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Home >> Signaling Pathways >> Chromatin/Epigenetics

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.

Targets for  Chromatin/Epigenetics

Products for  Chromatin/Epigenetics

  1. Cat.No. Product Name Information
  2. GC10382 CPI-637 CBP/EP300 bromodomain inhibitor CPI-637 Chemical Structure
  3. GC39365 CPTH2 CPTH2 is a potent histone acetyltransferase (HAT) inhibitor. CPTH2 selectively inhibits the acetylation of histone H3 by Gcn5. CPTH2 induces apoptosis and decreases the invasiveness of a clear cell renal carcinoma (ccRCC) cell line through the inhibition of acetyltransferase p300 (KAT3B). CPTH2 Chemical Structure
  4. GC14428 CPTH2 (hydrochloride) inhibitor of HAT activity of Gcn5 CPTH2 (hydrochloride) Chemical Structure
  5. GC43321 CPTH6 (hydrobromide) CPTH6 is a thiazole derivative that inhibits the lysine acetyltransferase activity of Gcn5 and pCAF but not p300 or CBP. CPTH6 (hydrobromide) Chemical Structure
  6. GC35742 CPUY074020 CPUY074020 is a potent and oral bioavailable inhibitor of histone methyltransferase G9a, with an IC50 of 2.18 μM. CPUY074020 possesses anti-proliferative activity. CPUY074020 Chemical Structure
  7. GC32565 CRA-026440 CRA-026440 is a potent, broad-spectrum HDAC inhibitor. CRA-026440 Chemical Structure
  8. GC67674 CRA-026440 hydrochloride CRA-026440 hydrochloride Chemical Structure
  9. GC68900 CrBKA

    CrBKA is a weakly active fluorescent small molecule substrate of SIRT6.

     CrBKA Chemical Structure
  10. GC70432 Crebinostat Crebinostat is a potent histone deacetylase (HDAC) inhibitor with IC50 values of 0.7 nM, 1.0 nM, 2.0 nM and 9.3 nM for HDAC1, HDAC2, HDAC3 and HDAC6, respectively. Crebinostat Chemical Structure
  11. GC38412 Crotonoside

    2-Hydroxyadenosine, Isoguanine riboside, Isoguanosine, NSC 12161

     Crotonoside is a FLT3 and HDAC3/6 inhibitor that can be used to study acute myeloid leukemia (AML). Crotonoside Chemical Structure
  12. GC19891 CTB

    Cholera Toxin B subunit

    A potent p300 histone acetyltransferase activator

     CTB Chemical Structure
  13. GC14524 CTPB selective activator of the histone acetyltransferase (HAT) p300 CTPB Chemical Structure
  14. GC16008 CUDC-101 A multi-target inhibitor of HDACs, EGFR, and HER2 CUDC-101 Chemical Structure
  15. GC12115 CUDC-907

    CUDC-907

     CUDC is an orally bioavailable small molecule PI3K and HDAC dual inhibitor that acts on PI3K α And HDAC1 / 2 / 3 / 10 with IC50 of 19 nm and 1.7 nm / 5 nm / 1.8 nm / 2.8 nm. CUDC-907 Chemical Structure
  16. GN10442 Curculigoside Curculigoside Chemical Structure
  17. GC14787 Curcumin

    Indian Saffron, Turmeric yellow

     A yellow pigment with diverse biological activities Curcumin Chemical Structure
  18. GC40226 Curcumin-d6 Curcumin-d6 is intended for use as an internal standard for the quantification of curcumin by GC- or LC-MS. Curcumin-d6 Chemical Structure
  19. GC13056 CX-6258

