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Epigenetic Reader Domain

Epigenetic reader domains can be thought of as effector proteins that recognize and are recruited to specific epigenetic marks.

AU-15330
T399542380274-50-8In house
AU-15330 is a proteolytic targeting chimera (PROTAC) that simultaneously targets SMARCA4, SMARCA2, and PBRM1 for degradation and exhibits cytotoxicity in H3.3K27M cells but not in H3 wild-type cells. [2]
  • $139
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PROTAC BRD4 ligand-1
T125512313230-51-0In house
PROTAC BRD4 ligand-1, a component of Protac GNE-987, is a ligand for BRD4 and acts as an inhibitor of BET.
  • $125
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(+)-JQ-1
T21101268524-70-4
(+)-JQ-1 (JQ1) is a specific, reversible BET bromine domain inhibitor that targets BRD4 (1 2) with IC50 values of 77 33 nM. (+)-JQ-1 induces cell autophagy and inhibits cell proliferation.
  • $30
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A-485
T140731889279-16-6
A-485 is a potent and selective catalytic p300 CBP inhibitor with IC50 values of 9.8 nM for p300 and 2.6 nM for CBP.
  • $89
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ICG-001
T6113780757-88-2
ICG001 is a β-catenin TCF-mediated transcription inhibitor that selectively blocks β-catenin CBP interaction without interfering with β-catenin p300 interaction. It specifically binds to CREB protein with an IC50 of 3 μM.
  • $30
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Curcumin
T1516458-37-7
Curcumin (Natural Yellow 3) is a phenolic natural product, an inhibitor of histone acetyltransferase p300 CREB (IC50=25 μM) with specificity. Curcumin has a wide range of pharmacological activities such as antitumor, anti-inflammatory and antioxidant.
  • $30
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Inobrodib
T107172222941-37-7
Inobrodib (CBP-IN-1) is a potent inhibitor of p300 CBP bromodomain.
  • $64
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FHD-286
T97492671128-05-3
FHD-286 is an inhibitor of BRM BRG1 ATPase and can be used for studies on the treatment of BAF-related disorders such as acute myeloid leukemia.
  • $148
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ARV-825
T54341818885-28-7
ARV-825, a heterobifunctional PROTAC (Proteolysis Targeting Chimera) that recruits BRD4 to the E3 ubiquitin ligase cereblon leading to fast, efficient, and prolonged degradation of BRD4 in all BL cell lines tested.
  • $60
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VTP50469
T133362169916-18-9
VTP50469 is a highly selective and orally active small molecule inhibitor of the Menin-MLL protein-protein interaction with potent anti-leukemic activity with a Ki of 104 pM.
  • $176
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NEO2734
T86582081072-29-7In house
NEO2734 (EP31670) is an orally active, selective inhibitor of p300 CBP and BET bromodomains, with an IC50 of less than 30 nM for both targets.
  • $116
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666-15
T53181433286-70-4
666-15 is a selective CREB inhibitor with an IC50 of 81 nM. 666-15 can effectively inhibit the growth of breast cancer.
  • $52
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ICG001
T2237847591-62-2
ICG001 antagonizes Wnt β-catenin TCF-mediated transcription and specifically binds to element-binding protein (CREB)-binding protein (CBP) with IC50 of 3 μM, but is not the related transcriptional coactivator p300.
  • $30
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BI-7273
T67831883429-21-7In house
BI-7273 is an effective, specific, BRD9 BD Inhibitor, which can infiltrate cell.
  • $35
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CPI-0610 carboxylic acid
T108791380089-81-5In house
CPI-0610 carboxylic acid is an effective and selective small molecule inhibitor of bromine domain and outer end (BET) protein as a ligand of PROTAC target protein. CPI-0610 carboxylic acid may have anticancer and anticancer activities.
  • $316
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MI-136
T68891628316-74-4
MI-136 inhibits expression of androgen receptor (AR) target genes that DHT induced.
  • $39
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BBC0403
T881182644662-83-7
BBC0403 is a selective BRD2 inhibitor that inhibits BRD2 and BRD2, suppressing NF-κB and MAPK signaling pathways. It can be used in osteoarthritis (OA) research.
  • $63
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C646
T2452328968-36-1
C646, a histone acetyltransferase inhibitor, inhibits p300 (Ki: 400 nM, in a cell-free assay).
