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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. GC61595 (+)-JQ-1-aldehyde (+)-JQ-1-aldehyde is the aldehyde form of (+)-JQ1. (+)-JQ-1-aldehyde can be uesd as a precursor to synthesize PROTACs, which targets BET bromodomains. (+)-JQ-1-aldehyde Chemical Structure
  3. GC34958 (+)-JQ1 PA

    A clickable form of (+)-JQ1

     (+)-JQ1 PA Chemical Structure
  4. GC13822 (-)-JQ1 A selective inhibitor of BET bromodomains (-)-JQ1 Chemical Structure
  5. GC34443 (R)-BAY1238097 (R)-BAY1238097 is the R-isomer with lower activity of BAY1238097. BAY1238097 is a potent and selective inhibitor of BET binding to histones and has strong anti-proliferative activity in different AML (acute myeloid leukemia) and MM (multiple myeloma) models through down-regulation of c-Myc levels and its downstream transcriptome. (R)-BAY1238097 Chemical Structure
  6. GC34446 (rac)-BAY1238097 (Rac)-BAY1238097 is a BET inhibitor, with an IC50 of 1.02 μM for BRD4. Used in cancer research. (rac)-BAY1238097 Chemical Structure
  7. GC72866 (S)-GSK852 (S)-GSK852 is a diastereomer of GSK852. (S)-GSK852 Chemical Structure
  8. GC33198 (S)-JQ-35 (TEN-010)

    TEN-010

     (S)-JQ-35 (TEN-010) (TEN-010) is an inhibitor of the Bromodomain and Extra-Terminal (BET) family bromodomain-containing proteins with potential antineoplastic activity. (S)-JQ-35 (TEN-010) Chemical Structure
  9. GC73208 (Z)-JQ1-TCO JQ1-TCO (JQ1-trans-cyclooctene) is a derivative of JQ1 , an inhibitor of BET. (Z)-JQ1-TCO Chemical Structure
  10. GC35175 6-Demethoxytangeretin 6-Demethoxytangeretin is a citrus flavonoid isolated from Citrus depressa. 6-Demethoxytangeretin Chemical Structure
  11. GC62279 653-47 653-47, a potentiator, significantly potentiates the cAMP-response element binding protein (CREB) inhibitory activity of 666-15. 653-47 is also a very weak CREB inhibitor with IC50 of 26.3 μM. 653-47 Chemical Structure
  12. GC62144 653-47 hydrochloride 653-47 hydrochloride, a potentiator, significantly potentiates the cAMP-response element binding protein (CREB) inhibitory activity of 666-15. 653-47 hydrochloride is also a very weak CREB inhibitor with IC50 of 26.3 μM. 653-47 hydrochloride Chemical Structure
  13. GC32689 666-15

    Compound 3i

     666-15 is a selective cyclic AMP response element binding protein (CREB) inhibitor with an IC50 value of 0.081±0.04μM. 666-15 Chemical Structure
  14. GC32677 A-485 A-485 is a potent and selective p300/CBP (histone acetyltransferase paralog/CREB binding protein) catalytic inhibitor with IC50 of 60nM for p300 HAT. A-485 inhibits the activity of p300-BHC (bromodomain HAT-C/H3) and CBP-BHC domains with IC50 of 9.8nM and 2.6nM, respectively. A-485 Chemical Structure
  15. GC33280 A1874 A1874 is a nutlin-based (MDM2 ligand) and BRD4-degrading PROTAC with a DC50 of 32 nM (induce BRD4 degradation in cells). Effective in inhibiting many cancer cell lines proliferation. A1874 Chemical Structure
  16. GC19409 ABBV-744

    ABBV-744 is a BDII-selective BET bromodomain inhibitor

     ABBV-744 Chemical Structure
  17. GC35227 ACBI1 ACBI1 is a potent and cooperative SMARCA2, SMARCA4 and PBRM1 degrader with DC50s of 6, 11 and 32 nM, respectively. ACBI1 is a PROTAC degrader. ACBI1 shows anti-proliferative activity. ACBI1 induces apoptosis. ACBI1 Chemical Structure
  18. GC73359 ACBI2 ACBI2 is a highly potent and orally active VHL PROTAC SMARCA2 degrader (EC50: 7 nM), which selectively degrades SMARCA2 with a DC50 value of 1 nM in RKO cells. ACBI2 Chemical Structure
  19. GC35297 Alobresib