    CX6258;CX 6258

     A pan-Pim kinase inhibitor CX-6258 Chemical Structure
  20. GC19747 CX-6258 HCl

    Pim-Kinase Inhibitor X

     CX-6258 HCl is a potent and kinase selective pan-Pim kinases inhibitor, with IC50s of 5 nM, 25 nM and 16 nM for Pim-1, Pim-2 and Pim-3, respectively. CX-6258 HCl Chemical Structure
  21. GC35762 CX-6258 hydrochloride hydrate CX-6258 hydrochloride hydrate is a potent and kinase selective pan-Pim kinases inhibitor, with IC50s of 5 nM, 25 nM and 16 nM for Pim-1, Pim-2 and Pim-3, respectively. CX-6258 hydrochloride hydrate Chemical Structure
  22. GC15106 CYC116 A potent Aurora kinase inhibitor CYC116 Chemical Structure
  23. GC74310 Cyclo(CKLIIF) TFA Cyclo CKLIIF is a dual inhibitor for poxia inducible factor (HIF) 1 and 2, with affinity for HIF1-α and HIF2-α PAS-B domains KD of 2.6 and 2.2 μM, respectively. Cyclo(CKLIIF) TFA Chemical Structure
  24. GC43354 Cysmethynil

    Icmt Inhibitor

     Post-translational protein prenylation is a 3-step process that occurs at the C-terminus of a number of proteins involved in cell growth control and oncogenesis. Cysmethynil Chemical Structure
  25. GC17050 CYT387

    Momelotinib

     A potent inhibitor of JAK1 and JAK2 CYT387 Chemical Structure
  26. GC16468 CYT387 sulfate salt A potent inhibitor of JAK1 and JAK2 CYT387 sulfate salt Chemical Structure
  27. GC63780 D-Cl-amidine hydrochloride D-Cl-amidine hydrochloride is a potent and highly selective PAD1 inhibitor. D-Cl-amidine is well-torelated with no significant toxicity. D-Cl-amidine hydrochloride Chemical Structure
  28. GC48967 D-Homoserine lactone

    D-HSL

     An enantiomer of L-homoserine lactone D-Homoserine lactone Chemical Structure
  29. GC15830 Daminozide

    Alar, Aminozide, B 995, DIMG, DMASA, Kylar, SADH, Succinic Acid

     Selective inhibitor of KDM2/7 histone demethylases Daminozide Chemical Structure
  30. GC15217 Danusertib (PHA-739358)

    PHA-739358

     A pan-Aurora kinase and Abl inhibitor Danusertib (PHA-739358) Chemical Structure
  31. GC16647 Daprodustat(GSK1278863)

    GSK1278863

     Daprodustat(GSK1278863) (GSK1278863) is an orally active hypoxia-inducible factor prolyl hydroxylase (HIF-PH) inhibitor being developed for the treatment of anemia associated with chronic kidney disease. Daprodustat(GSK1278863) Chemical Structure
  32. GC68147 dAURK-4 hydrochloride dAURK-4 hydrochloride Chemical Structure
  33. GC68940 DB008

    DB008 is an effective selective inhibitor of PARP16 with an IC50 value of 0.27 μM and contains acrylamide electrophile. DB008 has membrane permeability and can selectively label PARP16.

     DB008 Chemical Structure
  34. GC19119 dBET1 dBET1 is a potent BRD4 protein degrader based on PROTAC technology with an EC50 of 430 nM. dBET1 Chemical Structure
  35. GC35815 dBET57 dBET57 is a potent and selective degrader of BRD4BD1 based on the PROTAC technology. dBET57 mediates recruitment to the CRL4Cereblon E3 ubiquitin ligase, with a DC50/5h of 500 nM for BRD4BD1, and is inactive on BRD4BD2. dBET57 Chemical Structure
  36. GC32719 dBET6

    dBET6 is a highly potent, selective and cell-permeable PROTAC connected by ligands for Cereblon and BET, with an IC50 of 14 nM, and has antitumor activity.

