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Home >> Signaling Pathways >> Chromatin/Epigenetics >> Epigenetic Reader Domain

Epigenetic Reader Domain

Epigenetic regulators of gene expression and chromatin state include so-called writers, erasers, and readers of chromatin modifications.Well-characterized examples of reader domains include bromodomains typically binding acetyllysine and chromatin organization modifier (chromo), malignant brain tumor (MBT), plant homeodomain (PHD), and Tudor domains generally associating with methyllysine. Research on epigenetic readers has been tremendously influenced by the discovery of selective inhibitors targeting the bromodomain and extraterminal motif (BET) family of acetyl-lysine readers. The human genome encodes 46 proteins containing 61 bromodomains clustered into eight families. Distinct experimental approaches are used to identify the first BET inhibitors, GSK 525762A and (+)-JQ-1.

The Polycomb group (PcG) protein, enhancer of zeste homologue 2 (EZH2), has an essential role in promoting histone H3 lysine 27 trimethylation (H3K27me3) and epigenetic gene silencing. This function of EZH2 is important for cell proliferation and inhibition of cell differentiation, and is implicated in cancer progression. Cyclin-dependent kinases regulate epigenetic gene silencing through phosphorylation of EZH2. In many types of cancers including lymphomas and leukemia, EZH2 is postulated to exert its oncogenic effects via aberrant histone and DNA methylation, causing silencing of tumor suppressor genes.

p300/CBP is not only a transcriptional adaptor but also a histone acetyltransferase.