    GS-5829

     A BET bromodomain inhibitor Alobresib Chemical Structure
  20. GC67912 Amredobresib Amredobresib Chemical Structure
  21. GC17284 Anacardic acid

    Hydroginkgolic acid; Ginkgolic Acid C15

    A histone acetyltransferase inhibitor

     Anacardic acid Chemical Structure
  22. GC32685 ARV-771 ARV-771 is a potent BET PROTAC based on E3 ligase von Hippel-Lindau with Kds of 34 nM, 4.7 nM, 8.3 nM, 7.6 nM, 9.6 nM, and 7.6 nM for BRD2(1), BRD2(2), BRD3(1), BRD3(2), BRD4(1), and BRD4(2), respectively. ARV-771 Chemical Structure
  23. GC19038 ARV-825 ARV-825 is a BRD4 Inhibitor based on PROTAC technology. ARV-825 Chemical Structure
  24. GC64271 AU-15330 AU-15330 is a proteolysis-targeting chimera (PROTAC) degrader of the SWI/SNF ATPase subunits, SMARCA2 and SMARCA4. AU-15330 induces potent inhibition of tumour growth in xenograft models of prostate cancer and synergizes with the AR antagonist enzalutamide. AU-15330 induces disease remission in castration-resistant prostate cancer (CRPC) models without toxicity. AU-15330 Chemical Structure
  25. GC74035 AU-24118 AU-24118 is orally bioavailable proteolysis targeting chimera (PROTAC) degrader of mSWI/SNF ATPases (SMARCA2 and SMARCA4) and PBRM1. AU-24118 Chemical Structure
  26. GC68711 AZ13824374

    AZ13824374 is an efficient selective inhibitor of ATAD2, which has anti-proliferative activity against breast cancer. In ATAD2 FRET and ATAD2 NanoBRET assays, AZ13824374 showed pIC50 values of 8.2 and 6.2 for ATAD2, respectively.

     AZ13824374 Chemical Structure
  27. GC35448 AZD5153 6-Hydroxy-2-naphthoic acid AZD5153 6-Hydroxy-2-naphthoic acid is the 6-Hydroxy-2-naphthoic acid of AZD5153. AZD5153 is a potent, selective, and orally available BET/BRD4 bromodomain inhibitor; disrupts BRD4 with an IC50 of 1.7 nM. AZD5153 6-Hydroxy-2-naphthoic acid Chemical Structure
  28. GC18508 BAY-299 BAY-299 is a potent and selective inhibitor of the bromodomain and PHD finger-containing (BRPF) family protein BRD1 (IC50 = 6 nM), also known as BRPF2, and the second bromodomain of transcription initiation factor TFIID subunits 1 (TAF1; IC50 = 13 nM). BAY-299 Chemical Structure
  29. GC33104 BAY1238097 BAY1238097 is a potent and selective inhibitor of BET binding to histones and has strong anti-proliferative activity in different AML (acute myeloid leukemia) and MM (multiple myeloma) models through down-regulation of c-Myc levels and its downstream transcriptome (IC50 <100 nM). BAY1238097 Chemical Structure
  30. GC63694 BAZ1A-IN-1 BAZ1A-IN-1 is a potent inhibitor of BAZ1A (bromodomain-containing protein). BAZ1A-IN-1 shows a KD value of 0.52 μM against BAZ1A bromodomain. BAZ1A-IN-1 shows good anti-viability activity against cancer cell lines expressing a high level of BAZ1A, but weak or no activity against cancer cells with a low expression level of BAZ1A. BAZ1A-IN-1 Chemical Structure
  31. GC15175 BAZ2-ICR Selective BAZ2 bromodomain inhibitor BAZ2-ICR Chemical Structure
  32. GC74003 BBC0403 BBC0403 is a selective BRD2 inhibitor with Kds of 7.64 μM and 41.37 μM for BRD2 (BD2) and BRD2 (BD1), respectively. BBC0403 Chemical Structure
  33. GC73279 BD-9136 BD-9136 is a highly selective BRD4 degrader. BD-9136 Chemical Structure
  34. GC16299 BET bromodomain inhibitor

