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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. GC40468 1,5-Isoquinolinediol

    1,5-二羟基异喹啉,NSC 65585

     An inhibitor of poly(ADP-ribose) polymerases
  3. GC19542 GeA-69 GeA-69 是一种多聚腺苷二磷酸核糖聚合酶 14 (PARP14) 的选择性变构抑制剂，靶向大结构域 2 (MD2)，Kd 值为 2.1 µM。 GeA-69 参与 DNA 损伤修复机制并阻止 PARP14 MD2 募集到激光诱导的 DNA 损伤部位。
  4. GC10456 Fucosterol

    岩皂甾醇,24-ethylidene Cholesterol

     A natural phytosterol with diverse biological activities
  5. GC34849 UBCS039 UBCS039 is the first synthetic SIRT6 activator with EC50 of 38 μM,induces a time-dependent activation of autophagy in several human tumor cell lines.
  6. GC34785 Sirt2-IN-1 Sirt2-IN-1(Compound9)是一种sirtuin2(Sirt2)抑制剂，IC50为163nM。
  7. GC34784 Sinefungin

    西奈芬净,Adenosyl-Ornithine; A-9145; Antibiotic 32232RP

    Sinefungin是病毒mRNA(鸟嘌呤-7-)-甲基转移酶、mRNA(核苷-2'-)-甲基转移酶和病毒增殖的有效抑制剂。Sinefungin是一种SET7/9抑制剂，通过抑制H3K4甲基化来改善肾纤维化。
  8. GC34778 SGC-iMLLT An inhibitor of MLLT1 and MLLT3 YEATS domains
  9. GC34742 Protosappanin A

    原苏木素A; PTA

    ProtosappaninA(PTA)，是一种免疫制剂，是从CaesalpiniasappanL中分离得到的一种主要联苯化合物，通过下调JAK2和STAT3的磷酸化，抑制JAK2/STAT3依赖的炎症通路。
  10. GC34692 NU6140 A Cdk2 inhibitor
  11. GC34675 Molibresib besylate

    GSK 525762C; I-BET 762 besylate

     Molibresibbesylate(GSK525762C;I-BET762besylate)是BET溴结构域抑制剂，IC50为32.5-42.5nM。
  12. GC34629 J22352 J22352是一种具有类似靶向嵌合体蛋白水解(PROTAC)特性、高度选择性HDAC6抑制剂，其IC50值为4.7nM，J22352通过抑制胶质母细胞瘤自噬、诱发抗肿瘤免疫反应来促进HDAC6降解和诱导抗癌效果，并通过降低PD-L1的免疫抑制活性，使宿主抗肿瘤活性恢复。
  13. GC34604 GSK467 GSK467 is a cell penetrant and selective inhibitor of KDM5B (JARID1B/PLU1) with Ki of 10 nM. GSK467 shows apparent 180-fold selectivity for KDM4C and no measurable inhibitory effects toward KDM6 or other JmJ family members.
  14. GC34595 GN44028 GN44028 是一种有效且具有口服活性的缺氧诱导因子 (HIF)-1α 抑制剂，IC50 为 14 nM。 GN44028 抑制缺氧诱导的 HIF-1α 转录活性，而不抑制 HIF-1α mRNA 表达、HIF-1α 蛋白积累或 HIF-1α/HIF-1β 异二聚化。 GN44028可用于癌症研究。
  15. GC34568 EHMT2-IN-2 EHMT2-IN-2是一种有效的EHMT抑制剂，对对EHMT1多肽,EHMT2多肽和细胞内EHMT2的IC50值均小于100nM。可用于血液疾病或癌症的研究。
  16. GC34567 EHMT2-IN-1 EHMT2-IN-1是一种有效的EHMT抑制剂，对EHMT1多肽,EHMT2多肽和细胞内EHMT2的IC50均小于100nM。用于血液疾病或癌症的研究。
  17. GC34517 CBP-IN-1

    CCS1477

     A p300 and CBP inhibitor
  18. GC34505 BRD7-IN-1 BRD7-IN-1是一种修饰的BI7273衍生物(BRD7/9抑制剂)，通过与VHL配体连接形成PROTACVZ185(VZ185抑制BRD7/9的DC50分别是4.5nM、1.8nM)。
  19. GC34498 Bobcat339 hydrochloride A cytosine derivative
  20. GC34458 ACY-1083

    ACY-1083是一种可渗透脑的选择性HDAC6抑制剂，IC50为3nM，ACY-1083对HDAC6的选择性比其他类别的HDAC亚型高260倍。ACY-1083可有效逆转化疗引起的周围神经病变。
  21. 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。
  22. 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。
  23. GC19505 RK-287107 A TNKS1/2 inhibitor
  24. GC40255 Citrulline-specific Probe-biotin An affinity probe for citrullinated proteins
  25. GC40251 TCEP-biotin

    Tris(2-carboxyethyl)phosphine-biotin

     An affinity probe for protein lysine crotonylation
  26. GC40226 Curcumin-d6

    (1E,4Z,6E)-5-羟基-1,7-二[4-羟基-3-(甲氧基-D3)苯基]-1,4,6-庚三烯-3-酮,Diferuloylmethane-d6; Natural Yellow 3-d6; Turmeric yellow-d6

