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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. GC50211 TAT-cyclo-CLLFVY TAT-cyclo-CLLFVY 是 HIF-1 异二聚化的环肽抑制剂，可抑制癌细胞中的缺氧信号传导。 TAT-cyclo-CLLFVY 破坏 HIF-1α/HIF-1β 蛋白质-蛋白质相互作用，IC50 为 1.3 μM。
  3. GC50182 ent-LP 99 ent-LP 99 是一种有效的选择性 BRD7 和 BRD9 抑制剂，对 BRD9 的 KD 为 99 nM。
  4. GC50136 NSC 636819

    OPC3689西洛酰胺

     NSC 636819 是 KDM4A/KDM4B 的竞争性和选择性抑制剂。 KDM4A/KDM4B 是前列腺癌的潜在进展因素。 NSC 636819 具有研究癌症疾病，尤其是前列腺癌的潜力。
  5. GC50128 TC-S 7009 An inhibitor of HIF-2α PAS-B domain heterodimerization
  6. GC50082 UNC 2399 UNC 2399 是一种生物素化的 UNC1999，是一种选择性 EZH2 降解剂，对 EZH2 保持高效的体外效力，IC50 为 17 nM。
  7. GC50070 I-BET 151 dihydrochloride

    GSK1210151A dihydrochloride

     A BRD2, BRD3, and BRD4 inhibitor
  8. GC50066 Atiprimod dihydrochloride JAK2 inhibitor
  9. GC50050 Hesperadin hydrochloride A multi-kinase inhibitor
  10. GC39302 PARP14 inhibitor H10 PARP14 inhibitor H10 (化合物 H10) 是针对 PARP14 的选择性抑制剂 (IC50=490 nM)，是其他 PARP 的抑制剂 (约为 PARP1 的 24 倍)。PARP14 抑制剂 H10 诱导 caspase-3/7 介导的细胞凋亡 (apoptosis)。
  11. GC39252 MS31 trihydrochloride MS31 trihydrochloride 是一种高亲和性和选择性的，片段样的甲基赖氨酸读写蛋白 spindlin 1 (SPIN1) 抑制剂，有效破坏 SPIN1 与 H3K4me3 蛋白互相作用 (IC50=77 nM，AlphaLISA；243 nM，FP). MS31 trihydrochloride 选择性结合 SPIN1 的 Tudor 结构域 II (Kd=91 nM)。MS31 trihydrochloride 能有效抑制含三甲基赖氨酸肽与 SPIN1 的结合，对非肿瘤性细胞无毒。
  12. GC39214 1-Naphthohydroxamic acid

    1-萘羟肟酸

     1-Naphthohydroxamic acid是强效、细胞渗透性和选择性组蛋白脱乙酰酶抑制剂 (HDAC8) 抑制剂（IC?50?= 14 μM）。在体外有抗癌活性。
  13. GC46226 SS-208 An HDAC6 inhibitor
  14. GC46213 Ro 41-0960 A COMT inhibitor
  15. GC46191 Oclacitinib-13C-d3 A neuropeptide with diverse biological activities
  16. GC46159 Histone H2AX (134-143) (human) (trifluoroacetate salt)

    H-Lys-Lys-Ala-Thr-Gln-Ala-Ser-Gln-Glu-Tyr-OH, KKATQASQEY

     A neuropeptide with diverse biological activities
  17. GC46152 GS-441524 An antiviral nucleoside analog
  18. GC46148 Filgotinib-d4

    GLPG0634-d4

     An internal standard for the quantification of filgotinib
  19. GC46104 Butyric Acid-d7

    氘代丁酸(D7),Butanoic acid-d7

     An internal standard for the quantification of sodium butyrate
  20. GC46081 A-395 (hydrochloride) A neuropeptide with diverse biological activities
  21. GC39180 PROTAC BRD4 ligand-1 PROTAC BRD4 ligand-1 是一种有效的 BET 抑制剂，是靶向 BRD4 蛋白的配体。
  22. GC39146 HIF-1 inhibitor-1 An inhibitor of HIF-1 signaling
  23. GC39081 Reticuline

    番荔枝碱

     Reticuline 分离自 Litsea cubeba，通过 JAK2/STAT3 和 NF-κB 信号通路显示抗炎作用。Reticuline 还可抑制 TNF-α 和 IL-6 的 mRNA 表达，并降低 JAK2 和 STAT3 的磷酸化水平。
  24. GC38839 Pseudoprotodioscin

    伪原薯蓣皂苷

     A steroidal saponin with diverse biological activities
  25. GC38767 Deoxyshikonin

    去氧紫草素

     Deoxyshikonin 是从 Lithospermum erythrorhizon Sieb 中分离得到的，具有抗肿瘤活性。
  26. GC38742 BRD-6929

    JQ12

     An HDAC1 and HDAC2 inhibitor
  27. GC45927 DS-437 A dual inhibitor of PRMT5 and PRMT7
  28. GC45908 (R)-BAY-598 An inhibitor of SMYD2
  29. GC45906 MC1742 An inhibitor of class I and class IIb HDACs
  30. GC45808 OUL35