     dBET6 Chemical Structure
  37. GC74000 DBPR728 DBPR728 is an acyl prodrug of 6K465 that carries fewer drogen bond donors. DBPR728 Chemical Structure
  38. GC73356 dBRD4-BD1 dBRD4-BD1 is a selective and durable BRD4 degrader with an DC50 value of 280 nM (Dmax=77%). dBRD4-BD1 upregulates BRD2/3 protein level and shows low cytotoxicity than iBRD4-BD1. dBRD4-BD1 Chemical Structure
  39. GC33148 DC-05 DC-05 is a DNA methyltransferase 1 (DNMT1) inhibitor, with an IC50 and a Kd of 10.3 μM and 1.09 μM, respectively. DC-05 Chemical Structure
  40. GC73295 DC-BPi-03 DC-BPi-03 is a potent BPTF-BRD inhibitor with an IC50of 698.3 nM and a Kd of 2.81 μM. DC-BPi-03 Chemical Structure
  41. GC68948 DC-BPi-11 hydrochloride

    DC-BPi-11 hydrochloride is an inhibitor of the bromodomain and PHD finger-containing transcription factor (BPTF), with an IC50 of 698 nM. DC-BPi-11 hydrochloride has a significant inhibitory effect on the proliferation of leukemia cells.

     DC-BPi-11 hydrochloride Chemical Structure
  42. GC65186 DC-S239 DC-S239 is a selective histone methyltransferase SET7 inhibitor with an IC50 value of 4.59 μM. DC-S239 also displays selectivity for DNMT1, DOT1L, EZH2, NSD1, SETD8 and G9a. DC-S239 has anticancer activity. DC-S239 Chemical Structure
  43. GC62211 dCBP-1 dCBP-1 is a potent and selective heterobifunctional degrader of p300/CBP based on Cereblon ligand. dCBP-1 is exceptionally potent at killing multiple myeloma cells and ablates oncogenic enhancer activity driving MYC expression. dCBP-1 Chemical Structure
  44. GC63627 DCH36_06 DCH36_06 is a potent and selective p300/CBP inhibitor with IC50s of 0.6 μM and 3.2 μM for p300 and CBP, respectively. DCH36_06 mediated p300/CBP inhibition leading to hypoacetylation on H3K18 in leukemic cells. Anti-tumor activity. DCH36_06 Chemical Structure
  45. GC63662 DCLX069 DCLX069 is a selective protein arginine methyltransferase 1 (PRMT1) inhibitor with an IC50 value of 17.9 ?M. DCLX069 shows less active against PRMT4 and PRMT6. DCLX069 has anticancer effects. DCLX069 Chemical Structure
  46. GC73966 DCPT1061 DCPT1061 potently inhibits PRMT1, PRMT6 and PRMT8 in vitro with less inhibitory effect on PRMT3, PRMT4, and PRMT5 or other epigenetic enzymes. DCPT1061 Chemical Structure
  47. GC73967 DCPT1061 hydrochloride DCPT1061 drochloride has a strong inhibitory effect on PRMT1, PRMT6, and PRMT8 in vitro, The epigenetic enzymes such as PRMT3, PRMT4 and PRMT5 had little inhibitory effect. DCPT1061 hydrochloride Chemical Structure
  48. GC32872 DC_517 DC_517 is a DNA methyltransferase 1 (DNMT1) inhibitor, with an IC50 and a Kd of 1.7 μM and 0.91 μM, respectively. DC_517 Chemical Structure
  49. GC35816 DC_C66 DC_C66 is a cell-permeable, selective coactivator associated arginine methyltransferase 1 (CARM1) inhibitor with an IC50 of 1.8 μM. DC_C66 has a good selectivity for CARM1 against PRMT1 (IC50=21 μM), PRMT6 (IC50= 47μM), and PRMT5. DC_C66 Chemical Structure
  50. GC67863 DDO-2093 dihydrochloride DDO-2093 dihydrochloride Chemical Structure
  51. GC33013 DDP-38003 dihydrochloride DDP-38003 dihydrochloride is an novel, orally available inhibitor of histone lysine-specific demethylase 1A (KDM1A/LSD1) with an IC50 of 84 nM. DDP-38003 dihydrochloride Chemical Structure
  52. GC34296 DDP-38003 trihydrochloride DDP-38003 trihydrochloride is an novel, orally available inhibitor of histone lysine-specific demethylase 1A (KDM1A/LSD1) with an IC50 of 84 nM. DDP-38003 trihydrochloride Chemical Structure
  53. GC10770 Decernotinib(VX-509)