     An internal standard for the quantification of curcumin
  27. GC40117 Histone H2B (21-35) (human, mouse, rat, bovine) (trifluoroacetate salt)

    AQKKDGKKRKRSRKE, AspH2B21-35, H2B21-35

     A peptide fragment of histone H2B
  28. GC40115 Histone H3K79Ac (73-83) (human, mouse, rat, porcine, bovine) (trifluoroacetate salt)

    EIAQDF-K(Ac)-TDLR, H-Glu-Ile-Ala-Gln-Asp-Phe-Lys(Ac)-Thr-Asp-Leu-Arg-OH, Histone H3 (73-83) (Lys79ac), H3K79Ac, Lys(Ac)79-Histone H3 (73-83)

     A peptide fragment of histone H3
  29. GC40114 Histone H3K4Me3 (1-10) (human, mouse, rat, porcine, bovine) (trifluoroacetate salt) Histone H3K4Me3 (1-10) is an N-terminal peptide fragment of histone H3 that corresponds to amino acid residues 2-11 of the human histone H3 sequence.
  30. GC40113 Histone H3K9Ac (1-24) (human, mouse, rat, porcine, bovine) (trifluoroacetate salt)

    ARTKQTAR-K(Ac)-STGGKAPRKQLATKA, H-Ala-Arg-Thr-Lys-Gln-Thr-Ala-Arg-Lys(Ac)-Ser-Thr-Gly-Gly-Lys-Ala-Pro-Arg-Lys-Gln-Leu-Ala-Thr-Lys-Ala-OH, Histone H3 (1-24) (Lys9ac), Lys(Ac)9-Histone H3 (1-24)

     A peptide fragment of histone H3
  31. GC40111 Histone H3 (21-44) (human, mouse, rat, bovine) (trifluoroacetate salt)

    ATKAARKSAPATGGVKKPHRYRPG

     A peptide fragment of histone H3
  32. GC40098 BB-Cl-Yne A clickable PAD inhibitor
  33. GC40094 all-trans Retinoic Acid-d5

    atRA-d5, RA-d5, Vitamin A Acid-d5

     An internal standard for the quantification of all-trans retinoic acid
  34. GC34437 IACS-9571 Hydrochloride (ASIS-P040 Hydrochloride) IACS-9571Hydrochloride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. GC34431 MC3482 MC3482是一种特异性sirtuin5(SIRT5)抑制剂。
  36. GC34424 CARM1-IN-1 hydrochloride CARM1-IN-1盐酸盐是CARM1高效选择性抑制剂，IC50值为8.6uM，对PRMT1和SET7抑制活性很抵。
  37. GC34377 L-45 dihydrochloride (L-Moses dihydrochloride) L-45dihydrochloride是第一个有效的选择性p300/CBP相关因子(PCAF)溴结构域(Brd)抑制剂，Kd为126±15nM。
  38. GC34325 PROTAC BET degrader-3 PROTACBETDegrader-3是基于PROTAC技术的BET降解剂。
  39. GC34319 TD-428 TD-428是一种高度特异的BRD4降解剂，DC50为0.32nM。
  40. GC34314 GSK 690 Hydrochloride GSK690(Hydrochloride)是赖氨酸特异性去甲基化酶1(LSD1)的可逆抑制剂，Kd值为9nM，IC50值为37nM。
  41. GC34296 DDP-38003 trihydrochloride DDP-38003trihydrochloride是新颖，有口服活性的KDM1A/LSD1抑制剂，IC50值为84nM。
  42. GC34195 K-756 K-756是一种直接的选择性tankyrase(TNKS)抑制剂，抑制TNKS1和TNKS2的ADP-核糖基化活性，IC50分别为31和36nM。
  43. GC34187 Dihydrocoumarin (Hydrocoumarin)

    二氢香豆素; Hydrocoumarin; Chroman-2-one

     A coumarin with enzyme inhibitory activity
  44. GC34165 Corin Corin是组氨酸赖氨酸特异性去甲基化酶(LSD1)和组氨酸脱乙酰化酶(HDAC)的双重抑制剂，其对LSD1的Ki(inact)值为110nM，对HDAC1的IC50值为147nM。
  45. GC34160 UNC0379 trifluoroacetate (UNC-0379 trifluoroacetate) A selective SET8 inhibitor
  46. GC34159 Ilorasertib (ABT-348)

    ABT-348

     A multi-kinase inhibitor
  47. GC34138 M-110 M-110是Pim激酶抑制剂，抑制前列腺癌细胞系增殖IC50为0.6-0.9uM。
  48. GC34136 EPZ011989 trifluoroacetate (EPZ-011989 trifluoroacetate)

    EPZ-011989 trifluoroacetate

     An orally bioavailable EZH2 inhibitor
  49. GC34120 Niraparib R-enantiomer (MK 4827 (R-enantiomer))

    MK 4827 (R-enantiomer)

     Niraparib R-enantiomer (MK-4827 R-enantiomer) 是一种出色的 PARP1 抑制剂，IC50 为 2.4 nM。
  50. GC34108 CARM1-IN-1

    Protein Arginine Methyltransferase 4/CoactivatorAssociated Arginine Methyltransferase 1 Inhibitor

     A selective inhibitor of PRMT4/CARM1
  51. GC34078 I-CBP112 A p300 and CBP inhibitor

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