DNA-Methyltransferase-Inhibitors-Modulators-MCE

1、 HYPERLINK https:/www.MedChemE/Targets/DNA Methyltransferase.html DNA HYPERLINK https:/www.MedChemE/Targets/DNA Methyltransferase.html HYPERLINK https:/www.MedChemE/Targets/DNA Methyltransferase.html MethyltransferaseDNMTs; DNA MTasesDNA methyltransferases (DNMTs) are a family of “writer” enzymes re

2、sponsible for DNA methylation that is the addition of a methylgroup to the carbon atom number five (C5) of cytosine. Mammalians encode five DNMTs: DNMT1, DNMT2, DNMT3A-DNMT3B (denovo methyltransferases), and DNMTL. DNMT1, DNMT3A, and DNMT3B are the three active enzymes that maintain DNAmethylation.

3、DNMT3L has no catalytic activity and functions as a regulator of DNMT3A and DNMT3B, whereas DNMT2 acts as atRNA transferase rather than a DNA methyltransferase.DNA methylation is a vital modification process in the control of genetic information, which contributes to the epigenetics byregulating gen

4、e expression without changing the DNA sequence. In prokaryotes, DNA methylation is essential for transcription, thedirection of post-replicative mismatch repair, the regulation of DNA replication, cell-cycle control, bacterial virulence, anddifferentiating self and non-self DNA. In mammalians, DNA m

5、ethylation is crucial in many key physiological processes, including theinactivation of the X-chromosome, imprinting, and the silencing of germline-specific genes and repetitive elements.www.MedChemE 1 HYPERLINK https:/www.MedChemE/Targets/DNA Methyltransferase.html DNA HYPERLINK https:/www.MedChemE

6、/Targets/DNA Methyltransferase.html HYPERLINK https:/www.MedChemE/Targets/DNA Methyltransferase.html Methyltransferase HYPERLINK https:/www.MedChemE/Targets/DNA Methyltransferase.html HYPERLINK https:/www.MedChemE/Targets/DNA Methyltransferase.html Inhibitors HYPERLINK https:/www.MedChemE/r-gsk-3685

7、032.html (R)-GSK-3685032 HYPERLINK https:/www.MedChemE/r-gsk-3685032.html HYPERLINK https:/www.MedChemE/2-3-5-triacetyl-5-azacytidine.html 2,3,5-Triacetyl-5-azacytidineCat. No.: HY-139664A Cat. No.: HY-112551(R)-GSK-3685032 is the R-enantiomer ofGSK-3685032. GSK-3685032 is a non-time-dependent,nonco

8、valently, first-in-class reversibleDNMT1-selective inhibitor, with an IC of500.036 M.2,3,5-Triacetyl-5-azacytidine is an orallyactive prodrug of 5-Azacytidine. 5-Azacytidine isan inhibitor of DNA methyltransferase.Purity: 98.02%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 25 mg, 50 mg, 1

9、00 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/2-deoxy-5-nitrocytidine.html 2-Deoxy-5-nitrocytidineCat. No.: HY-145950 HYPERLINK https:/www.MedChemE/5-Azacytidine.html 5-Azacytidine(Azacitidine; 5-AzaC; Ladakamycin) Cat. No.: HY-105862-Deoxy-5-ni

10、trocytidine is a DNAMethyltransferase inhibitor extracted frompatent CN108498529A. 2-Deoxy-5-nitrocytidine canbe used for the research of cancer.5-Azacytidine (Azacitidine; 5-AzaC; Ladakamycin)is a nucleoside analogue of cytidine thatspecifically inhibits DNA methylation.Purity: 98%Clinical Data: No

11、 Development ReportedSize: 1 mg, 5 mgPurity: 99.40%Clinical Data: LaunchedSize: 10 mM 1 mL, 100 mg, 200 mg, 500 mg HYPERLINK https:/www.MedChemE/5-fluoro-2-deoxycytidine.html 5-Fluoro-2-deoxycytidineCat. No.: HY-116217 HYPERLINK https:/www.MedChemE/5-methyl-2-deoxycytidine.html 5-Methyl-2-deoxycytid

12、ine(5-Methyldeoxycytidine) Cat. No.: HY-W0120785-Fluoro-2-deoxycytidine, a fluoropyrimidinenucleoside analogue, is a DNA methyltransferase(DNMT) inhibitor. 5-Fluoro-2-deoxycytidine isa tumor-selective prodrug of the potentthymidylate synthase inhibitor 5-fluoro-2-dUMP.5-Methyl-2-deoxycytidine in sin

