dnmt3b

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).

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.

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-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.

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

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

CM-579 trihydrochloride, a first-in-class reversible, dual inhibitor of G9a and DNMT, exhibits potent in vitro cellular activity across a broad spectrum of cancer cells. It demonstrates inhibition with IC50 values of 16 nM for G9a and 32 nM for DNMT, respectively.

PNMT-IN-1 (inhibitor 4) is a selective second generation inhibitor [1] of phenylethanolamine N-methyltransferase (PNMT), exhibiting a Ki value of 1.2 nM and an IC50 value of 81 nM. Additionally, it disrupts the activity of DNMT1 and DNMT3b, with IC50 values of 61 μM and 17 μM, respectively, and antagonizes the action of epinephrine.