    Decernotinib, VRT-831509

     Decernotinib(VX-509) is a potent, orally active JAK3 inhibitor, with Kis of 2.5, 11, 13 and 11 nM for JAK3, JAK1, JAK2, and TYK2, respectively. Decernotinib(VX-509) Chemical Structure
  54. GC15255 Decitabine(NSC127716, 5AZA-CdR)

    DAC, 5aza2’Deoxycytidine, NSC 127716

     Decitabine(DAC) is a deoxycytidine analogue antimetabolite with oral bioactivity and functions as an inhibitor of DNA methyltransferase. Decitabine(NSC127716, 5AZA-CdR) Chemical Structure
  55. GC47180 Decitabine-15N4

    5-aza-2’-Deoxycytidine-15N4, DAC-15N4

     A neuropeptide with diverse biological activities Decitabine-15N4 Chemical Structure
  56. GC68955 Deferoxamine

    Deferoxamine (Deferoxamine B) is an iron chelator (binding Fe(III) and many other metal cations), widely used to reduce the accumulation and deposition of iron in tissues. 

     Deferoxamine Chemical Structure
  57. GN10040 Dehydrocorydaline Dehydrocorydaline is one of the quaternary ammonium alkaloids from Corydalis Rhizoma. Dehydrocorydaline Chemical Structure
  58. GC31660 Delgocitinib (JTE-052) Delgocitinib (JTE-052) (JTE-052) is a specific JAK inhibitor with IC50s of 2.8, 2.6, 13 and 58 nM for JAK1, JAK2, JAK3 and Tyk2, respectively. Delgocitinib (JTE-052) Chemical Structure
  59. GC43406 Delphinidin (chloride)

    Ephdine

    Delphinidin (chloride) is an anthocyanidin, a natural plant pigment which serves as the precursor of certain anthocyanins that provide the blue-red colors of flowers, fruits, and red wine.

     Delphinidin (chloride) Chemical Structure
  60. GC31230 Dencichin (Dencichine) Dencichin is a non-protein amino acid originally extracted from Panax notoginseng, and can inhibit HIF-prolyl hydroxylase-2 (PHD-2) activity. Dencichin (Dencichine) Chemical Structure
  61. GC38767 Deoxyshikonin A natural products with anti-tumor activity Deoxyshikonin Chemical Structure
  62. GC32449 Desidustat

    P 1560, β-Zearalanol, β-Zearanol

     An inhibitor of HIF-PH Desidustat Chemical Structure
  63. GC71575 Deuruxolitinib Deuruxolitinib, a deuterated Ruxolitinib , modulates the activity of JAK1/JAK2. Deuruxolitinib Chemical Structure
  64. GC34187 Dihydrocoumarin (Hydrocoumarin)

    DHC

     Dihydrocoumarin (Hydrocoumarin) is a compound found in Melilotus officinalis. Dihydrocoumarin (Hydrocoumarin) is a yeast Sir2p inhibitor. Dihydrocoumarin (Hydrocoumarin) also inhibits human SIRT1 and SIRT2 with IC50s of 208 μM and 295 μM, respectively. Dihydrocoumarin (Hydrocoumarin) Chemical Structure
  65. GC68988 DKFZ-748

    DKFZ-748 is a selective HDAC10 inhibitor (pIC50=7.66) with anti-tumor activity.

     DKFZ-748 Chemical Structure
  66. GC14024 DL-AP3 A metabotropic glutamate receptor antagonist DL-AP3 Chemical Structure
  67. GC52368 DL-Sulforaphane Glutathione

    SFN-glutathione, SFN-GSH, Sulforaphane-GSH

     A metabolite of sulforaphane DL-Sulforaphane Glutathione Chemical Structure
  68. GC68994 DN02

    DN02 is an effective selective BRD8 bromodomain probe. DN02 has high affinity for BRD8 (1) (Ki=32 nM), with 30 times higher affinity than for BRD8 (2) (Ki＞1000 nM).

