dnmts

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.

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.

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.

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

5-Methyl-2'-deoxycytidine (5MedCyd) is a pyrimidine nucleoside that when incorporated into single-stranded DNA can act in cis to signal de novo.

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).

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.

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.

Hinokitiol (4-Isopropyltropolone) can inhibit ultraviolet B-induced apoptosis in keratinocytes and strongly suggest that the inhibitory mechanism is due to the antioxidant activity of metallothionein induced by the agent. Also, Hinokitiol modulates estrogen receptor signaling and inhibits proliferation of human breast cancer cells.

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

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.

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

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).

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

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

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

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.

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