    CPI-0610; CPI0610; CPI 0610

     Potent and selective inhibitor for BRD4 BET bromodomain inhibitor Chemical Structure
  35. GC63528 BET bromodomain inhibitor 1 BET bromodomain inhibitor 1 is an orally active, selective bromodomain and extra-terminal (BET) bromodomain inhibitor with an IC50 of 2.6 nM for BRD4. BET bromodomain inhibitor 1 binds to BRD2(2), BRD3(2), BRD4(1), BRD4(2), and BRDT(2) with high affinities (Kd values of 1.3 nM, 1.0 nM, 3.0 nM, 1.6 nM, 2.1 nM, respectively). bromodomain inhibitor 1 has anti-cancer activity. BET bromodomain inhibitor 1 Chemical Structure
  36. GC73742 BET bromodomain inhibitor 4 BET bromodomain inhibitor 4 (example 7) is an inhibitor of the BET bromodomain domain. BET bromodomain inhibitor 4 Chemical Structure
  37. GC35505 BET-BAY 002 BET-BAY 002 is a potent BET inhibitor; shows efficacy in a multiple myeloma model. BET-BAY 002 Chemical Structure
  38. GC35506 BET-BAY 002 S enantiomer BET-BAY 002 S enantiomer Chemical Structure
  39. GC31831 BET-IN-1 BET-IN-1 is a pan-inhibitor of all eight BET bromodomains, and selectivity over other representative bromodomain-containing proteins. BET-IN-1 Chemical Structure
  40. GC73423 BET-IN-14 BET-IN-14 is an orally active pan BET inhibitor (IC50: 5.35 nM). BET-IN-14 Chemical Structure
  41. GC72960 BET-IN-19 BET-IN-19 (Compound 146) is a BET inhibitor. BET-IN-19 Chemical Structure
  42. GC65506 BETd-246 BETd-246 is a second-generation and PROTAC-based BET bromodomain (BRD) inhibitor connected by ligands for Cereblon and BET, exhibiting superior selectivity, potency and antitumor activity. BETd-246 Chemical Structure
  43. GC32791 BETd-260 (ZBC 260)

    ZBC 260

     BETd-260 (ZBC 260) (ZBC 260) is a PROTAC connected by ligands for Cereblon and BET, with as low as 30 pM against BRD4 protein in RS4;11 leukemia cell line. BETd-260 (ZBC 260) potently suppresses cell viability and robustly induces apoptosis in hepatocellular carcinoma (HCC) cells. BETd-260 (ZBC 260) Chemical Structure
  44. GC12450 BI 2536

    BI-2536;BI2536

     A potent inhibitor of Plk1 BI 2536 Chemical Structure
  45. GC16726 BI-7273 BRD9 bromodomain inhibitor BI-7273 Chemical Structure
  46. GC16817 BI-9564 BRD9/7 specific inhibitor BI-9564 Chemical Structure
  47. GC64789 Biotinylated-JQ1

    Biotin-JQ1

     Biotinylated-JQ1 (Biotin-JQ1) is a biotinylated derivative of JQ1 with high affinity for the bromodomain of BRD4. Biotinylated-JQ1 inhibits MM1.S multiple myeloma cells proliferation with the EC50?of 0.4 μM. Biotinylated-JQ1 Chemical Structure
  48. GC32812 BMS-986158 A BET bromodomain inhibitor BMS-986158 Chemical Structure
  49. GC64538 BPTF-IN-BZ1 BPTF-IN-BZ1, a BPTF inhibitor, possesses a high potency (Kd = 6.3 nM). BPTF-IN-BZ1 Chemical Structure
  50. GC35552 BRD-IN-3 BRD-IN-3 ((R,R)-36n) is a highly potent PCAF bromodomain (BRD) inhibitor, with an IC50 of 7 nM. BRD-IN-3 also exhibits activity against GCN5 and FALZ. BRD-IN-3 Chemical Structure
  51. GC33017 BRD4 degrader AT1 BRD4 degrader AT1 is a PROTAC connected by ligands for von Hippel-Lindau and BRD4 as a highly selective Brd4 degrader, with a Kd of 44 nM for Brd4BD2 in cells. BRD4 degrader AT1 Chemical Structure
  52. GC64960 BRD4 Inhibitor-10 BRD4 Inhibitor-10 is a potent BRD4-BD1 inhibitor extracted from patent WO2015022332A1, Compound II-25, has an IC50 of 8 nM. BRD4 Inhibitor-10 Chemical Structure
  53. GC68803 BRD4 Inhibitor-20

    BRD4 Inhibitor-20 is an effective inhibitor of the bromodomain-containing protein 4 (BRD4) with oral activity. It has inhibitory activity against both BRD4 (BD1) and BRD4 (BD2), with IC50 values of 19 nM and 28 nM, respectively. BRD4 Inhibitor-20 also exhibits anti-proliferative activity in cancer cell lines. It can be used for research on various cancers such as colon cancer.