     DN02 Chemical Structure
  69. GC65546 DNMT3A-IN-1 DNMT3A-IN-1 is a potent and selective DNMT3A inhibitor. DNMT3A-IN-1 Chemical Structure
  70. GC35893 Domatinostat Domatinostat (4SC-202 free base) is a selective class I HDAC inhibitor with IC50 of 1.20 μM, 1.12 μM, and 0.57 μM for HDAC1, HDAC2, and HDAC3, respectively. It also displays inhibitory activity against Lysine specific demethylase 1 (LSD1). Domatinostat Chemical Structure
  71. GC14490 Donepezil HCl Donepezil HCl (E2020) is a reversible, selective AChE inhibitor with an IC50 of 6.7 nM for AChE activity. Donepezil HCl Chemical Structure
  72. GC33208 Dot1L-IN-1 Dot1L-IN-1 is a highly potent, selective and structurally novel Dot1L inhibitor with a Ki of 2 pM. Dot1L-IN-1 Chemical Structure
  73. GC69002 Dot1L-IN-1 TFA

    Dot1L-IN-1 TFA is a highly efficient and selective Dot1L inhibitor with a Ki of 2 pM and IC50<0.1 nM. Dot1L-IN-1 TFA effectively inhibits H3K79 dimethylation in HeLa cells (IC50=3 nM) as well as the activity of the HoxA9 promoter in Molm-13 cells (IC50=17 nM).

     Dot1L-IN-1 TFA Chemical Structure
  74. GC30530 Dot1L-IN-2 Dot1L-IN-2 is a potent, selective and orally bioavailable inhibitor of Dot1L (a histone methyltransferase), with an IC50 and Ki of 0.4 nM and 0.08 nM, respectively. Dot1L-IN-2 Chemical Structure
  75. GC62613 Dot1L-IN-4

    DOT1-like Inhibitor 4

     Dot1L-IN-4 is a potent disruptor of telomeric silencing 1-like protein (DOT1L) inhibitor with an IC50 SPA DOT1L of 0.11 nM. Dot1L-IN-4 Chemical Structure
  76. GC65962 Dot1L-IN-5 Dot1L-IN-5 is a potent disruptor of telomeric silencing 1-like protein (DOT1L) inhibitor with an IC50 SPA DOT1L of 0.17 nM. Dot1L-IN-5 Chemical Structure
  77. GC12680 DR 2313 A PARP inhibitor DR 2313 Chemical Structure
  78. GC13706 Droxinostat

    NS 41080

     An inhibitor of HDAC3, HDAC6, and HDAC8 Droxinostat Chemical Structure
  79. GC45927 DS-437 A dual inhibitor of PRMT5 and PRMT7 DS-437 Chemical Structure
  80. GC73397 DS-9300 DS-9300 is a potent, orally active, selective EP300/CBP HAT inhibitor with an IC50 value of 28 nM. DS-9300 Chemical Structure
  81. GC35904 dTRIM24 dTRIM24 is a selective bifunctional degrader of TRIM24 based on PROTAC, consists of ligands for von Hippel-Lindau and TRIM24. dTRIM24 Chemical Structure
  82. GC35914 DW14800 DW14800 is a protein arginine methyltransferase 5 (PRMT5) inhibitor, with an IC50 of 17 nM. DW14800 reduces H4R3me2s levels and enhances the transcription of HNF4α, but does not alter PRMT5 expression. Anti-cancer activity. DW14800 Chemical Structure
  83. GC71490 DW71177 DW71177 is a novel [1,2,4]triazolo[4,3-a] quinoxaline-based potent and BD1-Selective BET inhibitor, and can be used for study of acute myeloid leukemia. DW71177 Chemical Structure
  84. GC69030 DY-46-2

    DY-46-2 is a new and highly efficient, selective inhibitor of DNA methyltransferase 3A (DNMT3A) that has an IC50 value of 1.3 μM.