Targets for  Epigenetic Reader Domain

Products for  Epigenetic Reader Domain

  1. Cat.No. Product Name Information
  2. GC34078 I-CBP112 I-CBP112 is a specific and potent acetyl-lysine competitive protein-protein interaction inhibitor, that inhibits the CBP/p300 bromodomains, enhances acetylation by p300. I-CBP112 Chemical Structure
  3. GC43889 I-CBP112 (hydrochloride) cAMP-responsive element-binding protein binding protein (CREBBP) and E1A-associated protein p300 (EP300) are transcriptional co-activators that modulate DNA replication, DNA repair, cell growth, transformation, and development. I-CBP112 (hydrochloride) Chemical Structure
  4. GC33042 IACS-9571 (ASIS-P040) IACS-9571 (ASIS-P040) is a potent and selective inhibitor of TRIM24 and BRPF1, with IC50 of 8 nM for TRIM24, and Kds of 31 nM and 14 nM for TRIM24 and BRPF1, respectively. IACS-9571 (ASIS-P040) Chemical Structure
  5. GC60925 IACS-9571 hydrochloride IACS-9571 (ASIS-P040) hydrochloride is a potent and selective inhibitor of TRIM24 and BRPF1, with an IC50 of 8 nM for TRIM24, and Kds of 31 nM and 14 nM for TRIM24 and BRPF1, respectively. IACS-9571 hydrochloride Chemical Structure
  6. GC34437 IACS-9571 Hydrochloride (ASIS-P040 Hydrochloride) IACS-9571 Hydrochloride (ASIS-P040 Hydrochloride) Chemical Structure
  7. GC48548 iBET-BD2 A BD2 bromodomain inhibitor iBET-BD2 Chemical Structure
  8. GC19200 INCB-057643 INCB-057643 is a novel, orally bioavailable BET inhibitor. INCB-057643 Chemical Structure
  9. GC33026 INCB054329 INCB054329 is a potent BET inhibitor. INCB054329 Chemical Structure
  10. GC30644 INCB054329 Racemate INCB054329 Racemate is a BET protein inhibitor. INCB054329 Racemate Chemical Structure
  11. GC19210 JQ-1 carboxylic acid JQ-1 carboxylic acid is a highly potent, selective and cell-permeable BRD4 inhibitor with IC50s of 77 nM and 33 nM for BRD4(1) and BRD4(2), respectively. JQ-1 carboxylic acid Chemical Structure
  12. GC31654 KG-501 (Naphthol AS-E phosphate) KG-501 (Naphthol AS-E phosphate) is a CREB inhibitor, with an IC50 of 6.89 μM. KG-501 (Naphthol AS-E phosphate) Chemical Structure
  13. GC50395 L Moses dihydrochloride High affinity and selective PCAF bromodomain inhibitor L Moses dihydrochloride Chemical Structure
  14. GC33183 L-45 (L-Moses) L-45 (L-Moses) (L-45) is the first potent, selective, and cell-active p300/CBP-associated factor (PCAF) bromodomain (Brd) inhibitor with a Kd of 126 nM. L-45 (L-Moses) Chemical Structure
  15. GC34377 L-45 dihydrochloride (L-Moses dihydrochloride) L-45 dihydrochloride (L-Moses dihydrochloride) Chemical Structure
  16. GC18731 LP99 LP99 is a potent inhibitor of the bromodomain containing proteins BRD7 and BRD9 that binds with Kd values of 99 and 909 nM, respectively, as determined by isothermal titration calorimetry. LP99 Chemical Structure
  17. GC62591 LT052 LT052 is a highly selective BET BD1 inhibitor with an IC50 of 87.7 nM. LT052 Chemical Structure
  18. GC36521 M89 M-89 is a highly potent and specific menin inhibitor, with a Kd of 1.4 nM for binding to menin. M89 Chemical Structure
  19. GC63064 Menin-MLL inhibitor 19 Menin-MLL inhibitor 19, a potent exo-aza spiro inhibitor of menin-mll interaction, example A17, extracted from patent WO2019120209A1. Menin-MLL inhibitor 19 Chemical Structure
  20. GC63538 Menin-MLL inhibitor 20 Menin-MLL inhibitor 20 is an irreversible menin-MLL interaction inhibitor with antitumor activities (WO2020142557A1, Intermediate 6). Menin-MLL inhibitor 20 Chemical Structure
  21. GC11439 MG 149 HAT inhibitor MG 149 Chemical Structure
  22. GC11418 MI-2 An inhibitor of menin-MLL fusion protein interactions MI-2 Chemical Structure
  23. GC12199 MI-3 An inhibitor of menin-MLL fusion protein interactions MI-3 Chemical Structure
  24. GC19246 MI-463 MI-463 is a highly potent and orally bioavailable small molecule inhibitor of the menin-mLL interaction. MI-463 Chemical Structure
  25. GC19247 MI-503 MI-503 is a highly potent and orally bioavailable small molecule inhibitor of the menin-mLL interaction. MI-503 Chemical Structure
  26. GC32798 MI-538 MI-538 is an inhibitor of the interaction between menin and MLL fusion proteins with an IC50 of 21 nM. MI-538 Chemical Structure
  27. GC19248 Mivebresib Mivebresib is a potent and orally available bromodomain and extraterminal domain (BET) bromodomain inhibitor. Mivebresib Chemical Structure
  28. GC34675 Molibresib besylate Molibresib besylate (GSK 525762C; I-BET 762 besylate) is a BET bromodomain inhibitor with IC50 of 32.5-42.5 nM. Molibresib besylate Chemical Structure
  29. GC36657 MS31 MS31 is a potent, highly affinity and selective fragment-like methyllysine reader protein spindlin 1 (SPIN1) inhibitor. MS31 potently inhibits the interactions between SPIN1 and H3K4me3 (IC50=77 nM, AlphaLISA; 243 nM, FP). MS31 selectively binds Tudor domain II of SPIN1 (Kd=91 nM). MS31 potently inhibits binding of trimethyllysine-containing peptides to SPIN1. MS31 is not toxic to nontumorigenic cells. MS31 Chemical Structure
  30. GC39252 MS31 trihydrochloride MS31 trihydrochloride is a potent, highly affinity and selective fragment-like methyllysine reader protein spindlin 1 (SPIN1) inhibitor. MS31 trihydrochloride potently inhibits the interactions between SPIN1 and H3K4me3 (IC50=77 nM, AlphaLISA; 243 nM, FP). MS31 trihydrochloride selectively binds Tudor domain II of SPIN1 (Kd=91 nM). MS31 trihydrochloride potently inhibits binding of trimethyllysine-containing peptides to SPIN1, and is not toxic to nontumorigenic cells. MS31 trihydrochloride Chemical Structure
  31. GC44250 MS351

    MS351 is an antagonist of chromobox 7 (CBX7) that acts by binding the CBX7 chromodomain.

