DNA Methyltransferase Inhibitor

N-Acetyl-S-geranylgeranyl-L-cysteine is a Methyltransferase inhibitor. N-Acetyl-S-geranylgeranyl-L-cysteine inhibits beta 2 integrin-induced actin polymerization with an IC₅₀ of 45 nM.

SC83288 is a Plasmodium falciparum PfDNMT2 inhibitor with an IC₅₀ of 7 μM. SC83288 disrupts the epigenetic regulation of malaria parasites, blocks DNA replication and nuclear division, arrests the development of the asexual blood stage, induces the formation of pyknotic morphology in malaria parasites, and does not affect cytokinesis after nuclear division or parasite egress. SC83288 is applicable to malaria-related research.

Antitumor agent-226 is a DNMT3A inhibitor and epigenetic modulator. Antitumor agent-226 inhibits cell proliferation and migration by downregulating DNA Methyltransferase, reducing global DNA methylation, and modulating JNK, ERK1/2, and p38 phosphorylation through the MAPK pathway to induce mitochondria-dependent apoptosis, G2/M phase arrest, autophagy, and ROS production. Antitumor agent-226 can be used for research on prostate cancer.

Go 6983 GMP is Go 6983 (HY-13689) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. Go 6983 is a dual inhibitor targeting Suv39h1/2 (KMT1A/KMT1B) and PKC, as well as a transcriptional activator capable of inducing DNA hypomethylation. Go 6983 stimulates the transcription of Prdm14 by reducing Suv39h1/2 protein levels, decreasing histone modifications in the Prdm14 promoter region, and increasing the recruitment of RNA polymerase II. Go 6983 induces genome-wide DNA hypomethylation by inhibiting de novo methyltransferase expression and increasing Tet1/Tet2 levels, thereby promoting self-renewal and pluripotency maintenance of stem cells. Meanwhile, Go 6983 can block PKC-mediated signaling pathways to reduce the expression of EMT-related genes and eliminate the upregulation of antioxidant genes downstream of NRF2. Go 6983 is mainly used in mechanism studies related to myocardial ischemia/reperfusion injury.

CM-444 is inhibitor for HDAC (IC₅₀ is 6 nM-0.6 μM) and DNA methyltransferases (DNMT, IC₅₀ is 1.8-2.3 μM). CM-444 is an inducer for the differentiation of acute myeloid leukemia cells. CM-444 exhibits anti-leukemic activity and improves the survival rate in mouse models.

(S)-Tubercidinylhomocysteine (Page 46) is a potent inhibitor of S-adenosylmethionine-dependent methyltransferase. (S)-Tubercidinylhomocysteine can be used for the study of herpesviruses (HSV) and vaccinia (VV).

Nanaomycin A (Standard) is the analytical standard of Nanaomycin A (HY-103397). This product is intended for research and analytical applications. Nanaomycin A is a selective DNMT3B inhibitor with an IC₅₀ of 500 nM. Nanaomycin A inhibits the in vitro growth of human Plasmodium falciparum with an IC₈₀ of 33.1 nM.

(Rac)-RG108 (NSC401077), a DNMT1 inhibitor, inhibits DNA methyltransferases.

Bobcat339 hydrochloride (Standard) is the analytical standard of Bobcat339 (hydrochloride) (HY-111558A). This product is intended for research and analytical applications. Bobcat339 hydrochloride is a potent and selective cytosine-based inhibitor of TET enzyme, with the IC₅₀s of 33 μM and 73 μM for TET1 and TET2, respectively. Bobcat339 hydrochloride is useful to the field of epigenetics and serves as a starting point for new therapeutics that target DNA methylation and gene transcription.

DNMT1-IN-4 is a potent non-nucleoside DNA methyltransferase 1 (DNMT1) inhibitor with an IC₅₀ value of 2.5 µM and selectivity towards other AdoMet-dependent protein methyltransferases. DNMT1-IN-4 significantly inhibits cancer cell proliferation.

CNP0296775 is an inhibitor of dengue virus methyltransferase (DENV MTase) that has the potential to disrupt the viral replication process.

CM-272 (Standard) is the analytical standard of CM-272 (HY-101925). This product is intended for research and analytical applications. CM-272 is a first-in-class, potent, selective, substrate-competitive and reversible dual G9a/DNA methyltransferases (DNMTs) inhibitor with antitumor activities. CM-272 inhibits G9a, DNMT1, DNMT3A, DNMT3B and GLP with IC₅₀s of 8 nM, 382 nM, 85 nM, 1200 nM and 2 nM, respectively. CM-272 inhibits cell proliferation and promotes apoptosis, inducing IFN-stimulated genes and immunogenic cell death.