13、gle-stranded DNAcan act in cis to signal de novo DNA methylation.Purity: 99.10%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mgPurity: 98.15%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 100 mg HYPERLINK https:/www.MedChemE/6-Methyl-5-azacytidine.html 6-Methyl-5-azacytidine HYP

14、ERLINK https:/www.MedChemE/6-Methyl-5-azacytidine.html HYPERLINK https:/www.MedChemE/6-Thioguanine.html 6-ThioguanineCat. No.: HY-111644(Thioguanine; 2-Amino-6-purinethiol) Cat. No.: HY-137656-Methyl-5-azacytidine is a potent DNMT inhibitor.6-Thioguanine (Thioguanine; 2-Amino-6-purinethiol)is an ant

15、i-leukemia and immunosuppressant agent,acts as an inhibitor of SARS and MERS coronaviruspapain-like proteases (PLpros) and also potentlyinhibits USP2 activity, with IC s of 25 M and5040 M for Plpros and recombinant humanPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 99.0%Cl

16、inical Data: LaunchedSize: 10 mM 1 mL, 100 mg, 500 mg HYPERLINK https:/www.MedChemE/aa-cw236.html AA-CW236 HYPERLINK https:/www.MedChemE/aa-cw236.html HYPERLINK https:/www.MedChemE/benzyl-selenocyanate.html Benzyl HYPERLINK https:/www.MedChemE/benzyl-selenocyanate.html HYPERLINK https:/www.MedChemE/

17、benzyl-selenocyanate.html selenocyanateCat. No.: HY-119390 Cat. No.: HY-131991AA-CW236 is a MGMT (O6-methylguanine DNAmethyltransferase) inhibitor. AA-CW236 targetsMGMT active site Cys145 for covalent modification.Benzyl selenocyanate is a chemopreventive agentfor various chemically induced tumors i

18、n animalmodels at both the initiation and postinitiationstages. Benzyl selenocyanate is an inhibitor ofDNA (cytosine-5)-methyltransferase (Mtase),with an with an IC of 8.4 M.50Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg

19、, 5 mg2 Tel: 609-228-6898 Fax: 609-228-5909 Email: salesMedChemE HYPERLINK https:/www.MedChemE/bobcat339.html Bobcat339 HYPERLINK https:/www.MedChemE/bobcat339.html HYPERLINK https:/www.MedChemE/Bobcat339_hydrochloride.html Bobcat339 HYPERLINK https:/www.MedChemE/Bobcat339_hydrochloride.html HYPERLI

20、NK https:/www.MedChemE/Bobcat339_hydrochloride.html hydrochlorideCat. No.: HY-111558 Cat. No.: HY-111558ABobcat339 is a potent and selective cytosine-basedinhibitor of TET enzyme, with IC s of 33 M50and 73 M for TET1 and TET2, respectively.Bobcat339 hydrochloride is a potent and selectivecytosine-ba

21、sed inhibitor of TET enzyme, withthe IC s of 33 M and 73 M for and ,50 TET1 TET2respectively.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 99.02%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/cm-272.html CM-

22、272 HYPERLINK https:/www.MedChemE/cm-272.html HYPERLINK https:/www.MedChemE/CM-579.html CM-579Cat. No.: HY-101925 Cat. No.: HY-117421CM-272 is a first-in-class, potent, selective,substrate-competitive and reversible dual G9a/DNAmethyltransferases (DNMTs) inhibitor withantitumor activities.CM-579 is

23、a first-in-class reversible, dualinhibitor of G9a and DNMT, with IC values of5016 nM, 32 nM for G9a and DNMT, respectively. Haspotent in vitro cellular activity in a wide range ofcancer cells.Purity: 99.27%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mgPurity: 98%C

24、linical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/CM-579_hydrochloride.html CM-579 HYPERLINK https:/www.MedChemE/CM-579_hydrochloride.html HYPERLINK https:/www.MedChemE/CM-579_hydrochloride.html trihydrochloride HYPERLINK https:/www.MedChemE/CM-579_hydrochloride.htm

25、l HYPERLINK https:/www.MedChemE/DC_05.html DC-05Cat. No.: HY-117421A Cat. No.: HY-12746CM-579 trihydrochloride is a first-in-classreversible, dual inhibitor of G9a and DNMT,with IC values of 16 nM, 32 nM for G9a and DNMT,50respectively. Has potent in vitro cellularactivity in a wide range of cancer

