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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. 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
  3. GC62613 Dot1L-IN-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
  4. 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
  5. GC12680 DR 2313 A PARP inhibitor DR 2313  Chemical Structure
  6. GC13706 Droxinostat An inhibitor of HDAC3, HDAC6, and HDAC8 Droxinostat  Chemical Structure
  7. GC45927 DS-437 A dual inhibitor of PRMT5 and PRMT7 DS-437  Chemical Structure
  8. 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
  9. 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
  10. GC33403 E-7386 E-7386 is an orally active CBP/beta-catenin modulator. E-7386  Chemical Structure
  11. GC64209 E7016 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
  12. GC18172 E7449 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
  13. GC12991 EB 47 A PARP1 and TNKS2 inhibitor EB 47  Chemical Structure
  14. 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
  15. GC18236 Echinomycin An inhibitor of HIF1mediated gene transcription Echinomycin  Chemical Structure
  16. GC19129 EDO-S101 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
  17. GC19130 EED226 EED226 is a potent, selective, and orally bioavailable embryonic ectoderm development (EED) inhibitor with an IC50 of 22 nM. EED226  Chemical Structure
  18. GC67934 EEDi-5285 EEDi-5285  Chemical Structure
  19. 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
  20. 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
  21. GC14756 EI1 EZH2 inhibitor EI1  Chemical Structure
  22. 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
  23. GC64191 Elevenostat Elevenostat (JB3-22) is a selective HDAC11 inhibitor (IC50=0.235??M). Anti-multiple myeloma (MM) activity. Elevenostat  Chemical Structure
  24. GC31245 EML 425 An inhibitor of p300 and CBP EML 425  Chemical Structure
  25. GC49124 EN219 EN219 is a moderately selective synthetic covalent ligand against an N-terminal cysteine (C8) of RNF114 with an IC50 of 470 nM. EN219 inhibits RNF114-mediated autoubiquitination and p21 ubiquitination. EN219  Chemical Structure
  26. GC33634 Enarodustat (JTZ-951) Enarodustat (JTZ-951) is a potent and orally active hypoxia-inducible factor prolyl hydroxylase inhibitor, with an EC50 of 0.22 μM. Enarodustat (JTZ-951)  Chemical Structure
  27. GC33170 ENMD-119 (ENMD 1198) ENMD-119 (ENMD 1198) (IRC-110160), an orally active microtubule destabilizing agent, is a 2-methoxyestradiol analogue with antiproliferative and antiangiogenic activity. ENMD-119 (ENMD 1198) is suitable for inhibiting HIF-1alpha and STAT3 in human HCC cells and leads to reduced tumor growth and vascularization. ENMD-119 (ENMD 1198)  Chemical Structure
  28. GC16519 ENMD-2076 A multi-kinase inhibitor ENMD-2076  Chemical Structure
  29. GC12145 ENMD-2076 L-(+)-Tartaric acid ENMD-2076 L-(+)-Tartaric acid  Chemical Structure
  30. GC50182 ent-LP 99 ent-LP 99 is a potent and selective BRD7 and BRD9 inhibitor with an KD of 99 nM for BRD9. ent-LP 99  Chemical Structure
  31. GC17334 Entacapone A reversible COMT inhibitor Entacapone  Chemical Structure
  32. GC47294 Entacapone-d10 An internal standard for the quantification of entacapone Entacapone-d10  Chemical Structure
  33. GC11625 Entinostat (MS-275,SNDX-275) A histone deacetylase inhibitor Entinostat (MS-275,SNDX-275)  Chemical Structure
  34. GC14062 EPZ-6438