  • $41
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AZD5153 6-Hydroxy-2-naphthoic acid
T35041869912-40-2
AZD5153 6-Hydroxy-2-naphthoic acid (AZD5153) is a potent triazolopyridazine-based Bromodomain (BRD4) and Extraterminal (BET) inhibitor utilized in cancer treatments.
  • $53
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A947
T746862378056-80-3
A947 is a potent and selective SMARCA2 protein hydrolysis-targeted chimeric molecule (PROTAC) that induces the degradation of SMARCA2 by binding to VHL E3 ubiquitin ligase, with significant antitumor activity in vivo and in vitro, especially in SMARCA4-mutant non-small cell lung cancer (NSCLC) cells.
  • $1,070
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GNE-781
T154051936422-33-1
GNE-781 is a highly potent and selective inhibitor of CBP (IC50: 0.94 nM in TR-FRET assay). GNE-781 also inhibits BRET and BRD4(1) (IC50s: 6.2 nM and 5100 nM, respectively).
  • $166
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ABBV-744
T46972138861-99-9In house
ABBV-744 is a BDII-selective BET bromodomain inhibitor that inhibits BRD2 3 4. It is used in the research on inflammatory diseases, cancer, and AIDS.
  • $39
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dBET6
T51301950634-92-0
dBET6 is a selective and cell-permeable degrader of BET based on PROTAC (IC50: 14 nM). It has antitumor activity.
  • $48
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BRM/BRG1 ATP Inhibitor-1
T106162270879-17-7
BRM BRG1 ATP Inhibitor-1 is an allosteric dual Brahma homolog (BRM) SWI SNF related matrix-associated actin-dependent regulator of chromatin subfamily A member 2 (SMARCA2) and BRG1 SMARCA4 ATPase activity inhibitor (IC50s<0.005 μM).
  • $417
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SNDX-5613
T129432169919-21-3
Revumenib (SNDX-5613) is a potent and selective oral inhibitor of menin-KMT2A interaction with Ki of 0.149 nM and IC50 between 10 and 20 nM, which can be used in the study of acute leukemia with MLL gene rearrangement.
  • $67
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TRIM24/BRPF1-IN-2
T742713033288-68-2In house
TRIM24 BRPF1-IN-2 is a selective dual TRIM24 BRPF1 inhibitor with anticancer activity that inhibits proliferation, gene and protein expression, and colony formation of prostate cancer cells in a dose-dependent manner.
  • $335
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GSK778
T97032451862-42-1
GSK778 is a potent and selective inhibitor of BD1 bromodomain such as BRD2 BD1 (IC50s = 75 nM), BRD3 BD1 (IC50s = 41 nM), BRD4 BD1 (IC50s = 41 nM), and BRDT BD1 (IC50s = 143 nM). GSK778 inhibits proliferation, induces a cell cycle arrest and apoptosis.
  • $163
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Bisdemethoxycurcumin
TL000724939-16-0
Bisdemethoxycurcumin (Curcumin III) is a natural demethoxy derivative of curcumin. It is a potent activator of macrophage phagocytosis, interacting with 1α, 25-dihydroxy vitamin D3 to stimulate amyloid-β clearance by macrophages (optimal stimulation at 100 nM BDMC) [1]. More stable than curcumin in physiological media, BDMC suppresses proliferation of cancer cells [2]. It down-regulates the transcriptional coactivator p300, suppressing the Wnt β-catenin pathway, and inhibits LPS induction of iNOS expression [3].
  • $31
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GSK620
T90202088410-46-0
GSK620 is a pan-BD2 inhibitor, which shows an anti-inflammatory phenotype in human whole blood with excellent broad selectivity, developability, and in vivo oral pharmacokinetics.GSK620 is highly selective for the BET-BD2 family of proteins, with >200-fol
  • $30
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MG 149
T65841243583-85-8
MG 149 (Tip60 HAT inhibitor) is a selective and potent Tip60 inhibitor with IC50 of 74 uM, similar potentcy for MOF(IC50= 47 uM).
  • $48
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AZD5153
T3504L1869912-39-9
AZD5153 is a reversible inhibitor of BRD4, a bromodomain and extra-terminal family protein, with antitumor activity.AZD5153 inhibits hepatocarcinogenesis by altering the BRD4 chromosome landscape and regulating the transcriptome of HCC cells.AZD5153 is used in the study of lymphomas and solid tumors.
