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Home >> Signaling Pathways >> Chromatin/Epigenetics

Chromatin/Epigenetics

Epigenetics

Epigenetics means above genetics. It determines how much and whether a gene is expressed without changing DNA sequences. Epigenetic regulations include, 1. DNA methylation: the addition of methyl group to DNA, converting cytosine to 5-methylcytosine, mostly at CpG sites; 2. Histone modifications: posttranslational modificationEpigeneticss of histone proteins including acetylation, methylation, ubiquitylation, phosphorylation and sumoylation; 3. miRNAs: non-coding microRNA downregulating gene expression; 4. Prions: infectious proteins viewed as epigenetic agents capable of inducing a phenotype without changing the genome.

Products for  Chromatin/Epigenetics

  1. Cat.No. 产品名称 Information
  2. GC31365 γ-Oryzanol γ-Oryzanol有效抑制小鼠纹状体中的DNA甲基转移酶(DNMTs)。抑制DNMT1和DNMT3a，IC50分别为3.2μM和22.3μM。
  3. GC45258 (+)-Biotin 4-Amidobenzoic Acid (sodium salt) (+)-Biotin 4-amidobenzoic acid is a substrate of biotinidase, which cleaves biotin amide to give biotin in vivo.
  4. GC61595 (+)-JQ-1-aldehyde (+)-JQ-1-aldehyde是(+)-JQ1的醛形式。(+)-JQ-1-aldehyde可作为合成PROTACs的前体，靶向BET溴结构域.。
  5. GC34958 (+)-JQ1 PA (+)-JQ1 PA 是溴结构域和额外末端结构域 (BET) 抑制剂 JQ1 的衍生物，其 IC50 值为 10.4 nM。
  6. GC13822 (-)-JQ1

    BET bromodomain inhibitor
  7. GC34964 (1S,3R,5R)-PIM447 dihydrochloride (1S,3R,5R)-PIM447 (dihydrochloride)是PIM的抑制剂，来自专利US 20100056576 A1化合物实例72。对Pim1，Pim2和Pim3的IC50分别为0.095，0.522和0.369 μM。
  8. GC62130 (2R,5S)-Ritlecitinib (2R,5S)-Ritlecitinib (2R,5S)-PF-06651600) 是一种有效的选择性的 JAK3 抑制剂 (IC50=144.8 nM)。详细信息请参考专利US20150158864A1，example 68。
  9. GC34971 (3R,4S)-Tofacitinib Tofacitinib(CP-690550)是高效JAK3抑制剂，IC50为1 nM，比对JAK2和JAK1的抑制性高20倍和100倍。
  10. GC34972 (3S,4R)-Tofacitinib Tofacitinib(CP-690550)是高效JAK3抑制剂，IC50为1 nM，比对JAK2和JAK1的抑制性高20倍和100倍。
  11. GC34973 (3S,4S)-Tofacitinib Tofacitinib(CP-690550)是高效JAK3抑制剂，IC50为1 nM，比对JAK2和JAK1的抑制性高20倍和100倍。
  12. GC41695 (6R,S)-5,6,7,8-Tetrahydrofolic Acid (hydrochloride) (6R,S)-5,6,7,8-Tetrahydrofolic acid (THFA), the reduced form of folic acid, serves as a cofactor in methyltransferase reactions and is the major one-carbon carrier in one carbon metabolism.
  13. GC41088 (6S)-Tetrahydrofolic Acid (6S)-Tetrahydrofolic acid is a diastereomer of tetrahydrofolic acid, a reduced form of folic acid that serves as a cofactor in methyltransferase reactions and is the major one-carbon carrier in one carbon metabolism.
  14. GC61807 (E/Z)-AG490

    (E/Z)-AG490((E/Z)-TyrphostinAG490)是(E)-AG490和(Z)-AG490的消旋体。(E)-AG490是一种酪氨酸激酶抑制剂，可抑制EGFR，Stat-3和JAK2/3。
  15. GC63864 (E/Z)-Zotiraciclib hydrochloride (E/Z)-Zotiraciclib ((E/Z)-TG02) hydrochloride 是一种有效的 CDK2，JAK2 和 FLT3 抑制剂，用于癌症研究。
  16. GC15104 (R)-(+)-Etomoxir sodium salt carnitine palmitoyltransferase I (CPT1) inhibitor
  17. GC63791 (R)-(-)-JQ1 Enantiomer (R)-(-)-JQ1 Enantiomer 是 (+)-JQ1的异构体。(+)-JQ1可降低 BRD4 基因表达，而(R)-(-)-JQ1 Enantiomer 没有此作用效果。
  18. GC45908 (R)-BAY-598
  19. GC34443 (R)-BAY1238097 (R)-BAY1238097是BAY1238097的低活性R型异构体。BAY1238097是一种有效的、BET与组蛋白结合的选择性抑制剂，通过下调c-Myc水平及下游转录组，在AML(急性髓性白血病)和MM(多发性骨髓瘤)模型中表现出较强的抗增殖活性。
  20. 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。
  21. GC11340 (R)-PFI 2 hydrochloride SETD7 histone lysine methyltransferase inhibitor
  22. GC34446 (rac)-BAY1238097 (rac)-BAY1238097是一种BET抑制剂，对BRD4的IC50值为1.02μM。用于癌症研究。
  23. GC60004 (rel)-Tranylcypromine D5 hydrochloride (rel)-Tranylcypromine D5 hydrochloride (2-Phenylcyclopropylamine D5 hydrochloride) 是 (rel)-Tranylcypromine hydrochloride 的氘代物。(rel)-Tranylcypromine hydrochloride 是一种不可逆的非选择性单胺氧化酶 (MAO) 抑制剂，用于治疗抑郁症。(rel)-Tranylcypromine hydrochloride 还是一种赖氨酸特异性脱甲基酶 1 (LSD1) 抑制剂，可抑制病变的生长并改善患有子宫内膜异位症的小鼠的全身痛觉过敏。
  24. GC33198 (S)-JQ-35 (TEN-010) (S)-JQ-35(TEN-010)是BET家族的抑制剂，有着潜在的抗肿瘤活性。
  25. GC13634 (S)-PFI-2 (hydrochloride) Negative control of (R)-PFI 2 hydrochloride
  26. GC17055 1,2,3,4,5,6-Hexabromocyclohexane JAK2 tyrosine kinase inhibitor
  27. GC61949 1,4-DPCA ethyl ester 1,4-DPCA ethyl ester 是 1,4-DPCA 的乙酯形式，可以抑制 FIH。
  28. GC40468 1,5-Isoquinolinediol