    A EZH2 inhibitor,potent and selective

    EPZ-6438  Chemical Structure
  35. GC64343 EPZ-719 EPZ-719 is a novel and potent SETD2 inhibitor ( IC50 = 0.005 μM) with a high selectivity over other histone methyltransferases. EPZ-719  Chemical Structure
  36. GC13383 EPZ004777 A potent inhibitor of DOT1L EPZ004777  Chemical Structure
  37. GC48980 EPZ004777 (formate) A potent inhibitor of DOT1L EPZ004777 (formate)  Chemical Structure
  38. GC15259 EPZ004777 HCl EPZ004777 HCl is a potent, selective DOT1L inhibitor with an IC50 of 0.4 nM. EPZ004777 HCl  Chemical Structure
  39. GC13878 EPZ005687 A potent, selective inhibitor of EZH2 EPZ005687  Chemical Structure
  40. GC19141 EPZ011989 EPZ011989 is a potent, selective orally bioavailable EZH2 inhibitor with Ki 3000-fold selectivity over other HMTase. EPZ011989  Chemical Structure
  41. GC34136 EPZ011989 trifluoroacetate (EPZ-011989 trifluoroacetate) EPZ-011989 trifluoroacetate is a potent and orally active Zeste Homolog 2 (EZH2) inhibitor with metabolic stability. EPZ-011989 trifluoroacetate has inhibitory inhibition for EZH2 with a Ki value of <3 nM. EPZ-011989 trifluoroacetate shows robust methyl mark inhibition and anti-tumor activity. EPZ-011989 trifluoroacetate can be used for the research of various cancers. EPZ011989 trifluoroacetate (EPZ-011989 trifluoroacetate)  Chemical Structure
  42. GC15302 EPZ015666 PRMT5 inhibitor EPZ015666  Chemical Structure
  43. GC15102 EPZ020411 PRMT6 inhibitor EPZ020411  Chemical Structure
  44. GC36000 EPZ020411 hydrochloride EPZ020411 hydrochloride is a selective inhibitor of PRMT6 with an IC50 of 10 nM, it has >10 folds selectivity for PRMT6 over PRMT1 and PRMT8. EPZ020411 hydrochloride can be used for the research of cancer. EPZ020411 hydrochloride  Chemical Structure
  45. GC16224 EPZ031686 A SMYD3 inhibitor EPZ031686  Chemical Structure
  46. GC12932 EPZ5676 A highly potent DOT1L inhibitor EPZ5676  Chemical Structure
  47. GC64575 Et-29 Et-29 is a potent and selective SIRT5 inhibitor (Ki=40 nM). Et-29  Chemical Structure
  48. GC61669 Ethyl 3,4-dihydroxybenzoate Ethyl 3,4-dihydroxybenzoate (Ethyl protocatechuate), an antioxidant, is a prolyl-hydroxylase inhibitor found in the testa of peanut seeds. Ethyl 3,4-dihydroxybenzoate  Chemical Structure
  49. GC10635 EX 527 (SEN0014196) A SIRT1 inhibitor EX 527 (SEN0014196)  Chemical Structure
  50. GC17126 EX-527 R-enantiomer EX-527 R-enantiomer ((R)-EX-527) is a R-enantiomer of Selisistat. Selisistat (EX-527) is a potent and selective SIRT1 inhibitor with IC50 of 98 nM. EX-527 R-enantiomer  Chemical Structure
  51. GC13417 EX-527 S-enantiomer EX-527 S-enantiomer ((S)-EX-527) is a potent and selective SIRT1 inhibitor, with an IC50 of 98 nM. EX-527 S-enantiomer  Chemical Structure
  52. GC65980 EZH2-IN-13 EZH2-IN-13 is a potent EZH2 inhibitor, for details please refer to compound 73 in patent WO2017139404. EZH2-IN-13 can be used to study cancers or precancerous lesions associated with EZH2 activity. EZH2-IN-13  Chemical Structure
  53. GC19149 EZM 2302 EZM 2302 is an inhibitor of coactivator-associated arginine methyltransferase 1 (CARM1) with an IC50 of 6 nM. EZM 2302  Chemical Structure
  54. GC64900 EZM0414 EZM0414 is a potent, selective, orally bioavailable inhibitor of SETD2 (IC50=18 nM in SETD2 biochemical assay; IC50=34 nM in cellular assay). EZM0414 can be used for the research of relapsed or refractory multiple myeloma and diffuse large B-cell lymphoma. EZM0414  Chemical Structure
  55. GC43651 F-Amidine (trifluoroacetate salt) F-amidine is an inhibitor of protein arginine deiminases (PADs) that is selective for PAD1 and PAD4 (IC50s = 29.5, 350, and 21.6 μM for PAD1, PAD3, and PAD4 in vitro, respectively). F-Amidine (trifluoroacetate salt)  Chemical Structure
  56. GC13139 FG-4592 (ASP1517) An inhibitor of HIF-PH enzymes FG-4592 (ASP1517)  Chemical Structure
  57. GC16638 FG2216 HIF-prolyl hydroxylase inhibitor FG2216  Chemical Structure
  58. GC64821 FHD-286 FHD-286 is a BRG1/BRM ATPase inhibitor for the treatment of BAF-related disorders such as acute myeloid leukemia. FHD-286  Chemical Structure
  59. GC65160 FHT-1015 FHT-1205 is a potent SMARCA4/SMARCA2 ATPase (BRG1 and BRM) inhibitor with IC50s of ≤10 nM (WO2020160180A1; compound 67). FHT-1015  Chemical Structure
  60. GC64777 FHT-1204 FHT-1204 is a potent SMARCA4/SMARCA2 ATPase (BRG1 and BRM) inhibitor with IC50s of ≤10 nM (WO2020160180A1; compound 70). FHT-1204  Chemical Structure
  61. GC46148 Filgotinib-d4 An internal standard for the quantification of filgotinib Filgotinib-d4  Chemical Structure
  62. GN10030 Fisetin Fisetin  Chemical Structure
  63. GC33015 FL-411 (BRD4-IN-1) FL-411 (BRD4-IN-1) is a potent and selective BRD4 inhibitor with an IC50 of 0.43±0.09 μM for BRD4(1). FL-411 (BRD4-IN-1)  Chemical Structure
  64. GC16875 FLLL32 STAT3 inhibitor FLLL32  Chemical Structure
  65. GC50506 Fluorescein-NAD+ Fluorescent NAD+; substrate for ADP-ribosylation for use in PARP assays Fluorescein-NAD+  Chemical Structure
  66. GC62121 Fluzoparib Fluzoparib (SHR3162) is a potent and orally active PARP1 inhibitor (IC50=1.46±0.72 nM, a cell‐free enzymatic assay) with superior antitumor activity. Fluzoparib selectively inhibits the proliferation of homologous recombination repair (HR)‐deficient cells, and sensitizes both HR‐deficient and HR‐proficient cells to cytotoxic agents. Fluzoparib exhibits good pharmacokinetic properties in vivo and can be used for BRCA1/2-mutant relapsed ovarian cancer research. Fluzoparib  Chemical Structure
  67. GC50537 FM19G11 A HIF α-subunit inhibitor FM19G11  Chemical Structure
  68. GC19408 FM381

