DNA Methyltransferase Inhibitor

Hinokitiol (Standard) is the analytical standard of Hinokitiol. This product is intended for research and analytical applications. 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.

Decitabine methanesulfonate (5-Aza-2'-deoxycytidine methanesulfonate) is an orally active Deoxycytidine analogue antimetabolite and DNA methyltransferase inhibitor. Decitabine methanesulfonate incorporates into DNA in place of cytosine can covalently trap DNA methyltransferase to DNA causing irreversible inhibition of the enzyme. Decitabine methanesulfonate induces cell G2/M arrest and cell Apoptosis. Decitabine has potent anticancer activity.

Procainamide (hydrochloride) (Standard) is the analytical standard of Procainamide (hydrochloride). This product is intended for research and analytical applications.

2′-Deoxy-4′-thiocytidine (T-dCyd) is a novel epigenetic agent. 2′-Deoxy-4′-thiocytidine administrations led to a significant p21 increase. 2′-Deoxy-4′-thiocytidine can eradicate of tumor cells in the double-mutant xenografts.

GSK-3484862 (Standard) is the analytical standard of GSK-3484862 (HY-135146). This product is intended for research and analytical applications. GSK-3484862 is a highly potent non-covalent inhibitor and demethylating agent of DNMT1. GSK-3484862 induces genome-wide DNA demethylation, including the regulatory elements of DNMT3B and the promoter region of TERT, and significantly inhibits cell viability, growth, proliferation and self-renewal. GSK-3484862 blocks the transformation of young AT2 cells, induces apoptosis, and generates transcriptomic features similar to those of senescent cells. GSK-3484862 is widely used in studies related to lung cancer, oral squamous cell carcinoma and lung adenocarcinoma.

MH44 is an efficient inhibitor targeting the SARS-CoV-2 nsp14 N7-methyltransferase (N7-MTase) with an IC₅₀ of 19 nM. MH44 exhibits moderate antiviral effects in SARS-CoV-2-infected A549-hACE2 cells and shows certain cytotoxicity at higher concentrations. MH44 can be used in the research on anti-SARS-CoV-2.

C188-9 (Standard) is the analytical standard of C188-9 (HY-112288). This product is intended for research and analytical applications. C188-9 (TTI-101) is a STAT3 inhibitor with a K_d value of 4.7 nM. C188-9 targets the SH2 domain of STAT3, blocks the processes of STAT3 ligand binding, receptor recruitment, homodimerization and phosphorylation, and regulates STAT3-mediated genes associated with tumorigenesis and radioresistance. C188-9 regulates STAT1-mediated genes related to radioresistance and reduces the activation level of STAT1. C188-9 downregulates the expression of DNMT1, enhances DAC-induced demethylation and re-expression of RASSF1A, and simultaneously potentiates the anti-tumor effect of DAC on pancreatic cancer cells. C188-9 inhibits both anchorage-dependent and anchorage-independent growth of cancer cells, induces Apoptosis, blocks the growth of tumor xenografts, and suppresses muscle atrophy. C188-9 maintains muscle mass, increases body weight and improves grip strength in tumor-bearing mice. C188-9 can be used in research related to head and neck squamous cell carcinoma, pancreatic cancer, sepsis-related skeletal muscle wasting, non-small cell lung cancer, acute myeloid leukemia and cancer cachexia.

S-Aristeromycinyl-L-homocysteine is an S-adenosylmethionine-dependent methyltransferase inhibitor.

5-Aza-dCTP (5-Aza-2'-deoxycytidine-5′-triphosphate) is a nucleotide analog that acts as a substrate for mammalian DNA polymerase α (K_m = 3.0 μM) and a weak competitive inhibitor of this enzyme (K_i = 4.3 μM). 5-Aza-dCTP inhibits DNA polymerase α via incorporation into DNA through Watson-Crick base pairing, inhibits DNA methyltransferases via incorporation into hemimethylated DNA, and induces mutations in HIV-1 via incorporation into viral DNA during synthesis. 5-Aza-dCTP reverses the inhibitory effect of dTTP on dCMP deaminase, and allosterically activates dCMP deamination to the same extent as dCTP. 5-Aza-dCTP is applicable to research related to leukemia and type 1 human immunodeficiency virus infection.