  • $38
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SGC-CBP30
T66681613695-14-9
SGC-CBP30 is an effective CREBBP EP300 inhibitor (IC50: 21 38 nM).
  • $45
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ZEN-3411
T133931952264-36-6In house
ZEN-3411 is an orally available and potent BET inhibitor that inhibits BRD4(BD1), BRD4(BD2), and BRD4(BD1BD2) and suppresses the growth of tumor cells overproducing BET proteins.
  • $350
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ZEN-3694
T292141643947-30-1In house
ZEN-3694 (ZEN 3694) is a bromo-structural domain extra-terminal inhibitor (BETi) with activity in androgen signaling inhibitor (ASI) resistance models and can be used in combination with enzalutamide to study metastatic desmoplasia-resistant prostate cancer.
  • $61
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Pocenbrodib
T696912304372-79-8In house
Pocenbrodib (FT-7051) is a potent inhibitor of the bromodomain of the CBP p300 family with potential antitumour activity and is palatable for cancer research.
  • $790
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M‑89
T119252363165-42-6
M-89, a highly potent and specific inhibitor of the menin-mixed lineage leukemia (Menin-MLL) protein-protein interaction, exhibits a Kd of 1.4 nM for menin binding. This compound holds potential for treating MLL leukemia.
  • $169
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BI 2536
T6173755038-02-9
BI2536 is an effective Plk1 inhibitor (IC50: 0.83 nM). It has 4- and 11-fold greater selectivity than Plk2 and Plk3.
  • $38
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Y06137
T133632226534-49-0In house
Y06137 is an effective and selective BET inhibitor with a Kd of 81 nM for BRD4(1) bromodomain. Y06137 can be used for research on the treatment of castration-resistant prostate cancer.
  • $55
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Molibresib
T19061260907-17-2
Molibresib (GSK525762) is an inhibitor of BET proteins (IC50: about 35 nM).
  • $36
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YD23
T779732951015-29-3
YD23 is a PROTAC that induces SMARCA2 degradation, has anticancer activity, and selectively inhibits the growth of SMARCA4 mutant lung cancer cells in vitro.
  • $339
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C-82
T106411422253-37-9
C-82 is a specific CBP β-catenin antagonist. It inhibits the binding between β-catenin and CBP and increases the binding between β-catenin and p300.
  • $453
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BY27
T106382247236-59-3In house
BY27, a potent and selective BET BD2 inhibitor (Ki: 3.1 nM) with anticancer activity, inhibits BD1 BD2 of BRD2, BRD3, BRD4, and BRDT, and suppresses tumor growth.
  • $483 TargetMol
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PNZ5
T125131629277-36-6In house
PNZ5, an isoxazole-based pan-BET inhibitor, demonstrates potent activity and high selectivity comparable to the established (+)-JQ1, exhibiting a dissociation constant (KD) of 5.43 nM for BRD4(1).
  • $117
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BRD7-IN-1
T176972448414-48-8
BRD7-IN-1, a modified derivative of BI7273 (BRD7 9 inhibitor), forms PROTAC VZ185 via linkage to a VHL ligand, demonstrating potent activity against BRD7 9 with DC50 values of 4.5 and 1.8 nM, respectively [1].
  • $100
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SMARCA-BD ligand 1 for Protac
T138481997319-92-2In house
SMARCA-BD ligand 1 for Protac is a compound that binds to SMARCA2, the BAF ATPase subunit, utilizing Protac technology to degrade SMARCA2.
  • $61
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Anacardic Acid
T638916611-84-0
Anacardic Acid (6-pentadecylsalicylic Acid) is an effective inhibitor of p300 and p300 CBP-associated factor histone acetyltranferases. It also has antimicrobial activity, antibacterial activity, and inhibits prostaglandin synthase, lipoxygenase, and tyrosinase.
  • $45
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Dbet57
T54401883863-52-2
dBET57 is heterobifunctional degrader of BRD4 based on the PROTAC technology, exhibits significant degradation of BRD4BD1 with a DC50 5h of 500 nM ,and inactive on BRD4BD2
  • $42
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Butyrolactone 3
T14839778649-18-6
Butyrolactone 3 (MB-3) is a histone acetyltransferase Gcn5 inhibitor with a weak affinity for CBP.Butyrolactone 3 has antimicrobial activity and has been used in cancer, metabolic and neurological disorders.
  • $199
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