    FM-381 is a highly potent and JAK3-selective janus kinase (JAK) inhibitor

    FM381  Chemical Structure
  69. GC62461 FNDR-20123 FNDR-20123 is a safe, first-in-class, and orally active anti-malarial HDAC inhibitor with IC50s of 31 nM and 3 nM for Plasmodium and human HDAC, respectively. FNDR-20123  Chemical Structure
  70. GC14395 Fostriecin sodium salt A potent inhibitor of protein phosphatases 2A and 4 Fostriecin sodium salt  Chemical Structure
  71. GC38044 Fraxinellone Fraxinellone  Chemical Structure
  72. GC65206 FT895 FT895 is a potent and selective HDAC11 inhibitor with an IC50 of 3 nM. FT895  Chemical Structure
  73. GC63545 FTX-6058 FTX-6058 ((S)-FTX-6058) is a potent and orally active inhibitor of Embryonic Ectoderm Development (EED). FTX-6058  Chemical Structure
  74. GC63546 FTX-6058 hydrochloride (S)-Pociredir ((S)-FTX-6058) hydrochloride is a potent and orally active inhibitor of Embryonic Ectoderm Development (EED). FTX-6058 hydrochloride  Chemical Structure
  75. GC10456 Fucosterol

    Fucosterol is a plant sterol found in algae

    Fucosterol  Chemical Structure
  76. GC43715 Furamidine (hydrochloride) Furamidine (hydrochloride) (DB75 dihydrochloride) is a selective protein arginine methyltransferase 1 (PRMT1) inhibitor with an IC50 of 9.4 μM. Furamidine (hydrochloride)  Chemical Structure
  77. GC13541 G007-LK tankyrase 1/2 inhibitor G007-LK  Chemical Structure
  78. GC62246 G5-7 G5-7, an orally active and allosteric JAK2 inhibitor, selectively inhibits JAK2 mediated phosphorylation and activation of EGFR (Tyr1068) and STAT3 by binding to JAK2. G5-7 induces cell cycle arrest, apoptosis and possesses antiangiogenic effect. G5-7 has the potential for glioma study. G5-7  Chemical Structure
  79. GC38062 Gambogenic acid Gambogenic acid is an active ingredient in gamboge, with anticancer activity. Gambogenic acid acts as an effective inhibitor of EZH2, specifically and covalently binds to Cys668 within the EZH2-SET domain, and induces EZH2 ubiquitination. Gambogenic acid  Chemical Structure
  80. GC40900 Ganoderic Acid D Ganoderic acid D is an oxygenated triterpenoid that has been found in G. Ganoderic Acid D  Chemical Structure
  81. GC13474 Garcinol

