively. Additionally, DS-437 inhibits the methylation of FOXP3.

DY-46-2 is a highly selective, potent, novel non-nucleoside DNA methyltransferase 3A (DNMT3A) inhibitor (IC50: 1.3 μM).

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.