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Home >> Signaling Pathways >> Chromatin/Epigenetics

Chromatin/Epigenetics(染色质/表观遗传学)

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. GC48408 TW9 A dual inhibitor of BRD4 and HDAC1
  3. GC48382 Ac-QPKK(Ac)-AMC A fluorogenic substrate for SIRT1, SIRT2, and SIRT3
  4. GC50721 iP300w Potent p300/CBP inhibitor
  5. GC50699 SGC 6870 Potent and selective protein arginine methyltransferase 6 (PRMT6) inhibitor (IC50 = 77 nM)
  6. GC50697 GSK 591 dihydrochloride A chemical probe for PRMT5
  7. GC50659 BIX NHE1 inhibitor BIX NHE1 inhibitor 是有效的钠氢交换异构体 1 (NHE1) 抑制剂，在细胞内 pH 恢复 (pHi) 和人血小板肿胀试验中的 IC50 分别为 6 和 31 nM。
  8. GC48263 YW3-56 (hydrochloride) (technical grade) A PAD2 and PAD4 inhibitor
  9. GC48084 Sodium 4-Phenylbutyrate-d11 An internal standard for the quantification of sodium 4-phenylbutyrate
  10. GC48066 SAHO2 A radical SAM enzyme substrate
  11. GC48065 SAHO A radical SAM enzyme substrate
  12. GC47693 m-Methoxybenzamide A PARP inhibitor
  13. GC47586 Lysine-specific Demethylase Inhibitor (1C) (hydrochloride) An LSD1 inhibitor
  14. GC47579 L-Pyrohomoglutamic Acid An amino acid building block
  15. GC47450 IL-4 Inhibitor An IL-4 inhibitor
  16. GC47294 Entacapone-d10 An internal standard for the quantification of entacapone
  17. GC47056 CAY10753 A TNKS2 inhibitor
  18. GC47055 CAY10749 A dual inhibitor of PARP and PI3K
  19. GC47050 CAY10727 A PAD3 inhibitor
  20. GC46935 Bobcat 339 A cytosine derivative
  21. GC46900 AZ9482 A PARP inhibitor
  22. GC46892 ATRA-BA Hybrid A prodrug form of all-trans retinoic acid and butyric acid
  23. GC46736 7-Bromoheptanoic Acid A building block
  24. GC46675 4-Phenyl-2-pyrrolidinone A precursor and synthetic intermediate
  25. GC46628 4-Chloro-6,7-bis(2-methoxyethoxy)quinazoline A building block and synthetic intermediate
  26. GC46607 4-(Methylnitrosamino)-1-(3-pyridyl)-1-butanone A tobacco-specific nitrosamine carcinogen
  27. GC46508 2',2'-Difluoro-2'-deoxyuridine An active metabolite of gemcitabine
  28. GC46503 2-(1,8-Naphthyridin-2-yl)phenol An enhancer of STAT1 activity
  29. GC61279 SIRT-IN-3 SIRT-IN-3是一种有效的SIRT抑制剂，对SIRT1的IC50为17μM。SIRT-IN-3对SIRT1的选择性分别是SIRT-2和SIRT3的4倍和14倍(IC50forSIRT2=74μM;IC50forSIRT3=235μM)。
  30. GC61212 PROTAC BRD4 Degrader-5 PROTACBRD4Degrader-5是一种基于PROTAC的BRD4降解剂，可有效降解HER2阳性和阴性乳腺癌细胞系中的BRD4。
  31. GC61142 NSC745885 NSC745885是一种有效的抗肿瘤(anti-tumor)试剂，对多种癌细胞株有选择性毒性，但对正常细胞没有毒性。NSC745885是一种有效的EZH2的下调因子通过蛋白酶体降解途径。NSC745885为晚期膀胱癌和口腔鳞癌的研究提供了可能性。