    NSC39047

     An inhibitor of PARP10
  31. GC45772 6(5H)-Phenanthridinone

    6(5H)-菲啶酮

     An inhibitor of PARP1 and 2
  32. GC45763 Tolcapone-d4

    托卡朋-D4,Ro 40-7592-d4

     An internal standard for the quantification of tolcapone
  33. GC45717 Chlamydocin An HDAC inhibitor
  34. GC45640 TP-238 (hydrochloride) A chemical probe for the bromodomains of CECR2 and BPTF
  35. GC45609 ZLD1039 An inhibitor of EZH2
  36. GC38709 KDOAM-25 citrate KDOAM-25 citrate 是有效，高选择性的 KDM5 抑制剂，对 KDM5A，KDM5B，KDM5C，KDM5D 的 IC50 分别为 71 nM，19 nM，69 nM，69 nM。KDOAM-25 citrate 可增加转录起始位点的整体 H3K4 甲基化，并损害多发性骨髓瘤 MM1S 细胞的增殖。
  37. GC38519 Ilorasertib hydrochloride

    ABT-348 hydrochloride

     A multi-kinase inhibitor
  38. GC38474 MS645 MS645 是一种 BET bromodomains (BrD) 抑制剂，对于 BRD4-BD1/BD2 的 Ki 值为 18.4 nM。MS645 在空间上限制 BRD4 BrDs 的二价抑制，从而导致实体肿瘤细胞中 BRD4 转录活性的持续抑制。
  39. GC38469 CBP/p300-IN-3 P300/CBP-IN-3, a p300/CBP 组蛋白乙酰转移酶 (histone acetyltransferase) 抑制剂，化合物 6，来源于专利 WO 2019049061 A1。
  40. GC38412 Crotonoside

    巴豆苷; Isoguanosine

     Crotonoside是一种FLT3和HDAC3/6抑制剂，可用于研究急性髓系白血病(AML)。
  41. GC38163 Tazemetostat hydrobromide Tazemetostat hydrobromide (EPZ-6438 hydrobromide) 是一种有效，选择性，口服的 EZH2 抑制剂。Tazemetostat hydrobromide 抑制含有 PRC2 复合体的野生型 EZH2 的活性， Ki 值为 2.5±0.5 nM。Tazemetostat hydrobromide 抑制 EZH2，在肽测定和核小体测定中 IC50 分别为 11 和 16 nM。Tazemetostat hydrobromide 抑制大鼠 EZH2，IC50 为 4 nM。Tazemetostat hydrobromide 还抑制 EZH1，IC50 为 392 nM。
  42. GC38062 Gambogenic acid

    新藤黄酸

     Gambogenic Acid, identified from Gamboge, is an inhibitor of the FGFR signaling pathway in erlotinib-resistant non-small-cell lung cancer (NSCLC) and exhibits anti-tumor effects. Gambogenic acid acts is also an effective inhibitor of EZH2 that specifically and covalently binds to Cys668 within the EZH2-SET domain, and triggers EZH2 ubiquitination.
  43. GC38049 GSK8573 GSK8573 是 GSK2801 的非活性对照化合物。GSK8573 与 BRD9 具有结合活性，Kd 值为 1.04 μM，并且对 BAZ2A/B 和其他溴结构域家族无抑制活性。
  44. GC38044 Fraxinellone

    梣酮

     A liminoid degradant with diverse biological activities
  45. GA20605 Ac-Lys-AMC Ac-Lys-AMC（己酰胺），也称为 MAL，是组蛋白去乙酰化酶 HDAC 的荧光底物。
  46. GA20481 Ac-Arg-Gly-Lys(Ac)-AMC

    Ac-Arg-Gly-Lys(Ac)-AMC 是 HDAC 的底物。
  47. GC45548 Photoswitchable PAD Inhibitor (technical grade) A photoactivated PAD inhibitor
  48. GC45503 L-Moses (hydrochloride)

    L-45

     A PCAF bromodomain inhibitor
  49. GC45489 K-Biotin-W-Histone H2B (108-125) (trifluoroacetate salt)

    Histone H2BK-Biotin (108-125), K(Biotin)-W-Histone H2B (108-125), K(Biotin)WKHAVSEGTKAVTKYTSSK

     A biotinylated peptide fragment of histone H2B
  50. GC45485 Histone H4R3Me2s (1-21)-GGK-biotin (trifluoroacetate salt)

    Ac-SG-R(me2s)-GKGGKGLGKGGAKRHRKV-GGK(Biotin), Arg(Me2s)3-Histone H4 (1-21)-GGK(Biotin), Histone H4 (1-21) (Arg3me2s)

     A biotinylated peptide fragment of histone H4
  51. GC45484 Histone H3K9Me3 (3-17) (human, mouse, rat, porcine, bovine) (trifluoroacetate salt)

    H-Thr-Lys-Gln-Thr-Ala-Arg-Lys(Me3)-Ser-Thr-Gly-Gly-Lys-Ala-Pro-Arg-OH, H3K9me3, Histone H3 (3-17) (Lys9me3), Lys(Me3)9-Histone H3 (3-17), TKQTAR-K(Me3)-STGGKAPR

     A peptide fragment of histone H3

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