GSK-3685032 (Standard) is the analytical standard of GSK-3685032 (HY-139664). This product is intended for research and analytical applications. 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.

Levetiracetam-d₃ is the deuterium labeled Levetiracetam. Levetiracetam, an antiepileptic agent, binds the synaptic vesicle protein SV2A. Levetiracetam enhances Temozolomide effect on glioblastoma stem cell proliferation and apoptosis. Levetiracetam modulates HDAC levels ultimately silencing MGMT, thus increasing Temozolomide effectiveness. A chemosensitizer agent.

O6-Benzylguanine sodium is an orally active, blood-brain barrier-penetrant inhibitor of O⁶-methylguanine-DNA methyltransferase (MGMT/AGT). O6-Benzylguanine sodium modulates p53 and its downstream p21 and cyclins to induce cell cycle arrest and apoptosis, and on the other hand activates mTORC1/MAPK and other signaling pathways to induce cellular senescence by inhibiting intracellular MGMT. O6-Benzylguanine sodium is used in research related to various tumors, cellular senescence, and vascular smooth muscle dysfunction.

Bobcat339 (Standard) is the analytical standard of Bobcat339 (HY-111558). This product is intended for research and analytical applications. Bobcat339 is a potent and selective cytosine-based inhibitor of TET enzyme, with IC₅₀s of 33 μM and 73 μM for TET1 and TET2, respectively. Bobcat339 is useful to the field of epigenetics and serves as a starting point for new therapeutics that target DNA methylation and gene transcription.

O6-Benzylguanine Standard is the analytical standard of O6-Benzylguanine (HY-W002585). This product is intended for research and analytical applications. O6-Benzylguanine is an orally active, blood-brain barrier-penetrant inhibitor of O⁶-methylguanine-DNA methyltransferase (MGMT/AGT). O6-Benzylguanine modulates p53 and its downstream p21 and cyclins to induce cell cycle arrest and apoptosis, and on the other hand activates mTORC1/MAPK and other signaling pathways to induce cellular senescence by inhibiting intracellular MGMT. O6-Benzylguanine is used in research related to various tumors, cellular senescence, and vascular smooth muscle dysfunction.

O6BTG-C8-αGlu is an O6-methylguanine-DNA methyltransferase (MGMT) inhibitor with an IC₅₀ of 0.45 μM. At a concentration of 0.1 μM, O6BTG-C8-αGlu can completely inhibit MGMT in HeLaS3 cells. Even when applied chronically at high doses (up to 20 μM), it does not exhibit cytotoxicity. O6BTG-C8-αGlu is suitable for research on MGMT-related cancer diseases.

Hydralazine (hydrochloride) (Standard) is the analytical standard of Hydralazine (hydrochloride). This product is intended for research and analytical applications. Hydralazine hydrochloride is an orally active, blood-brain barrier-permeable DNA methyltransferase inhibitor with vasodilatory, arterial smooth muscle relaxant and hypotensive activities. Hydralazine hydrochloride reactivates silenced tumor suppressor genes via mediating DNA demethylation, while exerting neuroprotective and anti-inflammatory properties. Hydralazine hydrochloride inhibits NOS-2 (iNOS) and COX-2, and reduces the production of NO and PGE_E2; meanwhile, Hydralazine hydrochloride scavenges reactive oxygen species and inhibits macrophage activation. Hydralazine hydrochloride alleviates motor dysfunction, neuropathic inflammatory pain, and formalin-induced somatic and emotional pain responses. In addition, Hydralazine hydrochloride directly induces DNA strand breaks and sister chromatid exchange, exhibiting certain mutagenic characteristics. Hydralazine hydrochloride has been widely used in studies on hypertension, various cancers (such as cervical cancer, leukemia), spinal cord injury and the mechanisms of inflammatory pain.

5-Azacytidine-¹⁵N₄ is ¹³C and ¹⁵N labeled 5-Azacytidine. 5-Azacytidine (Azacitidine; 5-AzaC; Ladakamycin) is a nucleoside analogue of cytidine that specifically inhibits DNA methylation. 5-Azacytidine is incorporated into DNA to covalently trap DNA methyltransferases and contributes to reverse epigenetic changes. 5-Azacytidine induces cell autophagy.