    Inhibitor of PCAF and p300 histone acetyltransferase (HAT) activity

    Garcinol  Chemical Structure
  82. GC60172 Gardenia yellow Gardenia yellow is an active member of crocin, increases mRNA expression of SIRT3, and acts as an orally active antidepressant agent. Gardenia yellow  Chemical Structure
  83. GC32958 GDC-0339 GDC-0339 is a potent, orally bioavailable and well tolerated pan-Pim kinase inhibitor, with Kis of 0.03 nM, 0.1 nM and 0.02 nM for Pim1, Pim2 and Pim3, respectively. GDC-0339 is discovered as a potential treatment of multiple myeloma. GDC-0339  Chemical Structure
  84. GC68378 GDC-4379 GDC-4379  Chemical Structure
  85. GC19542 GeA-69

    GeA-69 is a selective, highly cell permeable allosteric inhibitor

    GeA-69   Chemical Structure
  86. GN10473 Ginkgolide C Ginkgolide C  Chemical Structure
  87. GN10584 Ginsenoside Rk1 Ginsenoside Rk1  Chemical Structure
  88. GC48994 Girard’s Reagent P-d5 An internal standard for the quantification of Girard’s reagent P Girard’s Reagent P-d5  Chemical Structure
  89. GC33050 Givinostat (ITF-2357) Givinostat (ITF-2357) (ITF-2357) is a HDAC inhibitor with an IC50 of 198 and 157 nM for HDAC1 and HDAC3, respectively. Givinostat (ITF-2357)  Chemical Structure
  90. GC33159 Givinostat hydrochloride (ITF-2357 hydrochloride) Givinostat (ITF-2357) hydrochloride is a HDAC inhibitor with an IC50 of 198 and 157 nM for HDAC1 and HDAC3, respectively. Givinostat hydrochloride (ITF-2357 hydrochloride)  Chemical Structure
  91. GC12579 GLPG0634 GLPG0634 (GLPG0634) is a selective and orally active JAK1 inhibitor with IC50 of 10 nM, 28 nM, 810 nM, and 116 nM for JAK1, JAK2, JAK3, and TYK2, respectively. GLPG0634  Chemical Structure
  92. GC17222 GLPG0634 analogue GLPG0634 analogue (Compoun 176) is a broad spectrum JAK inhibitor with IC50 values of <100 nM against JAK1, JAK2 and JAK3. GLPG0634 analogue  Chemical Structure
  93. GC30263 Glucosamine (D-Glucosamine) Glucosamine (D-Glucosamine) (D-Glucosamine (D-Glucosamine)) is an amino sugar and a prominent precursor in the biochemical synthesis of glycosylated proteins and lipids, is used as a dietary supplement. Glucosamine (D-Glucosamine)  Chemical Structure
  94. GN10669 Glucosamine sulfate Glucosamine sulfate  Chemical Structure
  95. GC36153 Glucose-conjugated MGMT inhibitor Glucose-conjugated MGMT inhibitor is a potent O6-methylguanine-DNAmethyl-transferase (MGMT) inhibitor, with IC50s of 32 nM in vitro (cell extracts) and 10 nM in HeLa S3 cells. Glucose-conjugated MGMT inhibitor  Chemical Structure
  96. GC34595 GN44028 A HIF-1 inhibitor GN44028  Chemical Structure
  97. GC36168 GNA002 GNA002 is a highly potent, specific and covalent EZH2 (Enhancer of zeste homolog 2) inhibitor with an IC50 of 1.1 μM. GNA002 can specifically and covalently bind to Cys668 within the EZH2-SET domain, triggering EZH2 degradation through COOH terminus of Hsp70-interacting protein (CHIP)-mediated ubiquitination. GNA002 efficiently reduces EZH2-mediated H3K27 trimethylation, reactivates polycomb repressor complex 2 (PRC2)-silenced tumor suppressor genes. GNA002  Chemical Structure
  98. GC32960 GNE-049 GNE-049 is a highly potent and selective CBP inhibitor with an IC50 of 1.1 nM in TR-FRET assay. GNE-049 also inhibits BRET and BRD4(1) with IC50s of 12 nM and 4200 nM, respectively. GNE-049  Chemical Structure
  99. GC68439 GNE-064 GNE-064  Chemical Structure
  100. GC33212 GNE-207 GNE-207 is a potent, selective and orally bioavailable inhibitor of the bromodomain of CBP, with an IC50 of 1 nM, exhibits a selectively index of?>2500-fold against BRD4 (1). GNE-207 shows excellent CBP potency, with an EC50 of 18 nM for MYC expression in MV-4-11 cells. GNE-207  Chemical Structure
  101. GC32747 GNE-272 GNE-272 is a potent and selective CBP/EP300 inhibitor with IC50 values of 0.02, 0.03 and 13 μM for CBP, EP300 and BRD4, respectively. GNE-272 is also a selective in vivo probe for CBP/EP300. GNE-272  Chemical Structure

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