  32. GC61058 Metoprine Metoprine(BW197U)是一种有效的组胺N-甲基转移酶(HMT)抑制剂。Metoprine是一种二氨基嘧啶衍生物，可以透过血脑屏障，并通过抑制HMT增加脑组胺水平。Metoprine是一种抗叶酸(antifolate)和抗肿瘤药。
  33. GC61029 Marein A glucoside chalcone with diverse biological activities
  34. GC60925 IACS-9571 hydrochloride IACS-9571(ASIS-P040)hydrochloride是溴结构域蛋白TRIM24和BRPF1的抑制剂，对TRIM24的IC50和Kd值分别为8nM和31nM，对BRPF1的Kd值为14nM。
  35. GC60919 Hydroxycitric acid tripotassium hydrate Hydroxycitricacidtripotassiumhydrate(Potassiumcitratemonohydrate)是藤黄果的主要活性成分，也是柠檬酸的衍生物。Hydroxycitricacidtripotassiumhydrate可竞争性抑制柠檬酸裂解酶(ATPcitratelyase)，并具有减肥效果。Hydroxycitricacidtripotassiumhydrate有效抑制结石形成并抑制HIF，具有抗氧化，抗炎和抗肿瘤作用。
  36. GC60579 Amodiaquine dihydrochloride A prodrug form of N-desethyl amodiaquine
  37. 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。
  38. GC60184 GSK8814 GSK8814 是一种高效、选择性的 ATAD2/2B 溴代苯胺化学探针和抑制剂，结合常数pKd=8.1，在 BROMOscan 中的 pKi=8.9。GSK8814 分别以 7.3 和 4.6 的 pIC50 与 ATAD2 和 BRD4 BD1 结合。GSK8814 对 ATAD2 的选择性是 BRD4 BD1 的 500 倍。
  39. GC60172 Gardenia yellow Crocin-I, a major member of the crocin family, has antidepressant activity and ameliorates the disruption of lipid metabolism and dysbiosis of the gut microbiota induced by chronic corticosterone in mice.
  40. GC60004 (rel)-Tranylcypromine D5 hydrochloride Tranylcypromine-d5 (SKF 385-d5) hydrochloride 是氘标记的 (rel)-Tranylcypromine hydrochloride。
  41. GC39840 AMI-1 free acid AMI-1 is a potent and specific Histone Methyltransferase (HMT) inhibitor with IC50 of 3.0 μM and 8.8 μM for yeast Hmt1p and human PRMT1, respectively.
  42. GC39699 Aurintricarboxylic acid A protein synthesis inhibitor with diverse biological activities
  43. GC39679 CG347B CG347B 是一种选择性的 HDAC6 抑制剂。
  44. GC39665 CMP-5 CMP-5 是一种有效的选择性 PRMT5 抑制剂，对 PRMT1，PRMT4 和 PRMT7 酶无活性。CMP-5 在组蛋白的准备过程中，通过抑制 PRMT5 甲基转移酶活性选择性地阻断 S2Me-H4R3。CMP-5 阻断 EBV 驱动的 B 淋巴细胞转化，但对正常 B 细胞没有影响。
  45. GC39663 BI-9321 trihydrochloride BI-9321 trihydrochloride 是一种有效的，选择性的，具有细胞活性的 NSD3-PWWP1 拮抗剂，Kd 值为 166 nM。BI-9321 对 NSD2-PWWP1 和 NSD3-PWWP2 无效。BI-9321 trihydrochloride 在 U2OS 细胞中特异性破坏 NSD3-PWWP1 与组蛋白相互作用，IC50 为 1.2 μM。
  46. GC39485 CK2/ERK8-IN-1 A dual inhibitor of CK2 and ERK8
  47. GC39435 Scopolin A coumarin glucoside with anti-inflammatory activity
  48. GC39417 OXFBD04 OXFBD04 是一种有效的选择性 BRD4 抑制剂，IC50 为 166 nM。OXFBD04 是一种有效的 BET 溴结构域配体，对 CREBBP 溴结构域具有额外的适度亲和力。OXFBD04 具有抗癌活性。
  49. GC39365 CPTH2 A HAT inhibitor
  50. GC50633 BMS 986094 BMS 986094 (INX-08189) 是一种有效的丙型肝炎病毒 (HCV) 复制抑制剂，在 Huh-7 细胞中 24 小时的 EC50 为 35 nM。
  51. GC50576 MRK 740 Potent PRDM9 inhibitor

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