     BRD4 Inhibitor-20 Chemical Structure
  54. GC65569 BRD4 Inhibitor-24 BRD4 Inhibitor-24 (compound 3U) is a potent BRD4 inhibitor, BRD4 Inhibitor-24 shows antitumor activity against MCF7 and K652 cells, with IC50 values of 33.7 and 45.9 μM, respectively (extracted from patent CN107721975A). BRD4 Inhibitor-24 Chemical Structure
  55. GC73879 BRD4 Inhibitor-30 BRD4 inhibitor-30 (Compound 1) is a BRD4 inhibitor with a IC50 value of 415 nM. BRD4 Inhibitor-30 Chemical Structure
  56. GC73958 BRD4 ligand 6 TFA BRD4 ligand 6 TFA is the TFA salt form of BRD4 ligand 6. BRD4 ligand 6 TFA Chemical Structure
  57. GC66441 BRD4/CK2-IN-1 BRD4/CK2-IN-1 is the first highly effective and oral active dual-target inhibitor of BRD4/CK2 (bromodomain-containing protein 4/casein kinase 2), with IC50s of 180 nM and 230 nM for BRD4 and CK2, respectively. BRD4/CK2-IN-1 has strong anticancer activity without obvious toxicities. BRD4/CK2-IN-1 induces apoptosis and autophagy-associated cell death in triple-negative breast cancer (TNBC) BRD4/CK2-IN-1 Chemical Structure
  58. GC73953 BRD4/NAMPT-IN-1 BRD4/NAMPT-IN-1 (Compound A2) shows strong inhibitory effects on NAMPT and BRD4 (IC50=35 nM (NAMPT) and 58 nM (BRD4)). BRD4/NAMPT-IN-1 Chemical Structure
  59. GC34505 BRD7-IN-1 BRD7-IN-1, a modified derivative of BI7273 (BRD7/9 inhibitor), binds to a VHL ligand via a linker to form a PROTAC VZ185 (VZ185 against BRD7/9 with DC50s of 4.5 and 1.8 nM, respectively). BRD7-IN-1 Chemical Structure
  60. GC71086 BRD7-IN-2 BRD7-IN-2 (compound 2-77) is a potent inhibitor of bromodomain-containing protein 7 (BRD7), targeting to prostate cancer cells. BRD7-IN-2 Chemical Structure
  61. GC64541 BRM/BRG1 ATP Inhibitor-2 BRM/BRG1 ATP Inhibitor-2 is a BRG1/BRM ATPase inhibitor for the treatment of BAF-related disorders. BRM/BRG1 ATP Inhibitor-2 Chemical Structure
  62. GC35557 Bromodomain IN-1 Bromodomain IN-1 is a Bromodomain inhibitor extracted from patent WO2016069578A1, compound 4 . Bromodomain IN-1 Chemical Structure
  63. GC16531 Bromodomain Inhibitor, (+)-JQ1 A selective inhibitor of BET bromodomains Bromodomain Inhibitor, (+)-JQ1 Chemical Structure
  64. GC35558 Bromodomain inhibitor-8 Bromodomain inhibitor-8 (Intermediate 21) is a BET bromodomain inhibitor for treating autoimmune and inflammatory diseases. Bromodomain inhibitor-8 Chemical Structure
  65. GC10402 Bromosporine A non-specific bromodomain inhibitor Bromosporine Chemical Structure
  66. GC12733 C646 C646, a potent and selective p300/CBP histone acetyltransferase inhibitor (Ki 400 nM), has been shown to have pleiotropic activity, including neuroprotective, anti-cancer and anti-epithelial-mesenchymal transition (anti-EMT) effects. C646 Chemical Structure
  67. GC34517 CBP-IN-1