     DY-46-2 Chemical Structure
  85. GC73945 DYB-03 DYB-03 is an oral active HIF-1α/EZH2 inhibitor. DYB-03 Chemical Structure
  86. GC33403 E-7386 E-7386 is an orally active CBP/beta-catenin modulator. E-7386 Chemical Structure
  87. GC69033 E1231

    1-{4-[2-(5-Methylfuran-2-yl)quinoline-4-carbonyl]piperazin-1-yl}ethan-1-one

    E1231 is an orally effective activator of Sirtuin 1 (SIRT1) with an EC50 of 0.83 μM, which can regulate cholesterol and lipid metabolism. E1231 interacts with both SIRT1 and liver X receptor-α (LXRα) and increases the expression of ATP-binding cassette transporter A1 (ABCA1). E1231 also reduces the formation of atherosclerotic plaques in ApoE-/- mouse models. E1231 can be used for research on diseases related to cholesterol and lipid disorders.

     E1231 Chemical Structure
  88. GC64209 E7016

    GPI 21016

     E7016 (GPI 21016) is an orally available PARP inhibitor. E7016 can enhance tumor cell radiosensitivity in vitro and in vivo through the inhibition of DNA repair. E7016 acts as a potential anticancer agent. E7016 Chemical Structure
  89. GC18172 E7449

    E7449; 2X-121

     E7449 is an inhibitor of poly(ADP-ribose) polymerase 1 (PARP1) and PARP2 (IC50s = 1 and 1.2 nM, respectively) as well as tankyrase (TNKS) 1/2 (IC50s = 50-100 nM). E7449 Chemical Structure
  90. GC12991 EB 47 A PARP1 and TNKS2 inhibitor EB 47 Chemical Structure
  91. GC33220 EBI-2511 EBI-2511 is a highly potent and orally active EZH2 inhibitor, with an IC50 of 6 nM in Pfeffiera cell lines, respectively. EBI-2511 Chemical Structure
  92. GC18236 Echinomycin

    Antibiotic A 654I； NSC 13502； NSC 526417； Quinomycin A； SK 302B

     An inhibitor of HIF1mediated gene transcription Echinomycin Chemical Structure
  93. GC19129 EDO-S101

    Tinostamustine

     EDO-S101 is a pan HDAC inhibitor; inhibits HDAC1, HDAC2 and HDAC3 with IC50 values of 9, 9 and 25 nM, respectively. EDO-S101 Chemical Structure
  94. GC19130 EED226 EED226 is a potent, selective, and orally bioavailable embryonic ectoderm development (EED) inhibitor with an IC50 of 22 nM. EED226 Chemical Structure
  95. GC67934 EEDi-5285 EEDi-5285 Chemical Structure
  96. GC73753 EGFR/AURKB-IN-1 EGFR/AURKB-IN-1 (compound 7) is a dual-targeted EGFR/AURKB inhibitor, and inhibits the phpsphorylations of L858R EGFR and AURKB with IC50s of 0.07 and 1.1, respectively. EGFR/AURKB-IN-1 Chemical Structure
  97. GC34567 EHMT2-IN-1 EHMT2-IN-1 is a potent EHMT inhibitor, with IC50s of all <100 nM for EHMT1 peptide, EHMT2 peptide and cellular EHMT2. Used in the research of blood disorder or cancer. EHMT2-IN-1 Chemical Structure
  98. GC34568 EHMT2-IN-2 EHMT2-IN-2 is a potent EHMT inhibitor, with IC50s of all <100 nM for EHMT1 peptide, EHMT2 peptide and cellular EHMT2. Used in the research of blood disease or cancer. EHMT2-IN-2 Chemical Structure
  99. GC14756 EI1 EZH2 inhibitor EI1 Chemical Structure
  100. GC33043 EL-102 EL-102 is a hypoxia-induced factor 1 (Hif1α) inhibitor. EL-102 induces apoptosis, inhibits tubulin polymerisation and shows activities against prostate cancer. EL-102 can be used for the research of cancer. EL-102 Chemical Structure
  101. GC64191 Elevenostat

    JB3-22

     Elevenostat (JB3-22) is a selective HDAC11 inhibitor (IC50=0.235??M). Anti-multiple myeloma (MM) activity. Elevenostat Chemical Structure

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