26、cells.DC-05 is a DNA methyltransferase 1 (DNMT1)inhibitor, with an IC50 and a Kd of 10.3 M and1.09 M, respectively.Purity: 98.03%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mgPurity: 99.08%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg

27、HYPERLINK https:/www.MedChemE/DC_517.html DC_517 HYPERLINK https:/www.MedChemE/DC_517.html HYPERLINK https:/www.MedChemE/Decitabine.html DecitabineCat. No.: HY-12747(5-Aza-2-deoxycytidine; 5-AZA-CdR; NSC 127716) Cat. No.: HY-A0004DC_517 is a DNA methyltransferase 1 (DNMT1)inhibitor, with an IC and a

28、 of 1.7 M and50 Kd0.91 M, respectively.Decitabine (NSC 127716) is an orally activedeoxycytidine analogue antimetabolite and a DNAmethyltransferase inhibitor.Purity: 99.41%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mgPurity: 99.97%Clinical Data: LaunchedSize: 10 mM 1 mL,

29、100 mg, 500 mg, 1 g, 2 g HYPERLINK https:/www.MedChemE/dihydro-5-azacytidine.html Dihydro-5-azacytidine HYPERLINK https:/www.MedChemE/dihydro-5-azacytidine.html HYPERLINK https:/www.MedChemE/dnmt3a-in-1.html DNMT3A-IN-1(DHAC; NSC 264880) Cat. No.: HY-106689Cat. No.: HY-144433Dihydro-5-azacytidine (D

30、HAC), the nucleosideanalog, is incorporated into DNA and inhibits DNAmethylation. Dihydro-5-azacytidine has anantitumor activity.DNMT3A-IN-1 is a potent and selective DNMT3Ainhibitor. DNMT3A-IN-1 shows inhibitor activitiesagainst DNMT3A with k values range from 9.16-18.85IM (AdoMet) and 11.37-23.34

31、M (poly dI-dC) .Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgwww.MedChemE 3 HYPERLINK https:/www.MedChemE/gsk-3484862.html GSK-3484862 HYPERLINK https:/www.MedChemE/gsk-3484862.html HYPERLINK https:/www.MedChemE/gsk

32、-3685032.html GSK-3685032Cat. No.: HY-135146 Cat. No.: HY-139664GSK-3484862 is a non-covalent inhibitor forDnmt1. GSK-3484862 induces DNA hypomethylationto against cancer. GSK-3484862 mediates globaldemethylation in murine embryonic stem cells.GSK-3685032 is a non-time-dependent,noncovalently, first

33、-in-class reversibleDNMT1-selective inhibitor, with an IC of500.036 M. GSK-3685032 induces robust loss of DNAmethylation, transcriptional activation, andcancer cell growth inhibition.Purity: 99.94%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 10 mg, 50 mgPurity: 98.53%Clinical Data: No Dev

34、elopment ReportedSize: 5 mg, 10 mg, 25 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/SGI-110.html Guadecitabine(SGI-110) Cat. No.: HY-13542 HYPERLINK https:/www.MedChemE/S-110.html Guadecitabine HYPERLINK https:/www.MedChemE/S-110.html HYPERLINK https:/www.MedChemE/S-110.html sodium(SGI-110 sodium

35、; S-110 sodium) Cat. No.: HY-15229Guadecitabine (SGI-110) is a second-generationDNA methyltransferases (DNMT) inhibitor forresearch of acute myeloid leukemia (AML) andmyelodysplastic syndromes (MDS).Guadecitabine sodium (SGI-110 sodium) is asecond-generation DNA methyltransferases(DNMT) inhibitor fo

36、r research of acute myeloidleukemia (AML) and myelodysplastic syndromes(MDS).Purity: 98.0%Clinical Data: Phase 3Size: 1 mg, 5 mgPurity: 98.05%Clinical Data: Phase 3Size: 5 mg, 10 mg HYPERLINK https:/www.MedChemE/Hinokitiol.html Hinokitiol(-Thujaplicin) Cat. No.: HY-B2230 HYPERLINK https:/www.MedChem