     MS351 Chemical Structure
  32. GC64999 MS402 MS402 is a BD1-selective BET BrD inhibitor with Kis of 77 nM, 718 nM, 110 nM, 200 nM, 83 nM, and 240 nM for BRD4(BD1), BRD4(BD2), BRD3(BD1), BRD3(BD2), BRD2(BD1) and BRD2(BD2), respectively. MS402 Chemical Structure
  33. GC31881 MS417 (GTPL7512) MS417 (GTPL7512) is a selective BET-specific BRD4 inhibitor, binds to BRD4-BD1 and BRD4-BD2 with IC50s of 30, 46 nM and Kds of 36.1, 25.4 nM, respectively, with weak selectivity at CBP BRD (IC50, 32.7 μM). MS417 (GTPL7512) Chemical Structure
  34. GC13148 MS436 BRD4 inhibitor MS436 Chemical Structure
  35. GC38474 MS645 MS645 is a bivalent BET bromodomains (BrD) inhibitor with a Ki of 18.4 nM for BRD4-BD1/BD2. MS645 spatially constrains bivalent inhibition of BRD4 BrDs resulting in a sustained repression of BRD4 transcriptional activity in solid-tumor cells. MS645 Chemical Structure
  36. GC18729 MZ1 MZ1 is a hybrid compound that drives the selective proteasomal degradation of bromodomain-containing protein 4 (BRD4). MZ1 Chemical Structure
  37. GC33102 MZP-54 MZP-54 is a PROTAC connected by ligands for von Hippel-Lindau and BRD3/4, with a Kd of 4 nM for Brd4BD2. MZP-54 Chemical Structure
  38. GC33363 MZP-55 MZP-55 is a PROTAC connected by ligands for von Hippel-Lindau and BRD3/4, with a Kd of 8 nM for Brd4BD2. MZP-55 Chemical Structure
  39. GC61841 Naphthol AS-E Naphthol AS-E is a potent and cell-permeable inhibitor of KIX-KID interaction. Naphthol AS-E directly binds to the KIX domain of CBP (Kd:8.6 ?M), blocks the interaction between the KIX domain and the KID domain of CREB with IC50 of 2.26 ?M. Naphthol AS-E can be used for cancer research. Naphthol AS-E Chemical Structure
  40. GC62620 NHWD-870 NHWD-870 is a potent, orally active and selective BET family bromodomain inhibitor and only binds bromodomains of BRD2, BRD3, BRD4 (IC50=2.7 nM), and BRDT. NHWD-870 has potent tumor suppressive efficacies and suppresses cancer cell-macrophage interaction. NHWD-870 increases tumor apoptosis and inhibits tumor proliferation. NHWD-870 Chemical Structure
  41. GC36734 NI-42 An inhibitor of the BRPF1 bromodomain NI-42 Chemical Structure
  42. GC16763 NI-57 bromodomains of BRPF proteins inhibitor NI-57 Chemical Structure
  43. GC14103 NSC228155 EGFR activator NSC228155 Chemical Structure
  44. GC44477 NVS-CECR2-1 NVS-CECR2-1 is a potent inhibitor of CECR2 (cat eye syndrome chromosome region, candidate 2), a component of chromatin complexes that regulate gene expression controlling development. NVS-CECR2-1 Chemical Structure
  45. GC69601 OARV-771

    OARV-771 is a VHL-based BET degrader (PROTAC) with improved cell permeability. OARV-771 shows DC50 values of 6, 1, and 4 nM for Brd4, Brd2, and Brd3 respectively.