    CBP-IN-1

     CBP-IN-1 (CCS1477) is an orally active, potent, and selective inhibitor of the p300/CBP bromodomain. CBP-IN-1 binds to p300 and CBP with Kd values of 1.3 and 1.7 nM, respectively, and with 170/130-fold selectivity compared with BRD4 with a Kd of 222 nM. CCS1477 inhibits cell proliferation in prostate cancer cell lines and decreases androgen receptor (AR)- and C-MYC-regulated gene expression. CBP-IN-1 Chemical Structure
  68. GC61577 CBP/p300-IN-1 CBP/p300-IN-1 is a CBP/EP300 bromodomain inhibitor. CBP/p300-IN-1 Chemical Structure
  69. GC64696 CBP/p300-IN-12 CBP/p300-IN-12 is a potent and selective covalent histone acetyltransferases p300 (IC50 of 166 nM) and CBP inhibitor. CBP/p300-IN-12 decreases the levels of H3K27Ac of PC-3 cells (EC50 of 37 nM). CBP/p300-IN-12 forms a covalent adduct with C1450. CBP/p300-IN-12 Chemical Structure
  70. GC73365 CBP/p300-IN-20 CBP/p300-IN-20 is a potent and selective p300/CBP inhibitor, with a pIC50 of 10.1 for p300. CBP/p300-IN-20 Chemical Structure
  71. GC62330 CC-90010

    BMS-986378, CC-90010

     CC-90010 (compound 1) is a reversible and orally active BET inhibitor. CC-90010 is applied in the study for advanced solid tumors. CC-90010 Chemical Structure
  72. GC19098 CeMMEC1 CeMMEC1 is an inhibitor of BRD4, and also has high affinity for TAF1, with an IC50 of 0.9 uM for TAF1, and a Kd of 1.8 uM for TAF1 (2). CeMMEC1 Chemical Structure
  73. GC33028 CF53 CF53 is a highly potent, selective and orally active inhibitor of BET protein, with a Ki of <1 nM, Kd of 2.2 nM and an IC50 of 2 nM for BRD4 BD1. CF53 binds to both the BD1 and BD2 domains of BRD2, BRD3, BRD4, and BRDT BET proteins with high affinities, very selective over non-BET bromodomain-containing proteins. CF53 shows potent anti-tumor activity both in vitro and in vivo. CF53 Chemical Structure
  74. GC65602 CFT8634 CFT8634 is a degrader targeting BRD9 extracted from patent WO2021178920A1 compound 174. CFT8634 can be used for the research of synovial sarcoma and SMARCB1-deleted solid tumors. CFT8634 Chemical Structure
  75. GC72800 cis-MZ 1 hydrate cis-MZ 1 drate is a negative control for BRD4-targeted PROTAC MZ 1. cis-MZ 1 hydrate Chemical Structure
  76. GC16599 CPI-169 EZH2 inhibitor CPI-169 Chemical Structure
  77. GC14699 CPI-203 BET bromodomain inhibitor CPI-203 Chemical Structure
  78. GC10382 CPI-637 CBP/EP300 bromodomain inhibitor CPI-637 Chemical Structure
  79. GC14787 Curcumin

    Indian Saffron, Turmeric yellow

     A yellow pigment with diverse biological activities Curcumin Chemical Structure
  80. 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
  81. GC19119 dBET1 dBET1 is a potent BRD4 protein degrader based on PROTAC technology with an EC50 of 430 nM. dBET1 Chemical Structure
  82. 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
  83. 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
  84. 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
  85. 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
  86. 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
  87. 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
  88. 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
  89. 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
  90. 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
  91. GC33403 E-7386 E-7386 is an orally active CBP/beta-catenin modulator. E-7386 Chemical Structure
  92. GC31245 EML 425 An inhibitor of p300 and CBP EML 425 Chemical Structure
  93. 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
  94. 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
  95. GC69108 FHD-609

    FHD-609 is an inhibitor and degrader of the bromodomain-containing protein BRD9 with a bromine-containing structure domain. FHD-609 targets ncBAF and can be used to study various cancers that contain BAF complex subunit mutations. FHD-609 in combination with Telomelysin or INO5401 may have potential effects on research into adrenocortical carcinoma (ACC).

     FHD-609 Chemical Structure
  96. 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
  97. 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
  98. 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
  99. 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
  100. GC68439 GNE-064 GNE-064 Chemical Structure
  101. 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

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