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DNA Methyltransferase(DNA甲基转移酶)

DNA methyltransferases (DNMTs) are a family of enzymes that catalyze the transfer of a methyl group from the methyl donor, usually S-adenosyl-L-methionine (SAM) for all known DNMTs, to the 5-position of cytosine residues in DNA. In mammals, four members of the DNMT gene family have been identified and designated, DNMT1, DNMT3A, DNMT3B and DNMT3L respectively, in which DNMT1 encodes the maintenance methyltransferase, DNMT3A/3B encode the de novo methyltransferases, and DNMT3L encodes an enzyme without any inherent enzymatic activity. Mammalian DNMTs are involved in transcriptional silencing of several sequence classes and play an important role in maintaining genome stability and genomic integrity.

  1. Cat.No. 产品名称 Information
  2. GC69194 GSK3735967 GSK3735967 是一种选择性、可逆、非核苷类 DNMT1 抑制剂。GSK3735967 含有一个平面二氰基吡啶核心,能特异性地嵌入 DNMT1 结合的半甲基化 CpG 二核苷酸中。GSK3735967 有三个结合位点,其中一个能与组蛋白 H4K20me3 结合。
  3. GC69030 DY-46-2 DY-46-2 是一种高效、选择性高的新型非核苷 DNA 甲基转移酶 3A (DNMT3A) 抑制剂,其IC50 值为 1.3 μM。
  4. GC65546 DNMT3A-IN-1 DNMT3A-IN-1 是一种有效的选择性 DNMT3A 抑制剂。 DNMT3A-IN-1 显示出针对 DNMT3A 的抑制剂活性,KI 值范围为 9.16-18.85 μM (AdoMet) 和 11.37-23.34 μM (poly dI-dC)[1]。
  5. GC65242 TFMB-(S)-2-HG TFMB-(S)-2-HG 是 5'-甲基胞嘧啶羟化酶 TET2 的有效抑制剂。TFMB-(S)-2-HG 也抑制 EglN 脯氨酰羟化酶。TFMB-(S)-2-HG 具有研究急性髓性白血病 (AML) 的潜力。
  6. GC64733 Procainamide An Analytical Reference Standard
  7. GC64210 (R)-GSK-3685032 (R)-GSK-3685032 是 GSK-3685032 的 R 型异构体。GSK-3685032 是一种非时间依赖性、非共价、可逆的 DNMT1 选择性抑制剂,IC50=0.036 μM。GSK-3685032 诱导 DNA 甲基化丧失、转录激活和癌细胞生长抑制。
  8. GC63483 GSK-3685032 GSK3685032 is a non-time-dependent, highly selective enzymatic inhibitor of DNA methyltransferase (DNMT1) with IC50 of 0.036 μM, and over 2500-fold more selective than DNMT3A/3L and DNMT3B/3L.
  9. GC61662 5-Fluoro-2'-deoxycytidine 2'-Deoxy-5-fluorocytidine (5-fluoro-2(')-deoxycytidine, FCdR), a pyrimidine analog, is a DNA methyltransferase (DMNT) inhibitor currently in clinical trials for solid tumors.
  10. GC60310 Psammaplin A PsammaplinA是一种海洋代谢产物,是HDAC和DNA甲基转移酶(DNAmethyltransferases)的有效抑制剂。PsammaplinA是一种高效的选择性HDAC1抑制剂,IC50为0.9nM,对HDAC1的选择性是DAC6的360倍,对HDAC7和HDAC8的效力低1000倍以上。PsammaplinA对革兰氏阳性细菌(Gram-positivebacteria)具有抗菌作用,并抑制DNA合成和DNA促旋酶(DNAgyrase)活性。抗肿瘤活性。
  11. GC36196 Guadecitabine sodium Guadecitabine sodium (SGI-110 sodium) 是第二代 DNA 甲基转移酶 (DNMT) 抑制剂,用于研究急性髓性白血病 (AML) 和骨髓增生异常综合征 (MDS)。
  12. GC36153 Glucose-conjugated MGMT inhibitor Glucose-conjugated MGMT inhibitor 是一种有效的 O6-甲基鸟嘌呤-DNA甲基转移酶 (MGMT) 抑制剂,体外(细胞提取物)的 IC50 为 32 nM,在 HeLa S3 细胞中的 IC50 为 10 nM。
  13. GC35714 CM-579 trihydrochloride CM-579 trihydrochloride 是一线的、可逆的,G9a 和DNA 甲基转移酶 (DNMT) 的双抑制剂,其IC50 值分别为 16 nM 和32 nM。在多种癌细胞中发挥有效活性作用。
  14. GC35180 6-Methyl-5-azacytidine 6-Methyl-5-azacytidine 是一种有效的甲基转移酶抑制剂。
  15. GC42562 5-Methyl-2'-deoxycytidine A pyrimidine nucleoside
  16. GC34498 Bobcat339 hydrochloride A cytosine derivative
  17. GC33320 CM-579 CM-579是一线的、可逆的,G9a和DNA甲基转移酶(DNMT)的双抑制剂,其IC50值分别为16nM和32nM。在多种癌细胞中发挥有效活性作用。
  18. GC33148 DC-05 A non-nucleoside DNMT1 inhibitor
  19. GC32872 DC_517 DC_517是一种DNMT1抑制剂,IC50和Kd值分别为1.7μM和0.91μM。
  20. GC31365 γ-Oryzanol Gamma-oryzanol (GO), a nutriactive phytochemical naturally occurring in crude rice bran oil, is an antioxidant compound used to treat hyperlipidemia, disorders of menopause and to increase the muscle mass. γ-Oryzanol is a potent DNA methyltransferases (DNMTs) inhibitor in the striatum of mice. γ-Oryzanol significantly inhibits the activities of DNMT1 (IC50=3.2 μM), DNMT3a (IC50=22.3 μM).
  21. GC11302 Hinokitiol A tropolone with diverse biological activities
  22. GC12367 CM-272 An inhibitor of G9a, GLP, and DNA methyltransferases
  23. GC14364 SGI-1027 A DNA methyltransferase inhibitor
  24. GC17428 SGI-110 SGI-110 (SGI-110) 是第二代 DNA 甲基转移酶 (DNMT) 抑制剂,用于研究急性髓性白血病 (AML) 和骨髓增生异常综合征 (MDS)。
  25. GC14366 Thioguanine A thiopurine analog
  26. GC12153 Zebularine A DNA methyltransferase inhibitor
  27. GC13398 RG 108 DNA methyltransferase inhibitor
  28. GC11778 Lomeguatrib

    Inactivator of O6-methylguanine-DNA methyltransferase

  29. GC10946 5-Azacytidine A DNA methyltransferase inhibitor
  30. GC15255 Decitabine(NSC127716, 5AZA-CdR) 地西他滨(Decitabine, DAC)是一种具有口服生物活性的脱氧胞苷类似物抗代谢物,具有DNA甲基转移酶抑制剂的功能。

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