     OARV-771 Chemical Structure
  46. GC66067 ODM-207 ODM-207 (BET-IN-4) is a potent BET bromodomain protein (BRD4) inhibitor, with an IC50 of ≤ 1 μM. ODM-207 Chemical Structure
  47. GC17482 OF-1 BRPF1B and BRPF2 bromodomain inhibitor OF-1 Chemical Structure
  48. GC17973 OTX-015 A BRD2, BRD3, and BRD4 inhibitor OTX-015 Chemical Structure
  49. GC39417 OXFBD04 OXFBD04 is a potent and selective BRD4 inhibitor with an IC50 of 166?nM. OXFBD04 is a potent BET bromodomain ligand with additional modest affinity for the CREBBP bromodomain. OXFBD04 has anti-cancer activity. OXFBD04 Chemical Structure
  50. GC36887 PF-CBP1 hydrochloride PF-CBP1 hydrochloride is a highly selective inhibitor of the CREB binding protein bromodomain (CBP BRD). PF-CBP1 hydrochloride Chemical Structure
  51. GC14361 PFI 3 inhibitor of polybromo 1 and SMARCA4 PFI 3 Chemical Structure
  52. GC10979 PFI 4 Potent and selective BRPF1 Bromodomain inhibitor PFI 4 Chemical Structure
  53. GC15375 PFI-1 (PF-6405761) A BET bromodomain inhibitor PFI-1 (PF-6405761) Chemical Structure
  54. GC19298 PLX51107 PLX51107 is a potent and selective BET inhibitor, with Kds of 1.6, 2.1, 1.7, and 5 nM for BD1 and 5.9, 6.2, 6.1, and 120 nM for BD2 of BRD2, BRD3, BRD4, and BRDT, respectively; PLX51107 also interacts with the bromodomains of CBP and EP300 (Kd, in the 100 nM range). PLX51107 Chemical Structure
  55. GC36943 PNZ5 PNZ5 is a potent and isoxazole-based pan-BET inhibitor with high selectivity and potency similar to the well-established (+)-JQ1, with a KD of 5.43 nM for BRD4(1). PNZ5 Chemical Structure
  56. GC33109 PROTAC BET Degrader-1 PROTAC BET Degrader-1 is a PROTAC connected by ligands for Cereblon and BET, decreasing BRD2, BRD3, and BRD4 protein levels at low concentration. PROTAC BET Degrader-1 Chemical Structure
  57. GC32980 PROTAC BET degrader-2 PROTAC BET degrader-2 is a PROTAC connected by ligands for Cereblon and BET with an IC50 value of 9.6 nM in cell growth inhibition in the RS4;11 cells and capable of achieving tumor regression. PROTAC BET degrader-2 Chemical Structure
  58. GC34325 PROTAC BET degrader-3 PROTAC BET Degrader-3 is a PROTAC connected by ligands for von Hippel-Lindau and BET. PROTAC BET degrader-3 Chemical Structure
  59. GC61212 PROTAC BRD4 Degrader-5 PROTAC BRD4 Degrader-5 is a PROTAC connected by ligands for von Hippel-Lindau and BRD4. PROTAC BRD4 Degrader-5 can potent degrade BRD4 in HER2 positive and negative breast cancer cell lines. PROTAC BRD4 Degrader-5 Chemical Structure
  60. GC62606 PROTAC BRD4 Degrader-8 PROTAC BRD4 Degrader-8 is a PROTAC connected by ligands for von Hippel-Lindau and BRD4, with IC50s of 1.1 nM and 1.4 nM for BRD4 BD1 and BD2, respectively. PROTAC BRD4 Degrader-8 is capable of potently degrading the BRD4 protein in PC3 prostate cancer cells. PROTAC BRD4 Degrader-8 Chemical Structure
  61. GC39180 PROTAC BRD4 ligand-1 PROTAC BRD4 ligand-1 is a potent BET inhibitor and a ligand for target BRD4 protein for PROTACT GNE-987. PROTAC BRD4 ligand-1 Chemical Structure
  62. GC33372 PROTAC BRD9 Degrader-1 PROTAC BRD9 Degrader-1 is a PROTAC connected by ligands for Cereblon and BRD9 (IC50=13.5 nM), which can be used as a selective probe useful for the study of BAF complex biology. PROTAC BRD9 Degrader-1 Chemical Structure
  63. GC33217 QCA570 QCA570 is a PROTAC connected by ligands for Cereblon and BET, with an IC50 of 10 nM for BRD4 BD1 Protein. QCA570 Chemical Structure
  64. GC14199 RVX-208 RVX-208 (RVX-208) is an inhibitor of BET transcriptional regulators with selectivity for the second bromodomain. The IC50s are 87 μM and 0.51 μM for BD1 and BD2, respectively. RVX-208 Chemical Structure
  65. GC63178 RVX-297 RVX-297 is a potent, orally active BET bromodomain inhibitor with selectivity for BD2. RVX-297 Chemical Structure
  66. GC19328 SF2523 SF2523 is a highly selective and potent inhibitor of PI3K with IC50s of 34 nM, 158 nM, 9 nM, 241 nM and 280 nM for PI3Kα, PI3Kγ, DNA-PK, BRD4 and mTOR, respectively. SF2523 Chemical Structure
  67. GC10174 SGC-CBP30 A potent inhibitor of CREBBP/EP300 bromodomains SGC-CBP30 Chemical Structure
  68. GC34778 SGC-iMLLT An inhibitor of MLLT1 and MLLT3 YEATS domains SGC-iMLLT Chemical Structure
  69. GC63887 SGC-SMARCA-BRDVIII SGC-SMARCA-BRDVIII is a potent and selective inhibitor of SMARCA2/4 and PB1(5), with Kds of 35 nM, 36 nM, and 13 nM, respectively. SGC-SMARCA-BRDVIII Chemical Structure
  70. GC65574 SNIPER(BRD)-1 SNIPER(BRD)-1, consists of an IAP antagonist LCL-161 derivative and a BET inhibitor, (+)-JQ-1, connected by a linker. SNIPER(BRD)-1 induces the degradation of BRD4 via the ubiquitin-proteasome pathway. SNIPER(BRD)-1 also degrades cIAP1 , cIAP2 and XIAP with IC50s of 6.8 nM, 17 nM, and 49nM, respectively. SNIPER(BRD)-1 Chemical Structure
  71. GC32863 Target Protein-binding moiety 4 Target Protein-binding moiety 4 (Molibresib carboxylic acid) is an I-BET762-based warhead ligand for conjugation reactions of PROTAC targeting on BET. Target Protein-binding moiety 4 (Molibresib carboxylic acid) is a BRD4 inhibitor with a pIC50 of 5.1. Target Protein-binding moiety 4 Chemical Structure
  72. GC50340 TC AC 28 High affinity BET bromodomain ligand TC AC 28 Chemical Structure
  73. GC34319 TD-428 TD-428 is a PROTAC connected by ligands for Cereblon and BRD4. TD-428 is a highly specific BRD4 degrader with a DC50?of?0.32?nM. TD-428 is a BET PROTAC, which comprises TD-106 (a CRBN ligand) linked to JQ1 (a BET inhibitor). TD-428 efficiently induce BET protein degradation. TD-428 Chemical Structure
  74. GC70037 TMX1