37、E/isofistularin-3.html Isofistularin-3Cat. No.: HY-19826Hinokitiol is a component of essential oilsisolated from Chymacyparis obtusa, reduces Nrf2expression, and decreases DNMT1 and UHRF1 mRNAand protein expression, with anti-infective,anti-oxidative, and anti-tumor activities.Isofistularin-3 is a d

38、irect, DNA-competitiveDNMT1 inhibitor, with an IC of 13.5 M.50Isofistularin-3, as a DNA demethylating agent,induces cell cycle arrest and sensitization toTRAIL in cancer cells. Isofistularin-3 can be usedas an ADC cytotoxin.Purity: 98.24%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 50 mg,

39、 100 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/levetiracetam.html Levetiracetam HYPERLINK https:/www.MedChemE/levetiracetam.html HYPERLINK https:/www.MedChemE/Lomeguatrib.html Lomeguatrib(UCB L059) Cat. No.: HY-B0106 (PaTrin-2) Cat. No.: HY-136

40、68Levetiracetam, an antiepileptic agent, binds thesynaptic vesicle protein SV2A. Levetiracetamenhances Temozolomide effect on glioblastoma stemcell proliferation and apoptosis.Lomeguatrib is a O6-methylguanine-DNAmethyltransferase (MGMT) inhibitor, with IC s50of 9 nM in cell-free assay and 6nM in MC

41、F-7cells.Purity: 99.99%Clinical Data: LaunchedSize: 10 mM 1 mL, 50 mg, 100 mg, 500 mgPurity: 99.70%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/nanaomycin-a.html Nanaomycin HYPERLINK https:/www.MedChemE/nanaomycin-a.html HYPERLINK h

42、ttps:/www.MedChemE/nanaomycin-a.html A HYPERLINK https:/www.MedChemE/nanaomycin-a.html HYPERLINK https:/www.MedChemE/glucose-conjugated-mgmt-inhibitor.html O6BTG-octylglucosideCat. No.: HY-103397(Glucose-conjugated MGMT inhibitor) Cat. No.: HY-13057Nanaomycin A is the first selective DNMT3Binhibitor

43、 with an IC of 500 nM. Nanaomycin A, a50quinone antibiotics, reactivates silenced tumorsuppressor genes in human cancer cells.O6BTG-octylglucoside is a potentO6-methylguanine-DNAmethyl-transferase(MGMT) inhibitor, with IC s of 32 nM in vitro50(cell extracts) and 10 nM in HeLa S3 cells.Purity: 98.18%

44、Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 25 mgPurity: 95.0%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mg4 Tel: 609-228-6898 Fax: 609-228-5909 Email: salesMedChemE HYPERLINK https:/www.MedChemE/procainamide.html Procainamide(Procaine amide; SP 100)

45、 Cat. No.: HY-A0084A HYPERLINK https:/www.MedChemE/psammaplin-a.html Psammaplin HYPERLINK https:/www.MedChemE/psammaplin-a.html HYPERLINK https:/www.MedChemE/psammaplin-a.html ACat. No.: HY-N2150Procainamide is a specific and potent inhibitor ofDNA methyltransferase 1 (DNMT1). Procainamideis a Class

46、 1A antiarrhythmic agent. Procainamidehas the potential for the research of cancer andarrhythmias.Psammaplin A, a marine metabolite, is a potentinhibitor of HDAC and DNA methyltransferases.Psammaplin A ia a highly potent and selectiveDAC1 inhibitor with an IC of 0.9 nM.50Purity: 95.31%Clinical Data:

47、 LaunchedSize: 1 mg, 5 mgPurity: 98%Clinical Data: No Development ReportedSize: 100 g HYPERLINK https:/www.MedChemE/RG108.html RG108(N-Phthalyl-L-tryptophan) Cat. No.: HY-13642 HYPERLINK https:/www.MedChemE/rsc133.html RSC133Cat. No.: HY-12310RG108 (N-Phthalyl-L-tryptophan) is anon-nucleoside DNA me

48、thyltransferases (DNMTs)inhibitor (IC =115 nM) that blocks the DNMTs50active site.RSC133 exhibits dual activity by inhibiting histonedeacetylase and DNA methyltransferase. RSC133effectively facilitates reprogramming of humansomatic cells to pluripotent stem cells andsupports the maintenance of an un

49、differentiatedstate of human pluripotent stem cells.Purity: 99.81%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 10 mg, 50 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/SGI-1027.html SGI-1027 HYPERLINK https:/www.MedChemE/SGI-1027.html HYPERLINK https