    The poly(ADP-ribose) polymerases (PARPs) form a family of enzymes with roles in DNA repair and apoptosis.
  29. GC41984 1-Alaninechlamydocin 1-Alaninechalmydocin is a fungal metabolite originally isolated from a Great Lakes-derived Tolypocladium sp.
  30. GC39214 1-Naphthohydroxamic acid 1-Naphthohydroxamic acid (Compound 2) 是一种有效的，选择性的 HDAC8 抑制剂，IC50 为 14 μM。1-Naphthohydroxamic acid 对 HDAC8 的选择性高于 I 类 HDAC1 和 II 类 HDAC6 (IC50 >100 μM)。1-Naphthohydroxamic acid 不会增加整体组蛋白 H4 的乙酰化，也不会降低总细胞内 HDAC 的活性。1-Naphthohydroxamic acid 可诱导微管蛋白乙酰化。
  31. GC46508 2',2'-Difluoro-2'-deoxyuridine
  32. GC12775 2',3',5'-triacetyl-5-Azacytidine prodrug form of 5-azacytidine, a DNA methyltransferase inhibitor
  33. GC11873 2,4-Pyridinedicarboxylic Acid Histone LSD inhibitor
  34. GC42075 2,4-Pyridinedicarboxylic Acid (hydrate) 2,4-Pyridinedicarboxylic Acid (2,4-PDCA) is a compound that structurally mimics 2-oxoglutarate (2-OG, also known as α-ketoglutarate) and chelates zinc, thus affecting a range of enzymes.
  35. GC62233 2,6-Dichloro-N-(2-(cyclopropanecarboxamido)pyridin-4-yl)benzamide GDC-046 是一种有效的，具有口服活性的选择性 TYK2 抑制剂，对 TYK2，JAK1，JAK2 和 JAK3 的 Ki 分别为 4.8、0.7、0.7 和 0.4 nM。
  36. GC46503 2-(1,8-Naphthyridin-2-yl)phenol
  37. GC10408 2-D08 Sumoylation inhibitor
  38. GC11249 2-hexyl-4-Pentynoic Acid Potent and robust HDACs inhibitor
  39. GC15084 2-Methoxyestradiol (2-MeOE2) Apoptotic, antiproliferative and antiangiogenic agent
  40. GC62781 2-Methylquinazolin-4-ol 2-Methylquinazolin-4-ol 是一种高效、竞争性的 poly(ADP-ribose) synthetase 抑制剂，其 Ki 值为 1.1 μM。2-Methylquinazolin-4-ol 是哺乳动物天冬氨酸氨基转移酶 (ATCase) 抑制剂，其 IC50 值为 0.20 mM。
  41. GC14282 3-acetyl-11-keto-β-Boswellic Acid A 5-lipoxygenase inhibitor
  42. GC17907 3-Deazaneplanocin A (DZNep) hydrochloride A SAHH and ENZ2 inhibitor
  43. GC13145 3-Deazaneplanocin,DZNep

    S-adenosylhomocysteine and EZH2 inhibitor
  44. GC18509 3-Methylcytidine (methosulfate)

    3-Methylcytidine (methosulfate) is a cytidine derivative used as an internal standard for HPLC.
  45. GC19013 3-TYP

    3-TYP inhibit SIRT3 with an IC50 of 16 nM, and is more potent over SIRT1 and SIRT2 with IC50 of 88 nM and 92 nM, respectively.
  46. GC62805 4’-Methoxychalcone 4’-Methoxychalcone 通过 PPARγ 活化调节脂肪细胞分化，并调节参与胰岛素敏感性的脂肪组织中各种脂肪因子的表达和分泌。
  47. GC17922 4'-bromo-Resveratrol Sirt1 and Sirt3 inhibitor
  48. GC46607 4-(Methylnitrosamino)-1-(3-pyridyl)-1-butanone
  49. GC46628 4-Chloro-6,7-bis(2-methoxyethoxy)quinazoline
  50. GC16474 4-HQN PARP inhibitor
  51. GC17005 4-iodo-SAHA class I and class II histone deacetylase (HDAC) inhibitor

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