    TMX1 is a BRD4 covalent molecular glue degrader. TMX1 selectively recruits DCAF16 to BRD4BD2, leading to the degradation of BRD4.

     TMX1 Chemical Structure
  75. GC50542 TP 238 CECR2 and BPTF/FALZ inhibitor TP 238 Chemical Structure
  76. GC40628 TP-472 TP-472 is an inhibitor of bromodomain BRD9 (Kd = 33 nM; EC50 = 320 nM in a NanoBRET assay). TP-472 Chemical Structure
  77. GC32880 TPOP146 TPOP146 is a selective CBP/P300 benzoxazepine bromodomain inhibitor with Kd values of 134 nM and 5.02 μM for CBP and BRD4. TPOP146 Chemical Structure
  78. GC62405 UMB298 UMB298 is a potent and selective CBP/P300 bromodomain inhibitor. UMB298 Chemical Structure
  79. GC12419 UNC 926 hydrochloride An antagonist of L3MBTL1, L3MBTL3, and L3MBTL4 UNC 926 hydrochloride Chemical Structure
  80. GC68025 UNC1021 UNC1021 Chemical Structure
  81. GC64040 VTP50469 fumarate VTP50469 fumarate is a potent, highly selective and orally active Menin-MLL interaction inhibitor with a Ki of 104 pM. VTP50469 fumarate has potently anti-leukemia activity. VTP50469 fumarate Chemical Structure
  82. GC65135 VZ185 VZ185 is a potent, fast, and selective von Hippel-Lindau based dual degrader probe of BRD9 and BRD7 with DC50s of 4.5 and 1.8 nM, respectively. VZ185 is cytotoxic in EOL-1 and A-402 cells, with EC50s of 3 nM and 40 nM, respectively. VZ185 Chemical Structure
  83. GC33285 Y06036 Y06036 is a potent and selective BET inhibitor, which binds to the BRD4(1) bromodomain with Kd value of 82 nM. Antitumor activity. Y06036 Chemical Structure
  84. GC33264 Y06137 Y06137 is a potent and selective BET inhibitor for treatment of castration-resistant prostate cancer (CRPC). Y06137 binds to the BRD4(1) bromodomain with a Kd of 81 nM. Y06137 Chemical Structure
  85. GC64518 Ziftomenib Ziftomenib (KO-539) is a menin-MLL interaction inhibitor with antitumor activities (WO2017161028A1, compound 151). Ziftomenib Chemical Structure
  86. GC19455 ZL0420

    ZL0420 is a potent and selective BRD4 inhibitor

     ZL0420 Chemical Structure
  87. GC65204 ZL0454 ZL0454 is a potent and selective Bromodomain-containing protein 4 (BRD4) inhibitor with an IC50 of 49 and 32 nM for BD1 and BD2. ZL0454 Chemical Structure
  88. GC64529 ZL0590 ZL0590 is a potent, orally active BRD4 BD1-selective inhibitor with an IC50 of 90 nM for human BRD4 BD1. ZL0590 Chemical Structure
  89. GC65269 ZXH-3-26 ZXH-3-26 is a PROTAC connected by ligands for Cereblon and BRD4 with a DC50/5h of 5 nM. The DC50/5h refers to half-maximal degradation after 5 hours of treatment of ~ 5 nM. ZXH-3-26 Chemical Structure

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